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

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Kıyan H. T., Üvez A., Erkisa M., Ikitimur-Armutak E. İ., Yılmazer N., Esener O. B. B., ...More

LETTERS IN DRUG DESIGN AND DISCOVERY, vol.20, no.7, pp.957-967, 2023 (SCI-Expanded)

  • Publication Type: Article / Article
  • Volume: 20 Issue: 7
  • Publication Date: 2023
  • Doi Number: 10.2174/1570180820666230110155332
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Biotechnology Research Abstracts, Chemical Abstracts Core, EMBASE
  • Page Numbers: pp.957-967
  • Anadolu University Affiliated: Yes


Introduction: Angiogenesis is involved in many physiological and pathological conditions including cancer. A number of TRP channels induce angiogenesis, promote cell 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 cell 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 cell viability in a dose-dependent manner, all concentrations of SKF-96365 significantly reduced cell viability in all cell lines. Pyr-3 and SKF-96365 at concentrations of 2.5 µg/pellet and 50 µg/pellet, respectively inhibited in vivo angiogenesis significantly. Conclusion: The concentration of 2.5 µg/pellet caused no irritation, whereas 50 µg/pellet 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.