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In vitro inhibition of Plasmodium falciparum by substances isolated from Amazonian antimalarial plants.

机译:从亚马逊抗疟疾植物中分离的物质对恶性疟原虫的体外抑制作用。

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摘要

In the present study, a quassinoid, neosergeolide, isolated from the roots and stems of Picrolemma sprucei (Simaroubaceae), the indole alkaloids ellipticine and aspidocarpine, isolated from the bark of Aspidosperma vargasii and A. desmanthum (Apocynaceae), respectively, and 4-nerolidylcatechol, isolated from the roots of Pothomorphe peltata (Piperaceae), all presented significant in vitro inhibition (more active than quinine and chloroquine) of the multi-drug resistant K1 strain of Plasmodium falciparum. Neosergeolide presented activity in the nanomolar range. This is the first report on the antimalarial activity of these known, natural compounds. This is also the first report on the isolation of aspidocarpine from A. desmanthum. These compounds are good candidates for pre-clinical tests as novel lead structures with the aim of finding new antimalarial prototypes and lend support to the traditional use of the plants from which these compounds are derived.
机译:在本研究中,分别从云杉青皮豆科(Simaroubaceae),吲哚生物碱玫瑰树碱和aspidocarpine的根和茎中分离出一种类quassinoid,新蛇菊内酯,它们分别从天冬青属植物Aspidosperma vargasii和角果曲霉A. desmanthum(Apocynaceae)的树皮中分离出来。从菜豆(Pothomorphe peltata)(Piperaceae)的根中分离出的神经酰儿茶酚均对恶性疟原虫的多药耐药K1菌株具有显着的体外抑制作用(比奎宁和氯喹更具活性)。 Neosergeolide的活性在纳摩尔范围内。这是有关这些已知天然化合物抗疟疾活性的首次报道。这也是关于从车前曲霉中分离阿斯匹卡地平的首次报道。这些化合物作为新的先导结构是临床前测试的良好候选者,目的是寻找新的抗疟原形,并为衍生这些化合物的植物的传统用途提供支持。

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