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Off White High School matrix metalloproteinase inhibitors and metal ions on the study of matrix metalloproteinase inhibition

Author: TianWeiHua
Tutor: ShenZuoHua
School: Northwestern University
Course: Analytical Chemistry
Keywords: Matrix metalloproteinase inhibitors Off white with Metal ion Antibacterial activity
CLC: R285
Type: Master's thesis
Year: 2009
Downloads: 113
Quote: 1
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Abstract


Matrix metalloproteinases (MMPs) are a class depends on the Zn 2 , degradation of the extracellular matrix (ECM) capabilities endopeptidase family. MMPs involved in apoptosis, morphogenesis, such as proliferation and development of a series of pathological and physiological processes, the inhibitor of many important diseases including cancer, cardiovascular disease, arthritis, eye diseases, immune system diseases, gynecological diseases, skin diseases, etc. drug treatment and has broad prospects. The MMPs inhibitor screening from natural plant extracts, and the development of new drugs has become a hot research field. This study molecular target MMPs, water extraction and alcohol precipitation, macroporous resin separation means, Methods in Enzymology, to track separation Off White High School inhibition of MMP-16 activity active ingredient, structural characterization of the separation of the monomer cell experiments, antibacterial activity on the part of the monovalent, divalent, trivalent rare earth metal ions inhibition of MMPs, antibacterial activity were studied. The thesis includes the following sections: an overview of the off white with matrix metalloproteinase, matrix metalloproteinase inhibitors and metal ions in the biological activity of the four aspects of the research status. Off-White High School MMP-16 inhibition monomer was isolated for the first time IC 50 for 3.4μmol / L, experiments show that the monomer is Off White High School MMP-16 main inhibitor. Infrared Spectroscopy, elemental analysis, atomic emission, the nature of experimental diffraction identification results showed that the monomer of ammonium aluminum sulfate dodecahydrate the (NH 4 Al (SO 4 ) 2 · 12H 2 O). Select containing NH 4 , the Al 3 , the SO 4 2 - compounds ( or complex salts), examining their inhibitory activity against MMP-16 of the results showed that the NH 4 Al (SO 4 ) 2 · 12H 2 O inhibit the activity of MMPs ion Al 3 . Further studies showed that the monomer of a variety of types of MMPs (such as MMP-2, MMP-9, MMP-13, MMP-3) have good inhibition (IC 50 <10 micromol / L), and cell experiment results showed that the monomer having cancer invasion inhibition, indicating that the monomer has a possibility of the development of anticancer drugs. The experiment also looked at off-white with extracts and active monomer inhibition of several bacteria and found off white High School antibacterial activity monomer NH 4 Al (SO 4 ) 2 · 12H 2 O, and speculated that the active groups as the Al 3 . The ScS part of the metal ions on the inhibitory activity of MMP-16 of the ScS monovalent, divalent metal ion for MMP-16 substantially free of active trivalent metal ions and rare earth metal ions on the inhibitory activity of MMP-16 were good , and the rare earth metal ions on the inhibition of MMP-16's showing a certain regularity in light, medium and heavy rare earth metal group, the inhibitory activity of the MMP-16's with increasing atomic number decreases. Investigated metal ions on the inhibition of bacteria and found that in addition to the salt of trivalent metal ions (including the study of the rare earth metal ions) have good inhibitory activity of a variety of bacteria, some monovalent, divalent metal salts The bacteria also to some extent.

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