Antitumor activity of two derivatives from 2-acylamine-1, 4-naphthoquinone in mice bearing S180 tumor.
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.
Bezerra
Daniel Pereira
DP
Department of Physiology and Pharmacology, School of Medicine, Federal University of Ceará, P.O. Box 3157, 60430-270 Fortaleza, Ceará, Brazil.
Alves
Ana Paula Negreiros Nunes
AP
de Alencar
Nylane Maria Nunes
NM
Mesquita
Rodney de Oliveira
Rde O
Lima
Michael Will
MW
Pessoa
Cláudia
C
de Moraes
Manoel Odorico
MO
Lopes
José Norberto Callegari
JN
Lopes
Norberto Peporine
NP
Costa-Lotufo
Letícia Veras
LV
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
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