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Photodynamic therapy (PDT) is a typical noninvasive method to treat various diseases based on the reactive oxygen species upon irradiation of photosensitizers (PSs).However,many of PSs are hydrophobic,hardly to dissolve and easily to aggregate in water,thus seriously limit the PDT efficiency.Herein,we fabricated a novel chem-and photo-active nanocomposite which combines the poly-L-lysine (PLL) functionalized grapheme (G-PLL),Zinc(II) phthalocyanine (ZnPc) and anticancer drug doxorubicin (DOX) with aim to improve the PDT effect.The nanocomposite G-PLL/DOX/ZnPc can generate high level of 1O2,i.e.80% of that of free ZnPc under the same conditions.And the in vitro biological results demonstrated that G-PLL/DOX/ZnPc exerts obvious anticancer effect and photo-cytotoxicity toward cancer cells.In summary,this study shows great promise of the chemo-and photo-active nanocomposite G-PLL/DOX/ZnPc for cancer PDT and chemotherapy