2. Academic Validation
  3. Singlet oxygen-activatable Paclitaxel prodrugs via intermolecular activation for combined PDT and chemotherapy

Singlet oxygen-activatable Paclitaxel prodrugs via intermolecular activation for combined PDT and chemotherapy

  • Bioorg Med Chem Lett. 2019 Jun 15;29(12):1537-1540. doi: 10.1016/j.bmcl.2019.03.053.
Moses Bio 1,  Kazi Md Mahabubur Rahman 1,  Irene Lim 1,  Pallavi Rajaputra 1,  Robert E Hurst 2,  Youngjae You 3
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Sciences, College of Pharmacy, University of Oklahoma, Oklahoma City, OK 73117, United States.
  • 2 Department of Urology, University of Oklahoma Health Sciences Center, Oklahoma City, OK 73117, United States.
  • 3 Department of Pharmaceutical Sciences, College of Pharmacy, University of Oklahoma, Oklahoma City, OK 73117, United States; Department of Chemistry and Biochemistry, University of Oklahoma, Norman, OK 73019, United States. Electronic address: youngjae-you@ouhsc.edu.
PMID: 30987891 DOI: 10.1016/j.bmcl.2019.03.053
Abstract

Systemic side effects and high hydrophobicity are major disadvantages of paclitaxel (PTX), one of the most popular Anticancer drugs. Here, we present singlet oxygen (SO)-activatable and mitochondria-targeted PTX prodrugs to overcome these problems and boost the cytotoxic effect of photodynamic therapy (PDT). Three PTX prodrugs were prepared by conjugating PTX with various cationic groups. Hydrophobicity was determined in LogD7.4 value. Mitochondrial localization was confirmed by fluorescence confocal microscopy and uptake of mitochondria-specific fluorescence probe. Dark- and photo-toxicity were measured in AY-27 cells with MTT assay. All three prodrugs showed better hydrophilicity than PTX and improved phototoxicity when combined with protoporphyrin IX (PpIX) PDT. In conclusion, SO-activatable and higher hydrophilic PTX prodrugs were successfully prepared. This approach could be used to improve the antitumor efficacy of PDT without the systemic side effects of PTX.

Keywords

Paclitaxel; Photo-unclick; Photodynamic therapy; Singlet oxygen.

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