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纳米乳剂的开发以增强油树脂的抗利什曼原虫活性。

Development of Nanoemulsions to Enhance the Antileishmanial Activity of Oleoresins.

机构信息

Department of Natural Products and Food, School of Pharmacy, Federal University of Rio de Janeiro, 21941-590 Rio de Janeiro, RJ, Brazil.

Laboratory of Medicinal Plants and Derivatives, Rua Sizenando Nabuco 100, Manguinhos, 21041-250 Rio de Janeiro, RJ, Brazil.

出版信息

Biomed Res Int. 2018 Apr 4;2018:9781724. doi: 10.1155/2018/9781724. eCollection 2018.

Abstract

Based on the ethnopharmacological evidences about the antileishmanial activity of spp. oleoresins, the effects of crude extracts and fractions of oleoresin of two specimens from were evaluated on and strains. The oleoresin rich in -copaene (38.8%) exhibited the best activity against (IC = 62.5 g/mL) and against (IC = 65.9 g/mL). The sesquiterpene -copaene isolated was tested alone and exhibited high antileishmanial activity with IC values for and of 17.2 and 11.4 g/mL, respectively. In order to increase antileishmanial activity, nanoemulsions containing copaiba oleoresin and -copaene were developed and assayed against and promastigotes. The nanoemulsion containing -copaene (NANOCOPAEN) showed the best activity against both species, with IC of 2.5 and 2.2 g/mL, respectively. This is the first report about the antileishmanial activity of -copaene.

摘要

基于关于 spp. 挥发油的抗利什曼原虫活性的民族药理学证据,评估了来自 2 种标本的挥发油粗提取物和馏分对 和 株的作用。富含 -古巴烯(38.8%)的挥发油对 (IC = 62.5 μg/mL)和 (IC = 65.9 μg/mL)表现出最好的活性。分离出的倍半萜 -古巴烯单独测试时表现出很高的抗利什曼原虫活性,对 和 的 IC 值分别为 17.2 和 11.4 μg/mL。为了提高抗利什曼原虫活性,制备了含有 Copaiba 挥发油和 -古巴烯的纳米乳液,并对 和 前鞭毛体进行了检测。含有 -古巴烯的纳米乳液(NANOCOPAEN)对两种物种均表现出最好的活性,IC 分别为 2.5 和 2.2 μg/mL。这是首次报道 -古巴烯的抗利什曼原虫活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/56dd/5904801/da17bcfdaa1e/BMRI2018-9781724.001.jpg

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