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      Real-time monitoring of cell apoptosis and drug screening using fluorescent light-up probe with aggregation-induced emission characteristics

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      Author
      Shi, Haibin
      Kwok, Ryan T. K.
      Liu, Jianzhao
      Xing, Bengang
      Tang, Ben Zhong
      Liu, Bin
      Date of Issue
      2012
      School
      School of Physical and Mathematical Sciences
      Abstract
      Real-time monitoring of cell apoptosis could provide valuable insights into early detection of therapy efficiency and evaluation of disease progression. In this work, we designed and synthesized a new live-cell-permeable, fluorescent light-up probe for real-time cell apoptosis imaging. The probe is comprised of a hydrophilic caspase-specific Asp-Glu-Val-Asp (DEVD) peptide and a hydrophobic tetraphenylethene (TPE) unit, a typical fluorogen with aggregation-induced emission characteristics. In aqueous solution, the probe is almost nonfluorescent but displays significant fluorescence enhancement in response to caspase-3/-7, which are activated in the apoptotic process and able to cleave the DEVD moieties. This fluorescence “turn-on” response is ascribed to aggregation of cleaved hydrophobic TPE residues, which restricts the intramolecular rotations of TPE phenyl rings and populates the radiative decay channels. The light-up nature of the probe allows real-time monitoring of caspase-3/-7 activities both in solutions and in living cells with a high signal-to-noise ratio. The probe provides a new opportunity to screen enzyme inhibitors and evaluate the apoptosis-associated drug efficacy.
      Type
      Journal Article
      Series/Journal Title
      Journal of the American chemical society
      Rights
      © 2012 American Chemical Society.
      Collections
      • SPMS Journal Articles
      http://dx.doi.org/10.1021/ja3064588
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