Abstract

In this study, the antileishmanial and cytotoxic activities of secondary metabolites isolated from Tabernaemontana ventricosa Hochst. ex A. DC., Aloe tororoana Reynolds, and Aloe schweinfurthii var. labworana Reynolds were investigated. Overall, nineteen known compounds were isolated from the three plant species. The compounds were characterized based on their spectroscopic data. Voacristine and aloenin were the most active compounds against promastigotes of antimony-sensitive Leishmania donovani (IC₅₀ 11 ± 5.2 μM and 26 ± 6.5 µM, respectively) with low toxicity against RAW264.7, murine monocyte/macrophage-like cells. The in silico docking evaluation and in vitro NO generation assay also substantially support the antileishmanial effects of these compounds. In a cytotoxicity assay against cancer and normal cell lines, ursolic acid highly inhibited proliferation of lung cancer cells, A549 (IC₅₀ 6.61 ± 0.7 μM) while voacristine was moderately active against human liver cancer cells, HepG2 (IC₅₀ 23.0 ± 0.0 μM). All other compounds were inactive against the test parasites and cell lines.

摘要

在这项研究中，从Tabernaemontana ventricosa Hochst 中分离出的次级代谢物的抗寄生虫和细胞毒活性。ex A. DC.、芦荟 tororoana Reynolds 和芦荟 schweinfurthii var。labworana Reynolds 进行了调查。总体而言，从这三种植物中分离出了 19 种已知化合物。基于它们的光谱数据表征化合物。Voacristine 和 aloenin 是对锑敏感的多诺瓦尼利什曼原虫前鞭毛体最有效的化合物（IC ₅₀分别为 11 ± 5.2 μM 和 26 ± 6.5 μM），对 RAW264.7、鼠单核细胞/巨噬细胞样细胞具有低毒性。计算机对接评估和体外NO 生成分析也基本上支持这些化合物的抗寄生虫作用。在针对癌症和正常细胞系的细胞毒性试验中，熊果酸高度抑制肺癌细胞 A549 的增殖（IC ₅₀ 6.61 ± 0.7 μM），而 voacristine 对人肝癌细胞 HepG2 具有中等活性（IC ₅₀ 23.0 ± 0.0 μM） . 所有其他化合物对测试寄生虫和细胞系均无活性。