【摘 要】
:
The furan-containing compounds widely exist in food, herb, synthetic drugs and air pollution, and many of them are toxic.It was proposed that metabolic activation of furan ring was related to their in
【机 构】
:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
【出 处】
:
2015年第一届药代动力学朝阳论坛
论文部分内容阅读
The furan-containing compounds widely exist in food, herb, synthetic drugs and air pollution, and many of them are toxic.It was proposed that metabolic activation of furan ring was related to their induced toxicity.In the present study, 13 furan-containing compounds, belonging to six structural classes (furan, 2-substituted, 3-substituted, 2, 3-substituted, 2, 5-substituted and 2,3,4,5-substituted furans), were incubated with trapping reagents N-(tert-butoxycarbonyl)-L-lysine (BocLys) with nucleophilic amino group and N-acetvl cysteine (NAC) with nucleophilic thiol group) in NADPH-supplemented human liver microsomes (HLM).
其他文献
Tanshinol has desirable antianginal and pharmacokinetic properties and is a key compound of Salvia miltiorrhiza roots (Danshen).The reported effective concentrations of tanshinol in vitro are higher (
Fast metabolism is one of key issues for many drug candidates, which could result in poor bioavailability, short half-life and significant drug-drug interactions.To identify the issue in early phase o
CPRC1 is a novel investigated proton pump inhibitor, which shows dramaticsuccess in the management of acid-related disorders.Now this drug is being developed in Phase Ⅱ study in China.In this paper fo
Drug ADME experiment in humans is a pivotal drug metabolism study in support of drug development and registration.Human ADME study provides information on the exposure of drug related components, excr
There are extensive reports on drug-metabolizing enzymes dysregulation in inflammatory diseases and the distinct regulatory effects of different cvtokines.The present study aimed to depict the changes
Trastuzumab Emtansine(T-DM1, KadcylaTM, Genentech Inc.) is an antibody-drug conjugate(ADC) that received US FDA approval in 2013 for the treatment of human epidermal growth factor receptor 2 (HER2)-po
Herbal medicinal products belong to a main part of complementary and alternative medicine and have worldwide using integrated with conventional medicines for treatment.However, the increasing risk of
LAT1 overexpressed on membrane of various tumor cells, are potential targets for tumor-targeting therapy.This study aimed to develop a LAT1-mediated drug delivery to target chemotherapeutic agents to
Fasiglifam (TAK-875), a selective G-protein-coupled receptor 40 agonist, was developed for the treatment of type 2 diabetes mellitus.However, its clinical development was terminated in phase Ⅲ clinica
Metabolic profile of bile acids was used to evaluate hepatoprotec tion in Nrf2/ARE Oxidation/chemical stress defense pathway caused by Isoliquiritigenin (ISL) based on analysis of 16 bile acids in mic