[Studies on collagenase inhibitors. II. Inhibitory effects of anthraquinones on bacterial collagenase].
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 among them (IC50; 4.0 X 10(-5) M). The type of inhibition 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+ in the assay medium, it is considered that the inhibitory 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.
Tanaka
T
T
Department of Pharmacology, Kohno Clinical Medicine, Research Institute, Tokyo, Japan.
Metori
K
K
Mineo
S
S
Matsumoto
H
H
Satoh
T
T
D000880:Anthraquinones / Q000494:pharmacology*; D001419:Bacteria / Q000201:enzymology*; D003012:Microbial Collagenase / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D000880:Anthraquinones; D003012:Microbial Collagenase