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KMID : 0352819930090010023
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Kosin Medical Journal
1993 Volume.9 No. 1 p.23 ~ p.30
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Inhibition f Human Neutrophil Elastase by Tetracyclines and Possible Mechanism of Action of These Drugs
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Abstract
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Human neutrophil elastase, which is known to be a possible mediator in the pathophysiology of connective tissue breakdown, was effectively inhibited by tetracycline, oxytetracycline and demeclocycline. Among them, oxytetracycline showed the most
potent
inhibitory effect on elastase activity. Tetracycline inhibited human neutrophil elastase non-competitively, however oxytetracycline inhibited human neutrophil elastase competitively,
however oxytetracycline inhibited human neutrophil elastase competitively. Ki values of tetracycline and oxytetracycline were 4.9mM and 0.39mM, respectively.
De-dimethylaminotetracycline, which showed no antibiotic activity since the active dimethylamino radical was removed from the position #4 of the tetracycline, inhibited the activity of human neutrophil elastase by tetracyclines not depend on the
dimethylamino radical which is a critical active site for antibiotic effect, rather it depend on the hydoxyl radical of tetracyclines. The property of inhibiting elastase may be an additional molecular biochemical mechanism of action of these
drugs
as
an inhibitor of tissue destruction at the inflammatory sites.
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KEYWORD
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