A Comparative Study on In vitro Anti-cancer and In vivo Anti-angiogenic Effects of TRPC Blockers Pyr-3 and SKF-96365

KIYAN H. T., ÜVEZ A., Erkisa M., Ikitimur-Armutak E. İ., Yılmazer N., Burak Esener O. B., ...More

Letters in Drug Design and Discovery, vol.20, no.7, pp.957-964, 2023 (SCI-Expanded) identifier

  • Publication Type: Article / Article
  • Volume: 20 Issue: 7
  • Publication Date: 2023
  • Doi Number: 10.2174/1570180820666230110155332
  • Journal Name: Letters in Drug Design and Discovery
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Biotechnology Research Abstracts, Chemical Abstracts Core, EMBASE
  • Page Numbers: pp.957-964
  • Keywords: angiogenesis, cancer, corpus luteum formation, in vivo CAM assay, Pyr-3, SKF-96365
  • Bezmialem Vakıf University Affiliated: Yes


Introduction: Angiogenesis is involved in many physiological and pathological conditions including cancer. A number of TRP channels induce angiogenesis, promote cel proliferation or induce apoptosis in several types of human cancers. Therefore, TRP channels may be considered potential pharmacological targets for therapeutic options of disorders caused by insufficient angiogenesis or aberrant vascularization. Aims: This study aimed to comparatively investigate in vitro anti-cancer and in vivo anti-angiogenic effects of TRPC blockers Pyr-3 and SKF-96365. Methods: For anti-cancer effects, four cancer cel lines (MDA-MB-231, A549, PC-3, and HCT-116) were used. In vivo anti-angiogenic effects were investigated by employing in vivo CAM assay of fertilized hen eggs. Results: Pyr-3 affected cel viability in a dose-dependent manner, al concentrations of SKF-96365 significantly reduced cel viability in al cel lines. Pyr-3 and SKF-96365 at concentrations of 2.5 µg/pelet and 50 µg/pelet, respectively inhibited in vivo angiogenesis significantly. Conclusion: The concentration of 2.5 µg/pelet caused no irritation, whereas 50 µg/pelet produced some slight irritation. Apart from their anti-cancer effects, our findings indicate that Pyr-3 and SKF-96365 may be promising anti-angiogenic agents for the treatment of angiogenesis-related disorders.