Inhibitory effect on α-glucosidase by the fruits of Terminalia chebula Retz.
Inhibitory effect on α-glucosidase by the fruits of Terminalia chebula Retz.
复制标题
DOI：
10.1016/j.foodchem.2007.04.023
复制
发表时间：
2007-01-01
期刊：
影响因子：
8.8
通讯作者：
Kawabata, Jun
中科院分区：
文献类型：
--
作者：
Gao, Hong;Huang, Yi-Na;Kawabata, Jun
动物α -葡萄糖苷酶抑制活性研究。研究了水果。乙醇水提物对大鼠肠道麦芽糖酶有明显的抑制作用，而对肠道蔗糖酶和异麦芽糖酶均无抑制作用。采用生物测定法分离得到3种活性鞣花单宁，分别为chebulanin(1)、chebulagic acid(2)和chebulagic acid(3)，具有较强的肠道麦尔糖酶抑制活性，IC50值分别为690 μ M、97 μ M和36 μ M。2和3的肠道麦芽糖酶抑制活性甚至高于1,2,3,4,6-penta- o -没食子酰- β - d -葡萄糖（PGG） （4, IC50=140 mu M）， PGG是已知的有效的α -葡萄糖苷酶抑制剂。比较1- 4,1,2,3 - o -三烯丙基- β - d -葡萄糖(5)、新车黄酰酸(6)和芫花素(7)的活性表明，车黄酰和没食子酰基团的位置对药效影响最大。动力学研究表明，2、3和4非竞争性地抑制肠道α -葡萄糖苷酶的麦芽糖水解活性。本文首次报道了从板栗果实中分离得到的α -葡萄糖苷酶1、2和3的抑制作用。这些结果表明，使用T chebula果实提取物管理2型糖尿病。(c) 2007 Elsevier Ltd.版权所有。
Mammalian alpha-glucosidase inhibitory activity by Terminalia chebula Retz. fruits was investigated. The aqueous methanolic extract was found to have potent rat intestinal maltase inhibitory activity, whereas neither intestinal sucrase nor isomaltase activity was inhibited by this extract. Using bioassay-guided separation, three active ellagitannins were identified as chebulanin (1), chebulagic acid (2) and chebulinic acid (3) and were shown to possess potent intestinal maltase inhibitory activity, with the IC50 values of 690 mu M, 97 M and 36 l,mu M, respectively. The intestinal maltase inhibitory activities of 2 and 3 were even higher than that of 1,2,3,4,6-penta-O-galloyl-beta-D-glucose (PGG) (4, IC50=140 mu M), which is a known potent alpha-glucosidase inhibitor. Comparison of the activities of 1-4, 1,2,3-O-trigalloyl-beta-D-glucose (5), neochebulagic acid (6) and corilagin (7) suggested that the positions of chebulloyl and galloyl groups mostly affected the potency. Kinetic studies revealed that 2, 3, and 4 inhibited maltose-hydrolyzing activity of intestinal alpha-glucosidase, noncompetitively. This is the first report on mammalian alpha-glucosidase inhibition by 1, 2 and 3 isolated from T chebula fruits. These results suggest a use of the extract of T chebula fruits for managing Type 2 diabetes. (c) 2007 Elsevier Ltd. All rights reserved.