Department of Biotechnology, Nigerian Defence Academy, PMB 2109, Kaduna, Kaduna State, Nigeria.
Department of Biological Sciences, Nigerian Defence Academy, PMB 2109, Kaduna, Kaduna State, Nigeria.
Exp Parasitol. 2024 Aug-Sep;263-264:108807. doi: 10.1016/j.exppara.2024.108807. Epub 2024 Jul 21.
African trypanosomiasis and malaria are among the most severe health challenges to humans and livestock in Africa and new drugs are needed. Leaves of Hyptis suaveolens Kuntze (Lamiaceae) and Momordica charantia L. (Cucurbitaceae) were extracted with hexane, ethyl acetate, and then methanol, and subjected to silica gel column chromatography. Structures of six isolated compounds were elucidated through NMR and HR-EIMS spectrometry. Callistrisic acid, dehydroabietinol, suaveolic acid, suaveolol, and a mixture of suaveolol and suaveolic acid (SSA) were obtained from H. suaveolens, while karavilagenin D and momordicin I acetate were obtained from M. charantia. The isolated biomolecules were tested against trypomastigotes of Trypanosoma brucei brucei and T. congolense, and against Plasmodium falciparum. The most promising EC values were obtained for the purified suaveolol fraction, at 2.71 ± 0.36 μg/mL, and SSA, exhibiting an EC of 1.56 ± 0.17 μg/mL against T. b. brucei trypomastigotes. Suaveolic acid had low activity against T. b. brucei but displayed moderate activity against T. congolense trypomastigotes at 11.1 ± 0.5 μg/mL. Suaveolol and SSA were also tested against T. evansi, T. equiperdum, Leishmania major and L. mexicana but the antileishmanial activity was low. Neither of the active compounds, nor the mixture of the two, displayed any cytotoxic effect on human foreskin fibroblast (HFF) cells at even the highest concentration tested, being 200 μg/mL. We conclude that suaveolol and its mixture possessed significant and selective trypanocidal activity.
非洲锥虫病和疟疾是非洲人类和牲畜面临的最严重的健康挑战之一,需要新的药物。从 Hyptis suaveolens Kuntze(唇形科)和 Momordica charantia L.(葫芦科)的叶子中用己烷、乙酸乙酯和甲醇提取,并进行硅胶柱层析。通过 NMR 和 HR-EIMS 光谱学阐明了六种分离化合物的结构。从 H. suaveolens 中得到了 Callistrisic 酸、脱氢枞醇、suaveolic 酸、suaveolol 以及 suaveolol 和 suaveolic 酸的混合物(SSA),而从 M. charantia 中得到了 karavilagenin D 和 momordicin I 乙酸酯。分离的生物分子针对 Trypanosoma brucei brucei 和 T. congolense 的锥虫和 Plasmodium falciparum 进行了测试。从纯化的 suaveolol 部分获得了最有希望的 EC 值,为 2.71 ± 0.36 μg/mL,而 SSA 对 T. b. brucei 锥虫的 EC 值为 1.56 ± 0.17 μg/mL。suaveolic 酸对 T. b. brucei 的活性较低,但对 T. congolense 锥虫的活性适中,为 11.1 ± 0.5 μg/mL。Suaveolol 和 SSA 也针对 T. evansi、T. equiperdum、Leishmania major 和 L. mexicana 进行了测试,但抗利什曼原虫活性较低。即使在测试的最高浓度 200 μg/mL 下,也没有任何一种活性化合物或两者的混合物对人包皮成纤维细胞(HFF)细胞显示出任何细胞毒性作用。我们得出结论,suaveolol 及其混合物具有显著的选择性杀锥虫活性。