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Mar Drugs ; 9(7): 1293-1306, 2011.
Artículo en Inglés | MEDLINE | ID: mdl-21822417

RESUMEN

Neorogioltriol is a tricyclic brominated diterpenoid isolated from the organic extract of the red algae Laurencia glandulifera. In the present study, the anti-inflammatory effects of neorogioltriol were evaluated both in vivo using carrageenan-induced paw edema and in vitro on lipopolysaccharide (LPS)-treated Raw264.7 macrophages. The in vivo study demonstrated that the administration of 1 mg/kg of neorogioltriol resulted in the significant reduction of carregeenan-induced rat edema. In vitro, our results show that neorogioltriol treatment decreased the luciferase activity in LPS-stimulated Raw264.7 cells, stably transfected with the NF-κB-dependent luciferase reporter. This effect on NF-κB activation is not mediated through MAPK pathways. The inhibition of NF-κB activity correlates with decreased levels of LPS-induced tumor necrosis factor-alpha (TNFα) present in neorogioltriol treated supernatant cell culture. Further analyses indicated that this product also significantly inhibited the release of nitric oxide and the expression of cyclooxygenase-2 (COX-2) in LPS-stimulated Raw264.7 cells. These latter effects could only be observed for neorogioltriol concentrations below 62.5 µM. To our knowledge, this is the first report describing a molecule derived from Laurencia glandulifera with anti-inflammatory activity both in vivo and in vitro. The effect demonstrated in vitro may be explained by the inhibition of the LPS-induced NF-κB activation and TNFα production. NO release and COX-2 expression may reinforce this effect.


Asunto(s)
Antiinflamatorios no Esteroideos/farmacología , Antiinflamatorios/farmacología , Diterpenos/farmacología , Edema/tratamiento farmacológico , Laurencia/química , Extractos Vegetales/farmacología , Animales , Antiinflamatorios/aislamiento & purificación , Antiinflamatorios/metabolismo , Antiinflamatorios/toxicidad , Antiinflamatorios no Esteroideos/aislamiento & purificación , Antiinflamatorios no Esteroideos/metabolismo , Antiinflamatorios no Esteroideos/toxicidad , Artritis/tratamiento farmacológico , Aspirina/farmacología , Supervivencia Celular/efectos de los fármacos , Grupos Control , Dexametasona/farmacología , Modelos Animales de Enfermedad , Diterpenos/aislamiento & purificación , Diterpenos/metabolismo , Diterpenos/toxicidad , Relación Dosis-Respuesta a Droga , Edema/inducido químicamente , Mediadores de Inflamación/antagonistas & inhibidores , Mediadores de Inflamación/fisiología , Lipopolisacáridos/metabolismo , Lipopolisacáridos/fisiología , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Ratones , Fitoterapia , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/metabolismo , Extractos Vegetales/toxicidad , Ratas , Factores de Tiempo
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