精油成分的杀利什曼原虫活性及构效关系
Leishmanicidal Activity and Structure-Activity Relationships of Essential Oil Constituents.
作者信息
Silva Audrey R S T, Scher Ricardo, Santos Flaviane V, Ferreira Sebastião R, Cavalcanti Sócrates C H, Correa Cristiane B, Bueno Lilian L, Alves Ricardo J, Souza Damião P, Fujiwara Ricardo T, Dolabella Silvio S
机构信息
Department of Pharmacy, Federal University of Sergipe, 49100-000 São Cristóvão, Sergipe, Brazil.
Laboratory of Molecular Biology of Pathogenic Bioagents, Department of Morphology, Federal University of Sergipe, 49100-000 São Cristóvão, Sergipe, Brazil.
出版信息
Molecules. 2017 May 16;22(5):815. doi: 10.3390/molecules22050815.
Several constituents of essential oils have been shown to be active against pathogens such as bacteria, fungi, and protozoa. This study demonstrated the in vitro action of ten compounds present in essential oils against promastigotes. With the exception of -cymene, all evaluated compounds presented leishmanicidal activity, exhibiting IC between 25.4 and 568.1 μg mL. Compounds with the best leishmanicidal activity presented a phenolic moiety (IC between 25.4 and 82.9 μg mL). Alicyclic alcohols ((-)-menthol and isoborneol) and ketones ((-)-carvone) promoted similar activity against the parasite (IC between 190.2 and 198.9 μg mL). Most of the compounds showed low cytotoxicity in L929 fibroblasts. Analysis of the structure-activity relationship of these compounds showed the importance of the phenolic structure for the biological action against the promastigote forms of the parasite.
精油的几种成分已被证明对细菌、真菌和原生动物等病原体具有活性。本研究展示了精油中存在的十种化合物对前鞭毛体的体外作用。除对伞花烃外，所有评估的化合物均表现出杀利什曼原虫活性，IC50在25.4至568.1μg/mL之间。具有最佳杀利什曼原虫活性的化合物含有酚基部分（IC50在25.4至82.9μg/mL之间）。脂环醇（(-)-薄荷醇和异龙脑）和酮（(-)-香芹酮）对寄生虫具有相似的活性（IC50在190.2至198.9μg/mL之间）。大多数化合物在L929成纤维细胞中显示出低细胞毒性。对这些化合物的构效关系分析表明，酚类结构对针对寄生虫前鞭毛体形式的生物学作用具有重要性。
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