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来自马钱子属伊卡马钱树根的新型抗疟和细胞毒性的苏古辛衍生物。

New antimalarial and cytotoxic sungucine derivatives from Strychnos icaja roots.

作者信息

Frédérich M, De Pauw M C, Llabrès G, Tits M, Hayette M P, Brandt V, Penelle J, De Mol P, Angenot L

机构信息

Department of Pharmacognosy, University of Liège, Belgium.

出版信息

Planta Med. 2000 Apr;66(3):262-9. doi: 10.1055/s-2000-8559.

Abstract

Reinvestigation of Strychnos icaja Baillon resulted in the isolation of vomicine, isostrychnine and of three new sungucine derivatives, named isosungucine (8), 18-hydroxy-sungucine (9) and 18-hydroxy-isosungucine (10). They were identified by detailed spectroscopic methods. The complete 1H- and 13C-NMR study of sungucine was also realized. Some of these compounds were highly active against Plasmodium falciparum in vitro and more particularly against the chloroquine-resistant strain. Compound 10 showed a selective antiplasmodial activity, with > 100-fold greater toxicity towards Plasmodium falciparum, relative to cultured human cancer cells (KB and HeLa lines) or fibroblasts (WI38).

摘要

对伊卡毒鼠李(Strychnos icaja Baillon)的重新研究导致分离出了育亨宾碱、异士的宁碱以及三种新的孙古辛衍生物,分别命名为异孙古辛(8)、18-羟基孙古辛(9)和18-羟基异孙古辛(10)。它们通过详细的光谱方法进行了鉴定。还对孙古辛进行了完整的1H和13C核磁共振研究。其中一些化合物在体外对恶性疟原虫具有高度活性,尤其是对氯喹耐药菌株。化合物10表现出选择性抗疟原虫活性,相对于培养的人类癌细胞(KB和HeLa细胞系)或成纤维细胞(WI38),其对恶性疟原虫的毒性大100倍以上。

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