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茄属生物碱对克氏锥虫体外生长的抑制作用:与酮康唑的比较。

Inhibition of Trypanosoma cruzi growth in vitro by Solanum alkaloids: a comparison with ketoconazole.

作者信息

Chataing B, Concepción J L, Lobatón R, Usubillaga A

机构信息

Departamento de Biologia, Universidad de Los Andes, Mérida, Venezuela.

出版信息

Planta Med. 1998 Feb;64(1):31-6. doi: 10.1055/s-2006-957361.

Abstract

The glycoalkaloids alpha-chaconine, alpha-solamargine, alpha-solanine, solasonine, sycophantine, and tomatine, as well as the aglycones demissidine, solanidine, solanocapsine, solasodine, tomatidine, and veratrine were tested as growth inhibitors of Trypanosoma cruzi, strain EP, in LIT medium. Their activity was compared with the antifungal ketoconazole. Glycoalkaloids containing alpha-chacotriose showed trypanolytic activity against the epimastigote form and trypanocidal activity against the bloodstream and metacyclic trypomastigote form of Trypanosoma cruzi in culture medium in micromolar concentrations. Ketoconazole showed a lower activity, at the same concentrations of alpha-chaconine and alpha-solamargine. The observations indicate that the initial target of the compound is at the membrane level with a concomitant change in the parasite morphology. Moreover, internal compartments of the parasites were observed to be affected by the drugs, revealing the dissolution of some organelles as mitocondrias and glycosomes.

摘要

在LIT培养基中,对糖生物碱α - 查茄碱、α - 茄碱、α - 龙葵碱、茄解碱、蜀羊泉碱和番茄碱,以及苷元去甲澳洲茄碱、茄啶、茄解啶、澳洲茄胺、番茄胺和藜芦碱进行了测试,以评估它们对克氏锥虫EP株的生长抑制作用。将它们的活性与抗真菌药酮康唑进行了比较。含有α - 查考三糖的糖生物碱在微摩尔浓度下,对培养基中的克氏锥虫无鞭毛体形式具有溶锥虫活性,对血流和循环后期锥鞭毛体形式具有杀锥虫活性。在相同浓度的α - 查茄碱和α - 茄碱下,酮康唑的活性较低。观察结果表明,该化合物的初始作用靶点在膜水平,同时伴随着寄生虫形态的变化。此外,观察到寄生虫的内部隔室受到药物影响,显示出一些细胞器如线粒体和糖体的溶解。

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