PROPHYLACTIC AND THERAPEUTIC USE OF OLTIPRAZ AS AN ANTIFIBROTIC AND ANTICIRRHOTIC AGENT IN THE LIVER AND PHARMACEUTICAL COMPOSITION CONTAINING OLTIPRAZ

摘要

A pharmaceutical composition for prevention or treatment of progression of hepatic fibrosis and cirrhosis comprises 5-(2-Pyrazinyl)-4-methyl-1,2-dithiol-3-thione (oltipraz). ACTIVITY : Hepatotropic; Cytostatic. MECHANISM OF ACTION : TGF-beta production inhibitor. A test was conducted on macrophage cells by adding oltipraz in a dose dependent manner. The results showed that oltipraz may function as an anti-fibrotic agent in hepatic kupffer cells by inhibiting TGF-beta production. The increase in TGF-beta expression was inhibited by EGTA or genistein which was an inhibitor of tyrosine kinase. The TGF-beta inhibition was 30%. This result shows that the inhibition of TGF-beta production by oltipraz may be the result of intracellular calcium regulation and changes in protein kinase activity.