| The matrix metalloproteinases (MMPs) are a family of zinc-dependent endopeptidase involved in the degradation and remodeling the extracellular matrix proteins. The activities of these enzymes are well regulated by endogenous tissue inhibitors of metalloproteinases (TIMPs). Chronic stimulation of MMPs activities due to an imbalance in the levels of MMPs and TIMPs has been implicated in the pathogenesis of a variety of diseases such as cancer, osteoarthritis, rheumatoid arthritis. The MMPs which have been proved top lay key roles in the processes of tumor growth, invasion, metastasis and angiogenesis,are frequently overexpressed in malignant tumors, and have been associated with an aggressive malignant phenotype and poor prognosis inpatients with cancer. Thus it is believed that the growth and metastasis can be controlled by MMP inhibitors (MMPIs) which are expected to be useful for the treatment of cancer. Nowadays, many of the inhibitors of matrix metalloproteinase have come into clinical trial, but to most of our disappointment, none was tested to be a candidate for further curing disease. The main problem of this is the weak selectivity of MMPIs, because a long time non-selectivity inhibition of MMPs may bring out some unexpected biological disorder. In conclusion, it is foremost meaningful to find a MMPI with a high selectivity, affinity and biological availability.Forsythiaside belonging to the derivatives of caffeinic acid is the effective ingredient of the Chinese herb Forsythia. In this thesis, Forsythiaside has been obtained by using Macro-reticular resin D101 and HPLC, which have some obvious advantages: saving solve, time and having high performance. The inhibition ability to MMPs of forsythiaside was tested by monitoring the strength of fluorescent emissioning from the cleaved substrate of MMPs. Then we docked the forsythiaside to different MMPs providing a detailed inhibition mechanism. At last, we observed the affect of forsythiaside to HT1080 cells on the aspect of cell proliferation, 3-D culture, migration and invasion. All the results showed that forsythiaside has higher inhibition ability to MMP-13 than others with a dose-dependent way which is consistent to data of docking. The docking as well suggested that forsythiaside located the S1 and S1'pocket of MMPs. Forsythiaside can inhibit the migration and invasion of HT1080 cells in vitro. The specific mechanism to be further verified. As a result, the specific MMP inhibition of forsythiaside will not only greatly help us to find a leading more potent compound but provide a new strategy for MMPIs development.We can continue studying in the future, it is investigated to pay attention to the inhibition of this new MMPI, at the same time, we should take attention to activities, toxicities, pharmacology, biological, pharmacokinetic and drug metabolism of forsythiaside further. On one hand facilitate our synthesizing and finding new MMP inhibitor, thus develop and regard MMP as the molecule target new medicine with independent intellectual property right; On the other hand explain the function mechanism of traditional Chinese medicine have benefits greatly from molecule level for us, and has offered basis for developing, synthesizing and transforming the medicine guide compound and guidance. Continue launching animal's model experiment and clinical experiment in a situation that a large number of external experiments are ripe, the mechanism of treating tumour for traditional Chinese medicine studies opens up the new broad space.
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