文献类型：期刊文献

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

作者：Xu, Qi[1];Ji, Yunfan[1];Chen, Meijun[1];Shao, Xusheng[1,2]

机构：[1]East China Univ Sci & Technol, Shanghai Key Lab Chem Biol, Sch Pharm, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China

年份：2021

卷号：20

期号：4

起止页码：501

外文期刊名：PHOTOCHEMICAL & PHOTOBIOLOGICAL SCIENCES

收录：;EI(收录号：20211210122915);WOS:【SCI-EXPANDED(收录号:WOS:000630829400001)】；

基金：This work was financial supported by National Key Research and Development Program of China (2018YFD0200100), National Natural Science Foundation of China (No. 21877039), Science and Technology Commission of Shanghai Municipality (16391902300) and Innovation Program of Shanghai Municipal Education Commission (2017-01-07-00-02-E00037).

语种：英文

外文关键词：Oxoisoaporphine; Photosensitizer; Cell imaging; Singlet oxygen; Cytotoxicity

摘要：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 fluorescence (0.72) and improved water solubility. OHOA displays excellent fluorescence for cell imaging and exhibits light-induced cytotoxicity against cancer cell. In vitro model of human cervical carcinoma (HeLa) cell proved that singlet oxygen generated by OHOA triggered photosensitized oxidation reactions and exert toxic effect on tumor cells. The MTT assay using HeLa cells verified the low cytotoxicity of OHOA in the dark and high phototoxicity. Confocal experiment indicates that OHOA mainly distributes in mitochondria and western blotting demonstrated that OHOA induces cell apoptosis via the mitochondrial pathway in the presence of light. Our molecule provides an alternative choice as a theranostic agent against cancer cells which usually are in conflict with each other for most traditional theranostic agents.