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褐藻糖胶对α-淀粉酶和α-D-葡萄糖苷酶的体外和计算机抑制特性及其与 2 型糖尿病的关系。

In vitro and in silico inhibition properties of fucoidan against α-amylase and α-D-glucosidase with relevance to type 2 diabetes mellitus.

机构信息

CAS in Marine Biology, Annamalai University, Parangipettai, 608502, Tamil Nadu, India.

CAS in Marine Biology, Annamalai University, Parangipettai, 608502, Tamil Nadu, India.

出版信息

Carbohydr Polym. 2019 Apr 1;209:350-355. doi: 10.1016/j.carbpol.2019.01.039. Epub 2019 Jan 14.

Abstract

This study investigated the in vitro and in silico inhibitory properties of fucoidan extracted from Turbinaria conoides against α-amylase and α-D-glucosidase. Extracted fucoidan contained 59 and 35% of fucose and sulphate and was characterized using H NMR. Dose dependent inhibition assays showed maximum of 85 and 72% of inhibition for α-amylase and α-D-glucosidase at 2.07 and 1.03 μM concentration of fucoidan. The IC value of fucoidan was found to be 1.07 and 0.68 μM against α-amylase and α-D-glucosidase. In silico studies (grid based docking) by Schrödinger software revealed that fucoidan as a potent inhibitor for both α-amylase and α-D-glucosidase based on number of interactions, hydrogen bond length and binding energy. Furthermore, fucoidan fulfilled the pharmacokinetic properties thus promising to develop fucoidan as drug for type 2 DM.

摘要

本研究调查了从 Turbinaria conoides 中提取的褐藻糖胶对α-淀粉酶和α-D-葡萄糖苷酶的体外和计算抑制特性。提取的褐藻糖胶含有 59%和 35%的岩藻糖和硫酸盐,并通过 H NMR 进行了表征。剂量依赖性抑制试验表明,褐藻糖胶在 2.07 和 1.03 μM 浓度下对α-淀粉酶和α-D-葡萄糖苷酶的抑制率最高分别为 85%和 72%。褐藻糖胶对α-淀粉酶和α-D-葡萄糖苷酶的 IC 值分别为 1.07 和 0.68 μM。Schrödinger 软件的基于网格的对接计算研究表明,褐藻糖胶是一种有效的α-淀粉酶和α-D-葡萄糖苷酶抑制剂,基于相互作用的数量、氢键长度和结合能。此外,褐藻糖胶符合药代动力学特性,因此有望将褐藻糖胶开发为 2 型糖尿病的药物。

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