一种结合代谢的抗疟药体外筛选方法  

IN VITRO ASSAY INCORPORATED WITH METABOLISM FOR SCREENING ANTIMALARIALS

作　　者：倪奕昌[1] 徐月琴[1] 朱滋扬 

机构地区：[1]中国预防医学科学院寄生虫病研究所,上海200025

出　　处：《中国寄生虫学与寄生虫病杂志》1997年第2期93-95,共3页Chinese Journal of Parasitology and Parasitic Diseases

基　　金：国家自然科学基金

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 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。AIM:To develop an in vitro assay incorporated with metabolism for screening antimala- rials.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.falci- parum incorporated with a metabolic system comprising rat liver microsomes and NADP co- factors.RESULTS:Except proguanil,the three drugs per se all showed antimalarial activi- ties,but proguanil must be metabolized into its active metabolite for the antimalarial effect. CONCLUSION:The in vitro assay incorporated with metabolism could overcome the short- coming of miss- screening the potential antimalarials which must be metabolically biotrans- formed into the active metabolite.

关 键 词：体外筛选方法 代谢转化 抗疟药 

分 类 号：R978.61[医药卫生—药品]