Arginine-peptide complex-based assemblies to combat tumor hypoxia for enhanced photodynamic therapeutic effect  

作　　者：Yanxian Hou Yafei Kuang Qikun Jiang Shuang Zhou Jiang Yu Zhonggui He Jin Sun 

机构地区：[1]Shenyang Pharmaceutical University,No.103,Wenhua Road,Shenyang 110016,China

出　　处：《Nano Research》2022年第6期5183-5192,共10页纳米研究（英文版）

基　　金：supported by the National Natural Science Foundation of China(No.81773656);the Liaoning Revitalization Talents Program(No.XLYC1808017);the Shenyang Youth Science and Technology Innovation Talents Program(No.RC190454).

摘　　要：Tumor hypoxia is one of the major factors restricting the photodynamic therapy(PDT)efficacy.To address this problem,we designed an arginine-peptide complex,namely Fluorenylmethoxycarbonyl-Leucine-Leucine-Leucine-Arginine-OH(Fmoc-L_(3)-Arg),which is able to co-assemble with 5,10,15,20-Tetrakis(4-hydroxyphenyl)porphyrin(THPP)into stable nanoparticles(NPs)with uniform and spherical shapes.The THPP/Fomc-L_(3)-Arg NPs were ultra-sensitive to tumorous acidic and oxidative conditions,and could rapidly release photosensitizers in tumor cells.Meanwhile,the co-loaded Fmoc-L_(3)-Arg could efficiently generate nitric oxide(NO),inhibiting mitochondrial cellular respiration and increasing oxygen in tumor cells to support the profound improvement of reactive oxygen species(ROS)yield and PDT efficacy.After intravenous injection,the THPP/Fomc-L_(3)-Arg NPs greatly accumulated at tumor tissue and significantly inhibited tumor growth upon irradiation.In conclusion,such an arginine-peptide complex-based nanoassembly addresses the inevitable problem of hypoxia-induced tumor resistance to PDT.

关 键 词：ARGININE co-assembly nitric oxide tumor hypoxia photodynamic efficacy 

分 类 号：R73[医药卫生—肿瘤]