Synthesis and Evaluation of Gallotannin Derivatives as Antioxidants and α-Glucosidase Inhibitors
作者:Shota Machida、Maho Sugaya、Hiroaki Saito、Taketo Uchiyama
DOI:10.1248/cpb.c21-00566
日期:2021.12.1
D-glucose. Some gallotannins are reported to have antidiabetic properties, such as α-glucosidase inhibitory activity. In this study, fourteen unnatural gallotannin derivatives with 1,5-anhydroalditol and inositol as the cyclic polyol cores were synthesized to investigate how their structures affected antioxidative and α-glucosidase inhibitory activities. Tannic acid demonstrated the most potent antioxidative
没食子单宁是酚类天然产物,含有与多元醇核心连接的没食子酰基部分,例如D-葡萄糖。据报道,一些没食子单宁具有抗糖尿病特性,例如 α-葡萄糖苷酶抑制活性。在这项研究中,合成了 14 种以 1,5-脱水糖醇和肌醇作为环状多元醇核心的非天然没食子单宁衍生物,以研究它们的结构如何影响抗氧化和 α-葡萄糖苷酶抑制活性。单宁酸表现出最有效的抗氧化活性(EC 50 = 2.84 μM),效力与没食子酰基部分的数量成比例增加。合成肌醇衍生物在大鼠 α-葡萄糖苷酶抑制活性方面优于 1,5-脱水糖醇衍生物。五没食子酰葡萄糖是一种天然化合物,具有最高的活性 (IC 50 = 0.336 μM)。 全尺寸图像