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Inhibition of collagenase and metalloproteinases by aloins and aloe gel.

机译:芦荟蛋白和芦荟凝胶对胶原酶和金属蛋白酶的抑制作用。

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摘要

The effects of Aloe barbadensis gel and aloe gel constituents on the activity of microbial and human metalloproteinases have been investigated. Clostridium histolyticum collagenase (ChC) results dose-dependently inhibited by aloe gel and the activity-guided fractionation led to an active fraction enriched in phenolics and aloins. Aloins have been shown to be able to bind and to inhibit ChC reversibly and non-competitively. Aloe gel and aloins are also effective inhibitors of stimulated granulocyte matrix metalloproteinases (MMPs). The remarkable structural resemblances between aloins and the pharmacophore structure of inhibitory tetracyclines, suggest that the inhibitory effects of aloins are via an interaction between the carbonyl group at C(9) and an adjacent hydroxyl group of anthrone (C(1) or C(8)) at the secondary binding site of enzyme, destabilizing the structure of granulocyte MMPs.
机译:研究了芦荟凝胶和芦荟凝胶成分对微生物和人类金属蛋白酶活性的影响。溶组织梭状芽孢杆菌胶原酶(ChC)的结果受芦荟凝胶剂量依赖性抑制,而活性指导的分级分离导致富含酚类和芦荟素的活性级分。芦荟素已显示出能够可逆和非竞争性结合并抑制ChC的作用。芦荟凝胶和芦荟蛋白也是刺激的粒细胞基质金属蛋白酶(MMPs)的有效抑制剂。芦荟蛋白与抑制四环素的药效团结构之间的显着结构相似性表明,芦荟蛋白的抑制作用是通过C(9)上的羰基与蒽酮的相邻羟基(C(1)或C(8)之间的相互作用))在酶的二级结合位点上,会使粒细胞MMP的结构不稳定。

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