4-Hydroxyl-oxoisoaporphine, one small molecule as theranostic agent for simultaneous fluorescence imaging and photodynamic therapy as type II photosensitizer

Oxoisoaporphine (OA) is a plant phototoxin isolated from Menispermaceae, however, its weak fluorescence and low water solubility impede it for theranostics. We developed here 4-hydroxyl-oxoisoaporphine (OHOA), which has good singlet oxygen-generating ability (0.06), strong (0.72) improved solubility. OHOA displays excellent cell imaging exhibits light-induced cytotoxicity against cancer cell. In vitro model of human cervical carcinoma (HeLa) proved that oxygen generated by triggered photosensitized oxidation reactions exert toxic effect on tumor cells. The MTT assay using HeLa cells verified the in dark high phototoxicity. Confocal experiment indicates mainly distributes mitochondria western blotting demonstrated induces apoptosis via mitochondrial pathway presence light. Our molecule provides an alternative choice as theranostic agent usually are conflict with each other most traditional agents.