Photodynamic therapy of phthalocyanines has been shown to have antitumor activity in some tumor cells. However, the photodynamic therapy mechanism of amphiphilic phthalocyanine zinc in Human Hepatoma Bel-7402 cells has not been clarified. In the present study, therefore, the photodynamic therapy effect of amphiphilic phthalocyanine zinc on the proliferation and apoptosis in Bel-7402 cells was investigated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide, AnnexinV-FITC/ Propidium Iodide double staining, electron microscopy and inverted microscope assay, respectively. We found that photodynamic therapy of amphiphilic phthalocyanine zinc significantly led to inhibition of proliferation and induction of apoptosis in Bel-7402 cells. Therefore, we conclude that photodynamic therapy of amphiphilic phthalocyanine zinc inhibits the proliferation of Bel-7402 cells through the induction of apoptosis.