RESUMO
A comparative evaluation of the antiviral activity of a number of new and previously synthesized terpenophenols and their N- or O-containing derivatives against the A/Puerto Rico/8/34 (H1N1) virus strain was carried out. 2-Isobornylphenol, 1,2-dihydroxy-6-isobornyl-4-methylbenzene, 2-isobornyl-1,4-benzoquinone, and N-butyl-4-hydroxy-3,5-diisobornylbenzamide showed the highest activity.
RESUMO
2,6-Diisobornyl-4-methylphenol (Dibornol, 10 mg/kg intragastrically daily for 5 days after myocardial ischemia/reperfusion) 1.5-fold increased rat survival during the acute post-infarction period in comparison with the control group. In survivors, Dibornol reliably prevented post-ischemic progression of heart failure in the delayed post-infarction period (30 days after ischemia/reperfusion), which was seen from an increase in the left-ventricular developed pressure by 22%, left-ventricular contractility index by 19%, and +dP/dt by 34%. Left-ventricular end-diastolic pressure was by 39% lower than in control animals. Morphological study of heart sections from control group animals showed that Dibornol reduced the area of post-ischemic myocardial damage in the delayed period after ischemia/reperfusion to 3±1% (vs 18±2% in the control group).
Assuntos
Cresóis/uso terapêutico , Ventrículos do Coração/efeitos dos fármacos , Traumatismo por Reperfusão Miocárdica/tratamento farmacológico , Animais , Pressão Sanguínea/efeitos dos fármacos , Cresóis/química , Coração/efeitos dos fármacos , Ventrículos do Coração/metabolismo , Masculino , Reperfusão Miocárdica , Traumatismo por Reperfusão Miocárdica/metabolismo , RatosRESUMO
Neuroprotective activity of 2,6-diisobornyl-4-methylphenol (Dibornol) was studied under conditions of experimental focal cerebral ischemia/reperfusion modeled by intraluminal occlusion of the left middle cerebral artery for 1 h followed by recirculation. Dibornol administered in a dose of 10 mg/kg intragastrically 24 h and 30 min before and 24 h after focal ischemia/reperfusion modeling reduced the size of the brain infarction zone by 52% (48 h after recirculation) and neurological deficit by 1.7-2.4 times in comparison with that in control animals.
Assuntos
Isquemia Encefálica/tratamento farmacológico , Fármacos Neuroprotetores/uso terapêutico , Animais , Encéfalo/efeitos dos fármacos , Encéfalo/patologia , Infarto Encefálico/tratamento farmacológico , Canfanos/uso terapêutico , Cresóis/uso terapêutico , Masculino , Ratos , Ratos Wistar , Traumatismo por Reperfusão/tratamento farmacológicoRESUMO
We compared bioavailability of 4-methyl-2,6-diisobornylphenol after single intragastric administration to rats in a dose of 200 mg/kg in starch suspension and in almond oil. Absorption of 4-methyl-2,6-diisobornylphenol in the gastrointestinal tract after administration in almond oil was much more efficient than after administration in aqueous starch mucus.
Assuntos
Antioxidantes/administração & dosagem , Antioxidantes/farmacocinética , Canfanos/administração & dosagem , Canfanos/farmacocinética , Cresóis/administração & dosagem , Cresóis/farmacocinética , Fenóis/administração & dosagem , Fenóis/farmacocinética , Administração Oral , Animais , Trato Gastrointestinal/metabolismo , Absorção Intestinal/efeitos dos fármacos , Masculino , Óleos de Plantas/química , Ratos , Ratos WistarRESUMO
Synthesis of sulfanylimines based on neomenthane and isobornane thiol was carried out with yields up to 85%. On the model of H2O2- and AAPH-induced hemolysis of blood erythrocytes it was found that the sulfenimines have membrane protective and antioxidant activities and inhibit the accumulation of secondary products of lipid peroxidation and oxidation of hemoglobin.
Assuntos
Membrana Eritrocítica/química , Hemólise/efeitos dos fármacos , Iminas , Animais , Hemoglobinas/química , Peróxido de Hidrogênio/química , Peróxido de Hidrogênio/farmacologia , Iminas/síntese química , Iminas/química , Iminas/farmacologia , Peroxidação de Lipídeos/efeitos dos fármacos , Camundongos , Oxidantes/química , Oxidantes/farmacologiaRESUMO
Two diastereomers of methylpheophorbide a 13(2)-N-n-octyl-N-(2-hydroxy-3-isobornyl-5-methylbenzyl)amide were obtained from (+)- and (-)-enantiomers of 2-isobornyl-4-methylphenol. Evaluation of membrane protective and antioxidant activity of individual diastereomers on the model of H2O2-induced hemolysis of blood erythrocytes showed that the stereochemistry of isobornyl substituent in the synthesized conjugates has no effect on their biological activity.
