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¡@¡@Progression of hepatic fibrosis is a common and potentially lethal problem in chronic liver disease in Taiwan, affecting more than 4% of the population. Incidence of cirrhosis is growing as a result of the widespread occurrence of chronic hepatitis, as well as the evident lack of an established therapy for hepatic fibrosis. The quest for the identification of an effective drug treatment to improve the outcome of patients with liver fibrosis and to develop molecular markers for liver fibrosis diagnosis is an important task. Herbal medicines have been used in Chinese population for thousands of years and there has been a growing trend in Western countries to use as alternative medicine to treat a wide range of diseases, such as inflammatory diseases and chronic liver diseases (including hepatitis and fibrosis).? In the course of search for key therapeutic agents for hepatoprotective effect, a traditional Chinese medicine, Graptopetalum paraguayense, begins to emerge as the most potent one. Oral administration of Graptopetalum paraguayense extract significantly alleviated toxin-induced liver damage, inflammation and fibrosis. High levels of alanine transaminase, aspartate transaminase, bilirubin, prothrombin activity, collagen, and mortality rates also decreased in therapeutic rats compared with those of the liver-damaged rats. In the in vitro study, Graptopetalum paraguayense was found to inhibit proliferation, collagen I and alpha smooth muscle actin expression in primary cultured rat hepatic stellate cells. Furthermore, Graptopetalum paraguayense induced apoptotic cell death in activated rat hepatic stellate cells. Graptopetalum paraguayense also suppressed lipopolysaccharide-stimulated rat Kupffer cell activation by decreasing nitric oxide, tumor necrosis factor-ƒÑ and interleukin-6 production, and increasing interleukin-10 expression. Our observations show that the administration of Graptopetalum paraguayense attenuated toxin-induced hepatic damage and fibrosis in vivo and inhibited hepatic stellate cell and Kupffer cell activation in vitro, suggesting that Graptopetalum paraguayense might be a promising complementary or alternative therapeutic agent for liver inflammation and fibrosis. Using microarray analysis, we identified 44 necroinflammation-related and 62 fibrosis-related genes which provides useful insight into the molecular mechanisms underlying liver damage and provides potential candidates for the rational development of diagnostic markers and therapeutic targets. The active compounds with anti-chronic liver diseases have been identified from Graptopetalum paraguayense which belong to the condensed tannin family molecules.