Cytogenotoxicity assessment of 3‐(3,4‐dihydroxyphenyl)‐7,8‐dihydroxycoumarin on HepG2/C3A cells and leukocytes

Abstract

3-(3,4-Dihydroxyphenyl)-7,8-dihydroxycoumarin is a newly synthesized coumarin derivative with a potent antioxidant effect. The aim of the present study is to investigate the safety of this compound, determining the in vitro cytotoxic and genotoxic in human peripheral blood mononuclear cells (PBMC) and in HepG2/C3A cells. Cell viability has been investigated by the trypan blue staining test and MTT assay and the genotoxicity by the comet assay and micronucleus test, using concentrations between 0.01 and 10 μg/ml. The compound proved to be noncytotoxic in both cell lines, at all tested concentrations, protecting the cells from the DNA damage. In addition, this molecule does not show clastogenic/aneugenic effects when performing the micronucleus test with cytokinesis blockade. Based on the obtained data, and the conditions of the experiments, we can conclude that the 3-(3,4-dihydroxyphenyl)-7,8-dihydroxycoumarin is a safe molecule up to a concentration of 10 μg/ml, which encourages further studies aiming to explore its potential as a drug candidate.

Evaluation of in vitro cytotoxic and genotoxic effects of the 3‐(3,4‐dihydroxyphenyl)‐8‐hydroxycoumarin

“…Positive and negative results of cytotoxicity of different coumarins have been reported. Our research group recently reported the cytotoxicity studies of 3‐(3,4‐dihydroxyphenyl)‐7,8‐dihydroxycoumarin (Castanha et al, 2023), which is chemically very similar to the coumarin evaluated in the present study. Absence of cellular toxicity, for both PBMC and HepG2/C3A cells, through trypan blue staining and MTT assays, has been reported.…”

“…This absence of genetic toxicity has been previously reported for some other coumarins. Recently, our research group reported absence of genotoxicity of 3‐(3,4‐dihydroxyphenyl)‐7,8‐dihydroxycoumarin also on HepG2/C3A and leukocyte cells (Castanha et al, 2023). 6,7‐Dihydroxycoumarin, also known as esculetin, was administered to Swiss mice, and no genotoxic effects were observed in peripheral blood, liver, bone marrow, and testicular cells, as well as no occurrence of chromosomal mutations in polychromatic bone marrow erythrocytes has been described.…”

Effect of air, O2, Ar, and N2 plasma‐activated water on mildewing activity of moldy pathogen of Gannan navel oranges

“…Staining of cells with Trypan Blue to distinguish between dead and alive cells is a standard method of identification. [3,[31][32][33] The interior of inactivated cells is stained with Trypan Blue. Normal living cells have an intact cell membrane that rejects the Tapan Blue staining solution and the cells are not stained.…”