一种结合代谢的抗疟药体外筛选方法

中国寄生虫学与寄生虫病杂志 ›› 1997, Vol. 15 ›› Issue (2): 10-95.

一种结合代谢的抗疟药体外筛选方法

倪奕昌,徐月琴,朱滋扬

中国预防医学科学院寄生虫病研究所上海　200025

收稿日期:1900-01-01 修回日期:1900-01-01 出版日期:1997-04-30 发布日期:1997-04-30

IN VITRO ASSAY INCORPORATED WITH METABOLISM FOR SCREENING ANTIMALARIALS

Ni Yichang, Xu Yueqin, Zhu Ziyang

Institute of Parasitic Diseases, Chinese Academy of Preventive Medicine, Shanghai 200025

Received:1900-01-01 Revised:1900-01-01 Online:1997-04-30 Published:1997-04-30

摘要/Abstract

摘要：

目的: 建立一种结合肝微粒体代谢的抗疟药体外筛选方法。方法: 在恶性疟原虫体外培养筛选抗疟药的常规方法基础上, 加入以大鼠肝微粒体及氧化型辅酶II等辅助因子组成的体外代谢系统, 分别检测常用抗疟药氯喹、咯萘啶、环氯胍与氯胍的抗疟活性。结果: 除氯胍外, 其它3药的原药即有抗疟活性, 但氯胍必须经代谢转化成代谢产物后才有抗疟作用。结论: 结合代谢的抗疟药体外筛选方法可以避免漏筛那些需经代谢转化后才具抗疟作用的化合物。

关键词: 体外筛选方法, 代谢转化

Abstract:

AIM: To develop an in vitro assay incorporated with metabolism for screening antimalarials. METHODS: Antimalarial activities of chloroquine, pyronaridine, cycloproguanil and proguanil were tested with an in vitro assay based on the routine in vitro culture of P. falciparum incorporated with a metabolic system comprising rat liver microsomes and NADP cofactors. RESULTS: Except proguanil, the three drugs perse all showed antimalarial activities, but proguanil must be metabolized into its active metabolite for the antimalarial effect. CONCLUSION: The in vitro assay incorporated with metabolism could overcome the shortcoming of miss-screening the potential antimalarials which must be metabolically biotransformed into the active metabolite.

Key words: In vitro screening assay, metabolic transformation

倪奕昌;徐月琴;朱滋扬. 一种结合代谢的抗疟药体外筛选方法[J]. 中国寄生虫学与寄生虫病杂志, 1997, 15(2): 10-95.

NiYichang;XuYueqin;ZhuZiyang. IN VITRO ASSAY INCORPORATED WITH METABOLISM FOR SCREENING ANTIMALARIALS[J]. Chinese Journal of Parasitology and Parasitic Diseases, 1997, 15(2): 10-95.