盐酸苯环壬酯及其光学异构体的细胞毒性  

Cytotoxicity evaluation of phencynonate hydrochloride and its optical isomers

作　　者：王以美[1] 彭双清[1] 仲伯华[2] 刘克良[2] 

机构地区：[1]中国人民解放军疾病预防控制所,北京100071 [2]军事医学科学院毒物药物研究所,北京100850

出　　处：《中国新药杂志》2008年第6期465-467,493,共4页Chinese Journal of New Drugs

基　　金：国家自然科学基金重大项目(203900508)

摘　　要：目的:研究新型抗胆碱能药物盐酸苯环壬酯(CPG)及其光学异构体S(+)-CPG和R(-)-CPG的细胞毒性。方法:人肝肿瘤细胞HepG2、人近曲肾小管上皮细胞HK-2及人胚肺成纤维细胞HLF染毒不同浓度的CPG,S(+)-CPG和R(-)-CPG,采用中性红吸收法测定半数抑制浓度(IC50)。结果:CPG,S(+)-CPG和R(-)-CPG均以浓度依赖的方式降低细胞存活率,它们对HepG2细胞的IC50分别为192.5,193.6和217.0μmol.L-1,对HK-2细胞的IC50分别为181.8,196.0和208.8μmol.L-1,对HLF细胞的IC50分别为223.7,233.9和244.6μmol.L-1。结论:CPG与其光学异构体S(+)-CPG和R(-)-CPG的细胞毒性没有明显差异。Objective： To study the cytotoxicity of a novel anticholinergic agent phencynonate hydrocnlonue （CPG） and its optical isomers S（ ＋ ）-CPG and R（-）-CPG. Methods：HepG2, HK-2 and HLF cells were exposed to a series of concentrations of these anticholinergic agents, and the cytotoxicity was evaluated by neutral red uptake assay, and compared with the values of 50% inhibition concentration （IC50）- Results： CPG, S（ ＋ ）-CPG and R（-）- CPG induced a cytotoxicity on these three cell lines in a concentration-dependent manner. The IC50 values of CPG and its isomers S（ ＋ ）-CPG and R（-）-CPG were 192.5, 193.6 and 217.0μmol·L^-1 on HepG2 cells; 181.8, 196.0 and 208.8μmol· L^- 1 on HK-2 cells ; and 223.7, 233.9 and 244.6μmol· L^- 1 on HLF cells, respectively. Conclusions： There are no significant differences in the cytotoxicity among CPG and its isomers S（ ＋ ）-CTG and R（-）-CTG.

关 键 词：盐酸苯环壬酯 光学异构体 细胞毒性 中性红吸收法 

分 类 号：R969.4[医药卫生—药理学]