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体外评价对苯丙烯酸异戊烯基衍生物的抗利什曼原虫和抗血吸虫活性。

In vitro Evaluation of the Antileishmanial and Antischistosomal Activities of p-Coumaric Acid Prenylated Derivatives.

机构信息

Department of Chemistry, Faculty of Philosophy, Science and Letters at Ribeirão Preto, University of São Paulo, 14040-901, Ribeirão Preto, SP, Brazil.

Research Center in Exact and Technological Sciences, University of Franca, 14404-600, Franca, SP, Brazil.

出版信息

Chem Biodivers. 2024 May;21(5):e202400491. doi: 10.1002/cbdv.202400491. Epub 2024 Apr 12.

DOI:10.1002/cbdv.202400491
PMID:38470945
Abstract

We have evaluated eight p-coumaric acid prenylated derivatives in vitro for their antileishmanial activity against Leishmania amazonensis promastigotes and their antischistosomal activity against Schistosoma mansoni adult worms. Compound 7 ((E)-3,4-diprenyl-4-isoprenyloxycinnamic alcohol) was the most active against L. amazonensis (IC=45.92 μM) and S. mansoni (IC=64.25 μM). Data indicated that the number of prenyl groups, the presence of hydroxyl at C9, and a single bond between C7 and C8 are important structural features for the antileishmanial activity of p-coumaric acid prenylated derivatives.

摘要

我们评估了 8 种对香豆酸二萜类衍生物的体外抗利什曼原虫活性,以评估其对利什曼原虫亚马逊前鞭毛体的抗利什曼原虫活性,以及对曼氏血吸虫成虫的抗血吸虫活性。化合物 7((E)-3,4-二-3-甲基-2-丁烯基-4-异戊烯氧基肉桂醇)对 L. amazonensis(IC=45.92 μM)和 S. mansoni(IC=64.25 μM)的活性最高。数据表明,二萜类化合物的数量、C9 位的羟基以及 C7 和 C8 之间的单键是对香豆酸二萜类衍生物抗利什曼原虫活性的重要结构特征。

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