Anti-Angiogenic and Anti-Proliferative Activity of 4-2-(5-bromo-1H-indol-2-carbonyl)-N-(4-methoxyphenyl) Hydrazine-1-carbothioamide: Ex-vivo and in vitro Study.

Abstract

Angiogenesis, the formation of new blood vessels, stimulates tumor growth and spread by delivering oxygen and nutrients, and is a key component of metastasis. This work aimed to evaluate the anti-angiogenic properties of a new synthesized compound. Rat aorta angiogenesis assay was used to evaluate the ability of the carbothioamide derivative to inhibit blood vessels sprouting. The tetrazolium (MTT) assay was used to evaluate the anti-proliferative effect of the synthetic compound on human umbilical vein endothelial cell line (HUVECs) and A549 lung cancer cells line. The (2, 2-diphenyl-1-picrylhydrazyl) DPPH was used to investigate the free radical scavenging action. The study showed that the compound has anti-angiogenic activity with IC50 56.9 µg/mL, moreover the compound managed to inhibit the proliferation of HUVECs and A549 cells (IC50 76.3 µg/mL and 45.5 µg/mL, respectively), and The IC50 concentration for free radical scavenging activity of the compound was 27.8 µg/ml. The study concluded that the compound has significant anti-angiogenic activity may be related to its significant anti-proliferative effect against HUVECs, these pharmacological effect may attributed to its potent free radical scavenging activity.