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海南蒌叶中的咔唑生物碱及其潜在的抗增殖活性。

Carbazole alkaloids from Clausena hainanensis with their potential antiproliferative activities.

机构信息

Key Laboratory of Tropical Medicinal Plant Chemistry of Ministry of Education, Hainan Normal University, Haikou 571158, PR China; College of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350122, PR China; Key Laboratory of Southern Medicinal Plants Resources of Haikou City, Hainan Normal University, Haikou 571158, PR China.

Key Laboratory of Tropical Medicinal Plant Chemistry of Ministry of Education, Hainan Normal University, Haikou 571158, PR China; Key Laboratory of Southern Medicinal Plants Resources of Haikou City, Hainan Normal University, Haikou 571158, PR China.

出版信息

Bioorg Chem. 2018 Feb;76:359-364. doi: 10.1016/j.bioorg.2017.12.016. Epub 2017 Dec 5.

Abstract

Five new carbazole alkaloids, clausehainanines A-E (1-5), together with seven known analogues (6-12) were isolated from the stems and leaves of C. hainanensis. Their structures were elucidated by extensive spectroscopic methods. Among them, compounds 1-5 were an unusual type of carbazole alkaloids, possessing diverse isopentenyl derivatives as substituents at C-2. All isolated compounds were evaluated for their antiproliferative activities against five human cancer cell lines: HL-60, SMMC-7721, A-549, MCF-7 and SW480 in vitro. Alkaloids 1-12 showed significant antiproliferative effects against various human cancer cell lines with IC values ranging from 0.12 to 15.56 μM. These findings suggest that the discoveries of these carbazole alkaloids with significant cytotoxic activities isolated from C. hainanensis could be of great importance to the development of new anticancer agents.

摘要

从海南秤钩风中茎和叶部分离得到了五个新的咔唑生物碱,即 clausehainanines A-E(1-5),以及七个已知类似物(6-12)。通过广泛的光谱方法阐明了它们的结构。其中,化合物 1-5 是一种不寻常的咔唑生物碱类型,在 C-2 位具有不同的异戊烯基衍生物作为取代基。所有分离得到的化合物均在体外对五种人癌细胞系(HL-60、SMMC-7721、A-549、MCF-7 和 SW480)进行了抗增殖活性评价。生物碱 1-12 对各种人癌细胞系具有显著的抗增殖作用,IC 值范围为 0.12-15.56μM。这些发现表明,从海南秤钩风中分离得到的具有显著细胞毒性的这些咔唑生物碱的发现对于开发新型抗癌药物具有重要意义。

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