摘要
Matrix metalloproteinases（MMPs） are a family of zinc dependent enzymes that can degrade the components of the extracellular matrix（ECM） and basement membranes. Because MMPs play roles in many important physiological and pathological processes, many MMP inhibitors（MMPls） have been developed with the aim of interfering in and treating diseases. The authors conclude via a fluorescence based assay in vitro that luteolin inhibits the enzymatic activities of MMP-2, MMP-7, MMP-9, MMP-14, and MMP-16. This compound most specifically inhibits MMP-7 of all the MMPs tested. Finally, we used molecular modeling to dock luteolin with MMPs and revealed the binding mode of the luteolin-MMP interaction. Our results suggest that luteolin may exert its therapeutic effects via MMP inhibition.
Matrix metalloproteinases（MMPs） are a family of zinc dependent enzymes that can degrade the components of the extracellular matrix（ECM） and basement membranes. Because MMPs play roles in many important physiological and pathological processes, many MMP inhibitors（MMPls） have been developed with the aim of interfering in and treating diseases. The authors conclude via a fluorescence based assay in vitro that luteolin inhibits the enzymatic activities of MMP-2, MMP-7, MMP-9, MMP-14, and MMP-16. This compound most specifically inhibits MMP-7 of all the MMPs tested. Finally, we used molecular modeling to dock luteolin with MMPs and revealed the binding mode of the luteolin-MMP interaction. Our results suggest that luteolin may exert its therapeutic effects via MMP inhibition.
基金
Supported by the National Natural Science Foundation of China(No.30371656)
New Century Excellent Talent of Ministry of Education,China(No.NCET-08-0244)
