title: Enhanced Therapeutic siRNA to Tumor Cells by a pH-Sensitive Agmatine-Chitosan Bioconjugate.
abstract: Charge-conversional naturally occurring chitosan-agmatine bioconjugates are prepared by dimethylmaleic anhydride (DMA) modification and the nucleophilic reaction between tosyl of tosylated chitosan and primary amine of agmatine. These bioconjugates (CS-DM-Agm) are shown to condense siRNA into nanocomplexes, which are stable in the presence of serum at physical pH values. Furthermore, the surface charge of complexes can tune from negative to positive while pH is changed to weak acid tumor micromilieu, thus facilitating the target cancer cell internalization in resisting serum adsorption. More importantly, this smart biogenic system shows remarkable gene silencing efficiency and a high apoptotic rate of tumor cells both in vitro and in vivo, indicating its great potential for cancer therapy.
authors.affiliation: †School of Materials Science and Engineering, Tianjin Key Laboratory of Composite and Functional Materials, Tianjin University, Tianjin 300072, P. R. China.|‡Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Tianjin 300072, P. R. China.
authors.forename: Yongmao
authors.initials: Y
authors.lastname: Li
authors.affiliation: †School of Materials Science and Engineering, Tianjin Key Laboratory of Composite and Functional Materials, Tianjin University, Tianjin 300072, P. R. China.
authors.forename: Jianhai
authors.initials: J
authors.lastname: Yang
authors.affiliation: †School of Materials Science and Engineering, Tianjin Key Laboratory of Composite and Functional Materials, Tianjin University, Tianjin 300072, P. R. China.
authors.forename: Bing
authors.initials: B
authors.lastname: Xu
authors.affiliation: †School of Materials Science and Engineering, Tianjin Key Laboratory of Composite and Functional Materials, Tianjin University, Tianjin 300072, P. R. China.
authors.forename: Fei
authors.initials: F
authors.lastname: Gao
authors.affiliation: †School of Materials Science and Engineering, Tianjin Key Laboratory of Composite and Functional Materials, Tianjin University, Tianjin 300072, P. R. China.|§State Key Laboratory of Molecular Engineering of Polymers, Fudan University, Shanghai 200433, P. R. China.
authors.forename: Wei
authors.initials: W
authors.lastname: Wang
authors.affiliation: †School of Materials Science and Engineering, Tianjin Key Laboratory of Composite and Functional Materials, Tianjin University, Tianjin 300072, P. R. China.|‡Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Tianjin 300072, P. R. China.
authors.forename: Wenguang
authors.initials: W
authors.lastname: Liu
mesh_terms: D000818:Animals; D002470:Cell Survival / Q000187:drug effects / Q000235:genetics; D003692:Delayed-Action Preparations / Q000008:administration & dosage* / Q000737:chemistry; D004058:Diffusion; D015316:Genetic Therapy / Q000379:methods*; D006367:HeLa Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008422:Materials Testing; D051379:Mice; D008807:Mice, Inbred BALB C; D053769:Nanocapsules / Q000008:administration & dosage / Q000737:chemistry* / Q000648:ultrastructure; D058726:Nanoconjugates / Q000008:administration & dosage / Q000737:chemistry* / Q000648:ultrastructure; D034741:RNA, Small Interfering / Q000008:administration & dosage* / Q000235:genetics*; D042461:Vascular Endothelial Growth Factor A / Q000235:genetics
chemical_list: D003692:Delayed-Action Preparations; D053769:Nanocapsules; D058726:Nanoconjugates; D034741:RNA, Small Interfering; D042461:Vascular Endothelial Growth Factor A
keywords: agmatine; cancer therapy; charge conversion; chitosan; gene silencing