School of Chemistry, Sun Yat-sen University, 135 Xingang West Road, Guangzhou, 510275, PR China.
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510080, PR China.
Eur J Med Chem. 2017 Apr 21;130:51-59. doi: 10.1016/j.ejmech.2017.02.007. Epub 2017 Feb 7.
Two series of compounds (chalcones and bis-chalcones) were designed, synthesized, and evaluated as α-glucosidase inhibitors (AGIs) with 1-deoxynojirimycin as positive control in vitro. Most of the compounds with two or four hydroxyl groups showed better inhibitory activities than 1-deoxynojirimycin towards α-glucosidase with noncompetitive mechanism. Moreover, most of the hydroxy bis-chalcones exhibit good α-glucosidase inhibitory activities in enzyme test. Inspiringly, bis-chalcones 2g (at 1 μM concentration) has stronger effect than 1-deoxynojirimycin on reducing the glucose level in HepG-2 cells (human liver cancer cell line).
设计、合成了两个系列的化合物（查耳酮和双查耳酮），并将其作为α-葡萄糖苷酶抑制剂（AGIs）进行了评估，以 1-脱氧野尻霉素作为阳性对照进行了体外研究。大多数具有两个或四个羟基的化合物对α-葡萄糖苷酶的抑制活性均优于 1-脱氧野尻霉素，且具有非竞争性抑制机制。此外，大多数羟基双查耳酮在酶试验中均表现出良好的α-葡萄糖苷酶抑制活性。令人鼓舞的是，双查耳酮 2g（在 1μM 浓度下）在降低 HepG-2 细胞（人肝癌细胞系）中的葡萄糖水平方面比 1-脱氧野尻霉素的效果更强。
