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<p>Photodynamic therapy (PDT) has received much attention in cancer treatment because of its low toxicity and side effects. In this study, we successfully synthesized 14 novel porphyrin-formononetin derivatives. In reactive oxygen species detection experiments, the target compounds <b>4a–6d</b> caused a significant decrease in the fluorescence intensity of DPBF compared with the porphyrin parent and formononetin feedstock after illumination, and it was found that the target compound had a higher ROS quantum yield, among which the quantum yield of compound <b>6c</b> was higher. In the in vitro anti-tumor activity assay, the target compounds <b>4a–6d</b> exhibited a certain degree of growth inhibition against six cancer cells (A549, MDA-MB-231, HCT-116, HGC-27, DU145, and TCCSUP) under light conditions, whereas the cytotoxicity of the target compounds against the normal cells H9c2 was less. The results of the scratch assay showed that <b>6c</b> could inhibit the growth of tumor cells by inhibiting the migration of DU145 cells. The experimental results indicate that the target compounds achieve the synergistic effect of PDT and chemotherapy.</p> Graphical abstract <p></p>

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Synthesis of porphyrin-formononetin derivatives and their anti-tumor activity studies

  • 期刊论文

  • 发表日期：

    2025年4月9日

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  • Lingyan Yang,
  • Shan He,
  • Chen Tang,
  • Lei Shi,
  • Zhenhua Liu,
  • Zejie Tian,
  • Hui Li,
  • Xufeng He,
  • Jiding Liao,
  • Yunmei Liu

摘要

Photodynamic therapy (PDT) has received much attention in cancer treatment because of its low toxicity and side effects. In this study, we successfully synthesized 14 novel porphyrin-formononetin derivatives. In reactive oxygen species detection experiments, the target compounds 4a–6d caused a significant decrease in the fluorescence intensity of DPBF compared with the porphyrin parent and formononetin feedstock after illumination, and it was found that the target compound had a higher ROS quantum yield, among which the quantum yield of compound 6c was higher. In the in vitro anti-tumor activity assay, the target compounds 4a–6d exhibited a certain degree of growth inhibition against six cancer cells (A549, MDA-MB-231, HCT-116, HGC-27, DU145, and TCCSUP) under light conditions, whereas the cytotoxicity of the target compounds against the normal cells H9c2 was less. The results of the scratch assay showed that 6c could inhibit the growth of tumor cells by inhibiting the migration of DU145 cells. The experimental results indicate that the target compounds achieve the synergistic effect of PDT and chemotherapy.

Graphical abstract