药学实践与服务

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Synthesis of paclitaxel palmitate and the formulation optimization of its liposomes 紫杉醇棕榈酸酯的合成及其脂质体的制备与处方研究

CHEN Bingchen, WANG Sizhen, GUO Beibei, YANG Feng

2024, 42(9): 379-384, 410. doi: 10.12206/j.issn.2097-2024.202404062

Objective To improve the cellular uptake efficiency and the therapeutic effect 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 met 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. More>>

Establishment of mouse model of hand-foot syndrome induced by capecitabine 卡培他滨致小鼠手足综合征模型的建立及评价

WANG Peng, CHEN Shun, ZHAO Yi, GAO Shouhong, et al

2024, 42(9): 385-388, 398. doi: 10.12206/j.issn.2097-2024.202308045

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), to evaluate whether the animal model of hand-foot syndrome was successfully constructed through H&E staining of mouse foot skin samples and observe 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 was successfully established. Differences in exposure levels of capecitabine and metabolites may not be the cause of hand-foot syndrome. More>>

Pharmacodynamic effects of Qiwei Zhigan prescription on non-alcoholic steatohepatitis in animal model 七味脂肝方对非酒精性脂肪性肝炎动物模型的药效学评价

YANG Jianing, ZHAO Yiying, XIAO Wei

2024, 42(9): 389-398. doi: 10.12206/j.issn.2097-2024.202404096

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 index 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. More>>

Determination of phosphorus content in calcium hydrogen phosphate tablets by ³¹P-qNMR 核磁共振磷谱法测定磷酸氢钙咀嚼片中药物含量

XIA Zhewei, ZENG Yuanye, ZHU Haifei, LI Yu, et al

2024, 42(9): 399-401, 406. doi: 10.12206/j.issn.2097-2024.202404063

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 + 0.1836C. 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. More>>

Simultaneous determination of five flavonoids in Ganmao’an granules by HPLC-MS/MS HPLC-MS/MS同时测定感冒安颗粒中5种黄酮成分的含量

CHEN Fangjian, LUO Jinqian, WANG Zhijun, HU Yeshuai, et al

2024, 42(9): 402-406. doi: 10.12206/j.issn.2097-2024.202403030

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. More>>

Advances in chiral analysis and stereoselective pharmacokinetics of dihydropyridine calcium antagonists 二氢吡啶类钙离子拮抗药物手性分析及其立体选择性药动学研究进展

ZHANG Yixin, GUAN Xinyi, WANG Boning, WEN Jun, et al

2024, 42(8): 319-324. doi: 10.12206/j.issn.2097-2024.202308062

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. More>>

Exploration of the antidepressant mechanism of Baihe Zhimu decoction based on NLRP1 inflammasome 基于NLRP1炎症小体探讨百合知母汤抗抑郁的作用机制

YUE Chunhua, BEN Yongguang, WANG Haiqiao

2024, 42(8): 325-333. doi: 10.12206/j.issn.2097-2024.202401033

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. More>>

Pharmacoeconomic evaluation of pembrolizumab versus platinum chemotherapy as first-line treatment in advanced non-small cell lung cancer 帕博利珠单抗与铂类化疗方案在晚期非小细胞肺癌一线治疗中的药物经济学评价

SONG Yutong, XIA Derun, GU Heng, TANG Shaowen, et al

2024, 42(8): 334-340. doi: 10.12206/j.issn.2097-2024.202303023

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. More>>

Determination and pharmacokinetics investigation of prodrugs of paclitaxel fatty acid esters in mouse plasma by UPLC-MS/MS UPLC-MS/MS法测定小鼠血浆中紫杉醇脂肪酸酯前药及其药代动力学研究

CHEN Bingchen, TONG Dafeng, WAN Miao, YAN Feihu, et al

2024, 42(8): 341-345. doi: 10.12206/j.issn.2097-2024.202404082

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 （t_1/2） 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 t_1/2 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. More>>

Prediction of characteristic chromatogram for Abri Herba based on network pharmacology and molecular docking 基于网络药理学与分子对接预测鸡骨草特征图谱研究

ZHANG Chengzhong, ZHU Xueyan, BU Qitao, WANG Hongrui, et al

2024, 42(8): 350-358. doi: 10.12206/j.issn.2097-2024.202303048

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. More>>

The roles of Bajitianwan formula on Aβ-injured osteoblasts and the mechanism based on network pharmacology 巴戟天丸组方对Aβ损伤成骨细胞的作用及基于网络药理学的机制研究

JIANG Tao, XU Weifan, JIANG Yiping, XIA Tianshuang, et al

2024, 42(7): 285-290, 296. doi: 10.12206/j.issn.2097-2024.202305011

Objective To explore the effect of Bajitianwan（BJTW）formula on bone formation of Aβ-injured osteoblasts and its mechanism. Methods Osteoblasts isolated from neonatal 24-hour Wistar rats were used for the study, and osteoblasts were subjected to damage with Aβ1-42 oligomers, and pharmacological intervention was performed with the aqueous extract of BJTW formula. The MTT assay, alkaline phosphatase（ALP）activity assay, catalase（CAT）activity assay, superoxide dismutase（SOD）activity assay, glutathione（GSH）activity assay and malondialdehyde（MDA）activity assay were carried out respectively. The expression levels of bone morphogenetic protein 2（BMP2）, osteogenic specific transcription factor（RUNX-2）and osteoprotective protein（OPG）were detected by Western blotting. After confirming the effect of BJTW formula on Aβ-injured osteoblasts, the network pharmacology method was used to predict the potential pathways. Results The BJTW formula significantly promoted the proliferation of Aβ-injured osteoblasts, increased ALP, SOD and GSH activity, inhibited MDA activity, and promoted the expression of bone formation-related proteins BMP2, RUNX-2 and OPG. Network pharmacological analysis showed that the effect of ameliorating of Aβ-injured osteoblasts by BJTW formula was mainly mediated by AGE-RAGE, PI3K-Akt, MAPK and neuroactive ligand-receptor interaction signaling pathways. Conclusion In this study, the effect of BJTW formula on improving the osteoblasts damaged by Aβ was confirmed for the first time, and its related mechanism was explored based on network pharmacology method. The results lay a strong foundation for the clinical application of traditional formula BJTW against osteoporosis. More>>

Exploration of the role and mechanism of all-trans retinoic acid on activation and oxidative stress of hepatic stellate cell 全反式维甲酸对肝星状细胞活化及氧化应激的作用和机制探索

XIU Jianping, YANG Chaoai, LIU Xi’ao, PAN Qianyu, et al

2024, 42(7): 291-296. doi: 10.12206/j.issn.2097-2024.202312054

Objective To explore the role and potential mechanisms of all-trans retinoic acid （ATRA） on activation and oxidative stress of hepatic stellate cell （HSC）. Methods Platelet-derived growth factor （PDGF-bb, 10 ng/ml） was applied to induce the activation of HSCs, which was then treated with ATRA at a dosage of 5 μmol/L for 48 h. The effects of ATRA on HSC activation were evaluated by detecting changes in cell growth viability and phenotypic marker expression. The effects of ATRA on HSC oxidative stress were evaluated by detecting changes in intracellular reactive oxygen species （ROS）, reduced glutathione （GSH） and malondialdehyde （MDA）, and the expression of antioxidant genes. The effects of ATRA on HSC autophagic activity were evaluated by detecting changes in autophagy marker expression and autophagic flow. Results Compared with the PDGF-bb group, the cell viability was significantly reduced in ATRA-treated HSCs （P<0.01）, as well as the expression of α-SMA and Collagen I. The intracellular levels of ROS and MDA were significantly reduced in ATRA-treated HSCs （P<0.01）, whereas the GSH level was significantly increased （P<0.01）. The expression levels of antioxidant genes （NRF2, HO-1, and ATF4）, were significantly higher in ATRA-treated HSCs than those in the normal ones under PDGF-bb condition （P<0.01）. Meanwhile, the expression of autophagy markers Beclin 1 and LC3 Ⅱ/I, and signal of autophagy flow in ATRA-treated HSCs were found to be significantly reduced （P<0.01）. Conclusion ATRA significantly inhibited PDGF-bb-induced HSC activation and reduced the level of oxidative stress and autophagic activity of HSCs, which had potential applications in the prevention and treatment of liver fibrosis. More>>

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The inhibition effect of astaxanthin on calcification of aortic valve interstitial cells by activating the Nrf2/HO-1 Pathway

ZHAO Quangong, WANG Guokun, XU Zhiyun

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202412057

Abstract(80) HTML(55) PDF (1740KB)(5)

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Objective To clarify the effect and mechanisms of astaxanthin on the calcification of aortic valve interstitial cells （VICs） induced by osteogenic medium （OM）. Methods The CCK-8 assay was used to analyze the effects of different concentrations of astaxanthin on the proliferation of VICs. After treating VICs with astaxanthin in OM, Alizarin Red staining was performed to detect calcified nodules, and Western blotting was used to measure the expression levels of osteogenic differentiation markers ALP and Runx2. Additionally, Western blotting and immunofluorescence detection were utilized to assess the expression levels of Nrf2 and HO-1 proteins. The levels of intracellular reactive oxygen species （ROS） were measured by DCFH-DA fluorescence staining. Results The CCK-8 results indicated that the optimal concentration of astaxanthin for intervention was 25 μmol/L. Astaxanthin treatment reduced the formation of calcified nodules induced by OM in VICs, and inhibited the expression of osteogenic differentiation markers ALP and Runx2 （P<0.01）. Furthermore, Astaxanthin treatment decreased the expression levels of Nrf2 and HO-1 （P<0.01）, and reduced intracellular reactive oxygen species levels （P<0.01）. Conclusion Astaxanthin may mitigate oxidative stress and calcification in VICs by enhancing the Nrf2/HO-1 antioxidant signaling pathway.

Effects and mechanism of Triptolide on cerebral ischemia-reperfusion injury in rats

ZHU Dongjie, HE Xinzheng, ZOU Jie, YU Shidan, LI Hongxia

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202311021

Abstract(5770) HTML(2160) PDF (1354KB)(31)

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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.

Synthesis and Antitumor Activity of Novel RRx-001 Derivatives

WU Ruonan, TANG Wenmin, GAO Lin, WU Yuelin, LUO Chuan, MIAO Zhenyuan

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202408053

Abstract(121) HTML(76) PDF (948KB)(1)

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Objectives To study the antitumor activities of RRx-001 derivatives with novel covalent fragments Methods Four targeted compounds were designed and synthesized. The structures were confirmed by ¹H NMR and HRMS. A549 and HCT116 cancer cell lines were selected for antiproliferative activity assays. Results All the compounds revealed antitumor activities and compound ZM528 showed the best antitumor activity against these two cell lines with IC₅₀ values of （5.1±4.8） and （6.0±2.7） μmol/L, respectively. Conclusions The result indicated that bromoacetyl group of RRx-001 could be substituted with other covalent fragments.

Research progress on Sophora Flavescens of Traditional Chinese Medicine

LIU Mengxiao, CHEN Linlin, WANG Yan, ZHANG Junping

In Press doi: 10.12206/j.issn.2097-2024.202406053

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Sophora Flavescens is the dried root of the leguminous plant Sophora Flavescens Ait. It was first published in Shen Nong's Herbal Classic. Sophora Flavescens contains a variety of active ingredients, mainly including matrine and oxymatrine, with anti-inflammatory, anti-tumor, anti-arrhythmia, disease-resistant pathogenic microorganisms and other pharmacological effects. Clinically, the compound preparations of Sophora Flavescens include Compound KuShen injection and KuShen gel and so on, which can be used to treat many types of cancers and improve skin, mucous pruritus, pain and other symptoms. Due to the poor bioavailability, the structure of matrine needs to be reformed. MASM, matrine derivative, only needs a low concentration to have a good therapeutic effect on sepsis and liver fibrosis. In this article, the chemical composition, pharmacological effects, compound preparations and structural modification of matrine were mainly discussed, aiming to provide a theoretical basis for the clinical application of Sophora Flavescens and the development of new drugs.

A case of postoperative candida bloodstream infection occurred in patients with digestive tract perforation

FENG Guangwei, ZHANG Jing, LIU Yangxi, CUI Min

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202312012

Abstract(304) HTML(140) PDF (859KB)(0)

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Objective To explore the drug selection, usage, dosage and effect of clinical pharmacists in the treatment of secondary Candida bloodstream infection in patients with digestive tract perforation, and provide reference for rational clinical use of such anti-infection therapy. Methods During the treatment of Candida infection, anti-infection specialist clinical pharmacists suggested replacing fluconazole for anti-infection treatment, and adjusted the usage and dosage of caspofungin to ensure the application of full treatment course. Results The patient’s Candida bloodstream infection was effectively controlled. Conclusion Echininocandins such as caspofungin are the first choice for Candida infection. The maintenance dose should be reduced to 35 mg qd in patient of moderate liver function injury, and the anti-infection treatment should be done at least 14 days after the blood culture being negative. Clinical pharmacists participate in clinical pharmaceutical care practices such as clinical ward rounds, and actively assist doctors to develop individualized anti-infection programs, which could improve the level of clinical drug use and improve the clinical outcome of diseases.

Analysis of characteristics of adverse drug reactions in a hospital from 2021 to 2023

WANG Yan, FANG Ming, SONG Hongwei, ZHONG Chao, XU Feng, ZHOU Ting

In Press doi: 10.12206/j.issn.2097-2024.202404041

Abstract(5965) HTML(2024) PDF (872KB)(55)

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Objective To analyze the characteristics of adverse drug reactions （ADR） reported in Sixth People’s Hospital South Campus, Shanghai Jiaotong University from 2021 to 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（19.2%）, vitamins（7.5%）, Chinese patent medicine（7.2%）, equine tetanus immunoglobulin（6.3%）. 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.

Effect of hypertension on cardiovascular fibrosis and sFRP2 expression

XU Yao, MA Chunhui, LI Zhiyong

In Press doi: 10.12206/j.issn.2097-2024.202409055

Abstract(1899) HTML(890) PDF (1364KB)(6)

Abstract:
Objective To investigate the effect of spontaneous hypertension on the remodeling of cardiac and aortic tissues in rats, with special attention to the changes in the content of collagen fibers, elastic fibers and secreted Frizzled-related protein 2 （sFRP2） in cardiac and aortic tissues. Methods 28-week-old SHR rats （Spontaneously Hypertensive rats） and WKY （Wistar-Kyoto rats） of the same age were selected as experimental animals. Cardiac load is assessed by calculating the cardiac weight index. Collagen fibers and elastic fibers were isolated from the rat thoracic aorta by hot alkali method, and their content was determined by biochemical analysis. In addition, pathological evaluation of tissue sections of the left ventricle and thoracic aorta was performed by H&E staining, Sirius red staining, and lichen red staining. Western blotting was used to determine the expression level of sFRP2 protein in cardiac tissues. Results Compared with WKY rats, the heart weight index of SHR rats increased significantly （P<0.001）, and the results of biochemical analysis and staining of pathological sections showed that the content of collagen fibers in the aorta in the SHR group was higher than that in the WKY group, while the content of elastic fibers was lower, but the difference did not reach statistical significance. The content of collagen fibers in the heart of the SHR group was significantly higher than that in the WKY group （P<0.01）. Western blotting showed that there was no significant difference in the expression level of sFRP2 protein in heart tissues between the two groups. Conclusion The remodeling of cardiac and aortic tissues in a rat model of spontaneous hypertension may involve complex molecular mechanisms, not just changes in the content of collagen fibers and elastic fibers. The detailed mechanism of the progression of spontaneous hypertension and target organs damage still need further investigation.

Progress and prospect of the antihypertensive effect from Bidens pilosa L. and its

WANG Xinxia, LIU Zhijun, LYU Lei, ZHANG Shuang, GAO Shouhong

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202408021

Abstract(1558) HTML(1169) PDF (911KB)(2)

Abstract:
Hypertension is a systemic chronic vascular disease. From the perspective of Traditional Chinese Syndromes, hypertension belongs to the category of liver fire, vertigo, liver yang, headache and so on. Chinese medicine treatment of hypertension has gradually become a hot research topic, and using Chinese herbal medicine to reduce blood pressure has also achieved good results. In recent years, researches on anti-hypotension of Bidens pilosa L. has gradually increased. The related research of Bidens pilosa L., including the ancient literature, modern research, functional components and mechanism were mainly summarized, the application of Bidens pilosa L. in lowering blood pressure were anticipated, with a view to provide reference for the further development and utilization of Bidens pilosa L. in treatment of hypertension.

Using HPLC to determine antimicrobial preservatives thimerosal in eye drops

GAO Jin, HU Dan, WANG Xiwen, YU Xiaocui, WANG Zexin, LIU Jing, ZHU Yuwei, MA Zihui, XU Junwei, GAO Qing, HONG Xiaoxu

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202404059

Abstract(1618) HTML(709) PDF (1052KB)(10)

Abstract:
Objective To establish a HPLC method for determining thimerosal compounds in eye drops. Methods A gradient HPLC system was used in the quantitative analysis of thimerosal compounds on Shiseido MGII C₁₈ column （4.6 mm×250 mm, 5 μm）, using 1% triethylamine solution （ pH adjusted to 3.0 with phosphate） as mobile phase A, the methanol as mobile phase B, gradient elution, The column temperature was 40 ℃, the detection wavelength was 222 nm , the flow rate was 1 ml/min and the injection volume was 20 µl. Results The established method had good linearity within the concentration range of 4.3-216.7 μg/ml （r>0.999） for thimerosal, with average recoveries was 102.1%, RSD2.7%. Conclusion This method is simple, accurate and highly specific, and can be used for determination of thimerosal compound in eye drops.

The preventive and therapeutic effects of three ethanol extracts derived from three sources of Stellera chamaejasme L., on imiquimod-induced psoriasis in mice

PENG Ying, LIU Xin, NIE Yiwen, WANG Xinhe, NIAN Hua, ZHU Jianyong

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202406029

Abstract(3302) HTML(352) PDF (2882KB)(6)

Abstract:
Objective To investigate the preventive and therapeutic effects of ethanol extracts derived from three sources of traditional Chinese medicine: Stellera chamaejasme L., Euphorbia fischeriana Steud., and Euphorbia kansuensis Prokh., on imiquimod （IMQ）-induced psoriasis in mice. Methods Thirty-six male BALB/c mice were randomly divided into the following 6 groups with 6 mice in each group: blank control, model, Stellera chamaejasme, Euphorbia fischeriana, Euphorbia kansuensis, and calcipotriol. PASI （Psoriasis Area and Severity Index） scores were used to record the changes of skin lesions in each group; HE （hematoxylin-eosin） staining was used to observe the pathological morphology of skin and measure the thickness of the epidermis. Immunohistochemistry was used to detect the expression of nuclear antigen Ki67 in the skin tissues of mice. Results Compared with the model group, the three kinds of ethanol extracts can reduce the PASI score, inhibit epidermal thickening, and decrease expression of Ki67 in the psoriasis mice. Among them, the therapeutic effect of Stellera chamaejasme was the most significant and it was better than the commonly used topical drug calcipotriol. Conclusion The ethanol extract of Stellera chamaejasme has good anti-psoriatic activity, can inhibit the abnormal proliferation of keratinocytes, can reduce the expression of Ki67, and can significantly improve psoriasis-like skin lesions.

Determination of Lamotrigine in Human Plasma by Central cutting two-dimensional liquid Chromatography

LIN Junrong, ZHANG Minxin, ZHAO Xuemei, HUANG Aiwen

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202306020

Abstract(4828) HTML(1473) PDF (1115KB)(10)

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.

Study of 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

In Press doi: 10.12206/j.issn.2097-2024.202204094

Abstract(5988) HTML(3666) PDF (839KB)(53)

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.

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.

Abstract(3380) HTML(1254) PDF (0KB)(326)

Abstract:

Lactic acid bacteria as recombinant protein drug delivery carrier

WANG Xufang, WANG Yanting, YAO Chunmeng, LU Bin

Accepted Manuscript doi: 10.12206/j.issn.2097-2024.202309021

Abstract(8279) HTML(3256) PDF (863KB)(88)

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.

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(8643) HTML(2196) PDF (2083KB)(37)

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.

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Research progresses on Keap1-Nrf2 pathway in inflammatory diseases

ZHOU Wenyan, HU Shanshan, ZHANG Wannian, ZHUANG Chunlin

2025, 43(3): 97-108, 116. doi: 10.12206/j.issn.2097-2024.202405013

Abstract(7732) HTML(1264) PDF (1855KB)(55)

Abstract:
The Keap1-Nrf2 pathway has been shown to be an important defense mechanism against oxidative stress, which may be an effective therapeutic strategy for many diseases. The research progresses on Keap1-Nrf2 pathway in inflammatory diseases were mainly reviewed. The basic components and activation mechanism of Keap1-Nrf2 pathway were introduced. The relationship between Keap1-Nrf2 pathway and the crosstalk between NF-κB pathway and HO-1 pathway, the expression of inflammatory mediators and enzymes, and inflammatory bodies were expounded. Natural product-derived inhibitors, small molecule inhibitors targeting Keap1-Nrf2 pathway and their clinical progress were introduced, and the potential application value of Keap1-Nrf2 pathway in the treatment of inflammation was discussed.

Progress on mRNA tumor vaccine with non-viral delivery system

ZHOU Jiao, ZHENG Jianyu, WANG Sizhen, YANG Feng

2025, 43(3): 109-116. doi: 10.12206/j.issn.2097-2024.202410034

Abstract(5872) HTML(4049) PDF (2247KB)(31)

Abstract:
At the end of 2020, the FDA issued emergency use authorization for two mRNA vaccines（BNT162b2 and mRNA-1273）, which had provided important support in the response to the COVID-19 pandemic. The great success of these COVID-19 vaccines based on non-viral vectors has promoted the research and application of mRNA vaccines in the treatment of diseases such as tumors. Compared with virus-based delivery systems, non-viral carriers have significant advantages in biological safety and versatility. Therefore, non-viral vectors have become a research hotshot for mRNA tumor vaccines. In this paper, the latest research progress on lipid nanoparticles, polymers, peptides and inorganic materials were introduced. In addition, recent clinical trials of mRNA tumor vaccines were reviewed and the challenges and prospects of non-viral vectors in clinical transformation of mRNA tumor vaccines were discussed.

Original articles

Construction and validation of a platelet-specific Metrnl gene knockout mouse model

CHEN Canxin, MIAO Zhuwei, MIAO Chaoyu

2025, 43(3): 117-123. doi: 10.12206/j.issn.2097-2024.202409031

Abstract(5758) HTML(2102) PDF (2820KB)(24)

Abstract:
Objective To construct the platelet-specific Metrnl gene knockout （Plt-Metrnl^-/-）mice model. Methods Based on the Cre-LoxP system, Metrnl^loxp/loxp mice, previously constructed in our laboratory, were mated with Pf4-Cre mice to generate Plt-Metrnl^-/- mice. The genotypes of the offspring were identified, and tissues of the platelet, other peripheral blood cells, heart, liver, spleen, lung, kidney, brain, colon, and bone marrow were collected. The expression of the Metrnl gene in Plt-Metrnl^-/- mice was investigated by quantitative real-time PCR and western blot. Also, the blood routine index was tested in Plt-Metrnl^-/- mice. Results Compared with wild-type mice, the level of Metrnl protein in platelets was significantly decreased in Plt-Metrnl^-/- mice. There was no significant difference in mRNA and protein levels of other peripheral blood cells and tissues, as well as in blood routine index, growth, and development between Plt-Metrnl^-/- mice and WT mice. Conclusion Platelet-specific Metrnl knockout mice（Plt-Metrnl^-/- mice）model was successfully constructed.

Design, synthesis and antifungal and antitumor activity research of novel Hsp90 inhibitors

SHI Qiao, HAN Guiyan, ZHANG Junteng, LIU Na

2025, 43(3): 124-135. doi: 10.12206/j.issn.2097-2024.202501019

Abstract(1749) HTML(895) PDF (2604KB)(6)

Abstract:
Objective To design and synthesize novel Hsp90 inhibitors with dual functions of synergistically enhancing the antifungal activity of fluconazole （FLC） against drug-resistant fungi and anti-tumor activity based on the Hsp90 inhibitor Ganetespib. Methods The previous research found that Ganetespib had a good synergistic anti-resistant fungal activity with FLC, with a fractional inhibitory concentration index （FICI） of 0.023 to 0.039. In this study, structural modifications were made to Ganetespib by replacing its indole ring with a phenyl ring containing different substituents to design and synthesize a series of new compounds. The in vitro synergistic anti-resistant fungal activity against C. albicans 0304103 in combination with FLC, anti-tumor activity （against HEL, HL60 and A549 cells）, and Hsp90α inhibition activity were determined to explore their structure-activity relationship and mechanism of action. Results The chemical structures of 19 new compounds were confirmed by ¹H NMR, ¹³C NMR and HRMS. Most of the compounds exhibited strong Hsp90α inhibitory activity, good synergistic activity against drug-resistant fungi in combination with FLC and anti-tumor activity. The substitution of electron-donating groups on the benzene ring was beneficial to enhancing the synergistic activity against drug-resistant fungi in combination with FLC. Among them, compounds F3 and F5 showed excellent synergistic activity against drug-resistant fungi in combination with FLC （FICI were both 0.047） and anti-tumor activity （IC₅₀ were 0.025 to 0.15 μmol/L and 0.021 to 0.23 μmol/L respectively）, and could down-regulate the expression levels of drug resistance genes and efflux pump genes in fungi, inhibit the formation of fungal biofilms, and arrest the cell cycle of HEL cells at G0/G1 phase. Conclusion The novel Hsp90 inhibitors such as F3 and F5 could both effectively exert the dual activities of synergizing with FLC to combat drug-resistant fungi and fight against tumors, which provided a new idea for the development of new drugs with dual functions of synergizing with FLC to combat drug-resistant fungi and fight against tumors.

Study on the synergistic antifungal effects of caspofungin acetate loaded glyceryl monostearate nanoparticle on Candida albicans

GUO Lingyi, LIU Yanchao, GAO Lu, LIU Ruiyao, LYU Quanzhen, YU Yuan

2025, 43(3): 136-142, 150. doi: 10.12206/j.issn.2097-2024.202310043

Abstract(4486) HTML(1405) PDF (4631KB)(11)

Abstract:
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）. 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.

Network pharmacological mechanism of Danshen Baizhu prescription on the treatment of coronary heart disease, vascular dementia and idiopathic membranous nephropathy

XU Lulu, LIU Aijun

2025, 43(3): 143-150. doi: 10.12206/j.issn.2097-2024.202312027

Abstract(2090) HTML(933) PDF (6551KB)(25)

Abstract:
Objective To investigate the material basis and mechanism of Danshen Baizhu prescription in coronary heart disease, vascular dementia and idiopathic membranous nephropathy based on network pharmacology. Methods TCMSP, PubChem, UniProt, GeneCards, OMIM, and DrugBank databases were used to obtain drug and disease targets, and the TCM-compound-drug target network, compound-common target-disease network, and protein-protein interaction map were drawn by STRING database and Cytoscape software, and gene enrichment analysis was performed by Metascape database. Results A total of 164 active compounds, 509 potential targets, and 141 common targets were screened out. The main active ingredients were Tanshinone II A, Isorhamnetin, Quercetin, Luteolin, Kampferol, β-sitosterol, Stigmasterol, etc. The key targets were albumin, interleukin 6, Tumor necrosis factor , serine/threonine kinase 1, vascular endothelial growth factor A , mainly enriching in the positive regulation of cell migration, cell viability, protein phosphorylation, responsing to growth factors, oxidative stress and other biological processes and lipid and atherosclerosis, MAPK, atherosclerosis and fluid shear force, AGE-RAGE, IL-17, PI3K-Akt and other signaling pathways. Conclusion The mechanism of action of Danshen Baizhu prescription for coronary heart disease, vascular dementia and idiopathic membranous nephropathy may mainly play a role in multiple targets and pathways such as inhibition of inflammation, inhibition of oxidative stress, and vasodilation.

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Chief Editor: LI Jie Wei

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ISSN 2097-2024 CN 31-2185/R

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