RESUMO
The effects of α-asarone in four assays predictive of anxiolytic activity in male mice were studied, with diazepam as a positive anxiolytic control. The use of the elevated plus-maze test revealed that diazepam (2 mg/kg) or α-asarone (3.5 mg/kg) increased the percentage of entries into open arms and of the time spent on open arms. In the light/dark transition test, as with 2 mg/kg diazepam, 7 mg/kg α-asarone increased the time spent in the light area and the number of transitions between the two compartments. In the novel food consumption test, α-asarone (3.5, 7 and 14 mg/kg) caused significant increases in food intake during 5 min as well as diazepam (0.5 mg/kg). In the marble burying test, α-asarone also produced a significant inhibition of marble burying at doses of 14 and 28 mg/kg, as did diazepam (5 mg/kg). Thus, these findings indicated that α-asarone exhibited an anxiolytic-like effect. Further studies will be required to assess the generality of the present findings to other species and behavioral paradigms.
Assuntos
Anisóis/farmacologia , Ansiolíticos/farmacologia , Ansiedade/tratamento farmacológico , Comportamento Animal/efeitos dos fármacos , Derivados de Alilbenzenos , Animais , Diazepam/farmacologia , Ingestão de Alimentos/efeitos dos fármacos , Masculino , Aprendizagem em Labirinto/efeitos dos fármacos , CamundongosRESUMO
OBJECTIVE: To prepare coated micro-pellets of pH-dependent and enzyme-dependent kangfuxin colon targeting delivery system, to make them go to colon, then release, educe partial effect. METHOD: We eploy pan-pill to prepare simple pellets, and prepare tunicatus pellets with fluidized bed coating. We investigated the preparation and parameter of pellets, so, we bolting the best shaping and tunicatus artwork. RESULT: The ingredients for preparing the micro-pellets are 125% starch +2% CMC-Na, and add 30% ethanol to be binder, pellets were coated with Eudragit S100 to prepare ph-dependent and pectin-HPMC to prepare enzyme-dependent colon targeting micro-pellets. CONCLUSION: We get two micro-pellets of pH-dependent and enzyme-dependent kangfuxin colon targeting.
Assuntos
Colo/metabolismo , Materia Medica/administração & dosagem , Periplaneta , Animais , Preparações de Ação Retardada , Portadores de Fármacos , Composição de Medicamentos/métodos , Sistemas de Liberação de Medicamentos , Concentração de Íons de Hidrogênio , Derivados da Hipromelose , Materia Medica/isolamento & purificação , Materia Medica/metabolismo , Metilcelulose/análogos & derivados , Pectinas , Periplaneta/química , Ácidos PolimetacrílicosRESUMO
OBJECTIVE: To evaluate the release in fixed position of pH-dependent and enzyme-dependent Kangfuxin colon targeting capsules in vivo and in vitro. METHOD: The dissolution was tested in vitro and X-ray radiography was used for the evaluation in vivo. RESULT: After two hours pH-dependent colon targeting in man-made colon fluid, medicine release in fixed position on the whole, colon loc-release. Add enzyme into man-made colon, when enzyme-dependent colon targeting in it, then medicine release quickly, mainly release in fixed position; The conveying time in vivo of pH-dependent and enzyme-dependent capsules have big individuality difference. In the experiment, disintegration is stabilize among individuales, between 2.0-3.5 hours. CONCLUSION: Kangfuxin colon targeting capsules of two principles all release in fixed position to achieve the goal.
Assuntos
Colo/metabolismo , Sistemas de Liberação de Medicamentos , Materia Medica/farmacocinética , Animais , Cápsulas , Colo/diagnóstico por imagem , Preparações de Ação Retardada/química , Portadores de Fármacos , Feminino , Humanos , Concentração de Íons de Hidrogênio , Masculino , Materia Medica/administração & dosagem , Materia Medica/isolamento & purificação , Periplaneta/química , Poligalacturonase/química , RadiografiaRESUMO
In our previous studies, we have demonstrated the anxiolytic effects of angelica essential oil in three anxiety models using mice. This study aimed to characterize the similar behavior effects of angelica essential oil in the social interaction test of anxiety and the hole-board test of exploration and locomotor activity in rats. These results indicate that angelica essential oil possessed a wide range of anxiolytic properties. In the social interaction test, angelica essential oil decreased aggressive behaviors at the doses of 21 and 42 mg/kg, while the doses of 21 and 42 mg/kg significantly increased social interaction time of the high light, unfamiliar test condition and 21 mg/kg could also prolong social interaction time of the high light, familiar test condition. In the hole-board test, angelica essential oil at 10.5 mg/kg significantly increased head-dipping counts and duration. Thus, our findings suggest the potential usefulness of angelica essential oil against various types of anxiety-related disorders and social failure.
Assuntos
Angelica/química , Comportamento Animal/efeitos dos fármacos , Óleos Voláteis/farmacologia , Agressão/efeitos dos fármacos , Animais , Ansiolíticos/farmacologia , Diazepam/farmacologia , Relação Dose-Resposta a Droga , Masculino , Extratos Vegetais/farmacologia , Ratos , Ratos Wistar , Fatores de TempoRESUMO
The effects of angelica essential oil in three assays predictive of anxiolytic activity in male mice were studied, with diazepam as a positive anxiolytic control. In the elevated plus-maze test, compared to the positive control diazepam, angelica essential oil (30.0 mg/kg, PO) had a modest anxiolytic-like effect (increased the percentage of open-arm time and reduced the percent protected head dips). In the light/dark test, angelica essential oil (30.0 mg/kg) prolonged the time spent in the light area without altering the locomotor activity of the animals. In the stress-induced hyperthermia test, 60 and 70 min after drug administration, rectal temperature was measured twice, angelica essential oil at the dose of 30.0 mg/kg inhibited stress-induced hyperthermia. Thus, these findings indicate that angelica essential oil, as does diazepam, exhibits an anxiolytic-like effect. Further studies will be required to assess the generality of the present findings to other species and behavioural paradigms.
Assuntos
Angelica sinensis , Ansiolíticos/uso terapêutico , Ansiedade/tratamento farmacológico , Medicamentos de Ervas Chinesas/uso terapêutico , Fitoterapia , Óleos de Plantas/uso terapêutico , Animais , Ansiedade/etiologia , Escuridão , Diazepam/uso terapêutico , Modelos Animais de Doenças , Febre/tratamento farmacológico , Febre/etiologia , Luz , Masculino , Aprendizagem em Labirinto/efeitos dos fármacos , Camundongos , Estresse Fisiológico/complicaçõesRESUMO
AIM: To investigate whether total Panax notoginseng saponins (PNS) could protect endothelium of rabbit iliac artery against balloon endothelial denudation (BED) injury. METHODS: The morphology changes of the endothelium were observed with scanning electron microscope (SEM) and hematoxylin and eosin stain after BED of rabbit iliac artery at 0, 4, 6, and 8 week respectively. Vascular endothelial growth factor (VEGF) and matrix metalloproteinase-2 (MMP-2) was also determined by immunohistochemistry. PNS 10, 30, and 50 mg/kg were administered iv per day from 2 d before to 4 weeks after operation. RESULTS: The endothelium was denudated completely after BED. At the 4th week the endothelium was repaired in some degree, then recovered gradually at 6 and 8 week. The degree of intimal thickening at 4 week was significantly greater than that at 0, 6, or 8 week. The sequence of VEGF or MMP-2 staining from strong to weak was 4, 6, 0, 8 week, and normal control. However at 4 week, endothelial regeneration in PNS 30 and 50 mg/kg groups was significantly faster than that in saline group. The intimal thickness was significantly decreased and expressions of VEGF and MMP-2 were both down-regulated in PNS 30 or 50 mg/kg groups compared with saline control group. CONCLUSION: PNS promoted the endothelial regeneration and reduced ECM thickening, which was related to regulation of the expression of VEGF and MMP-2. PNS may have sustained antirestenotic effect after BED.
Assuntos
Cateterismo/efeitos adversos , Ginsenosídeos/farmacologia , Artéria Ilíaca/ultraestrutura , Panax , Substâncias Protetoras/farmacologia , Fator A de Crescimento do Endotélio Vascular/biossíntese , Animais , Regulação para Baixo , Endotélio Vascular/metabolismo , Endotélio Vascular/ultraestrutura , Ginsenosídeos/isolamento & purificação , Artéria Ilíaca/lesões , Artéria Ilíaca/metabolismo , Masculino , Metaloproteinase 2 da Matriz/biossíntese , Metaloproteinase 2 da Matriz/genética , Panax/química , Plantas Medicinais/química , Coelhos , Fator A de Crescimento do Endotélio Vascular/genéticaRESUMO
The putative anxiolytic activity of succinic acid was examined in male mice by using a number of experimental paradigms of anxiety and compared with that of the known anxiolytic compound diazepam. Use of the elevated plus-maze test revealed that diazepam (1.0, 2.0 and 4.0 mg/kg, PO) or succinic acid (3.0 or 6.0 mg/kg, PO) increased the percentage of entries into open arms and of time spent on open arms. In novel food consumption test, succinic acid (3.0, 6.0, and 12.0 mg/kg, IP) caused significant increases in food intake during 5 min when compared with the vehicle. In the stress-induced hyperthermia test, 40 min after drug administration rectal temperature was measured, succinic acid at dose of 1.5 mg/kg, inhibited stress-induced hyperthermia. Thus, these findings indicated that, in contrast with diazepam, succinic acid exhibits anxiolytic-like effect.
Assuntos
Ansiolíticos/farmacologia , Ansiedade/prevenção & controle , Comportamento Animal/efeitos dos fármacos , Ácido Succínico/farmacologia , Animais , Temperatura Corporal/efeitos dos fármacos , Diazepam/farmacologia , Relação Dose-Resposta a Droga , Ingestão de Alimentos/efeitos dos fármacos , Hipertermia Induzida , Masculino , Aprendizagem em Labirinto/efeitos dos fármacos , CamundongosRESUMO
OBJECTIVE: To investigate the anti-emetic effect of ethanol extract from "WuZhuYu broth" and its mechanism. METHOD: Three experiments were carried out test which extract has anti-emetic activity, such as CuSO4-induced pigeon's emetic response, gastric emptying in mice and ACh-induced or 5-HT-induced contraction in vitro gastric muscle in rats. Meanwhile, effect of anti-emetic extract on concentration-response curve to ACh, 5-HT, histamine was investigated. RESULT: 50% ethanol extract and 70% ethanol extract were identified as having significantly stronger anti-emetic activities with little side effect, which showed the significant effect on concentration-response curve to ACh, 5-HT, histamine. CONCLUSION: 50% ethanol extract and 70% ethanol extract contain more anti-emetic fractions, more anti-emetic fractions can be gained at the concentrations of 50% and 70% ethanol; the mechanism of anti-emetic effect is related to its antagonism to the receptors of ACh, 5-HT, histamine.