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α-Glucosidase Inhibitory Isomeric Corniculatolides from the Stems of the Indian Mangrove Plant, Xylocarpus granatum.
Journal of Natural Products ( IF 3.3 ) Pub Date : 2020-01-02 , DOI: 10.1021/acs.jnatprod.9b00414
Bolatito E Olanipekun 1, 2 , Mangala G Ponnapalli , Karimulla Shaik , Jagadeesh B Nanubolu , Vamsi K Kommalapati 3 , Anjana D Tangutur 3
Affiliation  

Three new isomeric corniculatolides (1, 2, and 3) with an unusual caffrane and isocorniculane framework, and five known metabolites were isolated from the chloroform extract of the stems of Xylocarpus granatum. The structures of the new metabolites were deduced as corniculatolide B (1), isocorniculatolide B (2), and corniculatolide C (3) by spectroscopic data analysis and a combination of chemical transformations and supported by single-crystal X-ray crystallographic data of 1 and 3. The isolated compounds were evaluated for their in vitro cytotoxicity and α-glucosidase (Saccharomyces cerevisiae) inhibitory potential. Compound 3 possessed α-glucosidase inhibitory activity with an IC50 value of 24.8 μM, whereas these rare macrolides showed no effect on the mammalian cancer cell lines MIAPaCa-2, DU145, MCF-7, and HTC-116.

中文翻译:

来自印度红树林植物木香木的茎中的α-葡萄糖苷酶抑制异构体山茱ula内酯。

从木果木茎的氯仿提取物中分离出三种新的异构体角鲨醛内酯(1、2和3),它们具有不寻常的樟脑和异角鲨烷骨架,以及五种已知的代谢物。通过光谱数据分析和化学转化的组合推论出新代谢物的结构为角鲨脲内酯B(1),异角鲨内酯B(2)和角鲨内酯C(3),并得到1的单晶X射线晶体学数据的支持3.评价分离的化合物的体外细胞毒性和α-葡萄糖苷酶(酿酒酵母)的抑制潜力。化合物3具有α-葡萄糖苷酶抑制活性,IC50值为24.8μM,而这些稀有的大环内酯类药物对哺乳动物癌细胞系MIAPaCa-2,DU145,MCF-7和HTC-116没有作用。
更新日期:2020-01-04
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