Determination of multi-index components and quality evaluation of Dilong Formula Granules 地龙配方颗粒多指标成分测定及质量评价
LI Lei, ZHANG Chengzhong, ZHANG Hanming, BU Qitao, et al
2023, 41(9): 547-551.
doi: 10.12206/j.issn.2097-2024.202209086
Preliminary pre-prescription study of Tetrodotoxin 河豚毒素处方前初步研究
XU Jiren, ZHENG Ziyun, LI Yuan, LU Ying, et al
2023, 41(9): 544-546, 551.
doi: 10.12206/j.issn.2097-2024.202304024
Basic research on toxin of Solenopsis invicta 红火蚁毒素物质基础研究进展
LI Anpeng, CHEN Shuai, SONG Jia, LIANG Lunhai, et al
2023, 41(9): 524-527.
doi: 10.12206/j.issn.2097-2024.202204119
Solenopsis invicta is a kind of invasive pest that causes serious damage to local agriculture, environment, and human health. They attack mainly with venom within stingers. Those who are allergic to the venom would suffer a systemic anaphylaxis, even fatal shock, after being stinged by these ants. Many studies reveal that their venom is mainly composed by water, insoluble alkaloids and trace proteins, within which alkaloids are the main cause of burning sensation and blisters, while allergic reactions are caused by proteins or peptides. The research progress of toxic substances in the venom of Solenopsis invicta as well as the roles and functions of each component were reviewed in this paper.
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Research Progress on Linear Ubiquitin Chain Assembly Complex and OTU Deubiquitinase With Linear Linkage Specificity in Tumor 线性泛素连接酶复合体与去线性泛素化酶在肿瘤中的研究进展
FANG Yuxin, LI Yu, LIU Baoshu, DONG Guoqiang
2023, 41(9): 534-539.
doi: 10.12206/j.issn.2097-2024.202307045
Linear ubiquitination is an important post-translational modification that has been discovered in recent years. The linear ubiquitin chain is formed by the linkage of glycine residue of one ubiquitin protein to the methionine residue of another ubiquitin. This process is regulated by the linear ubiquitin chain assembly complex (LUBAC) and the OTU deubiquitinase with linear linkage specificity (OTULIN). Linear ubiquitination is involved in various biological processes, including immune response, inflammation, and cell apoptosis. Recent studies have shown that linear ubiquitination is closely related to the occurrence, development, and drug resistance of tumors by affecting signaling pathways such as NF-κB and Wnt/β-catenin. The research progress on the function of LUBAC and OTULIN in tumors was reviewed in this paper.
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Study on chemical constituents of Hippocampus trimaculatus Leach 三斑海马的化学成分研究
QIAO Fangliang, XIA Tianshuang, ZHANG Chengzhong, JIANG Yiping, et al
2023, 41(9): 540-543, 560.
doi: 10.12206/j.issn.2097-2024.202212032
In vitro release study on self-microemulsion of curcumin and piperine 复方自微乳中姜黄素和胡椒碱的体外释放研究
REN Jinmei, LI Man, WANG Jing, GU Shenyong
2022, 40(1): 66-69, 75.
doi: 10.12206/j.issn.1006-0111.202009090
Comparative study on analgesic effect of tetrodotoxin in four acute pain models 河豚毒素对4种急性疼痛模型的镇痛效应比较研究
CHEN Xuejun, ZHANG Ruihua, SHI Tong, WANG Chen, et al
2022, 40(1): 70-75.
doi: 10.12206/j.issn.1006-0111.202101009
Antifungal activity study on HDAC inhibitor Rocilinostat 组蛋白去乙酰化酶抑制剂Rocilinostat的抗真菌活性研究
ZHU Tianbao, TU Jie, SHENG Chunquan, XU Defeng, et al
2022, 40(1): 44-47, 65.
doi: 10.12206/j.issn.1006-0111.202103008
Analysis on 59 cases of preparation deviation in our hospital from 2017 to 2019 我院2017−2019年59例次制剂偏差情况分析
LI Jie, YANG Yuru, YANG Bashi, WANG Qingfen, et al
2022, 40(1): 93-96.
doi: 10.12206/j.issn.1006-0111.202008006
The pharmaceutical care by clinical pharmacists for a foot injury patient with postoperative MRSA infection 临床药师参与1例足部损伤患者术后MRSA感染治疗的药学监护
LUO Jingjing, WU Xinan, XUE Gang, XIE Zhengdong, et al
2022, 40(3): 286-288.
doi: 10.12206/j.issn.1006-0111.202102004
Advances in mosquito repellents 驱蚊剂的研究新进展
CHEN Xinlu, TAI Zongguang, ZHU Quangang, GAO Shen
2023, 41(2): 81-85, 90.
doi: 10.12206/j.issn.2097-2024.202103036
Mosquitoes are the biological vectors of many diseases. Mosquito-borne infectious diseases are serious public health problems in tropical areas. With the increasing resistance of mosquitoes to insecticides, it becomes difficult to control mosquito-borne infectious diseases. The application of mosquito repellents can not only control the spread of mosquito-borne infectious diseases to a certain extent, but also reduce the use of insecticides and relieve the environmental pressure. This paper introduces and summarizes the research progresses of new mosquito repellents in recent years to provide reference resource for the further development of mosquito repellents.
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Quality standard improvement study of ginkgo semen decoction pieces 白果饮片质量标准修订研究
TU Yan, DONG Zhiying, HUANG Mengqiu, TAN Jingfu, et al
2022, 40(3): 270-273.
doi: 10.12206/j.issn.1006-0111.202103007
The total synthesis of natural cyclopeptide auyuittuqamide A 天然环肽auyuittuqamide A的全合成研究
GENG Chenchen, WANG Tiantian, LI Xiang, Wang Xiaoyan, et al
2022, 40(1): 53-56, 61.
doi: 10.12206/j.issn.1006-0111.202105087
Study on chemical constituents of sponge-associated Aspergillus terreus 海绵共附生土曲霉的化学成分研究
YU Xi, WANG Yuting, LIN Houwen, SUN Yating
2022, 40(2): 120-124.
doi: 10.12206/j.issn.1006-0111.202107019
Research progress on action mechanism and clinical application of hyaluronic acid 透明质酸的作用机制及临床应用研究进展
CAI Tongkai, LIU Mouzhi, DENG Jie, CAO Yongbing, et al
2022, 40(2): 103-107, 131.
doi: 10.12206/j.issn.1006-0111.202108002
Hyaluronic acid is widely present in the human body. It is an important component of extracellular matrix. It has unique hydrodynamic properties, good viscoelasticity and strain properties. At present, hyaluronic acid has been widely used in biomaterials, targeted-drug preparations, cosmetics and prevention of adhesion after abdominal surgery. With the expansion of the application scope of hyaluronic acid and the continuous emergence of new medical materials, the research on hyaluronic acid has been increasing in recent years. This paper reviews the clinical application of hyaluronic acid and its mechanism, in order to provide reference for the further development and safe application of hyaluronic acid products.
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Study on quality standard of compound Yuhong suppository 复方玉红栓的质量标准研究
HU Yeshuai, TANG Xiaomeng, WANG Zhijun, HUANG Yueying, et al
2022, 40(1): 76-78, 83.
doi: 10.12206/j.issn.1006-0111.202103003
Effects of liver-specific Nampt knockout on ischemic stroke 肝脏特异性Nampt基因敲除对缺血性脑卒中的影响
QING Shengli, WANG Shuna, WANG Dongsheng, LYU Xiaoqun, et al
2022, 40(1): 12-19.
doi: 10.12206/j.issn.1006-0111.202107068
Improvement of the quality standard for Kunxian capsules 昆仙胶囊的质量标准提升研究
XU Chunfang, LI Zhexuan, ZHOU Luoying, ZHANG Ni, et al
2022, 40(2): 152-156.
doi: 10.12206/j.issn.1006-0111.202106102
Research progresses on the main active components in Ningxia Sophora alopecuroides and the therapeutic activities for liver diseases 宁夏苦豆子主要活性成分及治疗肝脏疾病的研究进展
QUAN Danni, XU Yue, QU Zhuo, XU Weiheng, et al
2022, 40(1): 1-5, 37.
doi: 10.12206/j.issn.1006-0111.202105035
Sophora alopecuroides, a plant of the family Leguminosae, is one of the Daodi herbs in Ningxia. The active constituents of Sophora alopecuroides are abundant and complex, including alkaloids, flavonoids, volatile oils, steroids, polysaccharides, fatty acids and so on. In recent decades, a great number of domestic and overseas studies have been carried out on Sophora alopecuroides alkaloids, which have anti-hepatitis, anti-liver fibrosis, anti-cirrhosis, anti-liver failure and anti-liver cancer and other pharmacological effects. Clinically, Matrine-related drugs are used to treat hepatitis B virus infection and other diseases. This review aims to summarize the main active ingredients of Sophora alopecuroides, mainly focusing on the research progress in their treatment activities for liver diseases.
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Acetaminophen content assay with UHPLC in the sustained-release tablet exposed to radiation UHPLC法测定辐射后对乙酰氨基酚缓释片含量
YU Dexun, HUANG Xinhui, ZHU Kehan, HUANG Ting, et al
2022, 40(6): 550-552, 562.
doi: 10.12206/j.issn.2097-2024.202109100
Rapid prediction of antioxidant activity in aqueous extract solutions of melastoma dodecandrum by ultraviolet spectroscopy 地稔水提液抗氧化活性的紫外光谱快速预测方法
JIANG Cheng, XU Pingcui, WU Renjie, ZHANG Xiaoqing, et al
2022, 40(1): 48-52.
doi: 10.12206/j.issn.1006-0111.202101016
Characterization and function study of circadian rhythm gene CtPRR1 in Carthamus tinctorius L. 红花昼夜节律相关基因CtPRR1的特征及功能研究
WU Jianhui, HE Beixuan, JIA Xinlei, GUO Meili
2022, 40(1): 38-43.
doi: 10.12206/j.issn.1006-0111.202102007
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Articles in press have been peer-reviewed and accepted, which are not yet assigned to volumes /issues, but are citable by Digital Object Identifier (DOI).
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In Press
, Available online
doi: 10.12206/j.issn.2097-2024.202404062
Abstract:
Objective To improve the cellular uptake efficiency and the therapeutic effect of the drug through the structural modification of paclitaxel （PTX） and the preparation of corresponding liposomes. Methods The prodrug of paclitaxel, PTX-PA, was prepared by esterification reaction, and the quantitative detection method of PTX-PA was established. Next,the optimal formulation and preparation of PTX-PA/Lip was obtained through single factor screening based on their appearance, particle size, and encapsulation efficiency. Results The PTX-PA was successfully synthesized, and the established HPLC quantitative analysis method for PTX-PA meet the methodological requirements. After the optimal preparation and formulation research through single factor screening, the particle size of optimized PTX-PA/Lip was （62.75±1.81） nm with a PDI of （0.076±0.02）, while the drug encapsulation rate reached more than 90%. Conclusion This research successfully prepared palmitic acid modified paclitaxel liposomes based on nanotechnology, enhancing the drug delivery efficiency of paclitaxel and laying the foundation for the pharmacodynamics research of PTX-PA.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202403049
Abstract:
Metabolic dysfunction-associated steatotic liver disease（MASLD） is the most prevalent chronic liver disease globally, encompassing the entire spectrum of fatty liver pathogenesis. It progresses from simple steatosis to metabolic-associated steatohepatitis （MASH）, involving injury and inflammation, with or without fibrosis, ultimately leading to cirrhosis and hepatocellular carcinoma, which affects approximately a quarter of the world's population. Liver biopsy remains the gold standard for differentiating MASH from steatosis and assessing advanced fibrosis. However, its limitations, including costliness, invasiveness, and sampling bias, have spurred the development of noninvasive diagnostic techniques. In addition, there are no FDA-approved drugs for the treatment of MASLD. Enumerating noninvasive diagnostic markers that have the potential to replace liver biopsy were summarized, and the current treatment options for MASLD were discussed, with clinical trials designed to evaluate the efficacy and safety of single agents or combination therapies to halt or reverse disease progression, which could provide new insights for the clinical diagnosis and treatment of MASLD.
Metabolic dysfunction-associated steatotic liver disease（MASLD） is the most prevalent chronic liver disease globally, encompassing the entire spectrum of fatty liver pathogenesis. It progresses from simple steatosis to metabolic-associated steatohepatitis （MASH）, involving injury and inflammation, with or without fibrosis, ultimately leading to cirrhosis and hepatocellular carcinoma, which affects approximately a quarter of the world's population. Liver biopsy remains the gold standard for differentiating MASH from steatosis and assessing advanced fibrosis. However, its limitations, including costliness, invasiveness, and sampling bias, have spurred the development of noninvasive diagnostic techniques. In addition, there are no FDA-approved drugs for the treatment of MASLD. Enumerating noninvasive diagnostic markers that have the potential to replace liver biopsy were summarized, and the current treatment options for MASLD were discussed, with clinical trials designed to evaluate the efficacy and safety of single agents or combination therapies to halt or reverse disease progression, which could provide new insights for the clinical diagnosis and treatment of MASLD.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202405059
Abstract:
Sepsis is a severe and life-threatening condition that poses a significant risk to human health. Treatment mainly involves supportive care, but research for new drugs is ongoing. For example, advancements have been achieved in the management of immune function, inflammatory pathway, blood coagulation, and vascular endothelial homeostasis in sepsis. This article will review these advances in the treatment of sepsis in recent years.
Sepsis is a severe and life-threatening condition that poses a significant risk to human health. Treatment mainly involves supportive care, but research for new drugs is ongoing. For example, advancements have been achieved in the management of immune function, inflammatory pathway, blood coagulation, and vascular endothelial homeostasis in sepsis. This article will review these advances in the treatment of sepsis in recent years.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202403057
Abstract:
Objective To explore the risk signals of adverse events （ADE） in the use of exenatide microspheres by the FDA adverse event reporting system （ FAERS ）, and provide reference for clinical rational drug use and drug safety. Methods With exenatide microspheres as the target drug, the search keywords were Exenatide Microspheres for Injection, LY05006 , AC 2993 LAR and Bydureon . SAS software was used to extract the ADE report data from January 2, 2012 to March 31, 2023 in the FAERS database and the duplicates were removed. Data mining of exenatide microspheres-related ADE reports was performed by the reporting odds ratio method and the comprehensive standard method. Results A total of 27 248 exenatide microspheres-related ADE reports were retrieved, involving 27 SOCs, of which 4 719 were severe ADE reports. The reporting personnel were mainly consumers （18 435 cases, 67.66%）, and the reporting countries were mainly the United States （26 295 cases, 96.50%）. A total of 163 ADE risk signals were obtained by reporting odds ratio method and comprehensive standard method, including new adverse reactions such as abnormal blood cholesterol, elevated lipase and mixed hyperlipidemia. Conclusion Based on the FAERS database, the post-marketing ADE of exenatide microspheres was mined and analyzed, which could provide reference for clinical medication safety and improvement of patients' medication compliance.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202404006
Abstract:
Objective To establish an HPLC method to determine the concentration of inositol nicotinate（IN） in rat skin, and study the pharmacokinetic characteristics of IN after transdermal administration of heparin sodium inositol nicotinate cream（GJR） in rats. Methods HPLC method was used to establish a simple and rapid analytical method for the determination of IN concentration in the skin of rats at different time points after administration. The established method was used to study the pharmacokinetics of IN after transdermal administration of GJR in rats, and the pharmacokinetic parameters were fitted with DAS software. Results The linearity of the analytical method was good in the concentration range of 0.25~20 μg/ml, the quantitative limit was 0.25 μg/ml, and the average recovery rate was 96.18%. The pharmacokinetic parameters of IN after transdermal administration of GJR in rats were as follows: t1/2 was （4.555±2.054） h, Tmax was （6±0）h, Cmax was （16.929±2.153）mg/L, AUC0−t was （150.665±16.568） mg·h /L ,AUC0−∞ was （161.074±23.917） mg·h /L, MRT（0−t） was （9.044±0.618）h, MRT（0−∞） was （10.444±1.91） h, CLz/F was （0.19±0.03） L/（h·kg）, and Vz/F was （1.19±0.437） L/（h·kg）. Conclusion IN could quickly penetrate the skin and accumulate in the skin for a long time, which was beneficial to the pharmacological action of drugs on the lesion site for a long time. The method was simple, rapid, specific and reproducible, which could be successfully applied to the pharmacokinetic study of IN after transdermal administration in rats.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202402034
Abstract:
Objective To analyze the effectiveness of reasonable control measures for prophylactic use of antibiotics for urinary system lithotripsy. Methods By carrying out special rectification activities on rational use of antibiotics, strengthening special comments on antibiotics and information notification on rational use of antibiotics, adding and improving the pre-review rules for antibiotics prescriptions, conducting in-depth clinical training and consultation by clinical pharmacists, strengthening innovation in rational use of drugs, and taking various measures to actively improve rational use of prophylactic antibiotics of lithotripsy in urology department, the changes of indexes related to antibiotics in urology department from 2019 to 2022 were analyzed. Results After active and reasonable control, Antibiotics Use Density in urology department decreased year by year. The utilization rate of antibiotics in inpatients decreased from 94.27% in 2019 to 77.47% in 2022. Various rate of microbial inspection reached the standard in 2022; The imipenem and cilastatin sodium for injection ranking of prophylactic use of antibiotics consumption DDDs for urinary system lithotripsy decreased from the 4th place in 2019 to the 8th place in 2022. The ranking of the urology department on carbapenem consumption DDDs in the whole hospital decreased from the 8th place in 2019 to the 12th place in 2022. At the same time, the incidence of urinary tract lithotripsy postoperative infection showed a decreasing trend year by year, from 0.84% in 2019 to 0.49% in 2022. Conclusion Positive control measures can promote the rational use of prophylactic antibiotics for urinary system lithotripsy.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202310049
Abstract:
Objective Pulmonary oxygen poisoning resulting from hyperbaric oxygen, frequently occurs in specialized operations, without any current effective prevention or treatment measures. To elucidate the impact of neostigmine（NEO）in combination with anisodamine （ANI）（neoscopolamine）on pulmonary oxygen toxicity and its mechanism. Methods The animal model of pulmonary oxygen poisoning was established. C57BL/6 mice were exposed to 2.5 ATA 99.9% oxygen for 6 h. The control group mice were injected with normal saline ip, while the treatment group mice received injections of ANI （25 mg/kg, ip）and NEO（50 μg/kg, ip）. Lung tissues were collected and stained with HE to observe any pathological injuries after exposure. Evans blue stain was utilized to identify lung permeability, wet/dry lung ratio, and protein concentration in the bronchoalveolar lavage fluid （BALF）to assess the lung injury’s severity. The modifications in inflammatory factors, oxidative stress indicators, and iron content in lung tissue were assessed. Results The results showed that the 2.5 ATA 99.9% oxygen-exposed group experienced a significant worsening of lung injury, as well as increased lung permeability, lung wet/dry ratio, and protein content in alveolar lavage fluid when compared to the control group. Moreover, mRNA levels of pro-inflammatory cytokines IL-1β, IL-6, TNF-α, and IFN-γ in the lung tissue of the model group were significantly elevated, while the levels of anti-inflammatory cytokines IL-4 and TGF-β were significantly reduced. The oxidative index MDA also significantly increased, while the antioxidant index GSH significantly decreased. Additionally, the expression of GPX4, a marker of ferroptosis, increased with an increase in iron content. Neoscopolamine treatment successfully reversed those effects. Conclusion The combined use of ANI and NEO has a protective effect on pulmonary oxygen poisoning. Neoscopolamine may inhibit inflammation and oxidative stress by activating the cholinergic anti-inflammatory pathway, thereby reducing the content of free iron in lung tissue and finally inhibiting cell ferroptosis.
In Press
, Available online
doi: 10.12206/j.issn.2097-2024.202312075
Abstract:
Ferroptosis, discovered in 2012, is a newly form of non-apoptotic and non-necrotic cell death, which is characterized by an increasement in lipid peroxidation and accumulation of intracellular iron ions. Glutathione peroxidase 4（GPX4）is the fourth member of the selenoprotein GPx family and plays a crucial role in clearing lipid peroxides in cells, making it an important regulator of ferroptosis. Small molecule inhibitors targeting GPX4 can induce ferroptosis, offering a new strategy for treating drug-resistant cancers and neurodegenerative diseases. The protein structure and function of GPX4 were primarily discusseed, and the latest advances in small molecule inhibitors of GPX4 were summarized, which provided a research foundation for developing ferroptosis inducers based on GPX4 inhibition.
Ferroptosis, discovered in 2012, is a newly form of non-apoptotic and non-necrotic cell death, which is characterized by an increasement in lipid peroxidation and accumulation of intracellular iron ions. Glutathione peroxidase 4（GPX4）is the fourth member of the selenoprotein GPx family and plays a crucial role in clearing lipid peroxides in cells, making it an important regulator of ferroptosis. Small molecule inhibitors targeting GPX4 can induce ferroptosis, offering a new strategy for treating drug-resistant cancers and neurodegenerative diseases. The protein structure and function of GPX4 were primarily discusseed, and the latest advances in small molecule inhibitors of GPX4 were summarized, which provided a research foundation for developing ferroptosis inducers based on GPX4 inhibition.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202407037
Abstract:
Objective To investigate the efficacy of oral Danning tablets for bowel preparation for colonoscopy in diabetes mellitus patients. Methods A study was conducted from November 2022 to May 2024, 100 type 2 diabetic patients （aged≥30 years）admitted to endocrinology department in our hospital were selected and scheduled for colonoscopy as research subjects. These patients were randomly divided into two groups: ①A control group （n=50）, received 68.56 g of polyethylene glycol electrolyte powder 10 hours before the colonoscopy and an additional 137.12 g six hours before the procedure. ②An experimental group （n=50）, in addition to the bowel preparation regimen of the control group, orally took Danning tablets three times daily, five tablets each time, starting two days before the colonoscopy. Results The experimental group had a BBPS score of （7.44±1.03）, which was higher than the control group’s BBPS score of （5.58±1.98）, P<0.001. In the experimental group, 96% of the bowel preparations were rated as excellent or good （BBPS score≥6）, significantly higher than the 58% in the control group （P<0.001）. Conclusion In diabetic patients undergoing colonoscopy, oral administration of Danning tablets during bowel preparation could improve bowel cleanliness and significantly enhance the quality of bowel preparation.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202404063
Abstract:
Objective To establish a high-precision and high-specificity quantitative nuclear magnetic resonance phosphorus spectrometry method（31P-qNMR）for detecting the phosphorus content in calcium hydrogen phosphate chewable tablets. Methods Hexamethyl phosphoramide was used as an internal standard, phosphorus spectrum data of calcium hydrogen phosphate chewable tablets solution was collected. The linear relationship of calcium hydrogen phosphate within the concentration range of 1.0 to 9.0 mg/ml was studied, and sample recovery rate and repeatability experiments were conducted. Results Calcium hydrogen phosphate and the internal standard demonstrated a good linear relationship within the concentration range of 1.0 to 9.0 mg/ml, with a regression equation A = 0.0043 + 0.1836 C. The recovery rates for low, medium, and high concentrations were 98.0%, 98.1%, and 98.4%, respectively, with relative standard deviations（RSD）of 0.31%, 0.68%, and 0.62%, respectively（n= 9）. The average content of calcium hydrogen phosphate in the chewable tablets was determined to be 98.1%. Conclusion This study successfully established a high-precision and highly specific method for quantifying the content of calcium hydrogen phosphate in chewable tablets, which did not require a self-reference substance, was simple in sample preparation, and had a fast detection speed. The method could provide a new technical support for the quality control of phosphorus-containing drugs.
In Press
, Available online
doi: 10.12206/j.issn.2097-2024.202308045
Abstract:
Objective Hand-foot syndrome is a dose-limiting toxicity of capecitabine. At present, there is no unified gold standard for the establishment of hand-foot syndrome model. To induce hand-foot syndrome and provide a reference for the establishment of hand-foot syndrome model by administering capecitabine in ICR mice Methods 42 male ICR mice were randomly divided into control group (6 mice) and experimental group (36 mice). The experimental group was given capecitabine (275 mg/kg, twice/d) by intragastric administration for two weeks, and the control group was given 0.5% CMC-Na (4 ml/kg, twice/d), and evaluating whether the animal model of hand-foot syndrome was successfully constructed through H&E staining of mouse foot skin samples and observing morphological changes and the characteristic appearance of mouse foot skin. After the experiment, the mice were sacrificed, and plasma was collected to quantify the concentrations of capecitabine and metabolites. Results Control mice did not showed symptoms of hand-foot syndrome. The skin of the feet of 19 mice in the experimental group showed symptoms such as erythema and swelling, and H&E staining results showed that the plantar skin angular epidermis was thickened, and part of the keratin was exfoliated and damaged, which was considered to be hand-foot syndrome. There were no significant differences in the concentrations of capecitabine and its metabolites between mice with and without hand-foot syndrome. Conclusion The model of hand-foot syndrome induced by capecitabine in mice is successfully established. Differences in exposure levels of capecitabine and metabolites may not be the cause of hand-foot syndrome.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202310044
Abstract:
Objective To systematically evaluate the efficacy and safety of nivolumab in the treatment of non-small cell lung cancer. Methods PubMed, Embase, Cochrane Library, China National Knowledge Infrastructure（CNKI）, Weipu Chinese Science and Technology Journal Database, Wanfang Medical Database were searched for articles published from the establishment of the database to March 2023. Published randomized controlled trials of nivolumab in the treatment of patients with non-small cell lung cancer were selected, overall survival, progression-free survival, and adverse reaction rate as outcome indicators were used. A meta-analysis using STATA version 13.1 statistical software was conducted. Results A total of 8 phase Ⅲ randomized controlled trials involving 4945 subjects were included. Compared with the traditional chemotherapy group, patients in the nivolumab group had significantly reduced risk of death in terms of overall survival [HR=0.73, 95% CI=0.65-0.82, P<0.05], and in terms of progression-free survival, nivolumab significantly reduced the risk of recurrence compared with the traditional chemotherapy group [HR=0.74, 95% CI=0.63-0.88, P<0.05]. In terms of safety, there was no significant difference between the nivolumab group and the traditional chemotherapy group for diarrhea, but the incidence of nausea, neutropenia, anemia, decreased appetite, and fatigue in the nivolumab group was lower than that in the traditional chemotherapy group. However, it should be worth noting that the incidence of immune-related adverse events such as rash was higher in the nivolumab group than in the traditional chemotherapy group, and the difference was statistically significant [OR=3.85, 95％CI=2.05～6.25, P<0.05]. Conclusions Compared to traditional chemotherapy, the efficacy and safety of nivolumab in the treatment of non-small cell lung cancer were better, but the risk of immune-related adverse events increased.
In Press
, Available online
doi: 10.12206/j.issn.2097-2024.202404096
Abstract:
Objective To investigate the therapeutic effect of Qiwei Zhigan prescription on two classic animal models of non-alcoholic steatohepatitis（NASH）. Methods Methionine-choline-deficient（MCD）rat model and choline-deficient, L-amino acid-defined, high-fat and high cholesterol diet（CDAHFHC）mouse model were used. 48 rats and 96 mice were randomly divided into 6 groups: control group, model group, Qiwei Zhigan prescription group（low, medium and high dose group）, positive drug group. After 2 weeks of modeling, the drugs were administrated continuously for 28 days. The efficacy of Qiwei Zhigan prescription in the treatment of non-alcoholic steatohepatitis was evaluated by detecting the serum liver function, blood lipid biochemical indexes and liver tissue lipid levels of each group of animals, as well as by evaluating the liver histopathological changes. Results The gross anatomical morphology of the liver was improved by Qiwei Zhigan after oral administration of clinical equivalent dose or higher doses in two experimental animal models. the liver weight and liver index of NASH mice were reduced by the prescription. The levels of ALT, ALP and LDH in serum of NASH rats were decreased, and the level of HDL was increased. The levels of ALT, AST, TBIL, ALP, LDH and TG in serum of NASH mice were decreased, and the content of TG in liver was also decreased. The pathological damage of liver tissue was ameliorated, the inflammation of liver tissue was reduced, as well as the degree of ballooning of liver cells and the NAS score of the liver, and there was a certain dose-effect relationship between the groups; the proliferation of collagen fibers in the hepatic lobules and around the portal area of NASH mice was significantly reduced; the density of positive cells labeled by F4/80 was decreased, and the activation of Kupffer cells was alleviated. Conclusion Qiwei Zhigan prescription could effectively ameliorate the progression of two classic NASH models, and decrease the development trend from liver inflammation to liver fibrosis in NASH.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202405026
Abstract:
Remazolam is a new ultra-short-acting benzodiazepine that produces sedation by acting on γ-aminobutyric acid type A（GABAA）receptors. Remazolam has characteristics of rapid onset of action, short half-life, high clearance, and no accumulation in the body. It also has a low incidence of injection pain and mild effects on hepatic and renal function, respiration, and haemodynamics. Additionally, it can be rapidly reversed by flumazenil. The clinical research progress on remazolam in the areas of procedural sedation, induction, and maintenance of general anesthesia were reviewed to lay a foundation for its clinical application.
Remazolam is a new ultra-short-acting benzodiazepine that produces sedation by acting on γ-aminobutyric acid type A（GABAA）receptors. Remazolam has characteristics of rapid onset of action, short half-life, high clearance, and no accumulation in the body. It also has a low incidence of injection pain and mild effects on hepatic and renal function, respiration, and haemodynamics. Additionally, it can be rapidly reversed by flumazenil. The clinical research progress on remazolam in the areas of procedural sedation, induction, and maintenance of general anesthesia were reviewed to lay a foundation for its clinical application.
Accepted Manuscript
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doi: 10.12206/j.issn.2097-2024.202403030
Abstract:
[ Abstract]Objective To develop a high performance liquid chromatography-tandem mass spectrometry （HPLC-MS/MS） method for simultaneous determination of five flavonoids in Ganmao’an granules （GMA）. Methods Chromatographic separation was achieved on a Kromasil C18 column （150 mm× 4.6 mm,5 μm,100 Å）, which was eluted with methanol （A）-0.1 % formic acid （B） at the flow rate of 1.0 ml/min. The gradient condition was as follows: 0-20 min, 35% A, and 20-40 min, 45% A. The column temperature was 25 °C. Analytes were detected using a triple quadrupole tandem mass spectrometer equipped with an electrospray ionization source in the negative ion scanning. The multiple reaction monitoring mode was used for qualitative analysis. For each flavonoid, two precursor ion/product ion transitions were chosen: lutin m/z 609.1→300.1, hyperin and isoquercitrin m/z 463.0→300.1, quercetin m/z 301.0→151.0, luteolin m/z 285.0→132.9. Results Five flavonoids showed the good relationships within their own concentration ranges （correlation coefficient r>0.999 1）, whose average recoveries were in the range of 100.63 %-102.81 % with RSDs of 0.67 %-2.07 %. The content results of rutin, hyperoside, isoquercetin, quercetin, and luteolin in 10 batches of GMA were 32.23-479.83, 0.291-1.825, 11.44-20.54, 6.32-18.41, 3.46-6.51 μg/g, respectively. Conclusion The results indicated that the developed method was sensitive, accurate and could provide excellent specificity for simultaneous determination of five flavonoids in GMA.
[ Abstract]Objective To develop a high performance liquid chromatography-tandem mass spectrometry （HPLC-MS/MS） method for simultaneous determination of five flavonoids in Ganmao’an granules （GMA）.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202309059
Abstract:
Objective To analyze the current status of anti-bacterial activity of carbapenem-resistant Klebsiella pneumoniae and Escherichia coli clinically isolated from hospitalized patients, and detect their related resistance genes, providing reference for the clinical treatment of carbapenem resistant Enterobacteria （CRE） infections and the rational use of antibiotics. Methods A total of 400 non-repetitive isolates of Klebsiella pneumoniae and Escherichia coli isolated from clinical specimens of Punan Branch of Renji Hospital, Shanghai Jiao Tong University School of Medicine from January 2022 to December were collected. The minimum inhibitory concentrations of these strains against commonly used antibiotics were determined by the broth microdilution method. The carbapenemase and related resistance genes of CRE were detected by drug resistance phenotype testing and polymerase chain reaction （PCR）. Results Among the 400 strains, 51 strains were identified as CRE, accounting for 12.75% （51/400）. Among these, 49 strains produced carbapenemases, with 41 strains （80.39%, 41/51）being CR Klebsiella pneumoniae and 10 strains （19.61%, 10/51）being CR Escherichia coli. Among the CRE strains, 34 strains （66.67%, 34/51）carried blaKPC, 13 strains （25.49%, 13/51）carried blaNDM, and 2 strains （3.92%, 2/51）carried blaOXA-48. Conclusion Compared with other commonly used antibiotics, colistin and tigecycline exhibited good in vitro antibacterial activity against carbapenemase-producing Klebsiella pneumoniae and Escherichia coli. In addition, there was good concordance between drug resistance phenotype testing and genotyping. Clinical microbiology laboratories could continuously monitor the drug resistance phenotype and genotype of CRE and develop appropriate treatment plans based on actual conditions.
Accepted Manuscript
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doi: 10.12206/j.issn.2097-2024.202404005
Abstract:
Objective To investigate the effect and mechanism of miglitol on regulating the energy metabolism of brown adipocytes by activating UCP1 and improving cold injury in mice after cold exposure. Methods Primary brown adipocytes were induced into mature adipocytes, the effect of miglitol on the viability of brown adipocytes was investigated by MTT method, the lipid droplet consumption level of cells after drug administration was investigated by Oil Red O staining technology, and the level of UCP1, a key protein of thermogenesis in brown adipocytes, was detected by Western blotting. The activity of anti-frostbite was investigated in cold exposure at 4 ℃ and −20 ℃. KM mice, which were randomly divided into control group, cold exposure group, miglitol group and all-trans retinoic acid group, and after 7 days of repeated administration, the body surface temperature of mice was detected by infrared thermal imaging system, the anal temperature change was detected by anal thermometer, and the expression levels of UCP1 and PGC1-α in adipose tissue were detected by immunoblotting. Results Compared with the control group, the lipid droplet consumption and UCP1 expression levels in brown adipocytes in the miglitol group were significantly increased. The levels of body surface temperature and rectal temperature increased significantly after cold exposure, and the levels of UCP1 and PGC1α in the brown adipose tissue of mice increased significantly, which indicated that the miglitol could activate the critical proteins UCP1 and PGC1α of the thermogenesis pathway, increase the thermogenesis of mice after cold exposure, and thus improve the effect of cold injury for toe swelling. Conclusion Miglitol could play a role in improving cold injury and body temperature in mice by increasing the level of UCP1 and PGC1α, which are key targets of the thermogenesis pathway to promote the thermogenesis of brown fat.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202310043
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Objective To prepare and characterize caspofungin acetate-loaded solid lipid nanoparticles using glycerol monostearate （CAS-SLNs）, and investigate the antifungal effect of potentiation on Candida albicans in vitro and in vivo. Methods A high performance liquid chromatography method was established for the determination of caspofungin acetate （CAS）. CAS-SLNs were prepared by the melt-emulsification method and characterized. The minimum inhibitory concentration （MIC）and the inhibitory effect on Candida albicans biofilm were determined. A systemic infection model of Candida albicans was established in mice, and the growth curve models for body weight and fungal load of kidneys of the animals were investigated after intravenous infection. Results The retention time of CAS was 6.8 min. The calibration curve showed good linearity, and the precision and stability met the requirements of the assay. Transmission electron microscopy revealed that CAS-SLNs were spherical, with a particle size of 135.97±1.73 nm. The Zeta potential was 19.33±0.37 mV, drug loading was 7.55±0.68%, and encapsulation efficiency was 67.71±1.74%. CAS-SLNs showed significant in vitro antifungal inhibition with a MIC of 9.78×10−4 g/ml, which was significantly better than CAS group and the physical mixture group of CAS and GMS, as well as the same biofilm inhibition was observed（P<0.001, P<0.001）. Pharmacodynamic studies demonstrated that CAS-SLNs maintained stable body weight gain compared to the control（P<0.01）and CAS groups in Candida albicans invasive infection model, and that CAS-SLNs significantly reduced renal fungal burden load relative to the CAS group （P<0.05）. In vivo study revealed that a stable body weight was maintained in CAS-SLNs group compared to the control group （P<0.01）in Candida albicans invasive infection model. CAS-SLNs also significantly reduced renal fungal load compared to the CAS group（P<0.05）. Conclusion CAS-SLNs significantly enhanced the antifungal effects of CAS in vitro and in vivo, which provided a valuable insight for the research of new formulation of CAS.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202401072
Abstract:
Objective To establish a method for rapid detection of tramadol in urine by liquid-liquid extraction（LLE）-surface-enhanced Raman spectroscopy （SERS）. Methods Tramadol was extracted from urine with chloroform: isopropyl alcohol （9∶1）extractant and detected in urine samples by enhanced Raman spectroscopy （wavelength 785 nm）. Results The quantitative curve of tramadol was Y=204.35X−465.62, r=0.9952 , and the linear range was 1-100 μg/ml. The detection limit of tramadol by this method （S/N=3）was 0.53 μg/ml. The sensitivity of SERS was higher than that of conventional methods, and it had reasonable reproducibility. Conclusion This method is simple, efficient and economical, and can be used for qualitative and quantitative analysis of tramadol personalized medicine.
In Press
, Available online
doi: 10.12206/j.issn.2097-2024.202312009
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Objective Compared with traditional powder injection, the advantages of powder-liquid double-chamber bag products were comprehensively evaluated. Methods The systematic review method was used to collect the literature on powder-liquid double-chamber bag, extract common evaluation indicators, evaluate the use value of powder-liquid double-chamber bag products, and conduct a comprehensive comparison with traditional powder injection products. Results A total of 23 articles were included in the literature. The effectiveness indicators used for evaluation were the stability of the liquid medicine, the accuracy of the preparation concentration, and the residual amount of the liquid medicine; the safety indicators were the incidence of insoluble particles and the incidence of punctures and scratches. The economic indicators were preparation cost, occupied volume of preparation supplies, waste weight, hospitalization cost and incidence of blood infection. The applicability indicators were preparation time, average occupation of medical staff, packaging weight and storage and transportation volume, environmental adaptability, and ease of waste disposal. Accessibility indicators are the number of manufacturers, raw material supply capacity, and patient affordability. Through the rapid evaluation of literature evidence, it was found that the stability and concentration accuracy of the powder-liquid double-chamber bag were higher than those of the traditional powder injection, and the domestic supply had been achieved. The double-chamber bag method can reduce the infusion reaction and shorten the preparation time of the liquid medicine. Conclusion Compared with traditional powder injectabler products, powder-liquid double-chamber bags have advantages in the dimensions of effectiveness, safety, economy, suitability and innovation, and the accessibility dimension meets the requirements.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202404041
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Objective To analyze the characteristics of adverse drug reactions （ADR） reported in our hospital from 2021-2023, to provide reference for promoting rational clinical drug use. Methods ADR data reported in our hospital were collected retrospectively, including patients' basic information, drugs causing adverse reactions, types of adverse reactions and outcomes. Descriptive analysis methods were used to summarize and analyze the data. Results A total of 979 cases of ADR were reported in our hospital from 2021 to 2023. The highest proportion of patients with ADR occurred in the age range of 31 to 50, and more male patients （63.5%）. The top five drugs involved with adverse reactions were antibiotics （48.8%）, Chinese medicine injections, vitamins, Chinese patent medicine, equine tetanus immunoglobulin. Among antibiotics, cefuroxime, ceftazidime and cefotiam were the majority. The organs/systems involved in all ADR were mainly skin and accessories damage （55.4%）. The clinical manifestations were rash, itching, and maculopapular rash. Conclusion From 2021 to 2023, the most common drugs causing adverse drug reactions in our hospital are still mainly antibacterial drugs, and the rational clinical use of antibacterial drugs still needs to be paid attention to.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202309014
Abstract:
Surface plasmonresonance （SPR） sensoris anoptical detection technique enables real-time and dynamic monitoring of biological samples. SPR-based biosensors have remarkable characteristics such as label-free detection and high sensitivity, making them important tools for studying molecular interactions. The recognition element, which plays a critical role in SPR sensors, allows for specific identification and capture of target analytes, closely influencing the selectivity performance of the sensor. The progress on SPR sensors in pharmaceutical research were reviewed, which focused on the application of recognition elements such as antibodies, aptamers, molecularly imprinted polymers, and metal nanoparticles.
Surface plasmonresonance （SPR） sensoris anoptical detection technique enables real-time and dynamic monitoring of biological samples. SPR-based biosensors have remarkable characteristics such as label-free detection and high sensitivity, making them important tools for studying molecular interactions. The recognition element, which plays a critical role in SPR sensors, allows for specific identification and capture of target analytes, closely influencing the selectivity performance of the sensor. The progress on SPR sensors in pharmaceutical research were reviewed, which focused on the application of recognition elements such as antibodies, aptamers, molecularly imprinted polymers, and metal nanoparticles.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202306020
Abstract:
Objective To establish a central cutting two-dimensional liquid chromatography for the determination of lamotrigine in human plasma. Methods External standard method was used. The first dimensional chromatographic column: SNCB（T）-1A（silica gel, 4.6 mm×50 mm, 5 μm）, mobile phase A:VCV-1D mobile phase, flow rate: 0.4 ml/min; mobile phase B: water, flow rate: 1.0 ml/min; second dimensional chromatographic column: Symmetry C18 （4.6 mm×250 mm, 5 μm）, mobile phase: acetonitrile-10 mmol/L ammonium acetate solution（V/V=25∶75）, flow rate: 1.0 ml/min; Intermediate column: SBX 4-MA（resin, 3.0 mm×10 mm, 5µm）. The UV detection wavelength: 306 nm, the column temperature: 45 ℃, and the injection volume: 200 μl. Results The linear range of lamotrigine was 1.24-39.50 μg/ml, the lower limit of quantification was 1.24 μg/ml, the detection limit was 0.02 μg/ml, the intra-day precision RSD was less than 5%, the day-to-day precision RSD was less than 10%, the variation of intra-day accuracy ranged from 102.17% to 111.17%, and the daytime accuracy variation ranged from 99.80% to 107.31% the recovery RSD was less than 5%, and the variation range was 89.95% -96.16%. After 24 hours storage at room temperature, repeated freezing and thawing for 3 times and storage at-40 ℃ for 2 weeks, the ratio of the measured value / labeled value ranged from 87.01% to 115.88%. Conclusion In this study, a method with simple operation, good stability, high sensitivity and good reproducibility was established, which could be suitable for clinical monitoring of blood concentration of lamotrigine and provides reliable monitoring data support for clinical individualized medication guidance.
Objective To establish a central cutting two-dimensional liquid chromatography for the determination of lamotrigine in human plasma. Methods External standard method was used. The first dimensional chromatographic column: SNCB（T）-1A（silica gel, 4.6 mm×50 mm, 5 μm）, mobile phase A:VCV-1D mobile phase, flow rate: 0.4 ml/min; mobile phase B: water, flow rate: 1.0 ml/min; second dimensional chromatographic column: Symmetry C18 （4.6 mm×250 mm, 5 μm）, mobile phase: acetonitrile-10 mmol/L ammonium acetate solution（V/V=25∶75）, flow rate: 1.0 ml/min; Intermediate column: SBX 4-MA（resin, 3.0 mm×10 mm, 5µm）. The UV detection wavelength: 306 nm, the column temperature: 45 ℃, and the injection volume: 200 μl. Results The linear range of lamotrigine was 1.24-39.50 μg/ml, the lower limit of quantification was 1.24 μg/ml, the detection limit was 0.02 μg/ml, the intra-day precision RSD was less than 5%, the day-to-day precision RSD was less than 10%, the variation of intra-day accuracy ranged from 102.17% to 111.17%, and the daytime accuracy variation ranged from 99.80% to 107.31% the recovery RSD was less than 5%, and the variation range was 89.95% -96.16%. After 24 hours storage at room temperature, repeated freezing and thawing for 3 times and storage at-40 ℃ for 2 weeks, the ratio of the measured value / labeled value ranged from 87.01% to 115.88%. Conclusion In this study, a method with simple operation, good stability, high sensitivity and good reproducibility was established, which could be suitable for clinical monitoring of blood concentration of lamotrigine and provides reliable monitoring data support for clinical individualized medication guidance.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202405009
Abstract:
Objective To screen small molecule inhibitors against Fusobacterium nucleatum（Fn） based on commercially available compound libraries, followed to investigate their anti-colorectal cancer activities under Fn intervention in order to obtain novel anti-colorectal cancer lead compounds. Methods Firstly, to validate the promotion of colorectal cancer proliferation on organoid by Fn. Secondly, comparative investigation for the effects of anti-Fn compounds on their in vitro anticancer activity under Fn’s co-incubation with colorectal cancer HCT116 cells. Finally, evaluation for in vivo anticancer efficacy of highly active compounds on nude mouse colon cancer HCT116 transplanted tumor under the intervention of Fn by gavage. Results Fn could significantly promote the proliferation of rectal cancer organoids. 9 ant-Fn active compounds could significantly enhance their in vitro anticancer activity under Fn’s co-incubation with HCT116 cells. Methotrexate had the strongest anti-cancer activity with IC50 as 0.03 μmol/L. The combined use of methotrexate（0.5 mg/kg）and PD-1（5.0 mg/kg）had a stronger anti-tumor effect than their standalone use. Conclusion As new small molecule inhibitor against Fn, methotrexate exhibits good in vitro and in vivo anti-colorectal cancer activity against HCT116 cells and nude mouse xenografts under Fn intervention. This lays the foundation for subsequent structural optimization, and is expected to expand the new indications for methotrexate.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202310021
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Objective To establish quality evaluation method of Andrographis paniculata standard decoction by UPLC. Methods 21 batches of Andrographis paniculata standard decoctions were prepared according to the standardization method of TCM decoction pieces. The UPLC characteristic chromatograms analysis method was established. With andrographolide as a reference, quantitative analysis of multi-components by single marker（QAMS）was established for new neoandrographolide, 14 deoxyandrographolide and dehydrated andrographolide and the results were compared with the external standard method（ESM）to determine the accuracy of the method. Results Similarity Evaluation System for Chromatographic Fingerprint of TCM（2012 edition）was used to analyze and compare the characteristic chromatograms, and seven common peaks were determined and five were identified including luteolin-7-O-β-D-glucuronide, andrographolide, neoandrographolide, 14-deoxyandrographolide and dehydroandrographolide. The RSDs of content results of each component by QAMS and ESM were all within 3%. Conclusion The determination method is reliable and accurate, which can be used to reflect the intrinsic quality of Andrographis paniculata standard decoction more comprehensively and provide the basis for the quality evaluation of Andrographis paniculata formula granules and other preparations.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202402028
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It is difficult to treat malignant tumors, neurodegenerative diseases, and vascular diseases. For pathogenesis complexity of these diseases, researchers have focused on finding more drugs with high efficacy and low side effects. As a potential first-in-class drug, RRx-001 is expected to be an important first-line drug in tumor immunology, radiosensitizer and radio protecter. Currently, RRx-001 entered phase III clinical trials. The data of the phase II clinical trials demonstrated its safety and effectivity as a single agent and in combination with first-line clinical drugs. The novel mechanisms of RRx-001 and the result of main clinical trials were summarized, which could be valuable to further optimization and clinical application.
It is difficult to treat malignant tumors, neurodegenerative diseases, and vascular diseases. For pathogenesis complexity of these diseases, researchers have focused on finding more drugs with high efficacy and low side effects. As a potential first-in-class drug, RRx-001 is expected to be an important first-line drug in tumor immunology, radiosensitizer and radio protecter. Currently, RRx-001 entered phase III clinical trials. The data of the phase II clinical trials demonstrated its safety and effectivity as a single agent and in combination with first-line clinical drugs. The novel mechanisms of RRx-001 and the result of main clinical trials were summarized, which could be valuable to further optimization and clinical application.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202309009
Abstract:
Objective To evaluate the curative effect of anti-flatulence laxative cream on patients with advanced hepatocellular carcinoma and opioid-associated constipation（OIC）. Methods 120 patients with advanced liver cancer complicated with OIC who were treated at the Third Affiliated Hospital of Naval Medical University from June 2021 to December 2022 were selected as the study subjects. The patients were divided into a control group（lactulose + conventional treatment）and an experimental group（anti-flatulence and laxative cream + conventional treatment）using a randomized numerical table method. Two groups were compared in terms of defecation, quality of life, and comprehensive post-treatment evaluation（economic cost, number of occurrences of diarrhea, and whether or not there was a change in the dosage of opioids used）. Results After 28 days of intervention, both groups showed better results in relieving OIC（P < 0.05）, and the experimental group was significantly better than the control group in terms of the quality of life of patients with advanced hepatocellular carcinoma, the economic cost and the number of diarrhea（P < 0.05）. Conclusion In the treatment of OIC in patients with advanced hepatocellular carcinoma, constipation could be relieved by using both topical decongestant laxative cream and oral lactulose solution. Among them, anti-stagnation and laxative cream was more acceptable to patients and superior in terms of quality of life and economic cost, which could be a better choice for improving patient satisfaction and safety.
In Press
, Available online
doi: 10.12206/j.issn.2097-2024.202312014
Abstract:
Objective To investigate the possible mechanism of action of Jinqi Qingshu granules（JQQSG）in the treatment of community-acquired pneumonia（CAP）using network pharmacology and molecular docking technology. Methods The TCMSP database and SwissTargetPrediction database were used to obtain and screen the active ingredients and targets of JQQSG, and GeneCards, OMIM, TTD, and DisGeNET databases were used to search for the predicted targets of CAP, and the two targets were mapped and then imported into STRING database to construct a PPI network to screen the key targets, and then analyzed the GO and KEGG pathway enrichment by using the DAVID database, and carried out molecular docking by using the AutoDock Tools software. Results 209 active ingredients and 1041 targets of JQQSG were obtained after screening; 312 targets were co-activated with CAP, and 64 core targets were obtained after PPI network screening. 571 biological processes, 68 cellular components, and 199 molecular functions were analyzed by GO enrichment, and 165 KEGG pathways were analyzed by KEGG pathway enrichment. Mainly involved in protein action, apoptosis and MAPK signaling pathway. Molecular docking suggests that the core target and the core components all have good binding ability. Conclusion The mechanism of action of JQQSG in the treatment of CAP may be related to its regulation of Akt、MAPK signaling pathway, improvement of oxidative stress, and other pathways to exert anti-inflammatory and antioxidant effects, which lays the foundation for further in-depth study of its specific mechanism of action.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202306011
Abstract:
Objective To study the effect of MT-1207 on blood glucose, blood lipids and atherosclerosis. Methods The apolipoprotein E knockout (ApoE−/-) mice were fed with normal feed, drug feed containing losartan and drug feed containing MT-1207 at a dosage of 30 mg/kg. The body weight, blood glucose and blood lipids were detected, and the plaque area of atherosclerotic was evaluated. 8-week-old male C57 mice were fed a high fat diet and given intragastric administration of MT-1207 and losartan at a dose of 30 mg/kg per day. The body weight, blood glucose and lipids levels were also examined to further evaluate the effects of MT-1207 on blood glucose and lipids levels. Results ApoE−/- mice treated with MT-1207 feed and losartan feed gained weight faster. The blood glucose and lipids levels didn’t improve significantly and the plaque area of atherosclerosis didn’t change significantly. MT-1207 and losartan had no significant improvement effect on blood glucose and blood lipids of C57 mice. Conclusion MT-1207 and losartan couldn’t improve the levels of blood glucose, blood lipids and atherosclerosis, and couldn’t aggravate atherosclerosis.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202308065
Abstract:
Piper nigrum L. is an evergreen climbing vine, which belongs to the genus Piperia in the Piperaceae family. Piper nigrum L., which known as the “king of spices”, is used as both food and medicine. The main active substances in Piper nigrum L. are alkaloids mainly composed of amides, and essential oil, as well as phenolic compounds. In this paper, the chemical compositions, especially amide alkaloids, and their biological activities of Piper nigrum L. were summarized. These studies showed that Piper nigrum L., as a medicinal and food plant, had a wide range of biological activities and was deserved further research and in-depth utilization.
Piper nigrum L. is an evergreen climbing vine, which belongs to the genus Piperia in the Piperaceae family. Piper nigrum L., which known as the “king of spices”, is used as both food and medicine. The main active substances in Piper nigrum L. are alkaloids mainly composed of amides, and essential oil, as well as phenolic compounds. In this paper, the chemical compositions, especially amide alkaloids, and their biological activities of Piper nigrum L. were summarized. These studies showed that Piper nigrum L., as a medicinal and food plant, had a wide range of biological activities and was deserved further research and in-depth utilization.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202206072
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Objective To investigate the anti-fatigue effect of PTR-SeNPs in vivo by measuring the muscle relative length of hindlimb, load-bearing swimming time as well as serum and liver indexes of mice. Methods 48 male C57/BL6 mice were randomly assigned into 4 groups with 12 mice in each group, including vehicle control group (Control group), swimming training exercise group (EC group) with vehicle treatment, swimming training exercise with low dose of PTR-SeNPs group (LPTR-SeNPs) and high dose of PTR-SeNPs group (HPTR-SeNPs). The mice were intragastrically administrated with normal saline in both Control group and EC group, as well as 2.5 and 10 μmol/(kg·bw) PTR-SeNPs in LHPTR-SeNPs group, respectively, once per day for consecutively 21 days. After swimming training exercise, the muscle structures in the hind limb of mice were examined by magnetic resonance imaging. Furthermore, the burdened swimming time was measured, the serum content of blood lactic acid (BLA), urea nitrogen (BUN), alanine aminotransferase (ALT), glutamic oxalate aminotransferase (AST) and lactate dehydrogenase (LDH), as well as the hepatic level of glycogen (HG), malondialdehyde (MDA) and activity of catalase (CAT) and superoxide dismutase (SOD) were determined. Results Compared with the Control group, the serum contents of BLA, BUN, ALT, AST and LDH in EC group (P<0.05 or 0.01) and hepatic CAT in HPTR-SeNPs group (P<0.01) were significantly increased. The muscle relative length of hind limbs and the burdened swimming time were extended by HPTR-SeNPs markedly (P<0.05). There was no significant difference in MDA level in LHPTR-SeNPs group. Compared with EC group, the burdened swimming time of mice was significantly prolonged (P<0.01), the contents of BLA and BUN were obviously decreased in the HPTR-SeNPs group(P<0.05 or 0.01), the level of HG was significantly increased in the LHPTR-SeNPs groups (P<0.05 or 0.01), the serum content of ALT, AST and LDH were markedly decreased in the HPTR-SeNPs group (P<0.05 or 0.01). Hepatic SOD activity was remarkably increased in LPTR-SeNPs group (P<0.05), the level of CAT was evidently increased (P<0.01) and AST was decreased (P<0.05) in the HPTR-SeNPs group. Conclusion PTR-SeNPs could improve the liver physiological function, increase glycogen storage, reduce the accumulation of metabolites and enhance the body’s antioxidant capacity to ameliorate fatigue significantly, which could present the potential to be developed into health care products or drugs.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202311021
Abstract:
Objective To investigate the effect of Triptolide on cerebral ischemia- reperfusion injury (CIRI) and explore its molecular mechanism. Methods One hundred and forty-four Wistar rats were randomly divided into sham operation group, model group, low, medium, high dose of triptolide group and butylphthalide group, with 24 rats in each group. The CIRI rat model was established by blocking the middle cerebral artery for 2 hours. 3 days before modeling, the rats in each group were ip administration once a day. 24 hours after reperfusion, the neurological deficit score was detected, the rate of cerebral infarction was measured by TTC staining, the blood brain barrier (BBB) permeability was detected by EB penetration test. The pathological changes neurons in the ischemic penumbra cortex were observed by HE and TUNEL staining. The content of inflammatory factors in ischemic cerebral cortex were detected by ELISA method. The expression of TLR4/NF-κB pathway related proteins were detected by Western blot. Results Compared with the model group, the neurological deficit score, cerebral infarction rate and EB content in the Triptolide middle, high dose groups and the Butylphthalide group were significantly decreased (P<0.05). The pathological changes of cortical neurons in the ischemic penumbra were significantly improved, and the apoptosis rate of neurons was significantly decreased (P<0.05). The content of TNF-α, IL-1β and the expression of TLR4, p-NF-κB, cleaved Caspase-3, Bax were significantly decreased, the expression of Bcl-2 was significantly increased, the ratio of p-NF-κB/NF-κB and Bax/Bcl-2 were significantly decreased (P<0.05). The regulatory effect of the high dose triptolide group on various detection indexes were better than that of the Butylphthalide group (P<0.05). Conclusion Triptolide could protect the permeability of BBB, improve the neurological deficit and neuropathy in CIRI rats, and reduce the rate of cerebral infarction, its mechanism may be related to the inhibition of TLR4/NF-κB pathway and which mediated inflammatory response and neuronal apoptosis.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202309037
Abstract:
Corn silk, a Traditional Chinese Medicine, has the effect of calming liver, cholagogue, detumescence and diuresis. Corn silk is also widely used as tea and functional food. Natural flavonoids have multiple biological activities, which are also the main bioactive components of corn silk. In the past decade, many new advances have been made in the chemistry, analysis, pharmacology, pharmacokinetics, and safety evaluation of corn silk flavonoids. The chemical composition research of flavonoids has enriched the quantity of flavonoids in corn silk. Pharmacological studies have confirmed and expanded the efficacy of corn silk flavonoids. And safety evaluation has provided a theoretical basis for the safe application of corn silk flavonoids. Through literature search, the extraction, separation, compositional analysis, content determination, pharmacological effect, pharmacokinetics, and safety research progress of corn silk flavonoids in the past ten years were reviewed in this paper.
Corn silk, a Traditional Chinese Medicine, has the effect of calming liver, cholagogue, detumescence and diuresis. Corn silk is also widely used as tea and functional food. Natural flavonoids have multiple biological activities, which are also the main bioactive components of corn silk. In the past decade, many new advances have been made in the chemistry, analysis, pharmacology, pharmacokinetics, and safety evaluation of corn silk flavonoids. The chemical composition research of flavonoids has enriched the quantity of flavonoids in corn silk. Pharmacological studies have confirmed and expanded the efficacy of corn silk flavonoids. And safety evaluation has provided a theoretical basis for the safe application of corn silk flavonoids. Through literature search, the extraction, separation, compositional analysis, content determination, pharmacological effect, pharmacokinetics, and safety research progress of corn silk flavonoids in the past ten years were reviewed in this paper.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202309040
Abstract:
Objective To analyze the effect of hypoproteinemia on the use of cefoperazone in patients, and provide references for the rational use of cefoperazone in clinical practice. Methods Clinical data of patients with cefoperazone blood concentration monitoring in our hospital from July 2021 to March 2022 were collected, and divided into low albumin group and normal albumin group according to different albumin concentration. Statistical analysis were conducted based on gender, age, laboratory examination, cefoperazone valley concentration and clinical efficacy of the two groups. Results Age, gender, inflammation and liver function of two groups had not shown statistical difference (P>0.05). Low protein group had significantly higher levels of creatinine than those in group with normal albumin (P<0.05). The trough concentration of cefoperazone in the low protein group was 46.29±36.94 mg/L, and that in the normal albumin group was 38.18±33.79 mg/L. Among the low protein patient group, the plasma concentration of cefoperazone in those treated with human albumin was significantly higher than that in the patients without human albumin treatment (P<0.05). Comparison of the clinical efficacy of the two groups revealed that the low protein group had a lower clinical response rate (P<0.05). Conclusion Supplementation of human serum albumin in patients with hypoproteinemia could increase the plasma concentration of cefoperazone, and correcting hypoproteinemia could be helpful for anti-infection treatment.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202308034
Abstract:
Objective To observe the effect of Huoxin Pill (concentrated pill) combined with Baduanjin on the prognosis of patients with acute myocardial infarction complicated by Percutaneous Coronary Intervention (PCI). Methods 120 Patients with acute myocardial infarction complicated with heart failure who received emergency interventional treatment in our hospital from January 2022 to January 2023 were randomly divided into Western medicine treatment group and Traditional Chinese Medicine （TCM）comprehensive treatment group. Western medicine treatment: standard Western medicine treatment + five prescriptions for cardiac rehabilitation; Based on Western medicine treatment, Huaxin pill (concentrated pill) combined with Baduanjin therapy was added to the TCM comprehensive treatment group, and the follow-up was 6 months. The observed indexes were exertion angina pectoris scale, Chinese Medicine Syndrome Scale, Chinese medicine syndrome treatment effect evaluation, 6-minute walking test (6MWT), left ventricular ejection fraction (LVEF), and brain natriuretic peptide precursor (pro-BNP). Results Sixty patients were enrolled in the two groups respectively. During the treatment, 2 cases fell off in the Western medicine treatment group and 8 cases fell off in the TCM comprehensive treatment group, and a total of 110 cases were enrolled in the group. Compared with the western treatment group, TCM combined therapy significantly improved angina pectoris scale score, TCM Syndrome Scale score, pro-BNP, LVEF and 6MWT (P < 0.001). There were no significant differences in blood routine, liver and kidney function, potassium, blood glucose, blood lipids and cardiac Troponin I (cTnI) between the two groups (P > 0.05). No adverse cardiovascular events occurred during the entire treatment period in both groups. Conclusion Huaxin Pill (concentrated pill) combined with Baduanjin was more effective than Western therapy in improving LVEF, 6MWT distance, exercise tolerance and cardiac function in patients with acute myocardial infarction complicated with heart failure.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202305008
Abstract:
Objective To explore the protective effect of Rongmu Fugan Formula on ANIT induced cholestasis liver injury in mice. Methods 8-week old SPF Kunming mice were randomly divided into 6 groups, 10 mice in each group which were the blank control group (normal saline gavage), the model control group (normal saline gavage), the low (gavage dose:5.25 g/kg ) group, the medium (11.25 g/kg) group and the high (20.25 g/kg) group of Rongmu Fugan Formula, the positive control (Ursodeoxycholic acid, UDCA,0.1 g/kg). Mice were administered with continuous gavage once a day, for 7 consecutive days. On the 5th day, the blank normal control group was given an equal amount of olive oil by gavage, all other groups were given ANIT (65 mg/kg) by gavage for modeling. After 48 hours of modeling, 30 minutes after the last administration of each group of mice, blood and liver tissue samples were collected for testing of various indicators. The corresponding kits were used to detect the content of alanine transaminase (ALT), aspartate transaminase (AST), alkaline phosphatase (ALP), total bile acid (TBA),γ-glutamyl transpeptidase（γ-GT), total bilirubin (TBIL), superoxide dismutase (SOD), glutathione peroxidase (GSH-PX) and malondialdehyde (MDA) in peripheral blood of mice, respectively. HE staining was used to observe the pathological changes in the liver of mice. Results Compared with the model group, each dose group of Rongmu Fugan Formula reduced the levels of ALT, AST, AKP, TBA, TBIL,γ-GT and MDA (P<0.05) significantly, markedly increased the levels of SOD and GSH-PX (P<0.05). Compared with the model group, the low-dose and high-dose groups of Rongmu Fugan Formula showed a decrease in liver cell vacuolar degeneration and reduction in inflammatory infiltration. In the medium dose group, the vacuolar degeneration of liver cells was significantly reduced, the inflammatory infiltration was significantly improved, the liver cells were arranged in cords, and the structure of lobules of liver was intact. Conclusion Rongmu Fugan Formula could improve serum biochemical indicators of liver injury, reduce jaundice and eliminate oxidative free radicals, thereby exerting a protective effect against ANIT-induced cholestatic liver injury in mice.
In Press
, Available online
doi: 10.12206/j.issn.2097-2024.202204094
Abstract:
Objective To study the compliance and influencing factors of inhalation therapy in patients with stable chronic obstructive pulmonary disease (COPD),and carry out patient education and management accordingly. Methods COPD patients were selected from Respiratory Clinic of Luodian Hospital of Baoshan District of Shanghai from June to December of 2021. Compliance and inhalation techniques were assessed with the Morisky Medication Adherence Scale and the ten-step inhalation technique, and the factors influencing compliance were analyzed. Results A total of 58 outpatients with COPD were included, in which 25 cases (43.1%) with moderate or above compliance. Univariate analysis showed that the patients with course of disease ≥5 years, CAT(COPD assessment test)≥10 points, used 2 inhalation devices and inhalation technique score ≥8 points had better compliance when compared with other patients (P<0.05). Conclusion Patient education and management should be carried out actively. The patients with course of disease<5 years, CAT<10 points should be highly concerned. The patients' ability to use inhalation devices and personal preference should be fully considered. Training on the use of devices should be strengthened and regularly follow-up evaluation should be carried out.
In Press
, Available online
doi: 10.12206/j.issn.2097-2024.202306028
Abstract:
Objective To analyze chemical constituents of compound Maxing Shigan decoction by ultra-high perfor-mance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-QTOF/MS). Methods The separation was performed on a UPLC BEH C18 column (2.1 mm×100 mm, 2.5 µm), with a gradient elution applying 0.1% aqueous formic acid solution and 0.1% formic acid acetonitrile as a mobile phase. The column temperature was 40 °C. The flow rate was 0.4 ml/min and the analysis time was 15 min. Mass spectrometry (MS) data were collected in both positive and negative ESI ion modes. Results Through UPLC-QTOF/MS analysis and reference validation, a total of 59 chemical components in Maxing Shigan decoction were identified. Conclusion In this study, an ultra-high performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-QTOF/MS) method was established to identify the chemical components of Maxing Shigan decoction. This method is simple, efficient, sensitive and accurate, and provides a basis for the elucidation of the pharmacodynamic material basis and mechanism of Maxing Shigan decoction. It can provide data reference for the optimization of the compatibility of traditional Chinese medicine in the treatment of COVID-19.
In Press
, Available online
doi: 10.12206/j.issn.2097-2024.202208115
Abstract:
Objective To analyze the pharmacological mechanism of Shenling Baizhu powder in the treatment of cancer cachexia based on the network pharmacological method and provide a reference for the clinical application of classical traditional Chinese medicine(TCM) prescriptions. Methods Through TCMSP and BATMAN-TCM databases, the main chemical components and their targets of the TCM prescription of Shenling Baizhu powder were obtained, and the active components of the TCM were screened according to ADME. The main targets of cancer cachexia were obtained through OMIM, Genecards, Disgenet and DRUGBANK databases, and protein interaction analysis was conducted using String platform to build a PPI network. The “drug active ingredient target” network of Shenling Baizhu powder was constructed by Cytoscape 3.7.2 software, and then the biological processes and pathways involved were analyzed by using Metascape platform. Finally, molecular docking verification was conducted by Discovery Studio. Results The core active ingredients of Shenling Baizhu powder in the treatment of cancer cachexia are quercetin, kaempferol, pyrolignous acid, stigmasterol, luteolin, β-sitosterol, etc. The core targets are AKT1, TP53, TNF, IL-6, MAPK3, CASP3, JUN, CTNNB1, HIF1A, EGFR, etc. The molecular docking test also showed that the top 10 active ingredients, such as pyrolignous acid, stigmasterol and β-sitosterol, had good binding activities with most of the target sites. The biological pathway of Shenling Baizhu powder in treating cancer cachexia is mainly to regulate tumor related pathway, metabolism related pathway, inflammatory factors and appetite related pathway. Conclusion This study preliminarily revealed the mechanism of action of Shenling Baizhu powder in treating cancer cachexia with multi components, multi targets and multi pathways, which provided a basis for the clinical development and utilization of Shenling Baizhu powder.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202307034
Abstract:
Objective To investigate the potential mechanism of nicotinamide combined with amphotericin B against Candida albicans based on metabolomics. Methods The intracellular metabolites of C. albicans intervened by different drugs including NAM, AmB, and their combination with a proper concentration were analyzed by gas chromatography-mass spectrometry. The differential metabolites were screened by multivariate statistical analysis and identified by searching the NIST database. Results Compared with the control group, the NAM intervention group was hardly separated from it, while the AmB group and NAM+AmB group showed a clear trend separation. Under the intervention of AmB, 23 metabolites significantly changed compared with the control group, and 28 metabolites remarkably changed after NAM+AmB intervention, including amino acids, organic acids, sugars and other components. Conclusion NAM, as an endogenous metabolite of C. albicans, combined with AmB could enhance the effects of AmB in the original metabolic pathway and changed it to a certain extent. It is speculated that AmB combined with NAM may pose more antifungal effect on Candida albicans by regulating the tricarboxylic acid cycle, interfering with amino acid metabolism and influencing polyamine synthesis.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.
Abstract:
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202309021
Abstract:
Lactic acid bacteria is a good candidate in living drug delivery system for its safety, beneficial nature, and intestinal colonizability. At present, most studies use it as a protein drug delivery carrier for disease treatment. As a model organism, a variety of gene modification schemes enable it to be applied to various diseases and can play a significant therapeutic effect. Lactic acid bacteria drug carrier has many advantages, including non-invasive drug delivery, gene editing, large-scale production Therefore, the use of lactic acid bacteria as recombinant protein expression vector has attracted global attention. In this review, the application basis, bioavailability improvement, gene editing strategy and research and application status of lactobacillus drug delivery system were summarized.
Lactic acid bacteria is a good candidate in living drug delivery system for its safety, beneficial nature, and intestinal colonizability. At present, most studies use it as a protein drug delivery carrier for disease treatment. As a model organism, a variety of gene modification schemes enable it to be applied to various diseases and can play a significant therapeutic effect. Lactic acid bacteria drug carrier has many advantages, including non-invasive drug delivery, gene editing, large-scale production Therefore, the use of lactic acid bacteria as recombinant protein expression vector has attracted global attention. In this review, the application basis, bioavailability improvement, gene editing strategy and research and application status of lactobacillus drug delivery system were summarized.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202303006
Abstract:
Objective Study on the effect of Lishukang capsule on learning and memory impairment in mice with high altitude hypoxia based on Keap1/Nrf2/HO-1 signal pathway. Methods Sixty male Balb/C mice were randomly divided into normal control group, hypoxia model group, Rhodiola capsule group: 400 mg/kg, low, medium and high dose groups of Lishukang capsule: 400 mg/kg, 600 mg/kg, 800 mg/kg, with 10 mice in each group. The normal control group was fed at the local altitude (1500m) after 7 days of intragastric administration in each group, and the rest groups were fed at the low pressure and hypoxia animal experimental cabin to simulate the altitude of 7500 m for hypoxia for 3 days. During this period, the normal control group and the hypoxia model group were given normal saline once a day, and 1 hour after the last administration, the eight arm maze was used to test the spatial memory ability of mice under simulated high altitude hypoxia; HE staining was used to observe the morphological changes of hippocampus in mice; Western blot was used to detect the changes of protein content of Keap1/Nrf2/HO-1 signal pathway and apoptosis related protein in hippocampus of mice. Results Compared with the normal control group, the spatial memory ability of mice in the hypoxia model group was significantly impaired (P<0.01); HE staining showed that hippocampal neurons in mice were seriously injured; the content of brain tissue Keap1 protein and apoptosis related protein Bax and Caspase-3 increased (P<0.01); the content of Nrf2, HO-1 and apoptosis related protein Bcl-2 decreased (P<0.01). Compared with the hypoxia model group, the error rate of mice in the high dose group of Lishukang capsule in the eight arm maze behavior experiment was significantly reduced (P<0.05, P<0.01); HE staining showed that the neurons were arranged orderly and the cell morphology was good; the content of Keap1 protein and apoptosis related protein Bax and Caspase-3 decreased (P<0.01); the content of Nrf2, HO-1 and apoptosis related protein Bcl-2 increased (P<0.01). Conclusion High altitude hypoxia can lead to oxidative stress injury in mice and induce the expression of apoptosis related genes, thus aggravating the cognitive dysfunction of mice; Lishukang capsule can effectively improve the learning and memory impairment in mice caused by hypoxia, and its mechanism may be related to regulating the Keap1/Nrf2/HO-1 signal pathway and reducing apoptosis.
Accepted Manuscript
, Available online
doi: 10.12206/j.issn.2097-2024.202112011
Abstract:
Objective To determine the content of five alkaloids from extracts of piper longum and test the pharmacodynamic effect of them on rats with experimental myocardial ischemia induced by injection of pituitrin. Methods The content of five alkaloids was determined simultaneously by HPLC. The experimental myocardial ischemia in rats was induced by injection of pituitrin, and the absolute value of T wave change and change of heart rate before and after model establishment were chosen to be the observation index. The effects of large, medium and small dose groups were evaluated. Results Three batches of samples were analyzed, with the contents of piperine for 56.1%, 49.7%, 51.6%; N-isobutyl-(2E,4E)octadecatrienamide for 4.5%, 4.2%, 4.3%; guineensine for 0.46%, 0.38%, 0.40%; piplartine for 1.73%, 1.67%, 1.70% and piperamide for 0.55%, 0.46%, 0.49%, respectively. All dose groups from extracts of piper longum had significantly reduced the absolute value of T wave and almost have no effect on the change of heart rate, except the high dose group showed the effect of reducing heart rate at some time . Conclusion The HPLC method was suitable for the simultaneous determination of five alkaloids from extracts of piper longum. It was shown that extracts of piper longum had good bioactivity in anti-myocardial ischemia.
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2024, 42(8): 319-324.
doi: 10.12206/j.issn.2097-2024.202308062
Abstract:
Chiral drugs are closely related to the safety and effectiveness of drug use. Most dihydropyridine drugs have chiral carbon atoms, which are used as racemes and produce stereoselective disposal characteristics after entering the body, and may affect the safety and effectiveness of drugs. Therefore, based on the chiral resolution and pharmacokinetic characteristics of this class of drugs, the selection rules of chiral HPLC and CE methods and in vivo analysis applications of this class of drugs in recent years were reviewed. The stereoselective pharmacokinetics of this class of drugs were listed and compared. It was found that some of these drugs had obvious differences in stereoselective pharmacokinetics, and the pharmacokinetics and toxicity in vivo were also different.
Chiral drugs are closely related to the safety and effectiveness of drug use. Most dihydropyridine drugs have chiral carbon atoms, which are used as racemes and produce stereoselective disposal characteristics after entering the body, and may affect the safety and effectiveness of drugs. Therefore, based on the chiral resolution and pharmacokinetic characteristics of this class of drugs, the selection rules of chiral HPLC and CE methods and in vivo analysis applications of this class of drugs in recent years were reviewed. The stereoselective pharmacokinetics of this class of drugs were listed and compared. It was found that some of these drugs had obvious differences in stereoselective pharmacokinetics, and the pharmacokinetics and toxicity in vivo were also different.
2024, 42(8): 325-333.
doi: 10.12206/j.issn.2097-2024.202401033
Abstract:
Objective To study the mechanism of antidepressant effect of Baihe Zhimu decoction based on NLRP1 inflammasome. Methods A chronic unpredictable mild stress（CUMS）induced depression mouse model was constructed. C57BL/6J mice were randomly divided into a control group, CUMS group, low-dose Baihe Zhimu decoction group, high-dose Baihe Zhimu decoction group, and MDP group（NLRP1 activator）. After continuous administration for 4 weeks, the behavioral characteristic of mice was investigated. The levels of mice hippocampal inflammatory factors IL-1β、IL-6,TNF-α, and neurotransmitters 5-HT, NE, and DA were detected by ELISA. The expression of inflammasome related proteins NLRP1, ASC, and caspase-1, as well as related proteins in BDNF/TrkB and ERK/AKT/mTOR signaling pathway were detected by Western blot. Immunofluorescence was used to detect changes in BDNF expression in the hippocampus of mice. Results Baihe Zhimu decoction inhibited the activation of NLRP1 inflammasomes in the hippocampus of CUMS mice, improved their behavioral characteristics, increased the level of neurotransmitters in the hippocampus, and reduced the inflammatory response. The NLRP1 activator MDP reversed the above effects of Baihe Zhimu decoction. Baihe Zhimu decoction increased BDNF, TrkB expression, and phosphorylation levels of ERK, AKT, and mTOR proteins, which could be reversed by MDP. Conclusion Baihe Zhimu decoction improved depression like behavior in CUMS mice by inhibiting NLRP1 inflammasome activation and hippocampal neuroinflammatory response, and thereby activating BDNF/TrkB and ERK/AKT/mTOR signaling pathway.
2024, 42(8): 334-340.
doi: 10.12206/j.issn.2097-2024.202303023
Abstract:
Objective To make the cost-effectiveness analysis of pembrolizumab and platinum chemotherapy as the first-line treatment for advanced non-small cell lung cancer （NSCLC） in the population with tumor proportion score （TPS） ≥ 1% of PD-L1, and provide some reference for the clinical use and future price negotiation of pembrolizumab. Methods Based on Pubmed database, the published RCT literatures of pembrolizumab were analyzed, and the survival data were extracted, combined with the treatment plan of a tertiary hospital, the Markov model were established to simulate the cost and health effectiveness of patients for twenty years, and the stability of the model was tested by one-way sensitivity analysis and probability sensitivity analysis. Results Twenty years later, the cost-effectiveness ratio of pembrolizumab group and chemotherapy group was ￥58 517.60/quality adjusted life month (QALM) and ￥41 213.08/QALM. Compared with the chemotherapy group, the incremental cost effective ratio (ICER) was ￥104 485.36/QALM. Conclusion When the willingness to pay （WTP） value was ￥30 902/QALM, the pembrolizumab therapy was not more cost-effective advantages than platinum chemotherapy, and the sensitivity analysis showed that the results of the model were relatively stable.
2024, 42(8): 341-345.
doi: 10.12206/j.issn.2097-2024.202404082
Abstract:
Objective To establish an UPLC-MS/MS method for determinating content of three paclitaxel fatty acid esters such as paclitaxel myristate （PTX-MA）, paclitaxel palmitate （PTX-PA） and paclitaxel myristate （PTX-SA） in mouse plasma, and preliminarily investigate the pharmacokinetic characteristics of their liposomes in mice. Methods Eclipse Plus C8 chromatography column （2.1 mm×50 mm, 1.8 μm） was used with different proportions of 0.2% formic acid aqueous solution （A） and methanol （B） mixture as mobile phase for gradient elution at a flow rate of 0.3 ml/min. The collum temperature was 30℃. The sample injection volume was 10 μl. The triple quadrupole mass series spectrometer was used as multi-reaction monitoring （MRM）. Results PTX-MA, PTX-PA and PTX-SA all exhibited a good linear relationship in the range of 5.0~500.0 ng/ml （r>0.9950 ）. Their RSD of precision, stability, extraction recovery rate and matrix effect test results was all less than 10%. The half-lives （t1/2） for liposomes of three paclitaxel fatty acid esters PTX-MA-L、PTX-PA-L and PTX-SA-L in mice were 14.78 h, 44.49 h and 69.32 h individually, and their clearance rates （CL） were 29.06 L·kg/h, 24.94 L·kg/h and 13.74 L·kg/h, respectively. Conclusion This method had high specificity, sensitivity, easy operation and good stability, which could be used for the determination of paclitaxel fatty acid esters in mouse plasma. The results of pharmacokinetic studies in mice showed that t1/2 for paclitaxel fatty acid esters were significantly prolonged, and the clearance rate were significantly reduced with the length of fatty acid carbon chains increasement, which indicated that esterification of paclitaxel with different chain length saturated fatty acids could obviously alter its in vivo pharmacokinetic properties, which provided scientific basis for the research and development of nano formulations of paclitaxel fatty acid ester prodrug.
2024, 42(8): 346-349.
doi: 10.12206/j.issn.2097-2024.202211047
Abstract:
Objective To study the sedative and hypnotic effects of Yening Capsules and investigate its bioactive mechanism in mice. Methods The mice were randomly divided into control group, estazolam group （0.8 mg/kg）, low, medium and high-dose Yening Capsules groups （400, 600 and 800 mg/kg）. The locomotor activity, latency to persistent sleep, sleep duration and sleep rate were determined respectively in mice via the open field test and injection of pentobarbital sodium in subthreshold and suprathreshold doses. The content of GABA, 5-HT, DA and NE in brain tissue of mice were detected by enzyme-linked immunosorbent assay（ELISA）. Results Compared with the control group, Yening Capsules medium and high dose group （P<0.05, P<0.01）significantly decreased the locomotor activity of mice.The sleep latency in Yening Capsules medium and high dose group were significantly shorten （P<0.05, P<0.05）and the sleep duration （P<0.05, P<0.01）were extended. The sleep rate of Yening Capsules medium and high dose groups （P<0.05, P<0.01） was significantly increased. Compared with the control group, high dose of Yening Capsules can significantly increase GABA (P<0.05), 5-HT (P<0.05), DA (P<0.05), NE (P<0.01) in mouse brain tissue. Conclusion Yening Capsules had obvious sedative and hypnotic effects, and its mechanism may be related to the increasement of GABA, 5-HT, DA and NE level in brain tissue of mice.
2024, 42(8): 350-358.
doi: 10.12206/j.issn.2097-2024.202303048
Abstract:
Objective To predict the potential Q-markers of Abri Herba based on network pharmacology and molecular docking and establish a quality control characteristic. Methods The network relationship of “Abri Herba - component - target - pathway” was constructed by using a variety of databases and the method of network pharmacology. The potential Q-markers of Abri Herba were predicted and then the characteristic Chromatogram of Abri Herba was established by high performance liquid chromatography Results Through the network pharmacological prediction, it was found that the components of abrine hypaphorine, schaftoside in Abri Herba were closely associated with the main targets, such as AKT1, STAT3, HIF1A, GRB2, MMP9, which could act on HIF-1, PI3K-Akt, JAK-STAT and other signaling pathways and have good pharmacological activities to be potential Q-markers of Abri Herba. Then HPLC was used to establish the characteristic according to retention time. Conclusion Through network pharmacology and molecular dock-prediction combined with HPLC detection, the characteristic chromatogram was established with the components of abrine hypaphorine, schaftoside as Q-markers, which could control the quality of Abri Herba by combining the components and pharmacological activities.
2024, 42(8): 359-364.
doi: 10.12206/j.issn.2097-2024.202310015
Abstract:
Objective To explore the ideas and measures to further optimize China’s drug emergency approval system by comparing the drug emergency approval systems in China and other countries. Methods The current situation of China’s drug emergency approval system was analyzed and compared with the relevant systems of the United States, the European Union and Japan. Results The goal of drug emergency approval in other countries is clearly positioned to accelerate the review and listing of urgently needed clinical drugs for the purpose of clinical needs, forming a multi-channel, multi-mode and multi-mechanism priority review system covering the whole process, and the regulatory system is clear, complete, and operable. The corresponding approval system in China started late and is in the stage of continuous improvement, which needs to be improved in terms of system construction, government functions, personnel optimization, and post-market supervision. Conclusion Drug regulatory authorities in China should summarize their past work experience and draw on some feasible approval models and regulatory approaches in foreign countries, further improve the system and process of the drug emergency approval system and enhance the efficiency of drug approval and the ability to protect drugs in response to emergencies.
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Chief Editor: LI Jie Wei
Publication Number:
ISSN 2097-2024
CN 31-2185/R
Website: www.yxsjzz.cn or yxsj.smmu.edu.cn
Email: yxsjzzs@163.com
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