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巴西亚马逊地区传统上用于治疗疟疾的植物——退热香果树提取物及其成分的体外抗疟活性

In vitro antiplasmodial activity of extract and constituents from Esenbeckia febrifuga, a plant traditionally used to treat malaria in the Brazilian Amazon.

作者信息

Dolabela Maria Fâni, Oliveira Salma G, Nascimento José Maria, Peres José Maria, Wagner Hildebert, Póvoa Marinete Marins, de Oliveira Alaíde Braga

机构信息

Faculdade de Farmácia, Universidade Federal de Minas Gerais, Av. Antônio Carlos, 6627, 31270-901 Belo Horizonte, MG, Brazil.

出版信息

Phytomedicine. 2008 May;15(5):367-72. doi: 10.1016/j.phymed.2008.02.001. Epub 2008 Mar 11.

DOI:10.1016/j.phymed.2008.02.001
PMID:18337075
Abstract

Esenbeckia febrifuga (Rutaceae) is a plant traditionally used to treat malaria in the Brazilian Amazon region. Ethanol extract of stems displayed a good antiplasmodial activity against Plasmodium falciparum strains W-2 (IC(50) 15.5+/-0.71 microg/ml) and 3 D7 (IC(50) 21.0+/-1.4 microg/ml). Two coumarins (bergaptene 1 and isopimpinellin 2), five alkaloids (flindersiamine 3, kokusaginine 4, skimmiamine 5, gamma-fagarine 6 and 1-hydroxy-3-methoxy-N-methylacridone, 7), besides a limonoid (rutaevine 8), have been isolated for the first time from this species. Antiplasmodial activity of compounds 3, 5-8 has been evaluated in vitro against P. falciparum strains (W-2 and 3D7) and the furoquinolines 5 and 6 were the most potent displaying IC(50) values <50 microg/ml; flindersiamine (3) showed a weak activity while alkaloid 7 and rutaevine (8) were inactive (IC(50)>100 microg/ml).

摘要

巴西苦木(芸香科)是一种传统上用于治疗巴西亚马逊地区疟疾的植物。其茎的乙醇提取物对恶性疟原虫W-2株(半数抑制浓度(IC50)为15.5±0.71微克/毫升)和3D7株(IC50为21.0±1.4微克/毫升)显示出良好的抗疟活性。首次从该物种中分离出两种香豆素(佛手柑内酯1和异茴芹素2)、五种生物碱(弗林德胺3、谷树碱4、茵芋碱5、γ-崖椒碱6和1-羟基-3-甲氧基-N-甲基吖啶酮7)以及一种柠檬苦素(芸香苦素8)。已对化合物3、5 - 8针对恶性疟原虫菌株(W-2和3D7)的抗疟活性进行了体外评估,呋喃喹啉类化合物5和6活性最强,IC50值<50微克/毫升;弗林德胺(3)显示出较弱的活性,而生物碱7和芸香苦素(8)无活性(IC50>100微克/毫升)。

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