Planta Med 2004; 70(10): 1006-1008
DOI: 10.1055/s-2004-832630
Letter
© Georg Thieme Verlag KG Stuttgart · New York

Inhibition of Matrix Metalloproteinase-2 and -9 Activities by Selected Flavonoids

Christina Ende1 , Rolf Gebhardt1
  • 1Institute of Biochemistry, Medical Faculty, University of Leipzig, Leipzig, Germany
This work was supported by a grant from the Deutsche Forschungsgemeinschaft (SFB 610/B3)
Further Information

Publication History

Received: May 4, 2004

Accepted: June 23, 2004

Publication Date:
18 October 2004 (online)

Abstract

Matrix metalloproteinases (MMPs) play an important role in physiological and pathological matrix degradation. Here, we report that flavonoids, at physiologically relevant concentrations, inhibit two members of this enzyme family, namely MMP-2 and -9. Eight flavonoids with increasing number of hydroxy groups and other modifications were compared for their capacity to inhibit recombinant catalytic domains of these proteases. EC50 values ranged from 59 and 70 μM (primuletin/5-hydroxyflavone) to 9 and 4 μM (luteolin 7-O-glucoside) for MMP-2 and -9, respectively. Interestingly, the latter glucoside was an equal (MMP-2) or even stronger (MMP-9) inhibitor than its aglycone, luteolin. For luteolin, one of the strongest flavonoids tested, kinetic analysis revealed a non-competitive type of inhibition. Our results add a novel function to the long list of biological effects of these ubiquitous plant constituents that may contribute to and enhance their modulating influence on extracellular matrix degradation and remodelling.

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Rolf Gebhardt

Institute of Biochemistry

Medical Faculty

University of Leipzig

Liebigstr. 16

04103 Leipzig

Germany

Fax: +49-341-972-2109

Email: rgebhardt@medizin.uni-leipzig.de