1. Academic Validation
  2. Inhibitory effect on α-glucosidase by Adhatoda vasica Nees

Inhibitory effect on α-glucosidase by Adhatoda vasica Nees

  • Food Chem. 2008 Jun 1;108(3):965-72. doi: 10.1016/j.foodchem.2007.12.002.
Hong Gao 1 Yi-Na Huang 2 Bo Gao 2 Peng Li 1 Chika Inagaki 1 Jun Kawabata 3
Affiliations

Affiliations

  • 1 Division of Applied Bioscience, Graduate School of Agriculture, Hokkaido University, Kita-ku, Sapporo 060-8589, Japan.
  • 2 Department of Public Health, Hua Xi Medical Center of Sichuan University, Chengdu, PR China.
  • 3 Division of Applied Bioscience, Graduate School of Agriculture, Hokkaido University, Kita-ku, Sapporo 060-8589, Japan. Electronic address: junk@chem.agr.hokudai.ac.jp.
Abstract

Methanolic extracts from the medicinal parts of 40 traditional Chinese herbs were tested in screening experiments for rat intestinal α-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 125μM and 250μM, 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 α-glucosidase competitively with Ki values of 82μM and 183μM, respectively. This is the first report on the mammalian α-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.

Keywords

Adhatoda vasica; Postprandial hyperglycemia; Sucrase inhibitor; α-Glucosidase.

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