Aggregation Induced Emission Mediated Controlled Release by Using a Built-In Functionalized Nanocluster with Theranostic Features

Zhan Zhou, Chengcheng Zhang, Yuhui Zheng, Qianming Wang

Research output: Contribution to journalArticle

16 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)410-418
Number of pages9
JournalJournal of Medicinal Chemistry
Volume59
Issue number1
DOIs
StatePublished - Jan 14 2016

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery
  • Medicine(all)

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