Title:A Comparative Study on In vitro Anti-cancer and In vivo Anti-angiogenic
Effects of TRPC Blockers Pyr-3 and SKF-96365
Volume: 20
Issue: 7
Author(s): Hülya Tuba Kıyan*, Ayca Üvez, Merve Erkisa, Elif İlkay Ikitimur-Armutak, Nadim Yılmazer, Osman Behzat Burak Esener, Deniz Erol Kutucu, Savaş Üstünova, Engin Ulukaya, A. Alper Öztürk and Ebru Gürel-Gürevin
Affiliation:
- Department of Pharmacognosy, Faculty of Pharmacy, Anadolu University, Eskisehir 26470, Turkey
Keywords:
Pyr-3, SKF-96365, cancer, angiogenesis, in vivo CAM assay, corpus luteum formation.
Abstract:
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.