title: Antitumor activity of two derivatives from 2-acylamine-1, 4-naphthoquinone in mice bearing S180 tumor.
abstract: 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 50 mg/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.
authors.affiliation: Department of Physiology and Pharmacology, School of Medicine, Federal University of Ceará, P.O. Box 3157, 60430-270 Fortaleza, Ceará, Brazil.
authors.forename: Daniel Pereira
authors.initials: DP
authors.lastname: Bezerra
authors.forename: Ana Paula Negreiros Nunes
authors.initials: AP
authors.lastname: Alves
authors.forename: Nylane Maria Nunes
authors.initials: NM
authors.lastname: de Alencar
authors.forename: Rodney de Oliveira
authors.initials: Rde O
authors.lastname: Mesquita
authors.forename: Michael Will
authors.initials: MW
authors.lastname: Lima
authors.forename: Cláudia
authors.initials: C
authors.lastname: Pessoa
authors.forename: Manoel Odorico
authors.initials: MO
authors.lastname: de Moraes
authors.forename: José Norberto Callegari
authors.initials: JN
authors.lastname: Lopes
authors.forename: Norberto Peporine
authors.initials: NP
authors.lastname: Lopes
authors.forename: Letícia Veras
authors.initials: LV
authors.lastname: Costa-Lotufo
mesh_terms: D000410:Alanine Transaminase / Q000097:blood; D000813:Anilides / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D001219:Aspartate Aminotransferases / Q000097:blood; D001772:Blood Cell Count; D001835:Body Weight / Q000187:drug effects; D005260:Female; D007668:Kidney / Q000473:pathology; D051379:Mice; D009285:Naphthoquinones / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D009368:Neoplasm Transplantation; D009929:Organ Size / Q000187:drug effects; D012510:Sarcoma 180 / Q000188:drug therapy* / Q000473:pathology; D014508:Urea / Q000097:blood
chemical_list: C534398:2-butanoylamine-1,4-naphthoquinone; C534399:2-propanoylamine-1,4-naphthoquinone; D000813:Anilides; D000970:Antineoplastic Agents; D009285:Naphthoquinones; D014508:Urea; D001219:Aspartate Aminotransferases; D000410:Alanine Transaminase