新型抗胆碱能药物盐酸戊乙奎酶及其光学异构体的细胞毒性评价

中国临床药理学与治疗学 ›› 2007, Vol. 12 ›› Issue (12): 1389-1389.

新型抗胆碱能药物盐酸戊乙奎酶及其光学异构体的细胞毒性评价

王以美, 彭双清, 仲伯华, 刘克良

军事医学科学院毒物药物研究所,北京 100850

收稿日期:2007-07-20 修回日期:2007-11-16 发布日期:2020-11-10

Cytotoxicity evaluation of a novel anticholinergicdrug penehyclidine hydrochloride and its optical isomers

WANG Yi-mei, PENG Shuang-qing, ZHONG Bo-hua, LIU Ke-liang

Bejing Institule of Pharmacology and Toxicology, 27 Taiping Road. Haidian District, Beijing 100850, China

Received:2007-07-20 Revised:2007-11-16 Published:2020-11-10
Contact: PENG Shuang-qing, male, PhD, professor, engaged in phamuacokopy aual toxirvdogy researdh. Tel: 010-66949631 E-mail: pengsq@hotmail.com
About author:WANG Yi-zei, mede, PhD, engaged in phamacolngpy and toxicokory research. Tel:010-66949631 E-mail:wuagvime12006@ 126.com
Supported by:
This work was supported by the National Naturul Srienve Fourniation of China (32813251).

摘要/Abstract

摘要： 目的: 评价新型抗胆碱能药物盐酸戊乙奎趾 (PHC)及其4个光学异构体 R-L、R-2, S-1和 S-2的细胞毒性。方法: 不同浓度的PHC及其光学异构体作用HepG2细胞24 h后,采用MTT法和中性红吸收法测定细胞毒性。结果: PHC及其光学异构体均能浓度依赖性地降低细胞存活率。根据半数抑制浓度(IC₅₀)比较这5个抗胆碱能化合物的细胞毒性: MTT法所测定的细胞毒性强弱次序为PHC>R-2>R-1 > S-2 > S-1,中性红吸收法所测定的细胞毒性强弱;弱次序为 R-2> PHC ≈ R-1 > S-2 > S-1。结论: 就HepG2细胞而言,R构型异构体的细胞毒性强于S构型并且,在PHC的4个光学异构体中,R-2的细胞毒性相对最强,而 S-1相对最弱。

关键词: 抗胆碱能药物, 盐酸戊乙奎脏, 光学异构体, 细胞毒性

Abstract: AIM: To evaluate the cytotoxicity of anovelanticholinergic drug penehyelidine hydrochloridle(PHC) and its four optical isomers R-1, R-2, S-1, and S-2. METHODS: Two in vitro assays. MTT assay andneutral red uptake 198ay, were used to evaluate the cyto-toxicity following PHC and its isomers exposure to HepG2cells at different concentrations. RESULTS: PHC and itsisomers induced decreases of viability of HepG2 ceils in aconcentration-dependent manner. Comparison of the cyto-toxicity of the five anticholinergic agents with 50% inhibi-tory concentration (ICg) values indlicated that the orderof potency was PHC> R-2> R-1> S2> S-1 for MTTassay, and R-2> PHC ≈ R-1> S2> S-1 for neutral reduplake assay. CONCLUSION: With respect to the cyto-toxicity of the four isomers on HepG2 cells, the config-uration was more potent than the S configuration, and R-2 was the most potent isomer whereas S-! was the leastpotent isomer among the four optical isomers.

Key words: anticholinergic drug, penehyclidine hydnochloride, opieal isomers, cytotoxicity

中图分类号:

R965.2

王以美, 彭双清, 仲伯华, 刘克良. 新型抗胆碱能药物盐酸戊乙奎酶及其光学异构体的细胞毒性评价[J]. 中国临床药理学与治疗学, 2007, 12(12): 1389-1389.

WANG Yi-mei, PENG Shuang-qing, ZHONG Bo-hua, LIU Ke-liang. Cytotoxicity evaluation of a novel anticholinergicdrug penehyclidine hydrochloride and its optical isomers[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2007, 12(12): 1389-1389.

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