论文部分内容阅读
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。
Objective: To establish an in vitro screening method of antimalarial drugs combined with liver microsome metabolism. Methods: Based on the conventional method of culturing Plasmodium falciparum in screening antimalarial drugs in vitro, the in vitro metabolic system consisting of rat hepatic microsomes and oxidized coenzymes was added to detect the common anti-malaria drugs chloroquine, pyronaridine, Cycloguanidine and proguanil for anti-malarial activity. Results: In addition to the chloroguanidine, the other three drugs that anti-malarial drugs, but metformin must be metabolized into metabolites after the anti-malarial effect. CONCLUSIONS: The combination of metabolic antimalarial in vitro screening methods can avoid the screening of compounds that require malaria after metabolic conversion.