State Key Laboratory of Food Nutrition and Safety, Tianjin University of Science & Technology, Tianjin, P.R. China.
Key Laboratory of Food Nutrition and Safety, Ministry of Education, Tianjin University of Science and Technology, Tianjin, P.R. China.
Nat Prod Res. 2021 Jun;35(11):1874-1880. doi: 10.1080/14786419.2019.1639181. Epub 2019 Jul 15.
The synthesis of the methyl glycyrrhetinate glycosides and inhibition of α-glucosidase were studied. The carboxyl group of glycyrrhetinic acid was methylated, and glucose and galactose were introduced into the hydroxyl group to obtain compounds and . Compound , , , and glycyrrhizic acid (GL) were evaluated for their inhibitory activities against α-glucosidase. As a result, Compound , , , and GL all showed significant α-glucosidase inhibitory activity and IC values were 0.465, 1.352, 0.759, 0.687 and 2.085 mM, respectively, and acted as non-competitive inhibitors. The activity of the compound , , was lower than compound , but significantly higher than GL. Therefore, it was concluded that the change of structure in glycyrrhetinic acid by chemical modification had certain effect on bioactivity, and the change of carboxyl group, hydroxyl group and the type of monosaccharide introduced were the influencing factors.
研究了甘草次酸糖苷的合成及其对α-葡萄糖苷酶的抑制作用。对甘草次酸的羧基进行甲基化，在羟基上引入葡萄糖和半乳糖，得到化合物和。对化合物、、、和甘草酸（GL）进行了α-葡萄糖苷酶抑制活性评价。结果表明，化合物、、、和 GL 均表现出显著的α-葡萄糖苷酶抑制活性，IC 值分别为 0.465、1.352、0.759、0.687 和 2.085mM，均为非竞争性抑制剂。化合物、、的活性低于化合物，但明显高于 GL。因此，结论是化学修饰甘草次酸的结构变化对生物活性有一定影响，而羧基、羟基和引入的单糖类型的变化是影响因素。
