Inhibitory effect on α-glucosidase by Adhatoda vasica Nees
Inhibitory effect on α-glucosidase by Adhatoda vasica Nees
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DOI：
10.1016/j.foodchem.2007.12.002
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发表时间：
2008-06-01
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
对40种中草药药用部位的甲醇提取物进行了大鼠肠道α-葡萄糖苷酶的筛选实验。以蔗糖为底物时，紫茎针藤叶的甲醇提取物对蔗糖酶的抑制活性最高。该提取物经酶法分级分离得到vasicine（1）和vasicinol（2），并根据MS和NMR分析确定了这些化合物的结构。化合物1和2显示出高的蔗糖酶抑制活性，IC 50值分别为125 μ M和250 μ M。1和2都是蔗糖酶的可逆抑制剂。动力学数据表明，化合物1和2抑制蔗糖水解活性的大鼠肠道α-葡萄糖苷酶竞争性的Ki值分别为82 μ M和183 M。这是首次报道哺乳动物α-葡萄糖苷酶抑制A. vasica和1和2对蔗糖酶的抑制作用。这些结果表明，A. vasica作为抗糖尿病剂，并显示化合物1和2可能是代谢紊乱的有用治疗。(c)2007爱思唯尔有限公司保留所有权利。
Methanolic extracts from the medicinal parts of 40 traditional Chinese herbs were tested in screening experiments for rat intestinal alpha-glucosidase. The methanolic extract from the leaves of Adhatoda vasica Nees (Acanthaceae) showed the highest sucrase inhibitory activity with sucrose as a substrate. Enzyme assay-guided fractionation of this extract afforded vasicine (1) and vasicinol (2), and the structures of these compounds were elucidated on the basis of MS and NMR analysis. Compounds 1 and 2 showed a high sucrase inhibitory activity, and the IC50 values were 125 mu M and 250 mu M, respectively. Both 1 and 2 were shown to be reversible inhibitors of sucrase. Kinetic data revealed that compounds 1 and 2 inhibited sucrose-hydrolysing activity of rat intestinal alpha-glucosidase competitively with K-i values of 82 mu M and 183 M, respectively. This is the first report on the mammalian alpha-glucosidase inhibition of A. vasica and the inhibitory effect on sucrase by 1 and 2 from this herb species. These results suggest a use of the extract of A. vasica as an antidiabetic agent and show a possibility that compounds 1 and 2 could be an useful treatment for metabolic disorders. (c) 2007 Elsevier Ltd. All rights reserved.