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Protective effects of Yindanxinnaotong capsule in a rat model of myocardial ischemia/reperfusion injury

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Journal of Traditional Chinese Medicine 2014年第6期34卷 699-709页

作者： Wandan Wang Lan Wang Hongjun Yang Jianlu Wang Xiaojie Yin Haiyu Xu Long Cheng Rixin Liang Pharmacology and pharmacokinetics laboratory Institute of Chinese MaterialMedical China Academy of Chinese Medical Sciences Institute of Medical Plant Development Chinese Academy of Medical Sciences

OBJECTIVE: To investigate the effects of Yindanxinnaotong capsule(YDXNTC) and main components compatibility and ratios on myocardium against ischemia/reperfusion injury and the effect's underlying ***: Myocardial ischemia/reperfusion injury(MIRI) was induced by ischemia for 30 min and reperfusion for 30 min. Electrocardiogram data and coronary flow were recorded, and superoxide dismutase(SOD), malondialdehyde(MDA), lactate dehydrogenase, creatine kinase-MB, cardiac troponin T and I(cT nT, cT n I) and interleukin-1β, interleukin-8,interleukin-18(IL-1β, IL-8, IL-18) in myocardium were measured. Hypoxia/reoxygenation and hydrogen peroxide(H2O2) injury were induced by hypoxia for 3 h/reoxygenation for 2 h, and 100 μM H2O2 for 1 h, respectively, in vitro rat myocardial cells(H9c2). Cell viability, SOD, MDA, cT nT and inflamma-tory factors(IL-1β, IL-8 and IL-18) were determined,and Toll-like receptor 4(TLR-4) expression was measured by western ***: In the isolated heart experiment, elevated heart function, coronary flow and SOD levels,and decreased MDA levels and inflammatory factors were noted in the YDXNTC, main components and main components compatibility groups. Ventricular tachycardia/ventricular fibrillation occurrence decreased in the ginkgo biloba extract(GBE),and GBE and salvia miltiorrhiza ethanol extract compatibility(SM-E, GSEC) groups. Lactic dehydrogenase levels decreased in the YDXNTC and aqueous extract of salvia miltiorrhiza(SM-H) groups. Creatine kinase-MB decreased with GBE, SM-E, SM-H and GSEC treatment, and cT n I and cT nT levels decreased with GSEC. In the in vitro cell study,YDXNTC and main components ratios improved cell viability and SOD levels, and suppressed MDA,cT nT and inflammatory factors. TLR-4 expression was ***: YDXNTC and main components compatibility showed protective effects on MIRI in this rat model and in vitro study. Regulating the Toll-like receptor signaling pathway may affect the

关键词： Myocardial ischemia Reperfusion Components compatibility Yindanxinnaotong cap-sule

Inhibitory effect of medicinal plant-derived carboxylic acids on the human transporters hOAT1, hOAT3, hOATP1B1, and hOATP2B1

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Chinese Journal of Natural Medicines 2014年第2期12卷 131-138页

作者： ZHANG Zhi-Yu SI Duan-Yun YI Xiu-Lin LIU Chang-Xiao School of Chemical Engineering and Technology Tianjin University State Key laboratory of Drug Delivery Technology and pharmacokinetics Tianjin Institute of Pharmaceutical Research

A significant number of organic carboxylic acids have been shown to influence the absorption and distribution of drugs mediated by organic anion transporters(OATs). In this study, uptake experiments were performed to assess the inhibitory effects of cinnamic acid, ferulic acid, oleanolic acid, deoxycholic acid, and cynarin on hOAT1, hOAT3, hOATP1B1, and hOATP2B1. After a drug-drug interaction(DDI) investigation, cinnamic acid, ferulic acid, deoxycholic acid, and cynarin were found and validated to inhibit hOAT1 in a competitive manner, and deoxycholic acid was found to be an inhibitor of all four transporters. The apparent 50% inhibitory concentrations of cinnamic acid, ferulic acid, deoxycholic acid, and cynarin were estimated to be 133.87, 3.69, 90.03 and 6.03 μmol L 1for hOAT1, respectively. The apparent 50% inhibitory concentrations of deoxycholic acid were estimated to be 9.57 μmol L 1for hOAT3, 70.54 μmol L 1for hOATP1B1, and 168.27 μmol L 1for hOATP2B1. Because cinnamic acid, ferulic acid, and cynarin are ingredients of food or food additives, the present study suggests there are new food-drug interactions to be disclosed. In addition, deoxycholic acid may be used as a probe for studying the correlation of OATs and OATPs.

关键词： hOAT1 hOAT3 hOATP1B1 hOATP2B1 Transport Food-drug interactions

Combined obeticholic acid and apoptosis inhibitor treatment alleviates liver fibrosis

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Acta Pharmaceutica Sinica B 2019年第3期9卷 526-536页

作者： Jiyu Zhou Ningning Huang Yitong Guo Shuang Cui Chaoliang Ge Qingxian He Xiaojie Pan Guangji Wang Hong Wang Haiping Hao State Key laboratory of Natural Medicines Key Laboratory of Drug Metabolism and PharmacokineticsChina Pharmaceutical UniversityNanjing210009China First Affiliated Hospital of Anhui Medical University Hefei230022China

Obeticholic acid(OCA), the first FXR-targeting drug, has been claimed effective in the therapy of liver fibrosis. However, recent clinical trials indicated that OCA might not be effective against liver fibrosis, possibly due to the lower dosage to reduce the incidence of the side-effect of pruritus. Here we propose a combinatory therapeutic strategy of OCA and apoptosis inhibitor for combating against liver fibrosis. CCl4-injured mice, D-galactosamine/LPS(GalN/LPS)-treated mice and cycloheximide/TNFα(CHX/TNFα)-treated HepG2 cells were employed to assess the effects of OCA, or together with IDN-6556, an apoptosis inhibitor. OCA treatment significantly inhibited hepatic stellate cell(HSC)activation/proliferation and prevented fibrosis. Elevated bile acid(BA) levels and hepatocyte apoptosis triggered the activation and proliferation of HSCs. OCA treatment reduced BA levels but could not inhibit hepatocellular apoptosis. An enhanced anti-fibrotic effect was observed when OCA was co-administrated with IDN-6556. Our study demonstrated that OCA inhibits HSCs activation/proliferation partially by regulating BA homeostasis and thereby inhibiting activation of HSCs. The findings in this study suggest that combined use of apoptosis inhibitor and OCA at lower dosage represents a novel therapeutic strategy for liver fibrosis.

关键词： Obeticholic acid Liver fibrosis Bile acid Hepatocellular apoptosis IDN-6556 Farnesoid X receptor Hepatic stellate cell

Protective effects of ursodeoxycholic acid on chenodeoxycholic acid-induced liver injury in hamsters

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World Journal of Gastroenterology 2007年第37期13卷 5003-5008页

作者： Tomomichi Iwaki Kaoru Ishizaki Shuji Kinoshita Hideki Tanaka Atsushi Fukunari Makoto Tsurufuji Teruaki Imada Research laboratory Ⅲ (Immunology) Pharmaceuticals Research Division Mitsubishi Pharma Corporation Yokohama Japan pharmacokinetics laboratory Pharmaceuticals Research Division Mitsubishi Pharma Corporation Chiba Japan Discovery Technology laboratory Pharmaceuticals Research Division Mitsubishi Pharma Corporation Yokohama Japan

AIM： TO investigate the effects of ursodeoxycholic acid （UDCA） on chenodeoxycholic acid （CDCA）-induced liver injury in hamsters, and to elucidate a correlation between liver injury and bile acid profiles in the liver.METHODS： Liver injury was induced in hamsters by administration of 0.5% （w/w） CDCA in their feed for 7 d. UDCA （50 mg/kg and 150 mg/kg） was administered for the last 3 d of the experiment.RESULTS： At the end of the experiment, serum alanine aminotransferase （ALl） increased more than 10 times and the presence of liver injury was confirmed histologically. Marked increase in bile acids was observed in the liver. The amount of total bile acids increased approximately three-fold and was accompanied by the increase in hydrophobic bile acids, CDCA and lithocholic acid （LCA）. UDCA （50 mg/kg and 150 mg/kg） improved liver histology, with a significant decrease （679.3 ±77.5 U/L vs 333.6 ± 50.4 U/L and 254.3 ±35.5 U/ L, respectively, P 〈 0.01） in serum ALT level. UDCA decreased the concentrations of the hydrophobic bile acids, and as a result, a decrease in the total bile acid level in the liver was achieved.CONCLUSION： The results show that UDCA improves oral CDCA-induced liver damage in hamsters. The protective effects of UDCA appear to result from a decrease in the concentration of hydrophobic bile acids, CDCA and LCA, which accumulate and show the cytotoxicity in the liver.

关键词： Chenodeoxycholic acid Hamster Liver bileacids Ursodeoxycholic acid

Target-responsive subcellular catabolism analysis for early-stage antibody-drug conjugates screening and assessment

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Acta Pharmaceutica Sinica B 2021年第12期11卷 4020-4031页

作者： Hua Sang Jiali Liu Fang Zhou Xiaofang Zhang Jingwei Zhang Yazhong Liu Guangji Wang Hui Ye Jiangsu Provincial Key laboratory of Drug Metabolism and pharmacokinetics State Key Laboratory of Natural MedicinesChina Pharmaceutical UniversityNanjing 210009China Department of Pharmacy the Affiliated Hospital of Nantong UniversityNantong 226001China

Events including antibody-antigen affinity,internalization,trafficking and lysosomal proteolysis combinatorially determine the efficiency of antibody-drug conjugate(ADC) catabolism and hence the ***,an approach that conveniently identifies proteins requisite for payload release and the ensuing toxicity for mechanistic studies and quality assessment is *** the plethora of ADC candidates under development,we developed a target-responsive subcellular catabolism(TARSC) approach that examines ADC catabolism and probes changes in response to targeted interferences of proteins of *** firstly applied TARSC to study the commercial T-DM1 and the *** recorded unequivocal catabolic behaviors regardless of the absence and presence of the targeted *** negligible differences in TARSC profiles agreed with their undifferentiated anti-tumoral efficacy according to further in vitro viability and in vivo tumor growth assays,highlighting TARSC analysis as a useful tool for biosimilarity assessment and functional dissection of proteins requisite for ADC ***,we employed TARSC to investigate the catabolic behavior of a new trastuzumab-toxin ***,TARSC can not only characterize ADC catabolism at(sub)cellular level but also comprehensively determine which protein targets affect payload release and therapeutic *** use of TARSC is thus anticipated in early-stage screening,quality assessment and mechanistic investigations of ADCs.

关键词： ADC Target-responsive subcellular catabolism(TARSC) T-DM1 Therapeutic efficacy Screening Biosimilarity

Formulation,characterization and in vivo and in vitro evaluation of aloe-emodin-loaded solid dispersions for dissolution enhancement

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Journal of Traditional Chinese Medicine 2024年第1期44卷 54-62页

作者： LI Xiuyan LUO Yuting WANG Jinhui DU Zhimin Key laboratory of Basic and Application Research of Beiyao Heilongjiang University of Chinese MedicineMinistry of EducationHarbin 150040China College of Pharmacy Harbin Medical UniversityHarbin 150081China Institute of Clinical Pharmacology the Second Affliated Hospital of Harbin Medical University(University Key aboratory of Drug ResearchHeilongjiang Province)Harbin 150086China Department of Clinical Pharmacology College of Pharmacy Harbin Medical UniversityHarbin 150081China State Key laboratory of Quality Research in Chinese Medicines Macao University of Science and TechnologyMacao 999078China

OBJECTIVE:To prepare aloe-emodin solid dispersion(AE-SD)and determine the metabolic process of AE and AE-SD in ***:AE-SD was prepared via solvent evaporation or solvent melting using PEG-6000 and PVP-K30 as *** analysis,X-ray diffraction spectroscopy,differential scanning calorimetry,Fourier transform infrared spectroscopy and scanning electron microscopy were used to identify the physical state of *** prescriptions were screened via the dissolution degree determination *** Phoenix software,AE suspension and AE-SD were subjected to a pharmacokinetic comparison study analyzing the alteration of behavior in vivo after AE was prepared as a solid *** toxicity was assessed in mice,and the physiological toxicity was used as the determination criterion for ***:AE-SD showed that AE existed in the carrier in an amorphous *** with polyethylene glycol,polyvinylpyrrolidone(PVP)inhibited AE crystallization,causing the drug to transform from a dense crystalline state to an amorphous form and increasing the degree of drug ***,it was more suitable as a carrier material for *** addition of poloxamer(POL)was more beneficial to the stability of solid dispersions and could reduce the amount of *** dissolution test confirmed that the optimal ratio of AE to the composite vector AE-PVP-POL was 1:2:2,and its dissolution effect was also *** on the pharmacokinetic comparison,the drug absorption was faster and quickly reached the peak of blood drug concentration in AE-SD compared to AE,the Cmax of AE-SD was greater than that of AE,and t1/2 and mean residence time of AE-SD were less than *** results showed that the drug metabolism in AE-SD was better,and the residence time was *** toxicology study showed that both AE and AE-SD had no ***:This paper established that the solubility of the drug could be increased after preparing a solid dispersion,

关键词： aloe-emodin solid dispersion solvent evaporation drug liberation pharmacokinetics

Influence of CYP3A5 genetic polymorphism on cyclosporine A metabo-lism and elimination in Chinese renal transplant recipients

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Acta Pharmacologica Sinica 2006年第11期27卷 1504-1508页

作者： Xiao-man CHU~1 Hai-ping HAO~(2,3)Guang-ji WANG~2 Lian-qing GUO~1 Pei-qing MIN~1 1 Department of Clinical Pharmacology,General Hospital of Nanjing Military Area,Nanjing 210002,China 2 Key laboratory of Drug Metabolism and pharmacokinetics,China Pharmaceutical University,Nanjing 210038,China Department of Clinical Pharmacology General Hospital of Nanjing Military Area Nanjing China Key laboratory of Drug Metabolism and pharmacokinetics China Pharmaceutical University Nanjing China

Aim:To investigate whether the CYP3A5*3 polymorphism would affectcyclosporine A(CsA)metabolism in Chinese renal transplant ***:The CYP3A5*3 genotype was determined in Chinese renal transplant recipientsusing polymerase chain reaction and amplification of specific alleles(PCR-ASA).The concentrations of CsA and metabolites were separately measured by fluores-cence polarization immunoassay and dose-adjusted trough concentrations andmetabolic ratio(MR)values were ***:The trough concentrationsadjusted with the dose was significantly higher in the wild allele carriers comparedto both the homozygous(*3*3)and heterozygous variants(*1*3).However,nosignificant difference was found for the dose-adjusted metabolite *** MR values for the 3 genotype groups were as follows:0.92+0.62 for CYP3A5*3/*3(n=14),0.99±0.51 for CYP3A5*1/*3(n=15),and 1.45±0.62 for CYP3A5*1/*1(n=9),*** hoc comparisons showed that only the MR values be-tween the CYP3A5*3/*3 group and the CYP3A5*1/*1 group were ***:The CYP3A5*3 polymorphism exerted little effect oncyclosporine *** MR may be a more accurate indicator for therapeu-tic drug monitoring,considering its integrated information on body exposure ofboth parent drugs and metabolites.

关键词： cyclosporine genetic polymorphism CYP3A5 metabolic ratio renal transplant patients

New perspectives on the therapeutic potential of quercetin in non-communicable diseases:Targeting Nrf2 to counteract oxidative stress and inflammation

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Journal of Pharmaceutical Analysis 2024年第6期14卷 805-822页

作者： Li Zhang Li-Yue Xu Fei Tang Dong Liu Xiao-Lan Zhao Jing-Nan Zhang Jia Xia Jiao-Jiao Wu Yu Yang Cheng Peng Hui Ao State Key laboratory of Southwestern Chinese Medicine Resources School of PharmacyChengdu University of Traditional Chinese MedicineChengdu611137China Innovative Institute of Chinese Medicine and Pharmacy Chengdu University of Traditional Chinese MedicineChengdu611137China

Non-communicable diseases(NCDs),including cardiovascular diseases,cancer,metabolic diseases,and skeletal diseases,pose significant challenges to public health *** complex pathogenesis of these diseases is closely linked to oxidative stress and inflammatory *** factor erythroid 2-related factor 2(Nrf2),a critical transcription factor,plays an important role in regulating antioxidant and anti-inflammatory responses to protect the cells from oxidative damage and inflammation-mediated ***,Nrf2-targeting therapies hold promise for preventing and treating ***(Que)is a widely available flavonoid that has significant antioxidant and anti-inflammatory *** modulates the Nrf2 signaling pathway to ameliorate oxidative stress and *** modulates mitochondrial function,apoptosis,autophagy,and cell damage biomarkers to regulate oxidative stress and inflammation,highlighting its efficacy as a therapeutic agent against ***,we discussed,for the first time,the close association between NCD pathogenesis and the Nrf2 signaling pathway,involved in neurodegenerative diseases(NDDs),cardiovascular disease,cancers,organ damage,and bone ***,we reviewed the availability,pharmacokinetics,pharmaceutics,and therapeutic applications of Que in treating *** addition,we focused on the challenges and prospects for its clinical *** represents a promising candidate for the treatment of NCDs due to its Nrf2-targeting properties.

关键词： Quercetin Nrf2 Non-communicable diseases Antioxidant Anti-inflammatory Availability

TCP-1,a novel peptide to diagnose early colon cancer

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Chinese Chemical Letters 2024年第3期35卷 226-233页

作者： Hang Yu Baoying Wen Min Huang Ru Feng Libin Pan Manyi Xu Hao Lin Lin Cong Sen Zhang Yan Li Chi-Hin Cho Chongjing Zhang Xiaoguang Chen Yan Wang State Key laboratory of Bioactive Substances and Functions of Natural Medicines Institute of Materia MedicaChinese Academy of Medical SciencesBeijing 100050China School of Biomedical Sciences Faculty of MedicineThe Chinese University of Hong KongHong KongChina

A nine cyclic peptide(TCP-1)showed excellent specificity for colon ***-1 binds with human tumor tissues at early stages and mice tumor with diameters of 1-4 mm,suggesting that TCP-1 may be used for early diagnosis of colon *** mechanism of the targeted binding of TCP-1 to colon cancer was also studied using immunoprecipitation,LC-MS and *** screening and identifying of the possible binding target proteins of TCP-1,keratin,typeⅡcytoskeletal 5 was speculated to be the specific binding target protein of TCP-1 in human tumor *** studies were conducted to investigate the target-mediated drug disposition of the new tumor-specific peptide by LC-MS/*** tissue distribution study showed that TCP-1 was found only in colon tumors(the target site)in tumor mice did not bind to any other *** TCP-1 to tumor markedly increased its removal rate from blood circulation but mildly extended its staying time in *** tumor mice,a lower AUC of TCP-1(reduced by almost 35%)and 2-fold higher clearance were found compared to that of normal *** proposed metabolic pathway of TCP-1 in the kidney was also determined using LC-MS^(n)-*** high specificity and low toxicity of the peptide may be caused by its extremely tight binding to the *** applications for future clinical use,including MRI and PET/CT were also explored,and this research may promote the development of colon cancer diagnostic technology research and provide new ideas and technical routes for tumor diagnostic technology.

关键词： Colon cancer TCP-1 Peptide Cytokeratin 5 pharmacokinetics/pharmacodynamics(PK/PD)