Objective Ovalitenin A （1-（4-methoxybenzofuran-5-yl）-3-phenyl-2-propen-l-one） is a chalcone isolated from Millettia pulchra. The aim of the study was to investigate the antitumor effect of ovalitenin A on apoptosi...Objective Ovalitenin A （1-（4-methoxybenzofuran-5-yl）-3-phenyl-2-propen-l-one） is a chalcone isolated from Millettia pulchra. The aim of the study was to investigate the antitumor effect of ovalitenin A on apoptosis in vitro and in vivo and to identify the mechanism involved. Methods The effect of ovalitenin A in human cervical cancer HeLa cells was detected by 3-（4,5-dimethylthiazol-2-yl）-2,5-diphenyltetrazolium bromide （M-I-r） assay, morphological observation, flow cytometric measurement, Western blotting, and xenograft model. Results Ovalitenin A inhibited the proliferation of HeLa cells in a dose-dependent manner in vitro and in vivo and induced the apoptosis evidenced by characteristic apoptotic morphological changes, phosphatidylserine externalization, and activation of caspase-3. In addition, ovalitenin A induced G2/M cell cycle arrest and up-regulation of the Bax/Bcl-2 ratio. Furthermore, ovalitenin A decreased protein level of COX-2 and induced the loss of mitochondrial membrane potential. Conclusion These data suggest that ovalitenin A has the potential of anticancer properties for the treatment of cervical cancer.展开更多
基金Comprehensive Technology Platform of New Drug Research of the Ministry of Science and Technology(2012ZX09301-002-001)
文摘Objective Ovalitenin A （1-（4-methoxybenzofuran-5-yl）-3-phenyl-2-propen-l-one） is a chalcone isolated from Millettia pulchra. The aim of the study was to investigate the antitumor effect of ovalitenin A on apoptosis in vitro and in vivo and to identify the mechanism involved. Methods The effect of ovalitenin A in human cervical cancer HeLa cells was detected by 3-（4,5-dimethylthiazol-2-yl）-2,5-diphenyltetrazolium bromide （M-I-r） assay, morphological observation, flow cytometric measurement, Western blotting, and xenograft model. Results Ovalitenin A inhibited the proliferation of HeLa cells in a dose-dependent manner in vitro and in vivo and induced the apoptosis evidenced by characteristic apoptotic morphological changes, phosphatidylserine externalization, and activation of caspase-3. In addition, ovalitenin A induced G2/M cell cycle arrest and up-regulation of the Bax/Bcl-2 ratio. Furthermore, ovalitenin A decreased protein level of COX-2 and induced the loss of mitochondrial membrane potential. Conclusion These data suggest that ovalitenin A has the potential of anticancer properties for the treatment of cervical cancer.
