Abstract
PURPOSE: In this study, we examined the effects of LY52, a caffeoyl pyrrolidine derivative designed to fit the S'1 active pocket of gelatinases, on the expressions of matrix metalloproteinases and invasion abilities of hepatocellular carcinoma cells. METHODS: The effects of LY52 on the proliferations of HepG2 (hepatitis B virus (HBV) negative) and HepG2.2.15 (HBV-producing) cells were detected by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Gelatin zymography was used to detect the effects of LY52 on matrix metalloproteinases expressions and Western blot was used to detect matrix metalloproteinase-2 expressions. Transwell chamber assay was used to detect the effects of LY52 on invasion of the cells. RESULTS: Gelatin zymography and Western blot showed that matrix metalloproteinase-2 expressions were inhibited by LY52 in a dose-dependent manner, and inhibitory rates of LY52 on HepG2 cells were higher than on HepG2.2.15 cells. Transwell chamber showed that LY52 could significantly inhibit the invasion of both cells, although the inhibitory effects of LY52 on HepG2.2.15 cells were was not as obvious as on HepG2 cells. CONCLUSIONS: These results suggested that LY52 might inhibit the invasion of hepatocellular carcinoma cells by suppressing matrix metalloproteinase-2, although the inhibitory effects of LY52 on HBV-negative cells were more obvious than that of HBV-infected cells.