Catechol-Based Polymers with High Efficacy in Cytosolic Protein Delivery  

作　　者：Zhe Zhang Xin Gao Yanwen Li Jia Lv Hui Wang Yiyun Cheng 

机构地区：[1]Shanghai Frontiers Science Center of Genome Editing and Cell Therapy,Shanghai Key Laboratory of Regulatory Biology,School of Life Sciences,East China Normal University,Shanghai 200241 [2]Department of Orthopedic Oncology,The Second Affiliated Hospital of Naval Medical University,Shanghai 200003 [3]South China Advanced Institute for Soft Matter Science and Technology,School of Emergent Soft Matter,South China University of Technology,Guangzhou 510640

出　　处：《CCS Chemistry》2023年第6期1411-1421,共11页中国化学会会刊（英文）

基　　金：We gratefully acknowledge financial support from the National Key R&D Program of China,Synthetic Biology Research(grant no.2019YFA0904500);the National Natural Science Foundation of China(grant nos.22135002 and 21725402);the Basic Research Program of Science and Technology Commission of Shanghai Municipality(grant no.21JC1401800),and the Shanghai Frontiers Science Center of Genome Editing and Cell Therapy.

摘　　要：Polymers have been widely proposed as carriers for cytosolic protein delivery despite multiple barriers such as protein binding,cell internalization,and endosome escape during cytosolic delivery.Inspired by the strong binding affinity of natural polyphenols with proteins and cell membranes,herein we propose polyphenol modification to improve the efficacy of the protein delivery of cationic polymers.Catecholmodified dendrimers with balanced hydrophobic and hydrogen-bonding interactions show the highest efficacy for various cargo proteins and peptides while the pyrogallol-grafted ones exhibit the lowest efficacy due to increased ligand hydrophilicity.The catechol-based polymers efficiently deliver various bioactive proteins into the cytosol of live cells,exerting biofunctions after intracellular release,and successfully transmittingα-chymotrypsin into tumor cells in vivo to inhibit tumor growth.This study proves that polycatechols can serve as a family of highly efficient carriers for delivery of macromolecular biopharmaceuticals.

关 键 词：DENDRIMER cytosolic protein delivery polymer POLYPHENOL polycatechols 

分 类 号：TQ317[化学工程—高聚物工业]