Study on Anticancer Activity of Palbocilib Derivative on Hepatocellular Carcinoma
Objective To investigate the anticancer activity of Palbocilib derivative(PB)on hepatocellular carcinoma.Methods MCF-7 cells and HepG2 cells were treated with PB or palbocilib for 72 h,and then the anti-proliferative activity was determined by SRB method.The human HCC xenografts in vivo were established with nude mice and HepG2 cells.PB was administered by gavage for 21 consecutive days.The body weight and tumor volume were measured each 3 days during administration.The weight growth rate,tumor inhibiting rate and organ coefficient were measured.Results The IC50 for HepG2 and MCF-7 cells of PB were 32.26 μmol/L and 139.50 μmol/L,while the IC50 of Palbocilib were 129.69 μmol/L and 17.69 μmol/L,which showed PB had a better inhibitory effect on HepG2 than Palbocilib.The relative tumor proliferation rate(T/C％)of PB on HepG2 nude mouse transplanted tumors was 58.06％.The tumor inhibition rate was 40.76％.There was no significant decrease in body weight.The organ weight and organ coefficient of the heart were significantly lower than the model control group(P＜0.05).The weight and organ coefficients of the liver,spleen,lungs,brain,ovaries and uterus were not statistically different from the model group.Conclusion PB is a potential targeted drug against liver cancer,which can significantly inhibit HepG2 cells proliferation and xenografts growth.Under continuous dosing conditions,there is no weight loss or significant organ toxicity.
万方数据
维普
