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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

Objective To establish the method for the simultaneous determination of hypoxanthine, inosine, guanosine and adenosine in Dilong formula granules by HPLC and compare the fingerprints of Dilong formula granules from different manufacturers by HPLC chromatogram. Methods The contents of hypoxanthine, inosine, guanosine and adenosine were determined by Thermo Acclaim^TM120C₁₈ column (4.6 mm×250 mm 5 μm). The mobile phase was acetonitrile-water. Gradient elution with flow rate of 0.6 ml/min was used. Column temperature was 25 ℃. Detection wavelength was 254 nm. 10 batches of samples were tested. The HPLC chromatogram were compared and analyzed by using the similarity Evaluation system of chromatographic fingerprint of traditional Chinese Medicine (version 2012.130723). Results The linear ranges for the detection of hypoxanthine, inosine, guanosine and adenosine showed good linear relationships within their own ranges (r≥0.999 9). The average recoveries were 99.20%~102.98% with RSD of 0.26 %~0.71%. The contents of 4 components in 10 batches of samples were 0.740 0~4.457 4 mg/g, 2.132 3~7.805 0 mg/g, 0.325 4~1.596 1 mg/g, 0.537 2~2.222 9 mg/g respectively. The similarity between HPLC chromatogram and control fingerprints of Dilong formula granules from different manufacturers was greater than 0.91. Conclusion The method could be used to determine the contents of hypoxanthine, inosine, guanosine and adenosine in Dilong formula granule. HPLC fingerprints could be used to evaluation the quality in Dilong formula granule. The similarity of HPLC fingerprints from different manufacturer production of Dilong formula granule is high, but 4 contents in composition are difference. More>>

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

Objective To investigate the solubility and stability of Tetrodotoxin (TTX) in different solvents, and the effect of temperature and pH on its stability. Method Solutions of TTX in different matrices were prepared. Their concentrations at different temperatures and pH buffers were determined by high performance liquid chromatography and their solubility and stability were analyzed and calculated. Result TTX was most soluble at pH 3.5 and its solubility decreased as the pH increased. TTX degraded most rapidly under strong alkali conditions, with complete degradation after 20 min of reaction at 0.1 mol/L sodium hydroxide and 70 ℃. The stability test results similarly demonstrated that TTX was least stable under alkaline conditions. In a PBS buffered solution at 37 ℃, pH 7.4, TTX concentration began to decrease consistently at 1~10h, with a degradation rate of 88.07±0.27% after 28 days. Conclusion TTX is readily soluble in acidic aqueous solutions at pH 3.5 and almost insoluble in alkaline aqueous solutions. Its stability is closely related to the temperature and pH of the medium. It is more stable in acidic aqueous solutions and easily degrades under alkaline conditions, and its degradation process could be accelerated by increasing temperature. More>>

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. More>>

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. More>>

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

Objective To study the chemical constituents of Hippocampus trimaculatus Leach. Methods After extracted with ethanol, Hippocampus trimaculatus Leach was isolated and purified by silica gel column chromatography, Sephadex LH-20 gel column chromatography, and reversed-phase C₁₈ column chromatography. The structures of compounds were identified by physical and chemical properties, spectral data and literature comparison. Results Eight compounds were isolated from Hippocampus trimaculatus Leach and identified as L-phenylalanine (1), alanine (2), inosine (3), cholesterol (4), N-acetyltyramine (5), uracil (6), D-mannitol (7), tetrodoine (8), respectively. Conclusion Compounds 5, 7, 8 are isolated from Hippocampus trimaculatus Leach for the first time. More>>

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

Objective To study the release profile of curcumin and piperine from the compound self-microemulsion. Methods The release of curcumin and piperine in vitro was investigated by dynamic dialysis under the condition of phosphate buffer of pH 4.8 and 7.5 with 0.75% Tween-80. Results The cumulative release rates of curcumin in pH 4.8 and pH 7.5 were 94.85% and 84.38% in 108 h, respectively. The cumulative release rates of piperine were 92.85% and 90.05% in 36 h, separately. Conclusion Curcumin and piperine in self-microemulsion have sustained release properties and released more in the acidic environment similar to the environment in tumors. More>>

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

Objective To evaluate the analgesic effect of tetrodotoxin (TTX) in four types of acute pain models and provide experimental support for its rational application. Methods Mice or rats were intramuscularly pretreated with morphine (1 mg/kg) or TTX (0, 0.5, 1, 2, 4 and 8 μg/kg) 40 min before acetic acid writhing test, formalin stimulation test, hot plate test or tail flick test. Pain response or pain threshold were recorded, and inhibition rate was calculated during the tests. The arachidonic acid of serum was determined by Elisa. Results Significant analgesic effects were observed with morphine in all four acute pain models. TTX dose-dependently reduced the number of writhing induced by acetic acid and inhibited the pain response induced by formalin during phase I and phase II, with the highest inhibition rate of more than 80.00% in two pain models. TTX showed analgesic effect in tail flick test and hot plate test, with the highest inhibition rate of 25.00% and 19.79%, respectively. Both acetic acid and formalin increased arachidonic acid in animal serum, but TTX had no significant inhibitory effect on the releasing of arachidonic acid. Conclusion TTX showed significant analgesic effect in the chemical stimulation pain models induced by acetic acid and formalin, but limited analgesic effect was observed on the physical stimulation pain model induced by heat (hot plate and hot water). TTX may produce analgesic effect by blocking the inflammatory mediators mediating pain response. More>>

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

Objective To evaluate the in vitro synergistic antifungal activity of HDAC inhibitors in combination with azole drugs against azoles-resistant Candida strains. Methods The checkerboard microdilution method was used to evaluate the antifungal activity of the HDAC inhibitors in combination with azole drugs against clinically drug-resistant strains. The fungistatic activity and toxicity of Rocilinostat was determined through time-growth curve assay and cytotoxicity assay. Results The compound Rocilinostat combined with azole drugs showed excellent synergistic antifungal activity against a variety of azoles-resistant Candida albicans and Candida glabrata. The combination of high concentration Rocilinostat with FLC exhibited fungistatic effects. Very low toxicity was detected with Rocilinostat towards normal cells. Rocilinostat showed better HDAC inhibitory activity than SAHA. Conclusion As a fungi HDAC inhibitor, Rocilinostat has excellent in vitro synergistic antifungal activity and no severe toxicity to normal human cells. More>>

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

Objective To provide direction for the improvement of quality control of hospital preparations and ensure the safety for clinical use by analyzing the hospital preparation deviations in recent three years. Methods A retrospective analysis on 59 minor hospital preparation deviations from 2017 to 2019 was conducted. Brainstorming, fishbone drawing and, Minitab software were used to analyze the root causes of deviations from five aspects: personnel, machine, materials, methods and environment. The preventive and corrective measures were implemented. The results were evaluated. Results 1 significant deviation (1.7%), 24 major deviation (40.7%), and 34 minor deviation (57.6%) were identified among the 59 casses of preparation deviation. With the implementation of preventive and corrective measures, the total number of deviations in 2018 was significantly reduced compared to that in 2017. The total number of deviations in 2019 was about the same as that in 2018. The human factors need to be focused. Conclusion The pharmaceutical preparation deviations in our hospital have been reduced. The further quality improvements for pharmaceutical preparations will be carried out by following the regulations of pharmaceutical production quality management standards and pharmaceutical production supervision and administration measures. More>>

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

Objective To explore the clinical pharmacist’s role in drug therapy and monitoring for the patient with postoperative MRSA infection. Methods Clinical pharmacists participated in planning anti-infective treatment, antimicrobial medication selection, identification of high-risk factors for MRSA infection, evaluation of vancomycin efficacy, dosage adjustment using TDM technology, monitoring and management of vancomycin adverse reactions. Results With the pharmaceutical care provided by clinical pharmacists, the patient received effective treatment with minimal vancomycin-related adverse reactions. Conclusion Clinical pharmacists played an important role in accelerating patient recovery by rational and safe medication use. More>>

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. More>>

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

Objective To establish and improve the quality standard of ginkgo semen decoction pieces. Methods The morphological character for 29 batches of ginkgo gemen and 12 batches of stir-fried ginkgo gemen were observed, and the moisture contents were assayed using the method in Chinese Pharmacopoeia 2015 edition, the first supplement. Results The character of ginkgo gemen and stir-fried ginkgo gemen were consistent in different batches. The moisture content of ginkgo gemen was 8.8% to 12.2%, with an average of 10.5%. The moisture content of stir-fried ginkgo gemen was from 5.4% to 12.3%, with an average of 8.9%. Considering that ginkgo semen decoction pieces are stored for a long time, they are prone to the attack of mildew and insects, and the moisture limit is set to be no more than 10.0% in ginkgo gemen and stir-fried ginkgo. Conclusion Compared with the Chinese Pharmacopoeia 2015 edition, the first supplement, the character identification for ginkgo semen decoction pieces was added and the quality standards were improved. The moisture content of ginkgo semen decoction pieces needs to be strictly controlled under 10.0% to prevent mildew and insects. More>>

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

Objective To synthesize the natural cyclopeptide auyuittuqamide A by Fmoc-based solid phase linear synthesis and liquid phase cyclization. Methods Using 2-chlorotriphenylmethyl chloride (CTC) resin as the solid support, 1,3-diisopropylcarbodiimide (DIC) and 1-hydroxybenzotriazole (HOBt) as the condensing agents, 9-fluorenylmethoxycarbonyl (Fmoc) to protect amino acids were assembled in sequence, and then the linear peptide bearing the protected groups was obtained in presence of trifluoroethanol (TFE) cutting reagent. The protected linear peptide was cyclized with the aid of benzotriazole hexafluorophosphate (PyBOP) and 1-hydroxybenzotriazole (HOBt) in dichloromethane (DCM) solution, followed by trifluoroacetic acid (TFA) deprotection to obtain the cyclic peptide, auyuittuqamide A that was purified by preparative HPLC and characterized by HR-MS and 500MHz ¹H-NMR. Results The purity of auyuittuqamide A was more than 95% and the total yield was 5.48%. Conclusion This method has simple synthesis steps and high yield. It is the first to establish a fully synthesis method for the natural cyclic peptide auyuittuqamide A, which lays the foundation for further research of auyuittuqamide A. More>>

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

Objective To study the chemical constituents of Aspergillus terreus from sponge epiphytic fungal. Methods Sephadex LH-20 column chromatography, silica gel column chromatography and high performance liquid chroma-tography were used to separate and purify the compounds. The structures of compounds were identified by spectroscopic data. The α-glucosidase inhibitory activity and antioxidant activity of the compounds were tested by PNPG and DPPH methods, respectively. Results Eight compounds were isolated from Aspergillus terreus and identified as methyl-3,4,5-trimethoxy-2-(2-(nicotinamido) benzamido) benzoate ( 1 ), terrelumamide A ( 2) , emeheterone ( 3 ), (8R,9S)-dihydroisoflavipucine ( 4 ), (8S,9S)-dihydroisoflavipucine ( 5 ), cyclo(S-Pro-S-Phe) ( 6 ), brevianamide F ( 7 ), terrein ( 8 ). Compound 3 showed strong inhibitory activity against α-glucosidase and the IC₅₀ value was 14.28 μmol/L. Conclusion Compounds 3 , 4 , 5 , and 7 were obtained from Aspergillus terreus for the first time. More>>

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. More>>

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

Objective To establish the quality standard of compound Yuhong suppository. Methods Angelica dahurica, colophony and Sophora flavescens Alt. were identified by thin layer chromatography（TLC）method. The contents of sulfadiazine and dyclonine hydrochloride were determined by HPLC with diode array detection method. The mobile phase was methanol-0.02 mol/L potassium dihydrogen phosphate (adjusted to pH 3.3 with phosphoric acid) for gradient elution. The detection wavelength was 280 nm for sulfadiazine and dyclonine hydrochloride. Results The three Chinese traditional medicines were identified by TLC with clear spots. The linear ranges of sulfadiazine and dyclonine hydrochloride were good in 12.40-99.20 μg/ml (r=0.999 9) and 2.56-20.48 μg/ml (r=0.999 9). The average recovery was (99.21±0.43) % (n=9) and (99.54±0.68) % (n=9). Conclusion This method is accurate, sensitive, and reproducible. It can be used as a standard method for the quality control of compound Yuhong suppository. More>>

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

Objective Nicotinamide phosphoribosyltransferase (Nampt) is a new therapeutic target for ischemic stroke. The aim of this study was to investigate protective effect of liver-derived Nampt on ischemic stroke. Methods Liver-specific Nampt knockout mice were generated using the Cre/loxP system. Nampt^loxP/loxP mice were crossed with liver-specific Cre recombinase expression mice (Alb-Cre), and the progeny genotypes were identified by polymerase chain reaction. Body weight of knockout mice and control mice were measured. Nampt in liver and brain was determined by Western blot assay. Middle cerebral artery occlusion (MCAO), a classical ischemic stroke model, was generated in liver-specific Nampt knockout mice and control mice by electrocoagulation. After 24 h of modeling, neurological deficit scores of each group were evaluated and TTC staining was performed to determine the cerebral infarction volume. The level of plasma Nampt in each group was determined by ELISA. Results Liver-specific Nampt knockout mice with the genotype of Nampt^loxP/loxPAlb-Cre were successfully constructed. The hepatic Nampt expression in knockout mice was significantly decreased by 74.2% compared to control mice, while there was no significant difference in the expression of brain Nampt protein between the knockout group and the control group. Specific knockout of liver Nampt gene expression had no effect on the body weight of mice. Under normal physiological conditions, there was no significant difference in plasma Nampt levels between liver-specific Nampt knockout mice and control mice of the same gender. 24 h after MCAO modeling, there were no significant differences in neurological deficit scores, cerebral infarct volume and plasma Nampt concentration between liver-specific Nampt knockout group and control group. Conclusion Liver-specific Nampt knockout mice are successfully constructed. Liver-derived Nampt has no significant protective effects on ischemic stroke. More>>

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

Objective To improve the quality standards of Kunxian capsules (KC) and effectively control the product quality. Methods Triptolide, icariin and hypericin were used as the indicator components, to increase or improve the thin layer chromatography (TLC) identification methods of Kunming begonia, epimedium and dodder. Agilent ZORBA SB-C₁₈ (4.6 mm×250 mm, 5 μm) as a chromatographic column, the HPLC method for the determination of triptolide was improved with acetonitrile-0.1% formic acid solution as the mobile phase and 220 nm as the detection wavelength. Results The spots in the TLC method of Kunming begonia, epimedium and dodder has strong specificity, good and clear separation of characteristic spots, negative and no interference. The quantitative analysis of the content of triptolide in KC showed that there is a good linear relationship (r=0.9995) between the mass concentration of triptolide and the peak area in the range of 40.16-502.00 μg/ml, the average recovery was 98.12%, RSD was 8.25%, and the accuracy was good. Conclusion The TLC identification method and HPLC method established in this experiment have strong specificity and good reproducibility, and can effectively control the quality of KC. More>>

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. More>>

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

Objective To assay the contents of acetaminophen with ultra high-performance liquid chromatography (UHPLC) method in the sustained-release tablets radiated by Gamma ray. Methods Acetaminophen sustained-release tablets were radiated by ⁶⁰Co. UHPLC equipped with the Shim-pack GISS-C₁₈（2.1 mm×50 mm, 1.9 μm）was used for the assay. The mobile phase was methanol-0.05 % ammonium acetate solution (15∶85). The flow rate was 0.3 ml/min with the detection wavelength at 245 nm. Results The acetaminophen showed good linear relationship within the range of 20-100 μg/ml (r=0.999 4). The RSD values of repeatability was 0.9 %. The average recovery was 97.9 %-104.9 %. Acetaminophen content was 96.2 %, 92.2 %, 91.8 %, 83.9 % at 0, 8, 50 and 80 kGy radiation, respectively. Conclusion This method is speedy and accurate. It can be used to assay the content of acetaminophen in the sustained-release tablets after radiation. The content of acetaminophen decreased after radiation. More>>

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

Objective To establish a rapid prediction method of the antioxidant activity in aqueous extract solutions of Melastoma dodecandrum based on ultraviolet spectroscopy and partial least squares regression algorithm. Methods The DPPH free radical scavenging effect was used to characterize the antioxidant activity of aqueous extract solutions of Melastoma dodecandrum. The ultraviolet spectra of 190-600 nm were collected. The partial least squares regression model of antioxidant activity was established after optimizing the wavelength range and preprocessing method. The software was devised using Visual Basic as the integrated development environment to provide a convenient tool for the rapid determination of antioxidant activity. Results The optimal partial least squares regression model was established based on 200-290 nm as wavelength range and unit variance scaling as preprocessing method. The correlation coefficient of calibration, root mean square error of estimation, root mean square error of cross-validation was 0.887, 2.20% and 2.17%, respectively. The correlation coefficient of validation, root mean square error of prediction was 0.868, 2.08%. The average predicted recovery was 100.1±2.3%. With the predictive function in the software, the antioxidant activity of aqueous extract solution of Melastoma dodecandrum can be calculated automatically within 2 s after collecting the ultraviolet spectra. Conclusions This study provides a rapid method for the prediction of antioxidant activity in aqueous extract solutions of Melastoma dodecandrum. More>>

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

Objective To explore the effect of circadian rhythm genes on flavonoids biosynthesis in safflower and its molecular mechanism. Methods Based on the transcriptome and metabolomic database of safflower corolla, we screened the circadian rhythm genes that correlate with biosynthesis of flavonoids in safflower. qPCR was used to quantify the expressions of circadian rhythm genes in different flowering stages at different time points in a single day. LC-MS was performed to determine the accumulation of flavonoids. The correlation between them was analyzed as well. Yeast Two-Hybrid experiment was used to verify the interactive proteins of these genes. Results Seven circadian rhythm genes PRR1, PRR2, ELF3, FT, PHYB, GI and ZTL were obtained. PRR1 gene was positively correlated with flavonoids accumulation (r≥0.7). The full length of PRR1 is 3 201 bp, encoding 421 amino acids, which is highly homologous with rice OsPRR73 gene and named as CtPRR1 (GenBank accession number: MW492035). CtPRR1 was mainly expressed in flowers, and the expression level increased in the daytime and declined in the evening gradually. Correspondingly, the content of flavonoids showed an opposite variation. Both of them displayed a circadian rhythm with a negative correlation (r≥−0.7). In addition, 2 heat shock proteins along with 3 AP2 transcription factors interacting with CtPRR1 protein were obtained via Yeast Two-Hybrid experiment. Conclusion CtPRR1 negatively regulated the safflower flavonoids accumulation in a circadian rhythm way, which may be affected by these interacting proteins. More>>

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In vivo pharmacokinetics of silymarin phospholipid complex microporous osmotic pump-controlled release tablets in beagle dogs and evaluation of in vitro-in vivo correlation

ZENG Qiping, YANG Lina, LIU Jianqing, SONG Hongtao

In Press doi: 10.12206/j.issn.2097-2024.202206052

Abstract(11) HTML(7) PDF (1181KB)(1)

Abstract:
Objective To evaluate the release characteristics in vitro, pharmacokinetics in rabbits and in vivo-in vitro correlation of silymarin phospholipid complex microporous osmotic pump controlled release tablets（SM-PC MPOP）. Methods The release characteristics of SM-PC MPOP in vitro were detected by HPLC in the artificial gastric fluid. Six beagle dogs were subjected to double cycle cross control, which were given SM-PC MPOP and Legalon（30 mg/kg）. The concentration of silybin in plasma was determined by HPLC and the data were processed by software. Results The cumulative release rate of SM-PC MPOP in vitro was over 85% in 12 h. The pharmacokinetics in beagle dogs showed that SM-PC MPOP and legalon conformed to double compartment first-order absorption model and the pharmacokinetic parameters were obtained: t_max:（3.2±0.4）and（0.9±0.1）h, C_max:（0.298 6±0.068 9）and（0.629 9±0.076 5）μg/ml, AUC_0→24:（2.996 8±0.583 3）and（2.268 9±0.432 8）h·μg /ml. The relative bioavailability of SM-PC MPOP was（162.21 ± 30.82）%. Conclusion SM-PC MPOP could release slowly, which could increase the relative bioavailability significantly. The correlation between the absorption in vivo and release in vitro was fine（r = 0.839 0）.

Effects of metformin hydrochloride tablets on clinical efficacy and number of dominant follicles in polycystic ovary syndrome

LI Hui, TANG Huaiyun, GUAN Huijuan, ZHANG Shuai

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202208080

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Abstract:
Objective To explore the effect of metformin hydrochloride tablets on the clinical efficacy, number of dominant follicles and ovarian volume of polycystic ovary syndrome. Methods 150 patients diagnosed with polycystic ovary syndrome who were diagnosed and treated in our hospital from January 2019 to March 2021 were selected .The patients were divided into observation group and control group by random number table. The control group was treated with letrozole + gonadotropin, and the observation group was treated with letrozole + gonadotropin + hydrochloric acid + Metformin tablets. The clinical efficacy, endometrial thickness, number of high-quality follicles, sex hormone levels, blood lipid levels, and adverse reactions were compared between the two groups. Results ① The effective rate of treatment in the observation group was 90.67%, which was significantly higher than that in the control group, 78.67% (P<0.05). ② After treatment, the endometrial thickness of the observation group was lower than that of the control group, and the number of high-quality follicles was more than that of the control group. (P<0.05). ③ After treatment, the levels of Luteinizing Hormone-LH, Follicle Stimulating Hormone-FSH and Testosterone (T) in the observation group were lower than those in the control group (P<0.05). ④ After treatment, the total cholesterol (TC) and triglyceride (TG) in the observation group were lower than those in the control group (P<0.05). ⑤ The incidence of adverse reactions in the observation group was 8.00%, which was significantly lower than 20.00% in the control group (P<0.05). Conclusion Letrozole + gonadotropin + metformin hydrochloride tablets could significantly improve the sex hormone and blood lipid levels in patients with polycystic ovary syndrome, relieve the symptoms of the patients, and improve their uterine condition, which had a good clinical effect.

Exploration on the potential therapeutic mechanism of artemisinin in polycystic ovary syndrome based on network pharmacology and molecular docking technology

YU Weili, WEI Yifang, YE Zishao, LIU Aifen, WANG Chengniu, ZHANG Lei

In Press doi: 10.12206/j.issn.2097-2024.202209051

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Abstract:
Objective To explore the potential mechanism of artemisinin in the treatment of polycystic ovary syndrome (PCOS) by network pharmacology and molecular docking technology. Methods The corresponding targets of natural product artemisinin were obtained from PubChem, Swiss Target Prediction and PharmMapper databases, targets related to PCOS were obtained through GeneCards and DisGeNET databases; the intersection target genes of Artemisinin and PCOS were screened by Draw Venn diagram. Then the protein-protein interaction network (PPI) was constructed according to the intersection target genes through the STRING Database, and the core targets were screened by Cytoscape. Besides, gene ontology (GO) function and Kyoto encyclopedia of genes and genomes (KEGG) pathway analysis was performed by DAVID Database, and finally the data were analyzed visually by the online platform. Molecular docking of artemisinin and core targets were performed by Chemdraw, Pymol, Auto Dock Tools and RCSB PDB database. Results A total of 229 targets of artemisinin and 1292 targets of PCOS were screened out, 90 overlapping targets were obtained by Draw Venn diagram, and 5 potential core targets, AKT1, ESR1, MMP9, PPARG, MMP2, were mainly act on PI3K Akt, MAPK, RAS, endocrine resistance and other signal pathways. Molecular docking results showed that there were molecular binding sites between artemisinin and core targets. Conclusion It is preliminarily analyzed that artemisinin may play a therapeutic role in PCOS through multiple targets and mechanisms.

Design, synthesis and biological evaluation of 8-hydroxyquinoline derivatives as potential clostridium difficile antibiotics

YE Tengfei, CHENG Tao, SONG Ping, JI Weili, BIAN Xiaolan

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202303021

Abstract(97) HTML(36) PDF (1321KB)(6)

Abstract:
Objective To find a more effective alternative therapy for antibiotic therapy and fecal microbiota transplantation in current primary treatment of clostridioides difficile infection (CDI) because of the high recurrence rate. Methods A series of 8-hydroxyquinoline derivatives were designed and synthesized based on the hit molecule within the research group. Results The activity test against C. difficile showed that most of the molecules exhibited good antibacterial activity against C. difficile, and compounds 8 and 9f showed attractive anti-C. difficile activity. Conclusion A new type of 8-hydroxyquinoline derivatives with anti-clostridium difficile was found, which could be used as good lead compounds for further development.

Study on the treatment compliance and influencing factors of inhalation therapy in patients with stable chronic obstructive pulmonary disease

DUAN Hu, ZHOU Yanqing, QIAN Yulin, ZHAO Liang

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202204094

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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 our hospital from June to December in 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≥10 points, used 2 inhalation devices and inhalation technique score ≥8 points had better compliance (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 device should be strengthened and regularly follow-up evaluation should be carried out.

Study on the usual practices of traditional Chinese medicine in treatment of postembolization syndrome after TACE based on data mining

ZHONG Zhipeng, GUO Bingjie, XIAO Chulan, YIN Zifei, LI Bai

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202208101

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Objective To explore the usual practices of traditional Chinese medicine (TCM) in the treatment of postembolization syndrome (PES) after transcatheter arterial chemoembolization (TACE). Methods CNKI, WANFANG and VIP were used as data sources to search the journals and literatures related to TCM treatment from January 2000 to December 2021. Then, relevant TCM formula or Chinese patent medicines preparations were screened out. The Chinese medicinal materials contained were entered into Excel2019 table database, and the data were analyzed by SPSS Statistics 21.0 and SPSS Modeler 18.0 statistical software. Results 86 qualified prescriptions were included, containing 181 Chinese medicinal materials, with a total frequency of 942 times. Of the 181 Chinese herbs included, there were 28 herbs with frequency≥10%, with a total frequency of 587. The top 5 Chinese medicinal materials of frequency were licorice, Poria, Atractylodes, Bupleurum and Astragalus. Among the efficacy classifications, tonifying deficiency drugs, heat-clearing drugs and diuretics are most used. In four properties and five tastes, the top three of four properties were warm, flat and cold, and the top three of five tastes were sweet, bitter and pungent. In the classification of meridians, the first three meridians are spleen meridian, lung meridian and liver meridian. 30 association rules were obtained in association rules analysis, 11 common factors were obtained by factor analysis, 6 clustering combinations were obtained by cluster analysis, and 4 commonly used drug combinations were obtained. Conclusion The prescription drugs for the treatment of PES after TACE are mainly tonic drugs, heat-clearing drugs and diuresis and dampness-draining drugs. The treatment methods are mainly invigorating spleen and replenishing qi, clearing heat and dampness and detoxification.

Advances in metabolomics of cholangiocarcinoma

HE Yongping, JIAO Yang, LIU Yue

In Press doi: 10.12206/j.issn.2097-2024.202211025

Abstract(348) HTML(113) PDF (886KB)(7)

Abstract:
As a highly malignant tumor, the diagnosis of cholangiocarcinoma (CCA) is often late and the prognosis is poor for which the early symptoms are atypical and the lack of accurate biomarkers. Metabolomics is an emerging science that researches the alterations of all endogenous small molecule metabolites in an organism under the influence of pathological, physiological or genetic modification. The development and progress of CCA is closely related to metabolism. Metabolomic is characterized by global analysis, high throughput and reflects real-time alterations in biology system, providing a new avenue for biomarker screening and diseases diagnosis and treatment. The advances of metabolomics studies on CCA in the recent years were reviewed in this paper which could provide the reference for further research.

Research progress on transcription factor ZNF24 in Tumors

TIAN Shuo, LI Jianzhong

In Press doi: 10.12206/j.issn.2097-2024.202204043

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The transcription factor ZNF24 (also known as ZNF191 or KOX17) is a member of the Krüppel-like zinc finger transcription factor family, with a leucine-rich (Leu) SCAN domain (also known as LeR domain) at the N-terminus and four consecutive typical Kruppel-like zinc finger modities at the C-terminus. ZNF24 is a multifunctional transcription factor involved in the regulation of kinase transcriptional activity, vascular proliferation and development, especially in tumorigenesis and tumor progression. ZNF24 plays an important and complex dual-directional regulation role (promoting and inhibiting) in tumor development, invasion and metastasis by regulating the transcriptional expression of different target genes (such as VEGF, Wnt8B, Twist1, β-catenin and DGL1, etc.) and the competitive binding with protein factors (such as β-catenin). Therefore, elucidating the mechanism of ZNF24 in tumors would provide clues and ideas for the treatment of tumors. The researches status of ZNF24 in tumors were summarized in this paper.

Pharmaceutical care in a case of myocardial infarction complicated with antithrombotic therapy after tricuspid valve repair

LIU Yulan, LIU Mei, LU Yi, BI Hui, XU Guili

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202204122

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Objective To investigate the antithrombotic therapy for acute myocardial infarction patients after PCI stenting combined with tricuspid valve repair. Methods The risk of bleeding and embolization was evaluated, relevant data were reviewed, professional knowledges of pharmacy were utilized through the whole treatment process, individualized medication plan for patients was designed and used. Results A better therapeutic effect was achieved through the implementation of pharmaceutical care and medication education to the patients. Conclusion Clinical pharmacists carry out pharmaceutical care in antithrombotic drugs utilities to improve the safety level of drug use and provide basis for clinical rational drug use.

Preparation and cytotoxicity of doxorubicin-containing gold nanoparticles

XU Ziyi, SUN Yuhan, FAN Li, LU Guangzhao, ZHANG He

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202308043

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Abstract:
Objective Construction of methoxy polyethylene glycol (mPEG) modified gold nanoparticles (AuNPs) loaded with doxorubicin (DOX) AuNPs-mPEG@DOX to reduce the toxicity and side effects of DOX. Methods AuNPs-mPEG@DOX was prepared and characterized by Z-Average, Zeta potential and UV-Vis spectroscopy. The impact of thiol-linked DOX (HS-DOX) at various dosage concentrations on the drug adsorption rate and drug loading of AuNPs-mPEG@DOX was investigated. Furthermore, a HPLC method was developed to accurately determine the content of unadsorbed HS-DOX in AuNPs-mPEG@DOX. The specificity, linearity, precision, stability and average recovery of this method were thoroughly investigated. The cytotoxic effect of AuNPs-mPEG@DOX on MCF-10A and MCF-7 cells was evaluated using a CCK-8 assay. Results AuNPs-mPEG@DOX was successfully prepared with Z-Average of 46.12±0.49 nm, Zeta potential of 18.60±1.51 nm and the maximum absorption wavelength of 530 nm. An efficient HPLC method for the detection of unadsorbed HS-DOX in AuNPs-mPEG@DOX was devised. The optimal dosage concentration of HS-DOX for AuNPs-mPEG@DOX was determined to be 11.18 μg/ml, resulting in a drug adsorption rate of (9.21±2.88)% and a drug loading rate of (2.01±0.62)%. Cytotoxicity experiments demonstrated that AuNPs-mPEG@DOX significantly reduced the toxic and side effects of DOX on normal breast cells. Additionally, AuNPs-mPEG@DOX and free DOX exhibited comparable cytotoxic effects on breast tumor cells when DOX concentration was equal to or greater than 4.75 μmol/L. Conclusion AuNPs-mPEG@DOX effectively reduce the toxicity of DOX, providing a reference for future research on reducing the toxicity of AuNPs-linked drugs.

Mechanism of Qizhen Ziyin mixture in the treatment of hypogonadism based on network pharmacology analysis and molecular docking

PAN Yujiong, HE Zhigao, CHEN Shixiu, ZHOU Gui, ZHOU Xin, YU Chao

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202208111

Abstract(217) HTML(69) PDF (3499KB)(10)

Abstract:
Objective To investigate the mechanism of Qizhen Ziyin mixture in the treatment of hypogonadism by using the network pharmacology approach. Methods The active components of Qizhen Ziyin mixture were obtained by searching TCMSP , TCMID and HIT databases; The related targets of candidate compounds were obtained by searching STITCH databases. The potential targets of Qizhen Ziyin mixture in the treatment of hypogonadism were obtained by mapping the disease genes of hypogonadism with Genecards and DisGeNet databases. The protein interaction platform database (STRING) was used to construct the interaction relationship between action targets. The target protein interaction (PPI) network was constructed by introducing Cytoscape software. The mechanism of Qizhen Ziyin mixture in the treatment of hypogonadism was explained through the enrichment analysis of GO, KEGG and molecular docking technology. Results a total of 148 drug-disease chemical compound, 96 drug-disease intersection targets,1085 disease targets were obtained; the components for treating diseases are: quercetin, kaempferol, luteolin, etc.; go enrichment analysis revealed 1792 biological processes (BP), 31 cellular components (CC) and 79 molecular functions (MF); the results of KEGG pathway enrichment analysis indicate such as FOXO signaling pathway, prostate cancer, AGE-RAGE signaling pathway in diabetic complications, HIF-1 signaling pathway, etc.; The results of molecular docking showed that kaempferol and LEP had the best and stable binding energy. Conclusion The active components of Qizhen Ziyin mixture may play a role of the treatment of hypogonadism by improving insulin resistance and the expression of testosterone synthetase of Leydig cells.

Effects of light regulation on the synthesis of secondary metabolites in medicinal plants

ZHANG Wei, MENG Xiangqing, SU Xiaohui, WANG Jinyi, LI Lihua, JIA Min

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202305027

Abstract(265) HTML(163) PDF (1286KB)(18)

Abstract:
Secondary metabolites of medicinal plants are extremely important to human health because of their special pharmacological activities or efficacy. They are the main source of drugs, health care products, and cosmetics. As human beings continue to pursue health and longevity, the demand in the pharmaceutical market continues to grow. It becomes especially important to improve the production and quality of secondary metabolites of medicinal plants. Plant secondary metabolites are an adaptation of plants to their environment and are the result of the interaction between plants and biotic and abiotic factors during the long-term evolution process. The production and accumulation of secondary metabolites in medicinal plants are mainly affected by plant genetic factors and environmental factors. Among them, light environment is extremely important for their synthesis. Therefore, light regulation has long been a research focus for many scholars in China and abroad. In this article, we will review the recent research progress on the effects of light regulation on the secondary metabolites of medicinal plants, mainly focusing on the effects of light quality, light intensity and photoperiod, in order to provide theoretical basis and practical guidance for the efficient production of secondary metabolites with important pharmacological activities.

Network pharmacology study on the treatment of cerebral infarction with Chinese medicine Shenmajingfu granule

XU Yi, HE Ruihua, HUANG Jin

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202303013

Abstract(297) HTML(123) PDF (5133KB)(9)

Abstract:
Objective To explore the material basis and mechanism of the Chinese medicine Shenmajingfu granules in the treatment of cerebral infarction. Methods The potential active ingredients and targets of Shenmajingfu granules were retrieved through TCMSP, ETCM database and TCM Database. The related target genes of cerebral infarction were searched from OMIM database. The common targets of Shenmajingfu granules and cerebral infarction were obtained by the intersection method. Cytoscape was used to construct active components of Shenmajingfu granules-targets network. Protein-protein interaction network was constructed by STRING software. By using DAVID database was used for GO and KEGG enrichment analysis. Results The 183 potential active ingredients of Shenmajingfu granules were screened out. 1785 potential targets were screened in the TCMSP database, including 30 targets related to cerebral infarction. These target genes were mainly involved in the inflammatory response and apoptosis process, involving the TNF signaling pathway, HIF-1 signaling pathway and NF-κB signaling pathway. Conclusion The therapeutic effect of Shenmajingfu granules on cerebral infarction may be related to the regulation of inflammatory response, improvement of impaired neurological function and protection of cerebral ischemia-reperfusion injury.

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

MENG Panpan, SONG Muge, YANG Shichao, CHEN Keming, YANG Zhongduo, MA Huiping

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202303006

Abstract(252) HTML(77) PDF (2083KB)(6)

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.

Progress on the relationship of aldehyde dehydrogenase 2 with human diseases and its small-molecule activators

SUN Xiangpei, GAO Xing, ZHAO Fengping, WANG Wentao, ZHANG Tianyi, TIAN Wei, ZHENG Canhui, CHEN Xin

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202302038

Abstract(343) HTML(125) PDF (1987KB)(20)

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Aldehyde dehydrogenase 2 (ALDH2) is an important shield from the damage occurring under oxidative stress in human body, and a high proportion of East Asians carry ALDH2 inactive mutation gene. There are many diseases closely related to ALDH2, such as cardiovascular diseases, neurodegenerative diseases and liver diseases. Recent studies also found that ALDH2 is associated with ferroptosis. Therefore, ALDH2 has becoming a potential target for the treatment of the above related diseases. Several types of small molecule activators with potential value for clinical application have been reported. The research progress on the structure and function of ALDH2 , the relationship with human diseases and its activators were summarized in this paper.

The improvement of gefitinib-resistance of PC9/GR by thapsigargin combined with gefitinib

DU Jiangyuan, ZHANG Lanlin, CAI Tongkai, CAO Yongbing

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202209018

Abstract(283) HTML(94) PDF (1568KB)(7)

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Objective To study the effect and mechanism of the thapsigargin combined with gefitinib on the proliferation of human lung adenocarcinoma gefitinib resistance cell line PC9/GR. Methods The cell viability of PC9/GR treated with gefitinib alone or gefitinib combined with thapsigargin was evaluated by CCK8 assay; The flow cytometry was used to analyze the PC9/GR cell apoptosis indued by the two group drugs; The ATF-6 and IRE1α protein expression of PC9/GR cells treated with the two group drugs were detected by Western blotting. Results The group of drug combination exhibited enhanced ability to inhibit cell proliferation, promote cell apoptosis and upregulate the ATF-6 and IRE1α protein expression of the PC9/GR compared with the group gefitinib used alone. Conclusion The sensitivity of PC9/GR to gefitinib was increased when the cells were treated by thapsigargin, which may be related with the state of endoplasmic reticulum stress(ERS) induced by thapsigargin.

Anti-fatigue activity of selenium nanoparticles functionalized by polysaccharides from Pleurotus tuber-regium sclerotium

ZOU Si, WU Yanbin, WU Jinzhong, WU Jianguo, WONG Kahing

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202206072

Abstract(252) HTML(127) PDF (1745KB)(6)

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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 L/HPTR-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 L/HPTR-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 L/HPTR-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.

Determination and effect of five alkaloids from extracts of Piper longum on rats with experimental myocardial ischemia induced by injection of pituitrin

YI Bowen, LIU Huining, ZHENG Rui, REN Jiawei, LIU Yang

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202112011

Abstract(611) HTML(268) PDF (999KB)(7)

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.