Experimental Study On The Inhibitory Activity Of Pinelliae Tuber Caulis To Matrix Metalloproteinase And Its Antitumor Mechanism

Pinelliae is the dried stem tuber of Pinelliae ,which is a plant of Araceae .It is pungent in taste and warm in nature and toxic,acts on the Spleen,Stomach and Lung Meri-dians and has the effects of eliminating dampness.Elimi- nating phlegm,lowering the adverse flow qi to stop vomit ing,and disintegrating and dispersing masses. Indications: cough and asthma with profuse sputum,dizziness and pal- pitation due to retention of phlegm,dizziness due to wind phlegm,headache due to phlegm syncope,vomiting and regur -gitation, stuffiness and distension in the chest and upper abdomen and globus hystericus;the unprepared drug is usually used for the external treatment of carbuncles and other pyogenic skin infections,and subeutaneous nodules; the drug with ginger usually used for lowering the adverse flow of qi to stop vomiting.Rhizoma Pinellinae praeparata usually used for eliminating dampness and removing phlegm. Its clinical application is so wide that it has much valuable medical use .Recently ,a lot of research in domestic and overseas has manifested that pinellinae can reject oncosis . Pinellin,polyose,organic acid,Alkaloids and chemical compoundâ…¢contained in the drug has antineoplastic power.And these ingredients may beactive substance used to reject oncosis. While the research on its molecular level is scarce ,and it is not clear why the drug can reject oncosis;Furthermore,tumour,especially the malignant tumor is the main cause of people's death all over the world.The significant characteristic of malignant tumor is that it can form metastasis away from its former place.The death caused by tumor is mainly because the tumour invasion and metastasis.In order to control tumour metastasis more effectively ,we have to learn more about the reason of tumour metastasis .Nowadays , metalloproteinases (MMPs) seem to play an important role in the tumour progress.Tumour invasion and metastasis are the result of a multistep process that includes basement membrane disruption,stromal,infiltration,intravasation, extravasation and invasion of a target organ by tumour cells. All these processes require the degradation of basement membrane components and of extracellular matrix macromolecule by proteolytic enzymes. Among these prote -inases, matrix metalloproteinases (MMPs) seem to play an important role in the tumour progress. MMPs is a member of zinc peptidase ,and it is dispensable for the degradation process of connective extracellular matrix (ECM).It can degradate almost all ingredient in the ECM ,so it plays animportant role in the physioprocess and pathoprocess .The expression and activation of MMPs is correlated with the growth,invasion and diversion of tumor directly. MMPs is often expressed excessively in the malignant tumor . The degradation of matrix outside tumor is a committed step in the invasion and diversion of tumor ,MMPs can destroy the degradation balance of matrix ,it can promote cancer cell to break though the histology barricade made up of basal lamina and ECM ,so it invade can surrounding tissues and transfer to distant place.Furthermore , MMPs can also promote the formation of neogenesis blood vessel, control growth and apoptosis.Considering all these reasons,MMPs has become a new target of malignant tumor therapy .So,it is essential to explore high-performance and specific MMP inhibitor which is also a hot spot in the domain. The object of this experiment is practiced in order to study whether pinelliae tuber has the ability of res- training MMPs. Then compared with the blank unit and positive control ,the inhibition strength can be obtained.Methods:the decrea -sing of the degrade rate of substrate is associated with the inhibition of matrix metalloproteinase .We study the inhibitory activity of pinelliae tuber to MMP by observing the degrade rate of substrate. Results: pinelliae tuberstrongly inhibits the MMP-16 activity, and the IC50 is 23ug/ml.Conclusion:the pinelliae tuber has the inhibitory activity to MMP-16. The clinical application of pinelliae tuber in our country has been longstanding.And the experiment indicates that pinelliae tuber strongly inhibits the MMP-16 activity .So we may presume that its ability of anti-tumor is correlated with its ability of inhibiting the overexpression of MMPs in body. It estab -lishes foundation that why pinelliae tuber has the ability of anti-tumor in molecular level .We may abstract MMP inhibitor from pinelliae tuber ,then it will be true that we can explore new traditional Chinese drugs aiming to MMPs .