Data/hora: 16/06/2024 06:19:37

Provedor de dados: | 56
País: | Brazil
Título: | DNA topoisomerase inhibitors: biflavonoids from Ouratea species
Autores: | Grynberg,N.F.; Carvalho,M.G.; Velandia,J.R.; Oliveira,M.C.; Moreira,I.C.; Braz- Filho,R.; Echevarria,A.
Data: | 2002-07-01
Ano: | 2002
Palavras-chave: | Biflavonoids; Amentoflavone; 7"-O-Methyl-agathisflavone; DNA topoisomerases; Ehrlich carcinoma; Human K562 leukemia.
Resumo: | Topoisomerase inhibitors are agents with anticancer activity. 7"-O-Methyl-agathisflavone (I) and amentoflavone (II) are biflavonoids and were isolated from the Brazilian plants Ouratea hexasperma and O. semiserrata, respectively. These biflavonoids and the acetyl derivative of II (IIa) are inhibitors of human DNA topoisomerases I at 200 µM, as demonstrated by the relaxation assay of supercoiled DNA, and only agathisflavone (I) at 200 µM also inhibited DNA topoisomerases II-alpha, as observed by decatenation and relaxation assays. The biflavonoids showed concentration-dependent growth inhibitory activities on Ehrlich carcinoma cells in 45-h culture, assayed by a tetrazolium method, with IC50 = 24 ± 1.4 µM for I, 26 ± 1.1 µM for II and 10 ± 0.7 µM for IIa. These biflavonoids were assayed against human K562 leukemia cells in 45-h culture, but only I showed 42% growth inhibitory activity at 90 µM. Our results suggest that biflavonoids are targets for DNA topoisomerases and their cytotoxicity is dependent on tumor cell type.
Tipo: | Info:eu-repo/semantics/other
Idioma: | Inglês
Identificador: | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2002000700009
Editor: | Associação Brasileira de Divulgação Científica
Relação: | 10.1590/S0100-879X2002000700009
Formato: | text/html
Fonte: | Brazilian Journal of Medical and Biological Research  v.35 n.7 2002
Fonte: | info:eu-repo/semantics/openAccess