Inhibition of collagenase and metalloproteinases by aloins and aloe gel

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. (C) 2002 Elsevier Science Inc. All rights reserved.