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(MMPIs) 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.
JI Hai-taoSHI Xiu-juanHONG YuanWANG YeWANG Hui-lingWANG Zhi-yongFANG Xue-xun
Matrix metalloproteinases(MMPs) are known to be involved in a number of pathological processes including cancer, atherosclerosis, arthritis and neurodegenerative disease among others. The drive to develop MMP inhibitors as therapeutics has been put forward for years by pharmaceutical companies as well as academicians. In an attempt to screen for MMP inhibitors from Traditional Chinese Medicines(TCMs), a number of Chinese formulations used to treat inflammatory diseases such as nephritis and hepatitis have been studied. Strong inhibitory effects of three Chinese formulations toward the activity of MMP-16 have been discovered. These results suggest that these anti-inflammatory medicines contain some unknown MMP inhibitory compound(s) and provide reasonable molecular mechanisms for their therapeutic effects.
JIN Feng-haiWANG Hui-lingZHAO Shu-huaYANG Jin-gangFANG Xue-xun
Matrix metalloproteinases(MMPs) are a family of proteases that are required for many biological processes and are also elevated in many pathological conditions. MMP inhibitors(MMPIs) may therefore be useful as therapeutic {agents} in treating a number of diseases including cancer, cardiovascular diseases and arthritis. Attempts have been made to develop MMPIs. Recombinant MMPs have been used to screening MMPs in vitro assays. In this work, we report the expression of MMP-16 in E. coli and the characterization of the recombinant MMP-16 with a commonly used MMP substrate DQ-gelatin.
SHI Xiu-juanJIN Feng-haiWANG Hui-lingYANG Jin-gangWANG Zhi-yongFANG Xue-xun
