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考斯塔里辛,一种从柳叶楠树干树皮中提取的新型抗疟双苄基异喹啉生物碱。

Costaricine, a new antiplasmodial bisbenzylisoquinoline alkaloid from Nectandra salicifolia trunk bark.

作者信息

Böhlke M, Guinaudeau H, Angerhofer C K, Wongpanich V, Soejarto D D, Farnsworth N R, Mora G A, Poveda L J

机构信息

Program for Collaborative Research in the Pharmaceutical Sciences, College of Pharmacy, University of Illinois at Chicago 60612, USA.

出版信息

J Nat Prod. 1996 Jun;59(6):576-80. doi: 10.1021/np960195h.

DOI:10.1021/np960195h
PMID:8786363
Abstract

A MeOH extract of Nectandra salicifolia trunk bark, obtained during a diversity-based plant collection in a lower montane rainforest in Costa Rica, showed activity in an in vitro antiplasmodial assay measuring incorporation of [3H]-labeled hypoxanthie by Plasmodium falciparum. In addition to 15 known alkaloids isolated from samples of trunk bark, roots, and leaves/twigs of this species, a new bisbenzylisoquinoline alkaloid (+)-costaricine [(+)-12-O-methyllindoldhamine] (1) was isolated from bark (0.038% yield) and from roots (0.001%). (+)-Costaricine was active in the antiplasmodial assay, with IC50 values of 50 ng/mL vs. the chloroquine-sensitive D6 clone and 294 ng/mL vs. the chloroquine-resistant W2 clone of P. falciparum.

摘要

在哥斯达黎加低山地雨林进行的一次基于生物多样性的植物采集活动中,获得了柳叶楠树干树皮的甲醇提取物,该提取物在一项体外抗疟原虫试验中表现出活性,该试验通过测量恶性疟原虫对[3H]标记次黄嘌呤的摄取来进行。除了从该物种的树干树皮、根以及叶/嫩枝样品中分离出的15种已知生物碱外,还从树皮(产率0.038%)和根(产率0.001%)中分离出一种新的双苄基异喹啉生物碱(+)-哥斯达黎碱[(+)-12-O-甲基去甲劳丹碱](1)。(+)-哥斯达黎碱在抗疟原虫试验中具有活性,对氯喹敏感的D6克隆株的IC50值为50 ng/mL,对氯喹耐药的W2克隆株的IC50值为294 ng/mL。

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