Strychnogucines A and B, two new antiplasmodial bisindole alkaloids from Strychnos icaja
Strychnogucines A and B, two new antiplasmodial bisindole alkaloids from Strychnos icaja
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DOI：
10.1021/np000285t
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发表时间：
2001-01-01
影响因子：
5.1
通讯作者：
Angenot, L
中科院分区：
文献类型：
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作者：
Frédérich, M;De Pauw, MC;Angenot, L
对马钱子根的重新研究发现，分离出两种三级准对称双吲哚生物碱，分别命名为马钱子碱A（1）和B（2）。它们的结构通过光谱数据解释进行了鉴定。化合物2在体外对四种恶性疟原虫株具有高活性，化合物1具有中等活性。马钱子碱B（2）对氯喹耐药菌株的活性高于对氯喹敏感菌株的活性（最佳CI 50，对W2菌株为80 nM）。此外，该化合物显示出选择性抗疟原虫活性，相对于培养的人癌细胞（KB）或人成纤维细胞（WI 38），对恶性疟原虫的毒性大25-180倍。
A reinvestigation of Strychnos icaja roots has resulted in the isolation of two tertiary quasi-symmetric bisindole alkaloids named strychnogucines A (1) and B (2). Their structures were identified by means of spectroscopic data interpretation. Compound 2 was highly active in vitro and compound 1 moderately active against four strains of Plasmodium falciparum. Strychnogucine B (2) was more active against a chloroquine-resistant strain than against a chloroquine-sensitive one (best CI50, 80 nM against the W2 strain). In addition, this compound showed a selective antiplasmodial activity with 25-180 times greater toxicity toward P. falciparum, relative to cultured human cancer cells (KB) or human fibroblasts (WI38).