School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou, PR China.
Arch Pharm (Weinheim). 2011 Feb;344(2):71-7. doi: 10.1002/ardp.201000147. Epub 2010 Nov 25.
This experiment was designed to synthesize 18 kinds of polyhydroxybenzophenones by using Friedel-Crafts reaction, and to measure the inhibitory activity on α-glucosidase with p-nitrophenyl-β-D-galactopyranoside (PNPG) as a substrate. Here, acarbose (IC(50) = 1674.75 µmol L(-1) ) was used as the reference inhibitor. The results demonstrated that most of the target compounds had remarkable inhibitory activities on α-glucosidase. Among all these compounds, 2,4,4',6-butahydroxydiphenylketone (11) was found to be the most potent α-glucosidase inhibitor with an IC(50) value of 10.62 µmol L(-1) . In addition, we found these compounds were competitive inhibitors through the kinetic analysis. The results suggested that such compounds might be utilized for the development of new candidates for diabetes treatment.
本实验旨在通过傅克反应合成 18 种多羟基二苯甲酮，并以对硝基苯-β-D-吡喃半乳糖苷（PNPG）为底物测定对α-葡萄糖苷酶的抑制活性。这里，阿卡波糖（IC（50）= 1674.75 μmol L（-1））被用作参考抑制剂。结果表明，大多数目标化合物对α-葡萄糖苷酶具有显著的抑制活性。在所有这些化合物中，2,4,4',6-四羟基二苯甲酮（11）被发现是最有效的α-葡萄糖苷酶抑制剂，其 IC（50）值为 10.62 μmol L（-1）。此外，通过动力学分析发现这些化合物是竞争性抑制剂。结果表明，这些化合物可能被用于开发治疗糖尿病的新型候选药物。
