Navegando por Palavras-chave "Artesunate"

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    Genotoxic evaluation of the antimalarial drugs artemisinin and artesunate in human HepG2 cells and effects on CASP3 and SOD1 gene expressions
    (Funpec-editora, 2013-01-01) Aquino, Ivani; Tsuboy, Marcela Stefanini Ferreira; Marcarini, Juliana Cristina; Mantovani, Mário Sérgio; Perazzo, Fábio Ferreira [UNIFESP]; Maistro, Edson Luis; Universidade de São Paulo (USP); Univ Estadual Paulista; Universidade Estadual de Londrina (UEL); Universidade Federal de São Paulo (UNIFESP)
    The 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 mu g/mL of both substances with a resazurin cytotoxicity assay, and the concentrations used in the genotoxicity experiments (2.5, 5, and 10 mu g/mL) and gene expression analysis (5 mu g/mL) were determined. the results of the comet assay in cells treated with artemisinin and artesunate showed a significant dose-dependent 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.
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    Genotoxicity assessment of the antimalarial compound artesunate in somatic cells of mice
    (Elsevier B.V., 2011-06-01) Aquino, Ivani; Perazzo, Fábio Ferreira [UNIFESP]; Maistro, Edson Luis; Univ Estadual Paulista; Universidade de São Paulo (USP); Universidade Federal de São Paulo (UNIFESP)
    Artesunate is a derivate of artemisinin that is both an antimalarial agent and acts cytotoxically on tumor cells. Despite its therapeutic use, its in vivo genotoxic potential has still not been evaluated. This study, therefore, was an investigation into the effects of a single oral administration of artesunate with an in vivo comet assay that analyzed leukocytes from peripheral blood and liver cells, and a micronucleus (MN) assay of bone marrow cells from male Swiss mice. the artesunate was administered by oral gavage at doses of 5, 50 and 100 mg/kg. Cytotoxicity was assessed by scoring 200 consecutive polychromatic (PCE) and normochromatic (NCE) erythrocytes (PCE/NCE ratio). the results demonstrate that artesunate induced significant DNA damage only in liver cells and that high doses of artesunate caused an increase in the mean number of micronucleated polychromatic erythrocytes (MNPCE). Under our experimental conditions, artesunate showed weak genotoxic effects at low doses and clastogenic effects at high doses. the PCE/NCE ratio indicated no cytotoxicity. the data obtained suggest caution about either continuous or high-dose use of artesunate by humans. (C) 2011 Elsevier B.V. All rights reserved.