RESUMO
The photoinduced covalent binding of the title compound to native and heat denatured DNA is described. The level of binding has been measured by UV (for DNA) and atomic absorption (for Rh) analysis. Quantum efficiencies of 6.4 x 10(-4) mol Rh per mol photons and 1.6 x 10(-3) mol Rh per mol photons have been determined for binding to native and denatured calf thymus DNA, respectively. Levels of bound rhodium as high as 1 molecule per five bases have been achieved. There is no binding of the complex in the absence of light, and there is evidence that at least a portion of the binding may be due to the photolytic conversion of the complex into one or more stable intermediates. Studies with polyribonucleotides indicate a strong preference for binding to the purine bases.
Assuntos
DNA/metabolismo , Fotoquímica , Ródio/metabolismo , Animais , Bovinos , Fenômenos Químicos , QuímicaRESUMO
Tebufelone (NE-11740) is a member of the new di-tert-butylphenol class of anti-inflammatory agents. It exhibits good inhibitory activity against cyclooxygenase and 5-lipoxygenase in vitro. It also shows excellent anti-inflammatory activity and inhibits bone resorption in vivo in the rat adjuvant arthritis model at an oral dose level of 1 to 2 mg/kg. The absorption, bioavailability, and pharmacokinetics of tebufelone were investigated in male Sprague-Dawley rats. Tebufelone labeled with carbon-14 was administered intravenously at doses of 0.5 and 2 mg/kg and perorally at doses of 2 and 10 mg/kg to fasted rats. Plasma samples taken from the rats at timed intervals were analyzed for total radiolabel by scintillation counting and for tebufelone by a mass spectrometric method. Comparison of the total radiolabel and tebufelone areas under the curves (AUCs) of concentration of tebufelone versus time from the 2-mg/kg intravenous and 2-mg/kg oral doses indicates that tebufelone is completely absorbed and 100% bioavailable at this dose level in the rat. The AUCs are a linear function of dose at the 0.5- and 2-mg/kg dose levels, but the AUC of the 10-mg/kg dose exhibits a nonproportional increase, suggesting saturation of elimination processes at this higher dose.
Assuntos
Alcinos/farmacocinética , Anti-Inflamatórios não Esteroides/farmacocinética , Fenóis/farmacocinética , Absorção , Administração Oral , Animais , Disponibilidade Biológica , Meia-Vida , Injeções Intravenosas , Masculino , Ratos , Ratos Sprague-DawleyAssuntos
Melaninas/efeitos da radiação , Raios Ultravioleta , Animais , Galinhas , Cabelo , Humanos , Oxigênio , FotóliseRESUMO
The Salmonella typhimurium histidine reversion test of Ames et al. was used to demonstrate the pheomelanin, the red-brown polymeric pigment produced in human skin and hair, becomes mutagenic after exposure to long wave-length UV-light; a finding consistent with the UV-induced somatic mutation hypothesis for the origin of freckles and the high susceptibility of redheads and blonds to sunlight-induced skin cancers.