Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 23, Pages 7194-7197Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.09.049
Keywords
Hesperidin derivatives; Anti-hyperglycemic activity; Diabetic mice; alpha-Glucosidase inhibition
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Funding
- Fundamental Research Funds for the Central Universities of China [XDJK2009C087]
- Scientific Research Foundation for Ph. D of Southwest University of China [SWU111072, 111064]
- Chongqing Municipal Health Bureau of China [2011-1-114]
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A series of hesperidin derivatives were prepared and identified by IR, H-1 NMR, and MS spectra. These compounds were evaluated in vitro and in vivo based on alpha-glucosidase inhibition, glucose consumption of HepG2 cells, and blood glucose level in streptozotocin-induced diabetic mice. The results revealed that all the compounds exhibited anti-hyperglycemic activities. The inhibition at 10 (3) M of compounds 3 and 7a on alpha-glucosidase were 55.02% and 53.34%, respectively, as compared to 54.80% by acarbose. Treated by compound 3 and the reference drug metformin, glucose consumption of HepG2 cell were 1.78 and 2.11 mM, respectively. After the streptozotocin-induced diabetic mice were oral administrated with compound 3 at 100 mg kg (1) d (1) for 10 days, the blood glucose level of 3 treated mice (13.23 mM, P<0.05) showed significant difference when compared to model control (23.03 mM). Thus, compound 3 exhibited promising anti-hyperglycemic activity. (C) 2012 Elsevier Ltd. All rights reserved.
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