Studies on Collagenase Inhibitors. II. Inhibitory Effects of Anthraquinones on Bacterial Collagenase

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Abstract
The inhibitory activities of 44 anthraquinones against bacterial collagenase were assayed in vitro. Emodin (1,6,8-trihydroxy-3-methylanthraquinone, 41) was the most potent active inhibitor amogn them (IC50; 4.0 7x 10-5 M). The type of inhibiton by 41 was found to be a mixture type by use of Lineweaver-Burk plots. Since the inhibitory activities of anthraquinones were not affected by the concentration of Ca2+ i the assay medium, it is considered that the inhibitor mechanism is not a chelate effect on Ca2+. In mono-substituted anthraquinones, the compounds which have a substituent (OH or SO3Na) at 2-position show more potent inhibitory activity than the corresponding 1-substituted compound.

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