Aim To prepare the
prodrugs of curcumin,which could be selectively activated in tumor cells,in order to establish a basis
for further development of targeted chemotherapy for cancer.Methods Based on the molecular structure of
curcumin,the N-maleoyl-L-valine-curcumin(NVC) and N-maleoyl-glycine-curcumin(NGC) were chemically synthesized and identified using IR spectroscopy.After treatment with these two
prodrugs for 6～24 h,the growth inhibition rates on human bladder cancer EJ cells and renal tubular epithelial(HKC) cells were detected using MTT colorimetry.Results After treatment with 20～40 μmol·L~(-1) NVC and NGC for 6～24 h,the growth inhibitory effects on EJ cells were 6.71%～65.13%%(P<0.05) and 10.96%～73.01%(P<0.05),respectively,in a dose-and time-dependent manner.When compared with the curcumin of same concentrations,the growth inhibitory effects of these two prodrugs on HKC cells were significantly decreased(P<0.01).Conclusion The two curcumin prodrugs,N-maleoyl-L-valine-curcumin and N-maleoyl-glycinecurcumin were chemically synthesized successfully and both could inhibit the growth of tumor cell in vitro.Furthermore,the two prodrugs of curcumin were less toxic in HKC cells than curcumin.