二氢叶酸还原酶抑制剂对约氏疟原虫肝脏期的体外活性

Activity of dihydrofolate reductase inhibitors on the hepatic stages of Plasmodium yoelii yoelii in vitro.

作者信息

Eriksson B, Courtier B, Bjŏrkman A, Miltgen F, Mazier D

机构信息

Department of Infectious Diseases, Karolinska Institute, Roslagstull Hospital, Stockholm, Sweden.

出版信息

Trans R Soc Trop Med Hyg. 1991 Nov-Dec;85(6):725-6. doi: 10.1016/0035-9203(91)90429-3.

DOI:10.1016/0035-9203(91)90429-3

PMID:1801335

Abstract

The effects of the dihydrofolate reductase inhibitors proguanil and chlorproguanil, their active metabolites cycloguanil and chlorcycloguanil, and pyrimethamine, against the hepatic stages of Plasmodium yoelii yoellii were investigated in cultured BALB/c mouse hepatocytes. Proguanil was inactive at concentrations of 10(-8) M, whereas the other compounds were fully active at this and lower concentrations. Chlorcycloguanil was the most active compound and almost completely inhibited schizont development in concentrations as low as 10(-12) M.

摘要

在培养的BALB/c小鼠肝细胞中，研究了二氢叶酸还原酶抑制剂氯胍和氯丙胍、它们的活性代谢产物环氯胍和氯环氯胍以及乙胺嘧啶对约氏疟原虫肝脏期的作用。氯胍在10^(-8) M浓度下无活性，而其他化合物在此浓度及更低浓度下具有完全活性。氯环氯胍是最具活性的化合物，在低至10^(-12) M的浓度下几乎完全抑制裂殖体发育。