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首页> 外文期刊>Life sciences >2'-benzyloxychalcone derivatives stimulate glucose uptake in 3T3-L1 adipocytes.
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2'-benzyloxychalcone derivatives stimulate glucose uptake in 3T3-L1 adipocytes.

机译：2'-苄氧基查耳酮衍生物可刺激3T3-L1脂肪细胞摄取葡萄糖。

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摘要

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.
机译：通过基于细胞的葡萄糖摄取筛选测定法，鉴定了查耳酮衍生物3-硝基-2'-苄氧基查耳酮（化合物1）。化合物1在3T3-L1脂肪细胞中以浓度依赖的方式刺激了葡萄糖的摄取，并增强了胰岛素刺激的葡萄糖的摄取。当在化合物1存在下用各种浓度的胰岛素处理细胞时，在每种浓度下均观察到胰岛素刺激的葡萄糖摄取显着增强，表明该化合物可能起胰岛素增敏剂的作用。对结构-活性关系的初步研究表明，两个芳族苯环可以容忍多个取代基，但是被酸性或高极性基团取代可以消除该活性。在几种查耳酮衍生物中，4-氯-2'-苄氧基查耳酮（化合物8）显示出最高的活性水平。化合物8刺激的葡萄糖摄取几乎被渥曼青霉素完全抑制，渥曼青霉素是磷脂酰肌醇3-激酶（PI3K）的特异性抑制剂。这些结果表明查尔酮衍生物的作用是通过涉及PI3K的途径介导的。

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