Synthesis of furoxan and chlorin e6 conjugate and evaluation of photodynamic antitumor activity
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TQ463

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National Natural Science Foundation of China; Natural Science Foundation of Liaoning Province; Fundamental Research Funds for Central Universities

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    Abstract:

    Photodynamic therapy (PDT) is a non-invasive method of treating tumors.It is characterized by using light of a specific wavelength to excite the photosensitizer enriched in tumor cells to produce cytotoxic reactive oxygen species (ROS), and induce cell damage and death. However, the low oxygen concentration near the tumor tissue limits the level of active oxygen produced by the photosensitizer and affects the therapeutic effect of PDT. Using phenylpropenol as a raw material, 4-phenyl-3-hydroxymethyl-furoxan was synthesized, and it was esterified with chlorin e6 to obtain a chlorin e6 conjugate containing furazan. The results of the activity evaluation showed that the introduction of furazan group can significantly increase the level of intracellular NO, increase the number of intracellular ROS, and synergistically increase the photodynamic inhibitory activity of tumor cell proliferation by about 20 times. The results of this study indicate that the introduction of furoxan-like NO donor structure in the photosensitizer structure can significantly improve the photosensitizer’s activity in inhibiting tumor cell proliferation, providing a new idea for the synthesis of new and efficient photosensitizing anti-tumor therapeutic agents .

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History
  • Received:March 22,2021
  • Revised:April 28,2021
  • Adopted:April 28,2021
  • Online: August 05,2021
  • Published:
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