Citation: Ni Meng, Zeng Wen-Jun, Xie Xin, Chen Ze-Lin, Wu Hao, Yu Chang-Min, Li Bo-Wen. Intracellular enzyme-activatable prodrug for real-time monitoring of chlorambucil delivery and imaging[J]. Chinese Chemical Letters, ;2017, 28(6): 1345-1351. doi: 10.1016/j.cclet.2017.04.024 shu

Intracellular enzyme-activatable prodrug for real-time monitoring of chlorambucil delivery and imaging

College of Materials Science & Engineering, South China University of Technology, Guangzhou 510640, China

Corresponding author: Li Bo-Wen, msli860316@mail.scut.edu.cn

Received Date: 19 February 2017
Revised Date: 4 April 2017
Accepted Date: 20 April 2017
Available Online: 23 June 2017

Figures(6)

Carboxylesterase, a necessary enzyme in various mammalian cells, has been employed in various biological applications. Herein, we designed and synthesized a novel carboxylesterase-based prodrug, which can realize simultaneous drug-release imaging and cancer chemotherapy. This prodrug comprises three parts:coumarin as the fluorophore and the cleavable architecture, chlorambucil as the anticancer drug, and acetyl group as the enzyme-responsive unit. The presence of carboxylesterase leads to the activation of coumarin fluorescence, and this fluorescence serves as the reporting signal for assessing the enzyme level and drug release. Moreover, the prodrug was incorporated in liposome for monitoring drug release and chemotherapeutic effect in living cells. Upon internalization by HeLa cells, the prodrug can release chlorambucil and exhibit high cytotoxicity. This approach may provide some helpful insights for enhancing therapeutic effect and tracking the release of prodrug.
- Prodrug,
- Carboxylesterase,
- Chlorambucil,
- Fluorescent imaging,
- Liposomes
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