Proença Carina, Freitas Marisa, Ribeiro Daniela, Oliveira Eduardo F T, Sousa Joana L C, Tomé Sara M, Ramos Maria J, Silva Artur M S, Fernandes Pedro A, Fernandes Eduarda
a UCIBIO, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy , University of Porto , Porto , Portugal.
b UCIBIO, REQUIMTE, Faculty of Sciences, Department of Chemistry and Biochemistry , University of Porto , Porto , Portugal.
J Enzyme Inhib Med Chem. 2017 Dec;32(1):1216-1228. doi: 10.1080/14756366.2017.1368503.
α-Glucosidase inhibitors are described as the most effective in reducing post-prandial hyperglycaemia (PPHG) from all available anti-diabetic drugs used in the management of type 2 diabetes mellitus. As flavonoids are promising modulators of this enzyme's activity, a panel of 44 flavonoids, organised in five groups, was screened for their inhibitory activity of α-glucosidase, based on in vitro structure-activity relationship studies. Inhibitory kinetic analysis and molecular docking calculations were also applied for selected compounds. A flavonoid with two catechol groups in A- and B-rings, together with a 3-OH group at C-ring, was the most active, presenting an IC much lower than the one found for the most widely prescribed α-glucosidase inhibitor, acarbose. The present work suggests that several of the studied flavonoids have the potential to be used as alternatives for the regulation of PPHG.
α-葡萄糖苷酶抑制剂被认为是用于治疗2型糖尿病的所有现有抗糖尿病药物中，降低餐后高血糖（PPHG）最有效的药物。由于黄酮类化合物是这种酶活性的有前景的调节剂，基于体外构效关系研究，对一组44种黄酮类化合物（分为五组）进行了α-葡萄糖苷酶抑制活性筛选。还对选定的化合物进行了抑制动力学分析和分子对接计算。在A环和B环中有两个邻苯二酚基团以及在C环有一个3-OH基团的黄酮类化合物活性最高，其IC50远低于最广泛使用的α-葡萄糖苷酶抑制剂阿卡波糖。目前的研究表明，几种被研究的黄酮类化合物有潜力用作调节餐后高血糖的替代品。
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