RESUMEN
In an effort to detect potential inhibitors of cdc25 phosphatase, nineteen flavonoids belonging to the quercetin and kaempferol series have been evaluated, using a colorimetric assay of recombinant human cdc25A tyrosine phosphatase as a cell cycle-specific target. Compounds bearing two benzyl or methyl groups in positions 7 and 4' and acetyl on the hydroxy groups of the sugar moiety showed the maximal activity.
Asunto(s)
Quinasas Ciclina-Dependientes/antagonistas & inhibidores , Flavonoides , Quempferoles , Magnoliopsida/química , Quercetina/farmacología , Fosfatasas cdc25/antagonistas & inhibidores , Bioensayo , División Celular , Células Cultivadas , Colorimetría , Quinasas Ciclina-Dependientes/metabolismo , Escherichia coli/citología , Humanos , Magnoliopsida/citología , Factor Promotor de Maduración , Estructura Molecular , Quercetina/análogos & derivados , Quercetina/química , Fosfatasas cdc25/metabolismoRESUMEN
The antiviral activity of seven flavonoids, belonging to the kaempferol series, was evaluated against human cytomegalovirus (HCMV) by a rapid method of detection of the immediate-early (IE) antigen, induced by the virus in infected cells. Flavonoids bearing acyl substituents were found to be the most active compounds.
Asunto(s)
Antivirales/farmacología , Citomegalovirus/efectos de los fármacos , Flavonoides , Glicósidos/farmacología , Quempferoles , Quercetina/análogos & derivados , Estudios de Evaluación como Asunto , Humanos , Quercetina/química , Quercetina/farmacologíaRESUMEN
The cytotoxic activity of three flavonoids, belonging to the kaempherol series, was evaluated against 15 human leukemic cell lines. Flavonoids bearing acyl substituants, 2 and 3, were found to be the most active compounds. A further compound, 1, was examined for its ability to modulate the expression of MDR-1 and GST-pi resistance genes and compounds 2 and 3 for their effect on the uptake of [3H]-thymidine as a marker of DNA synthesis.
