Department of Life Science and Institute of Biotechnology, National Dong-Hwa University, Hualien 97401, Taiwan.
Neural Regeneration Laboratory, Neurological Institute, Taipei Veterans General Hospital, Taipei 11217, Taiwan.
Molecules. 2018 Sep 5;23(9):2260. doi: 10.3390/molecules23092260.
The inhibition of α-glucosidase and α-amylase is a clinical strategy for the treatment of type II diabetes, and herbal medicines have been reported to credibly alleviate hyperglycemia. Our previous study has reported some constituents from plant or herbal sources targeted to α-glucosidase and α-amylase via molecular docking and enzymatic measurement, but the hypoglycemic potencies in cell system and mice have not been validated yet. This study was aimed to elucidate the hypoglycemic efficacy of docking selected compounds in cell assay and oral glucose and starch tolerance tests of mice. All test compounds showed the inhibition of α-glucosidase activity in Caco-2 cells. The decrease of blood sugar levels of test compounds in 30 min and 60 min of mice after OGTT and OSTT, respectively and the decreased glucose levels of test compounds were significantly varied in acarbose. Taken altogether, in vitro and in vivo experiments suggest that selected natural compounds (curcumin, antroquinonol, HCD, docosanol, tetracosanol, rutin, and actinodaphnine) via molecular docking were confirmed as potential candidates of α-glucosidase and α-amylase inhibitors for treating diabetes.
抑制α-葡萄糖苷酶和α-淀粉酶是治疗 II 型糖尿病的临床策略，据报道，草药可有效缓解高血糖。我们之前的研究通过分子对接和酶测定，从植物或草药来源报告了一些针对α-葡萄糖苷酶和α-淀粉酶的成分，但尚未在细胞系统和小鼠中验证其降血糖作用。本研究旨在阐明对接选择化合物在细胞测定和小鼠口服葡萄糖和淀粉耐量试验中的降血糖功效。所有测试化合物均显示在 Caco-2 细胞中抑制α-葡萄糖苷酶活性。在 OGTT 和 OSTT 后 30 分钟和 60 分钟，测试化合物在小鼠中的血糖水平降低，并且与阿卡波糖相比，测试化合物的葡萄糖水平降低显著不同。总之，体外和体内实验表明，通过分子对接选择的天然化合物（姜黄素、安特曲醌醇、HCD、二十二烷醇、二十四烷醇、芦丁和actinodaphnine）被确认为治疗糖尿病的α-葡萄糖苷酶和α-淀粉酶抑制剂的潜在候选物。
