RESUMEN

<p><b>BACKGROUND</b>Xiaobuxin-Tang, a traditional Chinese herbal prescription recorded in a silk scroll unearthed from Mogao Caves of Dunhuang has been indicated that it can remit depressive disorder. The present study was designed to investigate its antidepressant effects in various animal depression models.</p><p><b>METHODS</b>Xiaobuxin-Tang was extracted by 70% alcohol, and then three behavioral despair models and 5-Hydroxytryptophan (HTP)-induced head twitch response model were adopted to assess the antidepressant effects of the ethanolic extract of Xiaobuxin-Tang with the study on spontaneous motor activity. Groups of mice and rats received oral treatment with Xiaobuxin-Tang (150 - 1200 mg/kg) only once acutely in all tests. The duration of immobility was measured during the last 4 minutes of the 6-minutes test period in mice forced swimming test, rats forced swimming test and mice tail suspension test. In 5-HTP-induced head twitch response, the mice were intraperitoneally administered with 120 mg/kg of L-5-HTP, and then the cumulative number of head twitches was counted in 20 minutes. Spontaneous motor activities of mice were recorded automatically in 10 minutes by VIDEOMEX-V image analytic system.</p><p><b>RESULTS</b>The extract at doses of 300 mg/kg (p.o.) and 600 mg/kg (p.o.) significantly decreased the duration of immobility time in a dose dependent manner in mice forced swimming test; also, the extract at dose of 1200 mg/kg (p.o.) significantly decreased the duration of immobility time in rat forced swimming test. Furthermore, the extract at a dose of 600 mg/kg had the same effect in mice tail suspension test. Meanwhile, the extract at the effective doses for behavioral despair models, had no effect on spontaneous motor activity in mice. The extract (300 - 1200 mg/kg, p.o.) also increased the accumulative number of the 5-HTP-induced head twitch response in mice in 20 minutes.</p><p><b>CONCLUSION</b>Our results suggested that the ethanolic extract of Xiaobuxin-Tang exerts antidepressant-like effect.</p>

Asunto(s)

Animales , Masculino , Ratones , Antidepresivos , Farmacología , Depresión , Quimioterapia , Modelos Animales de Enfermedad , Medicamentos Herbarios Chinos , Farmacología , Suspensión Trasera , Ratones Endogámicos ICR , Actividad Motora , Natación

RESUMEN

A series of mutual prodrugs derived from gabapentin, pregabalin, memantine, venlafaxine were synthesized and their pharmacological properties to treat neuropathic pain were investigated in a rat model of chronic sciatic nerve constriction injury (CCI). In vivo evaluation demonstrated that the mutual prodrugs 2002413A, 2002823A composed of two gabapentins, 2002414 composed of gabapentin and pregabalin were effective in reversal tactile allodynia in CCI rats. The prodrugs 2002413A, 2002414 had no significant influence on the rotarod activity. The result suggest that the prodrugs may be possible candidates for further development.

Asunto(s)

Aminas/síntesis química , Aminas/farmacología , Ácidos Ciclohexanocarboxílicos/síntesis química , Ácidos Ciclohexanocarboxílicos/farmacología , Neuropatía Ciática/tratamiento farmacológico , Ácido gamma-Aminobutírico/análogos & derivados , Ácido gamma-Aminobutírico/síntesis química , Ácido gamma-Aminobutírico/farmacología , Aminas/administración & dosificación , Animales , Enfermedad Crónica , Ácidos Ciclohexanocarboxílicos/administración & dosificación , Ciclohexanoles/administración & dosificación , Ciclohexanoles/síntesis química , Ciclohexanoles/farmacología , Modelos Animales de Enfermedad , Gabapentina , Memantina/administración & dosificación , Memantina/síntesis química , Memantina/farmacología , Dolor/tratamiento farmacológico , Umbral del Dolor/efectos de los fármacos , Pregabalina , Profármacos/síntesis química , Ratas , Relación Estructura-Actividad , Clorhidrato de Venlafaxina , Ácido gamma-Aminobutírico/administración & dosificación

RESUMEN

<p><b>OBJECTIVE</b>To study the possible mechanism of aqueous extract of detoxified cottonseeds (CTN-W).</p><p><b>METHOD AND RESULT</b>CTN-W 0.01, 0.03, 0.10, 0.30 mg.mL-1 was incubated directly with the synaptic membrane extracted from the cerebral cortex in rats, and adenylyl cyclase (AC) activity was detected by using radio-immunoassay.</p><p><b>RESULT</b>Showed that CTN-W could activate AC in a dose-dependend manner. After incubation with PC12 cells in the presence of corticosterone 2 x 10(-4)mol.L-1 for 48 h, CTN-W 0.08, 0.4, 2 mg.mL-1 protected PC12 cells from the lesion induced by corticosterone.</p><p><b>CONCLUSION</b>Antidepressant and anxiolytic effects of CTN-W are related with the activation of AC-cAMP pathway in signal transduction system, thus protecting neurons from the lesion. These two aspects maybe partly form the mechanism of CTN-W's action.</p>

Asunto(s)

Animales , Ratas , Adenilil Ciclasas , Metabolismo , Ansiolíticos , Farmacología , Antidepresivos , Farmacología , Corticosterona , Medicamentos Herbarios Chinos , Farmacología , Gossypium , Química , Fármacos Neuroprotectores , Farmacología , Células PC12 , Plantas Medicinales , Química , Ratas Wistar , Semillas , Química , Membranas Sinápticas