2. Academic Validation
  3. Synthesis and biological characterization of novel rose bengal derivatives with improved amphiphilicity for sono-photodynamic therapy

Synthesis and biological characterization of novel rose bengal derivatives with improved amphiphilicity for sono-photodynamic therapy

  • Eur J Med Chem. 2018 Feb 10:145:86-95. doi: 10.1016/j.ejmech.2017.12.091.
Hai-Jun Chen 1,  Xiao-Bin Zhou 1,  Ai-Lan Wang 1,  Bi-Yuan Zheng 1,  Chih-Kuang Yeh 2,  Jian-Dong Huang 3
Affiliations

Affiliations

  • 1 College of Chemistry, State Key Laboratory of Photocatalysis on Energy and Environment, Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and Chemotherapy, Fuzhou University, Fuzhou 350116, China.
  • 2 Department of Biomedical Engineering and Environmental Science, National Tsing Hua University, Hsinchu 30013, Taiwan.
  • 3 College of Chemistry, State Key Laboratory of Photocatalysis on Energy and Environment, Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and Chemotherapy, Fuzhou University, Fuzhou 350116, China. Electronic address: jdhuang@fzu.edu.cn.
PMID: 29324346 DOI: 10.1016/j.ejmech.2017.12.091
Abstract

Sono-Photodynamic therapy (SPDT) utilizing ultrasound and light has been demonstrated that this novel approach can lower dosage resulting in reduction of the potential side effects caused by sensitizers. Recently, a new formulation of rose bengal (RB) as an intralesional injection has completed clinical trials phase II for PDT treatment of melanoma Cancer. However, the inherent unfavorable pharmacological properties of RB hindered its extensive clinical development. With the aim to identify new RB derivatives (RBDs) with enhanced photodynamic and sonodynamic Anticancer efficiency, a series of amphiphilic RBDs have been designed, synthesized and biological characterized. Among them, RBD4 significantly improved cellular uptake and enhanced intracellular ROS generation efficiency upon light and ultrasound irradiation, resulting in dramatically improved Anticancer potency. Notably, RBD4 has a relative potency similar to sinoporphyrin sodium (DVDMS), indicating its further potential application for SPDT.

Keywords

Amphiphilicity; RB derivatives; Sensitizers; Sono-photodynamic therapy.

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