Evaluation of the Antiproliferative, Anti-angiogenic, and Antioxidant Activity of a Newly Synthesized Indole Derivative
DOI:
https://doi.org/10.32947/ajps.v26i3.1428Keywords:
Indole derivative, antiproliferative, anti-angiogenic, antioxidant activityAbstract
Background: Angiogenesis is a physiological process whereby preexisting blood vessels divide to generate new ones. Abnormal angiogenesis is the major cause of various diseases.
Objective: In this work, a newly synthesized indole derivative, 2-(5-bromo-1H-indole-2-carbonyl)-N-(p-tolyl) hydrazine-1-carbothioamide (BIHC), was evaluated for antiproliferative and antiangiogenic activities using experimental models of neovascularization, while its antioxidant activity was assessed using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical-scavenging assay. Methods: The antiproliferative effect on the human umbilical vein endothelial cell line (HUVECs) and MCF-7 cell line was assessed using the [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] MTT assay. An ex vivo rat aorta ring assay and an in vivo chorioallantoic membrane experimental model were used to investigate its antiangiogenic activity; these assays were also used to assess the dose-response effects of the tested compounds by preparing serial concentrations. Antioxidant activity was analyzed using the DPPH free radical scavenging assay.
Results: The compound inhibits the proliferation of HUVECs with an IC50 of 80.24 μg/mL and MCF-7 with an IC50 of 96.32 μg/mL. The tested compound at serial concentrations showed significant dose-dependent inhibitory activity (P < 0.0001) in the rat aorta ring (RAR) assay, with an IC50 of 30.47 μg/mL. The study proceeded by applying the chorioallantoic membrane (CAM) assay, in which serial dilutions of the derivative were added and tested separately. Furthermore, the tested compounds exhibited significant antioxidant activity in the DPPH radical scavenging assay (P < 0.0001), with an IC50 of 5.48 μg/mL.
Conclusion: The findings suggest that the new indole derivative has an antiproliferative effect and significant anti-angiogenic and antioxidant properties.
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