Department of Chemistry, University of Calicut, Calicut University P O, Kerala, India.
Department of Chemistry, University of Calicut, Calicut University P O, Kerala, India.
Int J Biol Macromol. 2019 Oct 15;139:712-718. doi: 10.1016/j.ijbiomac.2019.08.033. Epub 2019 Aug 5.
Diabetic control through the inhibition of carbohydrate hydrolysing enzymes is established as an effective strategy. Many of the inorganic materials have already been investigated as enzyme inhibitors. Present study investigates the in-vitro antidiabetic activity of ZnO nanoparticles assessing their inhibition efficiency on α-glucosidase and α-amylase. The nanoparticles obtained with average dimeson of 11, 32 and 49 nm via green strategy were subjected to in-vitro antidiabetic assays. The samples were particularly selective for α-glucosidase while very mild inhibitors for α-amylase. ZnO sample with particle dimension of 32 nm was found to be the most potent inhibitor capable of preventing 97.86% enzymatic action. The IC50, and CC50 values of the sample were determined as 1.24 μg/mL and 88.89 μg/mL respectively. The selectivity index (SI) value obtained is 71.68 which indicates good selectivity towards enzymes inhibition rather than the host body. Molecular docking models were generated for ZnO association with α-glucosidase and possible binding sites were recognized.
通过抑制碳水化合物水解酶来控制糖尿病已被确立为一种有效策略。许多无机材料已被用作酶抑制剂。本研究通过绿色策略，评估了氧化锌纳米粒子的体外抗糖尿病活性，以评估其对α-葡萄糖苷酶和α-淀粉酶的抑制效率。通过绿色策略获得的平均粒径为 11、32 和 49nm 的纳米粒子进行了体外抗糖尿病测定。这些样品对α-葡萄糖苷酶具有特别的选择性，而对α-淀粉酶的抑制作用则很轻微。发现粒径为 32nm 的 ZnO 样品是最有效的抑制剂，能够阻止 97.86%的酶活性。该样品的 IC50 和 CC50 值分别为 1.24μg/mL 和 88.89μg/mL。获得的选择性指数（SI）值为 71.68，表明其对酶抑制具有良好的选择性，而不是对宿主的选择性。生成了 ZnO 与α-葡萄糖苷酶结合的分子对接模型，并识别出可能的结合位点。
