Cell-penetrating riboflavin conjugate for antitumor photodynamic therapy  

作　　者：Chunlei Wu Yanyan Li Zhehong Cheng Pengxin Wang Zhilong Ma Ke Liu Yulian Cheng Yimin Zhou Xian Lin Ximing Shao Yong Yang Hongchang Li Lijing Fang 

机构地区：[1]Guangdong Key Laboratory of Nanomedicine,Institute of Biomedicine and Biotechnology,Shenzhen Institute of Advanced Technology,Chinese Academy of Sciences,Shenzhen 518055,China [2]University of Chinese Academy of Sciences,Beijing 100049,China [3]Department of Biomedical Engineering,Southern University of Science and Technology(SUSTech),Shenzhen 518055,China

出　　处：《Chinese Chemical Letters》2022年第9期4339-4344,共6页中国化学快报（英文版）

基　　金：supported by the National Natural Science Foundation of China(Nos.21977111 and 22007096);the National Key Research and Development Program of China(No.2021YFA0910000);the Natural Science Foundation of Guangdong Province(Nos.2019A1515012073 and 2018B030308001);the Shenzhen Science and Technology Innovation Commission(No.JCYJ20210324120200001).

摘　　要：Riboflavin(RF,vitamin B2)is an essential vitamin and has been considered as a promising natural photosensitizer for photodynamic therapy(PDT).However,further exploration of RF in antitumor application was limited by its poor cellular uptake.In this study,using cell-penetrating peptides Arg8,(Cha-Arg)3 and small molecule triphenylphosphine(TPP)as delivery compounds,three RF conjugates were prepared to increase the accumulation of RF in cells,termed as Arg8-RF,(Cha-Arg)3-RF and TPP-RF,respectively.Compared with TPP-RF and Arg8-RF,(Cha-Arg)3-RF exhibited better cell internalization and stronger cytotoxicity against HeLa cells upon exposure to blue light.Further researches proved that(Cha-Arg)3-RF generated reactive oxygen species(ROS)under irradiation,which could indiscriminately destroy endogenous proteins and mitochondria,ultimately inducing cell death.This work provides a new approach to explore RF as a natural photosensitizer for antitumor photodynamic therapy.

关 键 词：RIBOFLAVIN ANTITUMOR Photodynamic therapy Cell-penetrating peptides 

分 类 号：R730.5[医药卫生—肿瘤]