2'-benzyloxychalcone derivatives stimulate glucose uptake in 3T3-L1 adipocytes |
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Authors: | Kamei Reiko Kadokura Michinori Kitagawa Yoshinori Hazeki Osamu Oikawa Shinzo |
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Affiliation: | Daiichi Suntory Biomedical Research Co. LTD, 1-1-1 Wakayamadai, Shimamoto-cho, Mishima-gun, 618-8513 Osaka, Japan. |
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Abstract: | By a cell-based glucose uptake screening assay, a chalcone derivative, 3-nitro-2'-benzyloxychalcone (compound 1) was identified. Compound 1 stimulated glucose uptake and potentiated insulin-stimulated glucose uptake in a concentration-dependent manner in 3T3-L1 adipocytes. When cells were treated with various concentrations of insulin in the presence of compound 1, marked enhancement of insulin-stimulated glucose uptake was observed at each concentration, suggesting that the compound might function as an insulin sensitizer. Preliminary study on the structure-activity relationships revealed that two aromatic benzene rings tolerated several substituents, but substitution by acidic or highly polar groups abolished the activity. Among several chalcone derivatives, 4-chloro-2'-benzyloxychalcone (compound 8) showed the highest level of activity. Compound 8-stimulated glucose uptake was almost completely inhibited by wortmannin, a specific inhibitor of phosphatidylinositol 3-kinase (PI3K). These results suggest that the action of chalcone derivatives is mediated via a pathway involving PI3K. |
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