An ROS-Responsive Antioxidative Macromolecular Prodrug of Caffeate for Uveitis Treatment  

作　　者：Yu-Tong Li Si-Ting Sheng Bo Yu Fan Jia Kai Wang Hai-Jie Han Qiao Jin You-Xiang Wang Jian Ji 

机构地区：[1]MOE Key Laboratory of Macromolecule Synthesis and Functionalization of Ministry of Education,Department of Polymer Science and Engineering,Zhejiang University,Hangzhou 310027,China [2]Eye Center,the Second Affiliated Hospital,School of Medicine,Zhejiang University,Hangzhou 310009,China

出　　处：《Chinese Journal of Polymer Science》2022年第9期1101-1109,共9页高分子科学（英文版）

基　　金：financially supported by National Key Research and Development Project (No. 2020YFE0204400)

摘　　要：Uveitis is a sophisticated syndrome showing a high relevance with reactive oxygen species(ROS).Herein,an ROS-responsive PEGylated polypeptide based macromolecular prodrug of herbaceous antioxidant ethyl caffeate(EC)is designed via phenylboronic esters with improved solubility for the alleviation of uveitis.The antioxidative 4-hydroxybenzyl alcohol(HBA)and EC can be released from the macromolecular EC prodrug under the stimulation of ROS,which can effectively protect cells against oxidative stress-induced injury in an ROS-depletion way.The antioxidative and protective effects of the macromolecular EC prodrug in vivo are further verified in a uveitis mouse model.Overall,this work not only provides a handy method to synthesize a phenylboronic ester-bearing EC prodrug which is highly sensitive to pathological ROS,but also depicts a promising future to apply macromolecular antioxidative prodrugs in the treatment of uveitis as well as other ROS-related diseases.

关 键 词：Antioxidative therapy Macromolecular prodrug UVEITIS Ethyl caffeate(EC) Phenylboronic acid esters 

分 类 号：TQ460.1[化学工程—制药化工]