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水飞蓟宾衍生物与水飞蓟宾中的松柏醇轭合及其对胰腺 α-淀粉酶的抑制活性。

Silychristin derivatives conjugated with coniferylalcohols from silymarin and their pancreatic α-amylase inhibitory activity.

机构信息

Division of Fundamental AgriScience and Research, Research Faculty of Agriculture, Hokkaido University, Sapporo, Japan.

Division of Applied Bioscience, Graduate School of Agriculture, Hokkaido University, Sapporo, Japan.

出版信息

Nat Prod Res. 2020 Mar;34(6):759-765. doi: 10.1080/14786419.2018.1499639. Epub 2018 Nov 16.

DOI:10.1080/14786419.2018.1499639
PMID:30445852
Abstract

Silymarin is a mixture of flavonolignans extracted from the fruit of (milk thistle). The latter is used as a medicinal plant to treat liver and gallbladder disorders. Recently, silymarin has been investigated for its effects against diabetes mellitus, and shown to reduce serum levels of glucose in model animals and in clinical trials. This effect can be explained mainly by the protective effect of silymarin against pancreatic beta-cells, but the involvement of other mechanisms is possible. We demonstrated the α-amylase inhibitory activity of silymarin and investigated the components responsible for this effect. Two major flavonolignans, silibinin and silychristin, did not show inhibition against α-amylase, but two novel silychristin derivatives conjugated with dehydrodiconiferyl alcohol were isolated as the mildly inhibiting components of silymarin. Further analyses indicated the presence of various silychristin derivatives in silymarin that may act synergistically to show α-amylase inhibitory activity.[Formula: see text].

摘要

水飞蓟素是从(奶蓟草)的果实中提取的黄酮木脂素混合物。后者被用作治疗肝胆疾病的药用植物。最近,水飞蓟素因其对糖尿病的作用而受到研究,并在动物模型和临床试验中显示出降低血糖水平的作用。这种作用主要可以解释为水飞蓟素对胰腺β细胞的保护作用,但也可能涉及其他机制。我们证明了水飞蓟素的α-淀粉酶抑制活性,并研究了负责这种作用的成分。两种主要的黄酮木脂素,水飞蓟宾和水飞蓟素,对α-淀粉酶没有抑制作用,但分离出两种新型的与脱氢二松柏醇共轭的水飞蓟素衍生物作为水飞蓟素的轻度抑制成分。进一步的分析表明,水飞蓟素中存在各种水飞蓟素衍生物,它们可能协同作用表现出α-淀粉酶抑制活性。[公式:见文本]。

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