Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China ; Anhui University of Traditional Chinese Medicine, Anhui Key Laboratory of Modernized Chinese Material Medical,Hefei 230031, China
Abstract:
A series of novel glyco-gambogic acid(GA) compounds were synthesized and evaluated for their in vitro anti-proliferative activity against human hepatocellular carcinoma(HCC) cells.All compounds showed much better aqueous solubility(0.92- 1.89 mg/mL) than GA(0.013 mg/mL),and displayed potent inhibition on HCC cells(IC50:0.21-12.23μmol/L) and little affects on non-tumor liver cells(IC50:42.56-86.43μmol/L),suggesting that glyco-GA compounds selectively inhibit HCC proliferation,and may be promising candidates for further intensive study.