Evaluation of in vitro cytotoxic and hemolytic effects of a new series of hydroxy- and nitro-containing arylcoumarins

Coumarins are natural or synthetic compounds with a variety of biological applications, from fluorescent probes to therapeutic agents. Our group has been studying the importance of this moiety in the development of drugs targeting neurodegeneration. Based on the structure of the acenocoumarol, a frequently prescribed oral anticoagulant to treat and prevent thromboembolism, nitro groups have been commonly introduced in coumarin-containing compounds. Therefore, the assessment of their safety for humans is essential.^1,2

In the current work, twelve hydroxy- and nitro-substituted arylcoumarins have been synthetized, and cytotoxicity and hemolytic effects have been studied. Human embryonic kidney cells (HEK-293, strain ATCC CRL1573) and human red blood cells (RBC) have been used for the in vitro assays. Compounds were plated as a 2-fold dose response from 32 to 0.25 μg/mL, with a maximum of 0.5% DMSO. Values of CC₅₀ (cytotoxicity) and HC₁₀ (haemolytic activity) are presented in this communication.

⁽¹⁾ Martins Castanha AP, Moura Almeida-Terassi L, Guardado-Yordi E, Matos MJ, Maistro EL. Cytogenotoxicity assessment of 3-(3,4-dihydroxyphenyl)-7,8-dihydroxycoumarin on HepG2/C3A cells and leukocytes. J Appl Toxicol 2023, 43, 323−334. DOI: 10.1002/jat.4384.

⁽²⁾ dos Santos Silva E, Matos MJ, Maistro EL. Evaluation of in vitro Cytotoxic and Genotoxic Effects of the 3-(3,4-Dihydroxyphenyl)-8-hydroxycoumarin. J Appl Toxicol 2023. DOI: 10.1002/jat.4479.