墨西哥中部地区所产粉色-黄色栽培型 var. (L.) 的杀利什曼原虫活性化学成分研究。
Chemical Constituents with Leishmanicidal Activity from a Pink-Yellow Cultivar of var. (L.) Collected in Central Mexico.
机构信息
Posgrado en Ciencias Químico Biológicas, Facultad de Química, Universidad Autónoma de Querétaro, Cerro de las Campanas s/n, Querétaro 76010, México.
Laboratorio de Investigación Química y Farmacológica de Productos Naturales, Facultad de Química, Universidad Autónoma de Querétaro, Cerro de las Campanas s/n, Querétaro 76010, México.
出版信息
Int J Mol Sci. 2019 Feb 18;20(4):872. doi: 10.3390/ijms20040872.
(L.) is employed by several ethnical groups to treat numerous diseases. Although there are no ethnomedical reports on its use against leishmaniasis, organic extracts prepared from were shown to display leishmanicidal activity. In the present study, we carried out a bioassay-guided fractionation of the dichloromethane extract from Mexican in order to identify the compounds responsible for the leishmanicidal activity. Eighteen chromatographic fractions (FI⁻FXVIII) were evaluated in vitro against and . FII, FX, FXI, FXV, and FXVI showed significant activity against both strains, the most potent of which was FXV. Eicosane (), squalene (), β-ionone (), caryophyllene oxide (), β-caryophyllene (), hexanoic acid (), tiglic acid (), a mixture of lantanilic () and camaric () acids, and lantadene B () were identified and obtained from the active fractions and evaluated for their leishmanicidal activity. The mixture of lantanilic () and camaric () acids (79%/21%) was the most potent one (half maximal inhibitory concentration (IC) = 12.02 ± 0.36 μM). This study indicates that this cultivar of has high potential for the development of phytomedicines or as a source of natural products, which might represent lead compounds for the design of new drugs against leishmaniasis.
(L.)被多个族群雇佣来治疗多种疾病。尽管没有关于其用于治疗利什曼病的民族医学报告,但从 中制备的有机提取物显示出杀利什曼原虫活性。在本研究中,我们对来自墨西哥 的二氯甲烷提取物进行了基于生物测定的分离,以鉴定负责杀利什曼原虫活性的化合物。对 18 个色谱馏分(FI⁻FXVIII)进行了体外抗 和 的活性评价。FII、FX、FXI、FXV 和 FXVI 对两种 株均表现出显著的活性,其中最有效的是 FXV。二十烷()、角鲨烯()、β-紫罗兰酮()、石竹烯氧化物()、β-石竹烯()、己酸()、tiglic 酸()、lanthanilic()和 camaric()酸的混合物以及lantadene B()从活性馏分中鉴定和获得,并评估了它们的杀利什曼原虫活性。lanthanilic()和 camaric()酸的混合物(79%/21%)是最有效的(半最大抑制浓度(IC)= 12.02 ± 0.36 μM)。这项研究表明,这种 栽培品种具有开发植物药物或作为天然产物来源的巨大潜力,这可能代表着针对利什曼病的新型药物设计的先导化合物。