RESUMEN
BACKGROUND: We investigated both the efficacy and the sub-chronic toxicity of Tephrosia toxicariaâ Pers. in the zymosan-induced temporomandibular joint (TMJ) inflammatory hypernociception in rats evaluating the possible role of heme oxygenase-1 (HO-1). METHODS: Rats were pretreated with T. toxicaria (0.2, 2.0 or 20 mg/kg) 60 min before the intra-articular injection of zymosan (2 mg, 40 µL) in the left TMJ. In another series of experiments, rats were treated with ZnPP-IX (3 mg/kg), a specific HO-1 inhibitor, before T. toxicaria (20 mg/kg). Von Frey test was used to evaluate inflammatory hypernociception (g) 4 h after zymosan injection. Six hours after zymosan injection, the synovial lavage was collected for total cell count and myeloperoxidase (MPO) activity, and joint tissue for histopathological analysis and immunohistochemistry for HO-1. To evaluate the sub-chronic toxicity, mice received T. toxicaria (20 mg/kg) or saline once a day for 14 days to analyse body mass, organ weight and biochemical parameters. RESULTS: T. toxicaria partially reversed the zymosan-induced head withdrawal threshold, the number of cells and the MPO activity. T. toxicaria reduced the inflammatory cell influx in the synovial membrane. TMJ immunohistochemical analyses treated with T. toxicaria showed increased HO-1 expression. These effects of T. toxicaria were not observed in the presence of ZnPP-IX. T. toxicaria treatment for 14 days did not show significant signs of toxicity when administrated to mice. CONCLUSIONS: T. toxicaria did not produce any signs of toxicity and effectively decreased zymosan-induced TMJ inflammatory hypernociception dependent, at least in part, upon the HO-1 pathway integrity.
Asunto(s)
Hemo-Oxigenasa 1/metabolismo , Hiperalgesia/tratamiento farmacológico , Fitoterapia , Preparaciones de Plantas/farmacología , Trastornos de la Articulación Temporomandibular/tratamiento farmacológico , Tephrosia , Animales , Modelos Animales de Enfermedad , Inhibidores Enzimáticos/administración & dosificación , Inhibidores Enzimáticos/farmacología , Hemo-Oxigenasa 1/antagonistas & inhibidores , Hiperalgesia/inducido químicamente , Inflamación/inducido químicamente , Inflamación/tratamiento farmacológico , Masculino , Redes y Vías Metabólicas , Ratones , Preparaciones de Plantas/administración & dosificación , Preparaciones de Plantas/efectos adversos , Protoporfirinas/administración & dosificación , Protoporfirinas/farmacología , Ratas , Ratas Wistar , Trastornos de la Articulación Temporomandibular/inducido químicamente , Trastornos de la Articulación Temporomandibular/fisiopatología , Zimosan/farmacologíaRESUMEN
(1)H and (13)C NMR chemical shifts of praecansone B, pongaflavone and dehydrorotenone isolated from Tephrosia egregia Sandw and obovatin from T. toxicaria Pers. were unambiguously assigned by 1D and 2D NMR experiments including (1)H, (1)H COSY, gHMQC and gHMBC, allowing the correction of literature assignments.
Asunto(s)
Flavonas/química , Flavonoides/química , Protones , Tephrosia/química , Isótopos de Carbono , Flavonoides/aislamiento & purificación , Espectroscopía de Resonancia Magnética , Estructura Molecular , Estándares de Referencia , EstereoisomerismoRESUMEN
A atividade larvicida de quatro saponinas monodesmosídicas (1-4) isoladas de Pentaclethra macroloba e de uma saponina bidesmosídica (5) isolada de Cordia piauhiensis foi avaliada sobre larvas de estágio 3 de Aedes aegypti. As larvas foram expostas a várias concentrações (500, 250, 100, 50, 25 e 12,5 mg/mL) das saponinas por um período de 24 h. Os resultados indicam que somente as saponinas 1-3 mostraram alta atividade larvicida, com CL50 variando de 18,6 a 27,9 mg/mL. Estes resultados ressaltam as potencialidades destas saponinas como possíveis agentes larvicidas naturais.
The larvicidal activity of the four monodesmoside saponins (1-4) isolated from Pentaclethra macroloba and one bidesmoside saponin (5) from Cordia piauhiensis was evaluated on 3rd instar larvae of Aedes aegypti. The larvae were exposed to serial concentrations (500, 250, 100, 50, 25 and 12.5 mg/mL) saponins for a period of 24 h. The results indicate that, only the saponins 1-3 showed high larvicidal activity, with LC50 ranging of 18,6-27,9 mg/mL. These results suggest that these can be used as natural larvicidal agents.