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一种来自儿茶钩藤的新型α-葡萄糖苷酶抑制成分。

A novel α-glucosidase inhibitory constituent from Uncaria gambir.

作者信息

Kim Tae Hoon

机构信息

Department of Food Science and Biotechnology, Daegu University, 201 Daegudae-ro, Gyeongsan-si, Gyeongsangbuk-do, 38453, Republic of Korea.

出版信息

J Nat Med. 2016 Oct;70(4):811-5. doi: 10.1007/s11418-016-1014-0. Epub 2016 Jun 4.

DOI:10.1007/s11418-016-1014-0
PMID:27262298
Abstract

Bioactivity-guided fractionation of an aqueous methanolic extract of manufactured gambir product from Uncaria gambir with in vitro α-glucosidase inhibitory activity was performed to isolate a novel prenyl resorcinol derivative (1) together with seven known compounds, including two flavone glycosides (2, 3), three catechin analogues (4-6), and two simple phenolics (7, 8). Structures of the isolated compounds were determined by analysis of physical and spectroscopic data (NMR, UV, [α]D, and MS). All isolates were evaluated for in vitro α-glucosidase inhibitory activity. Among the compounds, novel compound 1, possessing an unprecedented spirocyclopropane ring in the molecule, showed the most potent α-glucosidase inhibitory activity in this assay. On the other hand, compounds 4 and 7 showed less potent inhibitory effects in this same bioassay, with half-maximal inhibitory concentration values of 17.3 ± 1.0 μM and 27.0 ± 0.9 μM, respectively.

摘要

对具有体外α-葡萄糖苷酶抑制活性的儿茶制成品的甲醇水提取物进行生物活性导向分离,以分离出一种新型异戊烯基间苯二酚衍生物(1)以及七种已知化合物,包括两种黄酮苷(2,3)、三种儿茶素类似物(4-6)和两种简单酚类(7,8)。通过物理和光谱数据(核磁共振、紫外、比旋光度和质谱)分析确定分离出的化合物的结构。对所有分离物进行体外α-葡萄糖苷酶抑制活性评估。在这些化合物中,分子中具有前所未有的螺环丙烷环的新型化合物1在此测定中显示出最有效的α-葡萄糖苷酶抑制活性。另一方面,化合物4和7在此相同生物测定中显示出较弱的抑制作用,其半数抑制浓度值分别为17.3±1.0μM和27.0±0.9μM。

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