小檗碱衍生物作为抗利什曼原虫药物

Berberine derivatives as antileishmanial drugs.

作者信息

Vennerstrom J L, Lovelace J K, Waits V B, Hanson W L, Klayman D L

机构信息

Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Washington, D.C. 20307.

出版信息

Antimicrob Agents Chemother. 1990 May;34(5):918-21. doi: 10.1128/AAC.34.5.918.

DOI:10.1128/AAC.34.5.918

PMID:2360830

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC171721/

Abstract

Berberine, a quaternary alkaloid, and several of its derivatives were tested for efficacy against Leishmania donovani and Leishmania braziliensis panamensis in golden hamsters. Tetrahydroberberine was less toxic and more potent than berberine against L. donovani but was not as potent as meglumine antimonate (Glucantime), a standard drug for the treatment of leishmaniasis. Only berberine and 8-cyanodihydroberberine showed significant activity (greater than 50% suppression of lesion size) against L. braziliensis panamensis.

摘要

小檗碱是一种季铵生物碱，对其几种衍生物在金黄仓鼠中进行了抗杜氏利什曼原虫和巴拿马利什曼原虫的疗效测试。四氢小檗碱对杜氏利什曼原虫的毒性比小檗碱低，效力更强，但不如治疗利什曼病的标准药物葡甲胺锑酸盐（葡糖胺锑）有效。只有小檗碱和8-氰基二氢小檗碱对巴拿马利什曼原虫显示出显著活性（病变大小抑制率大于50%）。