Aquino, I. [UNESP]Tsuboy, M. S F [UNESP]Marcarini, J. C. [UNESP]Mantovani, M. S.Perazzo, F. F.Maistro, Edson Luis [UNESP]2014-05-272014-05-272013-07-24Genetics and Molecular Research, v. 12, n. 3, p. 2517-2527, 2013.1676-5680http://hdl.handle.net/11449/76047The malaria treatment recommended by the World Health Organization involves medicines derived from artemisinin, an active compound extracted from the plant Artemisia annua, and some of its derivatives, such as artesunate. Considering the lack of data regarding the genotoxic effects of these compounds in human cells, the objective of this study was to evaluate the cytotoxicity and genotoxicity, and expressions of the CASP3 and SOD1 genes in a cultured human hepatocellular liver carcinoma cell line (HepG2 cells) treated with artemisinin and artesunate. We tested concentrations of 2.5, 5, 7.5, 10, and 20 μg/mL of both substances with a resazurin cytotoxicity assay, and the concentrations used in the genotoxicity experiments (2.5, 5, and 10 μg/mL) and gene expression analysis (5 mg/mL) were determined. The results of the comet assay in cells treated with artemisinin and artesunate showed a significant dosedependent increase (P < 0.001) in the number of cells with DNA damage at all concentrations tested. However, the gene expression analysis revealed no significant change in expression of CASP3 or SOD1. Our data showed that although artemisinin and artesunate exhibited genotoxic effects in cultured HepG2 cells, they did not significantly alter expression of the CASP3 and SOD1 genes at the doses tested. ©FUNPEC-RP.2517-2527engArtemisininArtesunateCASP3 and SOD1 genesComet assayGene expressionHepG2 cellsartemisininartesunatecaspase 3cell DNAdoxorubicinextracellular superoxide dismutaseresazurinCasp3 genecell countcell strain HepG2comet assayconcentration responsecontrolled studycytotoxicityDNA damagedrug effectdrug screeninggene expressiongenotoxicityhumanhuman cellSOD1 geneArtigo10.4238/2013.July.24.6WOS:000331717400035Acesso aberto2-s2.0-848808146502-s2.0-84880814650.pdf47875216130383150000-0003-0757-7876