Inhibition of Ovalitenin A on Proliferation of HeLa Cells via Apoptosis, G2/M Cell Cycle Arrest, and Down-regulation of COX-2

ObjectiveOvalitenin A (1-(4-methoxybenzofuran-5-yl)-3-phenyl-2-propen-1-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.MethodsThe effect of ovalitenin A in human cervical cancer HeLa cells was detected by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, morphological observation, flow cytometric measurement, Western blotting, and xenograft model.ResultsOvalitenin 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.ConclusionThese data suggest that ovalitenin A has the potential of anticancer properties for the treatment of cervical cancer.