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来自鼎湖地不容的氧代阿朴啡生物碱和醌类及其抗寄生虫活性评价

Oxoaporphine alkaloids and quinones from Stephania dinklagei and evaluation of their antiprotozoal activities.

作者信息

Camacho M R, Kirby G C, Warhurst D C, Croft S L, Phillipson J D

出版信息

Planta Med. 2000 Jun;66(5):478-80. doi: 10.1055/s-2000-8597.

DOI:10.1055/s-2000-8597
PMID:10909274
Abstract

Bioactivity-guided fractionation of Stephania dinklagei yielded six compounds including, two zwitterionic oxoaporphine alkaloids, N-methylliriodendronine, and 2-O,N-dimethylliriodendronine, two oxoaporphine alkaloids, liriodenine, and dicentrinone, one aporphine alkaloid, corydine, and one anthraquinone, aloe-emodin. Apart from corydine, the isolates have not been reported as constituents of S. dinklagei. N-Methylliriodendronine, and 2-O,N-dimethylliriodendronine are reported for the first time as natural products. All isolated compound were tested for antiprotozoal activity and cytotoxic activities in vitro. N-Methylliriodendronine was the most active against L. donovani amastigotes (IC50 = 36.1 microM). Liriodenine showed the highest activity against Leishmania donovani, and Plasmodium falciparum with IC50 values of 26.16 and 15 microM, respectively. Aloe-emodin was the only compound active (IC50 = 14 microM) against T. b. brucei.

摘要

对鼎湖地不容进行生物活性导向的分离,得到了六种化合物,包括两种两性离子型氧化阿朴啡生物碱,N-甲基鹅掌楸碱和2-O,N-二甲基鹅掌楸碱,两种氧化阿朴啡生物碱,鹅掌楸碱和二氢石蒜碱,一种阿朴啡生物碱,紫堇定,以及一种蒽醌,芦荟大黄素。除紫堇定外,这些分离物尚未被报道为鼎湖地不容的成分。N-甲基鹅掌楸碱和2-O,N-二甲基鹅掌楸碱作为天然产物首次被报道。所有分离出的化合物都进行了体外抗原生动物活性和细胞毒性活性测试。N-甲基鹅掌楸碱对杜氏利什曼原虫无鞭毛体最具活性(IC50 = 36.1微摩尔)。鹅掌楸碱对杜氏利什曼原虫和恶性疟原虫表现出最高活性,IC50值分别为26.16和15微摩尔。芦荟大黄素是唯一对布氏锥虫有活性的化合物(IC50 = 14微摩尔)。

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