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叶提取物对基质金属蛋白酶-2、8和9的酶抑制活性。

Enzymatic inhibitory activity of leaf extract on matrix metalloproteinase-2, 8 and 9.

作者信息

Abu Bakar Amirul Ridzuan, Ripen Adiratna Mat, Merican Amir Feisal, Mohamad Saharuddin Bin

机构信息

a Faculty of Science , Institute of Biological Sciences, University of Malaya , Kuala Lumpur , Malaysia.

b Allergy and Immunology Research Centre, Institute for Medical Research , Kuala Lumpur , Malaysia.

出版信息

Nat Prod Res. 2019 Jun;33(12):1765-1768. doi: 10.1080/14786419.2018.1434631. Epub 2018 Feb 2.

Abstract

Dysregulation of matrix metalloproteinases (MMPs) activity is known in many pathological conditions with which most of the conditions are related to elevate MMPs activities. (FD) is a plant known for its therapeutic properties. In order to evaluate the therapeutic potential of FD leaf extract, we study the enzymatic inhibition properties of FD leaf extract and its major bioactive compounds (vitexin and isovitexin) on a panel of MMPs (MMP-2, MMP-8 and MMP-9) using experimental and computational approaches. FD leaf extract and its major bioactive compounds showed pronounced inhibition activity towards the MMPs tested. Computational docking analysis revealed that vitexin and isovitexin bind to the active site of the three tested MMPs. We also evaluated the cytotoxicity and cell migration inhibition activity of FD leaf extract in the endothelial EA.hy 926 cell line. Conclusively, this study provided additional information on the potential of FD leaf extract for therapeutical application.

摘要

基质金属蛋白酶(MMPs)活性失调在许多病理状况中都有体现,其中大多数状况都与MMPs活性升高有关。毛地黄(FD)是一种以其治疗特性而闻名的植物。为了评估FD叶提取物的治疗潜力,我们使用实验和计算方法研究了FD叶提取物及其主要生物活性化合物(牡荆素和异牡荆素)对一组MMPs(MMP - 2、MMP - 8和MMP - 9)的酶抑制特性。FD叶提取物及其主要生物活性化合物对所测试的MMPs表现出显著的抑制活性。计算对接分析表明,牡荆素和异牡荆素与三种测试的MMPs的活性位点结合。我们还评估了FD叶提取物在内皮EA.hy 926细胞系中的细胞毒性和细胞迁移抑制活性。总之,本研究为FD叶提取物的治疗应用潜力提供了更多信息。

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