Biochemical Studies on Coumarin Derivatives as Antioxidant and Antitumor Agents

Background: Coumarin derivatives have attracted intense interest in recent years, because they have anti-tumor, antioxidant activities, and induce apoptosis.

Aims and Objective: Our study aims to evaluate the antitumor and anti-oxidant activities of new Coumarin derivatives: N-(P-chlorophenyl)-7-hydroxycoumarin-3-yl carboxamide and Ethyl 7-hydroxycoumarin-3-yl ester against in vivo tumor model.

Methodology: the toxicity for the synthesized compounds was determined. The anticancer and anti-oxidant activities were studied by evaluation the viability of tumor cells, life span prolongation, and estimation of antioxidants.

Results: Our compounds exhibited significant anti-oxidant activity towards Ehrlich ascites carcinoma (EAC) cells by reduction the MDA and NO concentration (p<0.001) compared to the positive control group. Whereas significantly increase in the G. peroxidase activity (p<0.001) in treated groups compared to the positive control group. Anticancer agent kills tumors by induction of apoptosis that showing significantly increases in Caspase-3 and Bax activity compared to positive control group.

Discussion: The compound N-(P-chlorophenyl)-7-hydroxycoumarin-3-yl carboxamide is better than Ethyl 7-hydroxycoumarin-3-yl ester compound because of the nature of the halogen atom (a chlorine or a bromine atom) in the ‘meta’ position of the phenyl ring relative to the ester oxygen atom of 2-oxo-2H-1-benzopyran- 3-carboxylate led to a better anti-tumor effect than that observed in the absence of any substituent.