中国药理学通报2017，Vol.33Issue(9)：1248-1252,5.DOI:10.3969/j.issn.1001-1978.2017.09.013
替芬泰对HepG2细胞的线粒体毒性
The mitochondrial toxicity of bentysrepinine on HepG2 cells
摘要
Abstract
Aim To provide references for clinical trials dose and rational drug use by evaluating mitochondrial toxicity of bentysrepinine on HepG2 cells.Methods Mitochondrial toxicity of bentysrepinine on HepG2 cells was cmomprehensively evaluated by measuring proliferation inhibition rate, lactic acid content in culture supernatant, reactive oxygen species(ROS) content, mitochondrial membrane potential (MMP) variation and the activity of mitochondrial respiratory chain complex enzymes Ⅰ to Ⅳ.Results The half inhibitory concentration of bentysrepinine of HepG2 cells was 359 μmol·L-1.Compared with the control group, bentysrepinine could reduce the MMP, raise the level of lactic acid, increase the content of ROS and lower the activity of mitochondrial respiratory chain complex enzymes Ⅰ to Ⅲ with the concentration of 400 μmol·L-1(196 mg·L-1), showing an obvious mitochondrial toxicity.Compared with lamivudine and adefovir dipivoxil, bentysrepinine exerted no influence on indexes above with the same concentration 100 μmol·L-1.Conclusions Bentysrepinine shows an obvious mitochondrial toxicity on HepG2 cells with the concentration of 400 μmol·L-1.This mitochondrial toxicity is not presented with the concentration of 200 μmol·L-1.It shows that the safety range of bentysrepinine about mitochondrial toxicity is relatively wide.The test plays a guiding role in clinical trial dose design as well as clinical treatment.关键词
替芬泰/线粒体毒性/线粒体膜电位/活性氧/线粒体呼吸链复合物酶/乳酸Key words
bentysrepinine/mitochondrial toxicity/MMP/ROS/mitochondrial respiratory chain complex enzymes/lactic acid分类
医药卫生引用本文复制引用
冯玥,霍璇,胡金芳,邸志权,张宗鹏,申秀萍..替芬泰对HepG2细胞的线粒体毒性[J].中国药理学通报,2017,33(9):1248-1252,5.基金项目
国家科技重大专项课题(No 2015ZX09501004-002-003) （No 2015ZX09501004-002-003）
