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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Research Article

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

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

Volume 20, Issue 7, 2023

Published on: 23 January, 2023

Page: [957 - 964] Pages: 8

DOI: 10.2174/1570180820666230110155332

open access plus


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.

Keywords: Pyr-3, SKF-96365, cancer, angiogenesis, in vivo CAM assay, corpus luteum formation.

Graphical Abstract
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