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青草药 Clinacanthus nutans 的化学成分表征、抗增殖和抗真菌活性。

Chemical characterization, antiproliferative and antifungal activities of Clinacanthus nutans.

机构信息

Institute of Microbial Pharmaceuticals, College of Life and Health Sciences, Northeastern University, Shenyang 110819, PR China.

School of Biotechnology and Health Sciences, Wuyi University, Jiangmen 529020, PR China.

出版信息

Fitoterapia. 2021 Nov;155:105061. doi: 10.1016/j.fitote.2021.105061. Epub 2021 Oct 18.

DOI:10.1016/j.fitote.2021.105061
PMID:34673146
Abstract

Clinacanthus nutans Lindau (Family: Acanthaceae) is a medicinal herb widely distributed in the tropic and subtropic areas of Asia. C. nutans is traditionally consumed as vegetable or herbal tea, as well as a folk medicine for anticancer and antifungal activities. However, to date, chemical constituent responsible for observed health beneficial effects of this medicinal plant is not clear. In the current study, 32 compounds (1-32), including three new megastigmanes (1-3) were isolated from the aerial parts of C. nutans. Their structures were elucidated on the basis of comprehensive NMR, MS, and CD spectroscopic data analysis, as well as chemical hydrolysis. Among the isolates, cycloartane triterpenoids (9, 10, and 12) displayed moderate anti-proliferative effects against HepG2 cell growth with IC values ranging from 9.12 to 19.89 μM. Data obtained from flow cytometry analysis and western blotting assays revealed that compounds 9 and 12 induced apoptosis of HepG2 cells by modulating the expression of proteins associated to mitochondrial-mediated apoptotic pathway. Furthermore, megastigmanes 1, 2, 7, and 8 enhanced the anti-Candida albicans activity of amphotericin B (AmB), supporting the synergistic effects between megastigmanes and AmB. This is the first report of anticancer and antifungal potential of cycloartane triterpenoids and megastigmanes in C. nutans, which shed useful insights on the relationship between C. nutans's chemical constituent and its beneficial effects to health. Findings from this study support further development of this medicinal plant for potential pharmaceutical applications.

摘要

灵南菜(爵床科)是一种广泛分布在亚洲热带和亚热带地区的药用草本植物。灵南菜通常被当作蔬菜或草药茶食用,也被民间用作具有抗癌和抗真菌活性的药物。然而,迄今为止,这种药用植物中负责观察到的健康有益效果的化学成分仍不清楚。在目前的研究中,从灵南菜的地上部分分离得到了 32 种化合物(1-32),包括三种新的巨豆三烯(1-3)。它们的结构是基于全面的 NMR、MS 和 CD 光谱数据分析以及化学水解来阐明的。在分离得到的化合物中,环阿屯三萜(9、10 和 12)对 HepG2 细胞的生长表现出中等的抗增殖作用,IC 值范围为 9.12-19.89 μM。流式细胞术分析和 Western blot 检测结果显示,化合物 9 和 12 通过调节与线粒体介导的凋亡途径相关的蛋白表达诱导 HepG2 细胞凋亡。此外,巨豆三烯 1、2、7 和 8 增强了两性霉素 B(AmB)对白色念珠菌的抗真菌活性,支持巨豆三烯与 AmB 之间的协同作用。这是首次报道环阿屯三萜和巨豆三烯在灵南菜中具有抗癌和抗真菌潜力的研究,为灵南菜化学成分与其对健康有益的关系提供了有用的见解。本研究结果支持进一步开发这种药用植物用于潜在的药物应用。

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