title: Aggregation Induced Emission Mediated Controlled Release by Using a Built-In Functionalized Nanocluster with Theranostic Features.
abstract: We report biological evaluation of a novel nanoparticle delivery system based on 1,1,2-triphenyl-2-(p-hydroxyphenyl)-ethene (TPE-OH, compound 1), which has tunable aggregation-induced emission (AIE) characteristics. Compound 1 exhibited no emission in DMSO. In aqueous media, compound 1 aggregated, and luminescence was observed. The novel membrane-cytoplasm-nucleus sequential delivery strategy could induce apoptosis in four different kinds of cancer cells (including three adherent cell lines and one suspension cell line). The nanoparticles remained in the cytoplasm with intense blue emissions, whereas doxorubicin was observed in the nucleus with striking red luminescence. The nanoassembly was internalized in cells through an energy-dependent process. Three sorts of chemical inhibitors were used to clarify the endocytosis mechanism based on the AIE type prodrug. Furthermore, we have developed the first AIE theranostic system where drug targeting and release have been applied in an animal model.
authors.affiliation: School of Chemistry & Environment, South China Normal University , Guangzhou 510006, China.
authors.forename: Zhan
authors.initials: Z
authors.lastname: Zhou
authors.affiliation: Departments of Physiology and Developmental Biology, University of Texas , Southwestern Medical Center, Dallas, Texas 75390-9133, United States.
authors.forename: Cheng Cheng
authors.initials: CC
authors.lastname: Zhang
authors.affiliation: School of Chemistry & Environment, South China Normal University , Guangzhou 510006, China.
authors.forename: Yuhui
authors.initials: Y
authors.lastname: Zheng
authors.affiliation: Key Laboratory of Theoretical Chemistry of Environment, Ministry of Education, School of Chemistry & Environment, South China Normal University , Guangzhou 510006, China.|School of Chemistry & Environment, South China Normal University , Guangzhou 510006, China.|Guangzhou Key Laboratory of Materials for Energy Conversion and Storage , Guangzhou 510006, P. R. China.
authors.forename: Qianming
authors.initials: Q
authors.lastname: Wang
mesh_terms: D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000494:pharmacology; D045744:Cell Line, Tumor; D002467:Cell Nucleus / Q000737:chemistry / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D003593:Cytoplasm / Q000737:chemistry / Q000187:drug effects; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004121:Dimethyl Sulfoxide / Q000737:chemistry; D004317:Doxorubicin / Q000494:pharmacology; D016503:Drug Delivery Systems; D004705:Endocytosis / Q000187:drug effects; D005260:Female; D051379:Mice; D008810:Mice, Inbred C57BL; D053758:Nanoparticles; D000068936:Theranostic Nanomedicine
chemical_list: D000903:Antibiotics, Antineoplastic; D003692:Delayed-Action Preparations; D004317:Doxorubicin; D004121:Dimethyl Sulfoxide