Characterization of Active molecules extracted from Graptopetalum paraguayense with Anti-Cancer Activity in Hepatocellular Carcinoma

• Main Authors: Yi-Chen Chen, 陳怡甄
• Other Authors: Chi-Ying F. Huang
• Format: Others
• Language: en_US
• Published: 2010
• Online Access: http://ndltd.ncl.edu.tw/handle/50912906924884682144

碩士 === 國立陽明大學 === 生物藥學研究所 === 98 === Hepatocellular carcinoma (HCC) is the sixth most common malignancy and the third most common cause of cancer deaths globally. Both hepatic fibrosis and cirrhosis are the risk factors for hepatocellular carcinoma. To identify the key therapeutic agents, we previously found that one of the Chinese herbal medicines, Graptopetalum paraguayense, can prevent DMN-induced hepatic inflammation and fibrosis in animal model and down-regulate the protein expression of several oncogenes in HSC-T6 cells. This observation raises the possibility that Graptopetalum paraguayense might have anti-cancer activity and we might use this down-regulation as a criterion for the purification of active components from Graptopetalum paraguayense. Graptopetalum paraguayense results in cytotoxicity effects and down-regulates AURKA, AURKB, and FLJ10540 expression in Huh7 and HepG2 cells. HH-F3, the fraction with active components, suppressed the protein expression of those above mentioned proteins. Unlike VE-465 (Aurora kinase inhibitor), Graptopetalum paraguayense and HH-F3 could not inhibit histone H3 phosphorylation on Ser10. The IC50 for HH-F3 at 48 hours on Huh7, PLC5, and Mahlavu cells was 50, 100, and 20 μg/ml, respectively. In addition, HH-F3 induced HCC to undergo apoptosis through down-regulation of JNK, ERK, and Akt pathway. In conclusion, HH-F3 was demonstrated the potential therapeutic effects on the treatment of HCC and liver fibrosis.