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1.
Metab Brain Dis ; 36(7): 2015-2027, 2021 10.
Artículo en Inglés | MEDLINE | ID: mdl-34460047

RESUMEN

A substantial number of epileptic patients are resistant to the current medication thus necessitating the search for alternative therapies for intractable forms of the disease. Previous studies demonstrated the acute anticonvulsant properties of the methanol extract of the stem bark of Psychotria camptopus (MEPC) in rats. This study investigated the effects of MEPC on pentylenetetrazole-kindled Wistar rats. Kindling was induced by intraperitoneal injection of pentylenetetrazole (37.5 mg/kg) on every alternate day, 1 h after each daily oral pretreatment of rats (8 ≤ n ≤ 10) with MEPC (40, 80 and 120 mg/kg), vehicle or diazepam (3 mg/kg) for 43 days. The kindling development was monitored based on seizure episodes and severity. Rats' brains were collected on day 43 for the determination of oxidative stress parameters. The histomorphological features and neuronal cell viability of the prefrontal cortex (PFC) and hippocampus were also assessed using H&E and Cresyl violet stains. Chronic administration of pentylenetetrazole time-dependently decreased the latency to myoclonic and generalized seizures, and increased seizure scores and the number of kindled rats. MEPC and diazepam significantly increased the latencies to myoclonic jerks and generalized tonic-clonic seizures. These substances also reduced seizure score and the number of rats with PTZ-kindling. MEPC improved glutathione status and decreased lipid peroxidation in the brains of kindled rats. MEPC also exhibited neuroprotection against pentylenetetrazole-induced hippocampal and PFC neuronal damages. These results suggest that P. camptopus has antiepileptogenic activity, which might be related to the augmentation of antioxidant and neuroprotective defense mechanisms, and further confirm its usefulness in the management of epilepsy.


Asunto(s)
Excitación Neurológica , Fármacos Neuroprotectores , Psychotria , Rubiaceae , Animales , Anticonvulsivantes/farmacología , Anticonvulsivantes/uso terapéutico , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , Humanos , Masculino , Metanol/farmacología , Fármacos Neuroprotectores/farmacología , Fármacos Neuroprotectores/uso terapéutico , Pentilenotetrazol/farmacología , Corteza de la Planta , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Ratas , Ratas Wistar
2.
J Ethnopharmacol ; 272: 113955, 2021 May 23.
Artículo en Inglés | MEDLINE | ID: mdl-33610704

RESUMEN

ETHNOPHARMACOLOGY RELEVANCE: The decoction from the stem bark of Psychotria camptopus (Rubiaceae) is used in the Cameroonian pharmacopoeia to treat neurological pathologies including epilepsy. AIM: The present work was undertaken to study the anticonvulsant properties of the aqueous (AE) and methanol (ME) extracts from the stem bark of P. camptopus in acute models of epileptic seizures in Wistar rats. METHOD: AE and ME were obtained by decoction and maceration of the stem bark powder in water and methanol, respectively. They were tested orally at the doses of 40, 80 and 120 mg/kg, on the latency of onset and duration of epileptic seizures induced by pentylene tetrazole (PTZ, 70 mg/kg, i.p.). The kinetic effect of both extracts at 120 mg/kg was evaluated. Their effects on diazepam (50 mg/kg) induced sleep and strychnine (STR, 2.5 mg/kg, i.p.) induced seizures were determined. ME was further tested on picrotoxin (PIC, 7.5 mg/kg, i.p.) and thiosemicarbazide (TSC, 50 mg/kg, i.p.) induced seizure models. The phytochemical composition of ME was assessed using LC-MS method, as well as its acute toxicity. RESULTS: AE and ME significantly (p < 0.001) reduced the duration of seizures in both PTZ and STR models. Their maximal effect was observed at 1 h after administration, though their effect at 120 mg/kg was maintained (p < 0.05) up to 24 h post-treatment. Both extracts significantly (p < 0.01) reduced sleep duration. ME significantly (p < 0.001) increased the latency of rat death on PIC-induced convulsions. In TSC rats, ME significantly (p < 0.001) delayed the latency to the first convulsion, and decreased the duration and frequency of convulsions. ME showed no acute toxicity while its phytochemical screening revealed the presence of two flavonoids (Rutin and Butin), two triterpenoid saponins (Psycotrianoside B and Bauerenone) and four alkaloids (10-Hydroxy-antirhine, 10-hydroxy-iso-deppeaninol, Emetine and Hodkinsine). In conclusion, AE and ME from the stem bark of P. camptopus have comparable anticonvulsant properties. The effect of ME is likely due to the presence of flavonoids and alkaloid and the activation of GABA pathway. These results further justify and support the use of P. camptopus in traditional medicine for the treatment of epilepsy.


Asunto(s)
Anticonvulsivantes/farmacología , Epilepsia/tratamiento farmacológico , Extractos Vegetales/farmacología , Psychotria/química , Convulsiones/tratamiento farmacológico , Animales , Anticonvulsivantes/uso terapéutico , Anticonvulsivantes/toxicidad , Conducta Animal/efectos de los fármacos , Diazepam/farmacología , Diazepam/uso terapéutico , Modelos Animales de Enfermedad , Epilepsia/inducido químicamente , Metanol/química , Ratones , Pentilenotetrazol/toxicidad , Fitoquímicos/química , Fitoquímicos/farmacología , Fitoquímicos/uso terapéutico , Picrotoxina/toxicidad , Corteza de la Planta/química , Extractos Vegetales/uso terapéutico , Extractos Vegetales/toxicidad , Tallos de la Planta/química , Ratas Wistar , Convulsiones/inducido químicamente , Semicarbacidas/toxicidad , Sueño/efectos de los fármacos , Latencia del Sueño/efectos de los fármacos , Estricnina/toxicidad , Agua/química
3.
Acta Crystallogr E Crystallogr Commun ; 71(Pt 7): o457-8, 2015 Jul 01.
Artículo en Inglés | MEDLINE | ID: mdl-26279906

RESUMEN

The title compound, C24H31NO3 {systematic name: (E)-3-[(1R*,2S*,4aS*,8aR*)-2-(benzo[d][1,3]dioxol-5-yl)-1,2,4a,5,6,7,8,8a-octa-hydro-naphthalen-1-yl]-N-iso-butyl-acryl-amide}, is a natural product isolated from the stem bark of B. obscura. It is composed of an octa-hydro-naphthalene ring system substituted with an essentially planar benzodioxole ring system [r.m.s. deviation = 0.012 Å] and an extended iso-butyl-acryl-amide group. In the crystal, mol-ecules are linked by N-H⋯O hydrogen bonds, forming chains propagating along [100]. The chains are linked by pairs of C-H⋯O hydrogen bonds, involving inversion-related benzodioxole ring systems, forming ribbons lying parallel to (010). There are also C-H⋯π inter-actions present within the ribbons.

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