Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 2 de 2
Filtrar
Más filtros

Bases de datos
Tipo del documento
País de afiliación
Intervalo de año de publicación
1.
Sci Rep ; 11(1): 24121, 2021 12 16.
Artículo en Inglés | MEDLINE | ID: mdl-34916536

RESUMEN

A novel synthetic compound from the 2-benzoyl-6-benzylidenecyclohexanone analogue, namely 2-benzoyl-6-(3-bromo-4-hydroxybenzylidene)cyclohexen-1-ol (BBHC), showed pronounced nitric oxide inhibition in IFN-γ/LPS-induced RAW 264.7 cells. Based on this previous finding, our present study aimed to investigate the antinociceptive effects of BBHC via chemical and thermal stimuli in vivo. The investigation of the antinociceptive activity of BBHC (0.1, 0.3, 1.0 and 3.0 mg/kg, i.p.) was initiated with 3 preliminary screening tests, then BBHC was subjected to investigate its possible involvement with excitatory neurotransmitters and opioid receptors. The potential acute toxicity of BBHC administration was also studied. Administration of BBHC significantly inhibited acetic acid-induced abdominal constrictions, formalin-induced paw licking activity and developed notable increment in the latency time. BBHC's ability to suppress capsaicin- and glutamate-induced paw licking activities, as well as to antagonise the effect of naloxone, had indicated the possible involvement of its antinociception with TRPV1, glutamate and opioid receptors, respectively. The antinociceptive activities of BBHC was not related to any sedative action and no evidence of acute toxic effect was detected. The present study showed that BBHC possessed significant peripheral and central antinociceptive activities via chemical- and thermal-induced nociceptive murine models without any locomotor alteration and acute toxicity.


Asunto(s)
Analgésicos , Dolor/tratamiento farmacológico , Analgésicos/farmacología , Analgésicos/uso terapéutico , Animales , Compuestos de Bencilo/farmacología , Compuestos de Bencilo/uso terapéutico , Compuestos de Bromina/farmacología , Compuestos de Bromina/uso terapéutico , Modelos Animales de Enfermedad , Evaluación Preclínica de Medicamentos/métodos , Glutamatos , Masculino , Ratones , Ratones Endogámicos ICR , Neurotransmisores , Óxido Nítrico/antagonistas & inhibidores , Células RAW 264.7 , Receptores Opioides , Canales Catiónicos TRPV
2.
Molecules ; 23(9)2018 Aug 21.
Artículo en Inglés | MEDLINE | ID: mdl-30134576

RESUMEN

Curcuminoids derived from turmeric rhizome have been reported to exhibit antinociceptive, antioxidant and anti-inflammatory activities. We evaluated the peripheral and central antinociceptive activities of 5-(3,4-dihydroxyphenyl)-3-hydroxy-1-(2-hydroxyphenyl)penta-2,4-dien-1-one (DHHPD), a novel synthetic curcuminoid analogue at 0.1, 0.3, 1 and 3 mg/kg (intraperitoneal), through chemical and thermal models of nociception. The effects of DHHPD on the vanilloid and glutamatergic systems were evaluated through the capsaicin- and glutamate-induced paw licking tests. Results showed that DHHPD significantly (p < 0.05) attenuated the writhing response produced by the 0.8% acetic acid injection. In addition, 1 and 3 mg/kg of DHHPD significantly (p < 0.05) reduced the licking time spent by each mouse in both phases of the 2.5% formalin test and increased the response latency of mice on the hot-plate. However, the effect produced in the latter was not reversed by naloxone, a non-selective opioid receptor antagonist. Despite this, DHHPD decreased the licking latency of mice in the capsaicin- and glutamate-induced paw licking tests in a dose response manner. In conclusion, DHHPD showed excellent peripheral and central antinociceptive activities possibly by attenuation of the synthesis and/or release of pro-inflammatory mediators in addition to modulation of the vanilloid and glutamatergic systems without an apparent effect on the opioidergic system.


Asunto(s)
Analgésicos/química , Analgésicos/farmacología , Nocicepción/efectos de los fármacos , Dolor Nociceptivo/tratamiento farmacológico , Animales , Conducta Animal/efectos de los fármacos , Modelos Animales de Enfermedad , Masculino , Ratones , Estructura Molecular , Actividad Motora/efectos de los fármacos , Dolor Nociceptivo/etiología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Prueba de Desempeño de Rotación con Aceleración Constante
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA