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Antitumor activity of two derivatives from 2-acylamine-1, 4-naphthoquinone 113 in mice bearing S180 tumor
Daniel Pereira Bezerra, Ana Paula Negreiros Nunes Alves, Nylane Maria Nunes de Alencar, Rodney de Oliveira Mesquita, Michael Will Lima, Cláudia Pessoa, Manoel Odorico de Moraes, José Norberto Callegari Lopes, Norberto Peporine Lopes and Letícia Veras Costa-Lotufo

Drugs containing a quinone moiety, such as anthracyclines, mitoxantrones and lapachol, show excellent anticancer activity. In this study, 2-butanoylamine-1,4-naphthoquinone (1) and 2-propanoylamine-1,4-naphthoquinone (2) derivatives from 2-amine-1,4-naphthoquinone were synthesized, and their antitumor activity in mice bearing Sarcoma 180 tumor were examined. In addition, hematology and biochemistry analyses, as well as, histopathological and morphological analyses were performed in order to evaluate the toxicological aspects of the naphthoquinones treatment. Both naphthoquinones showed potente antitumor activity. The inhibition rates were 33.48 and 42.35% for (1) and 37.65 and 55.24% for (2) at the dose of 25 and 50mg/kg/day, respectively. In the histopathological analysis, the naphthoquinones showed only weak toxicity. Neither enzimatic activity of transaminases (aspartate aminotransferase-AST nor alanine aminotransferase-ALT), urea level nor hematological paramenter were significantly modified after naphthoquinones treatment. These data reinforce the anticancer potential of naphthoquinones derivatives.

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