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Department of Experimental Biomedical Sciences, Medical School of Padova, Italy
Correspondence: Prof. Spiridione Garbisa, Dept. Experimental Biomedical Sciences, Medical School of Padova, viale G.Colombo 3, 35121 Padova, Italy. E-mail: garbisa{at}unipd.it
Flavanol (-)epigallocatechin-3-gallate is shown to be a potent natural
inhibitor of leukocyte elastase that may be used to reduce
elastase-mediated progression to emphysema and tumor invasion. This
phyto-factor, abundant in green tea, exerts a dose-dependent,
noncompetitive inhibition of leukocyte elastase at a noncytotoxic
concentration and is effective in neutrophil culture. This inhibition
shows an IC50 of 0.4 µM, 30 times higher than the
1-protease inhibitor but lower than other known natural and
synthetic elastase inhibitors. The flavanol inhibits leukocyte elastase
at concentrations of 50, 150, and 2500 times lower than that effective
on gelatinases (MMP-2 and MMP-9), thrombin, and cathepsin G,
respectively, and also blocks elastase-mediated activation of
MMP-9.
Key Words: proteinases • neutrophils • connective tissue • inhibition
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