Mizuno Cassia S, Souza Ariana B, Tekwani Babu L, Ambrósio Sérgio R, Veneziani Rodrigo C S
Department of Pharmaceutical Sciences, University of New England College of Pharmacy, 716 Stevens Ave, Portland, ME 04103, USA.
Núcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Av. Dr. Armando Salles de Oliveira, 201 Parque Universitário, 14404-600 Franca, SP, Brazil.
Bioorg Med Chem Lett. 2015 Dec 1;25(23):5529-31. doi: 10.1016/j.bmcl.2015.10.062. Epub 2015 Oct 21.
Polyalthic acid is a naturally occurring diterpene found in copaiba oil, one of the most popular natural medicines in the Amazon. Based on the reported antileishmanial activity of copaiba oil, a series of amides and diols derivatives of polyalthic acid were synthesized and tested against Leishmania donovani and Trypanosoma brucei. Polyalthic acid was active in both assays with IC50 ranging from 3.87 to 8.68 μg/mL. The compound with best antileishmanial activity was 2 h (IC50=3.84 μg/mL) and compound 2c showed the best antitrypanosomal activity with an IC50 of 2.54 μg/mL.
多球花酸是一种天然存在的二萜类化合物，存在于苦配巴油中，苦配巴油是亚马逊地区最受欢迎的天然药物之一。基于报道的苦配巴油的抗利什曼原虫活性，合成了一系列多球花酸的酰胺和二醇衍生物，并对杜氏利什曼原虫和布氏锥虫进行了测试。多球花酸在两种试验中均具有活性，IC50范围为3.87至8.68μg/mL。抗利什曼原虫活性最佳的化合物是2h（IC50 = 3.84μg/mL），化合物2c显示出最佳的抗锥虫活性，IC50为2.54μg/mL。
