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Synthesis and biological evaluation of indole derivatives containing thiazolidine-2,4-dione as α-glucosidase inhibitors with antidiabetic activity

2023; Elsevier BV; Volume: 264; Linguagem: Inglês

10.1016/j.ejmech.2023.115957

1768-3254

Chunmei Hu, Bingwen Liang, Jinping Sun, Jiangyi Li, Zhuang Xiong, Shao‐Hua Wang, Xue-Tao Xu,

Advanced Glycation End Products research

In order to develop potential α-glucosidase inhibitors with antidiabetic activity, twenty-six indole derivatives containing thiazolidine-2,4-dione were synthesized. All compounds presented potential α-glucosidase inhibitory activities with IC50 values ranging from 2.35 ± 0.11 to 24.36 ± 0.79 μM, respectively compared to acarbose (IC50 = 575.02 ± 10.11 μM). Especially, compound IT4 displayed the strongest α-glucosidase inhibitory activity (IC50 = 2.35 ± 0.11 μM). The inhibition mechanism of compound IT4 on α-glucosidase was clarified by the investigation of kinetics studies, fluorescence quenching, CD spectra, 3D fluorescence spectra, and molecular docking. In vivo antidiabetic experiments demonstrated that oral administration of compound IT4 would suppress fasting blood glucose level and ameliorate their glucose tolerance and dyslipidemia in diabetic mice.