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  3. Synthesis and evaluation of novel chlorophyll a derivatives as potent photosensitizers for photodynamic therapy

Synthesis and evaluation of novel chlorophyll a derivatives as potent photosensitizers for photodynamic therapy

  • Eur J Med Chem. 2020 Feb 1;187:111959. doi: 10.1016/j.ejmech.2019.111959.
Ying-Hua Gao 1,  Xue-Xue Zhu 1,  Wei Zhu 1,  Dan Wu 2,  Dan-Ye Chen 1,  Yi-Jia Yan 3,  Xiao-Feng Wu 3,  Donal F O'Shea 4,  Zhi-Long Chen 5
Affiliations

Affiliations

  • 1 Department of pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai, 201620, China.
  • 2 Department of Chemistry, Royal College of Surgeons in Ireland, 123 St. Stephen's Green, Dublin 2, Ireland.
  • 3 Shanghai Xianhui Pharmaceutical Co., Ltd, Shanghai, 200433, China.
  • 4 Department of Chemistry, Royal College of Surgeons in Ireland, 123 St. Stephen's Green, Dublin 2, Ireland. Electronic address: donalfoshea@rcsi.ie.
  • 5 Department of pharmaceutical Science & Technology, College of Chemistry and Biology, Donghua University, Shanghai, 201620, China. Electronic address: zlchen1967@qq.com.
PMID: 31846830 DOI: 10.1016/j.ejmech.2019.111959
Abstract

Chlorophyll a exhibits excellent photosensitive activity in photosynthesis. The unstability limited its application as photoensitizer drug in photodynamic therapy. Here a series of novel chlorophyll a degradation products pyropheophorbide-a derivatives were synthesized and evaluated for lung Cancer in PDT. These compounds have strong absorption in 660-670 nm with high molar extinction coefficient, and fluorescence emission in 660-675 nm upon excitation with 410-415 nm LIGHT. They all have much higher ROS yields than pyropheophorbide-a, and compound 10 was even higher than [3-(1-hexyloxyethyl)]-pyrophoeophorbide a (HPPH). Distinctive phototoxicity was observed in vitro and the inhibition effect was in LIGHT dose-dependent and drug dose-dependent style. They can effectively inhibit the growth of lung tumor in vivo. Among them, compound 8 and 11 have outstanding photodynamic anti-tumor effects without obvious skin photo-toxicity, so they can act as new drug candidates for photodynamic therapy.

Keywords

Chlorophyll derivatives; Photodynamic therapy; Photosensitizer; Tumor.

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