RESUMO
BACKGROUND: Gabapentin is an anticonvulsant and adjuvant analgesic. It is effective in several pain studies. Neuropathic pain is the most difficult type of pain to treat. In this study, we examined if intrathecal gabapentin could prevent nerve injury-induced pain. METHODS: Under isoflurane anaesthesia, male Sprague-Dawley rats (200-250 g) underwent right L5/6 spinal nerve ligation and placement of an intrathecal catheter connected to an infusion pump. After surgery, intrathecal saline or gabapentin (20 µg h(-1)) was given for 7 days (n=8 per group). The right hind paw withdrawal threshold to von Frey filament stimuli and withdrawal latency to radiant heat were determined before (baseline) and once daily for 7 days after surgery. Haematoxylin and eosin and toluidine blue staining were used to evaluate the neurotoxicity of gabapentin (40 µg h(-1)). RESULTS: Seven days after nerve ligation, the affected paw withdrawal threshold and latency of saline-treated rats decreased from the baseline 11.7 (11.7-22.2) [median (inter-quartile range)] to 1.6 (0.9-3.2) g and 10.8 (10.5-11.2) to 4.3 (4.2-7) s, respectively. Rats receiving gabapentin (20 µg h(-1)) had higher withdrawal threshold [9.9 (9.9-19.3) g] and latency [11.5 (9.7-11.9) s] on day 7 after ligation. No obvious histopathological change or growth retardation was detected after intrathecal gabapentin (40 µg h(-1)) infusion. CONCLUSIONS: We showed a preventative effect of intrathecal gabapentin on the development of nerve injury-induced mechanical allodynia and thermal hyperalgesia. Our data suggest that continuous intrathecal gabapentin may be considered as an alternative for the prevention of nerve injury-induced pain.
Assuntos
Aminas/administração & dosagem , Analgésicos não Narcóticos/administração & dosagem , Ácidos Cicloexanocarboxílicos/administração & dosagem , Hiperalgesia/prevenção & controle , Ácido gama-Aminobutírico/administração & dosagem , Aminas/uso terapêutico , Analgésicos não Narcóticos/uso terapêutico , Animais , Cauda Equina/efeitos dos fármacos , Cauda Equina/patologia , Ácidos Cicloexanocarboxílicos/uso terapêutico , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Esquema de Medicação , Avaliação Pré-Clínica de Medicamentos/métodos , Gabapentina , Hiperalgesia/etiologia , Infusões Parenterais , Ligadura/efeitos adversos , Masculino , Medição da Dor/métodos , Desempenho Psicomotor/efeitos dos fármacos , Ratos , Ratos Sprague-Dawley , Medula Espinal/efeitos dos fármacos , Medula Espinal/patologia , Nervos Espinhais/lesões , Aumento de Peso/efeitos dos fármacos , Ácido gama-Aminobutírico/uso terapêuticoRESUMO
BACKGROUND: Magnesium sulphate (MgSO(4)) has potent anti-inflammatory capacity. It is a natural calcium antagonist and a potent L-type calcium channel inhibitor. We sought to elucidate the possible role of calcium, the L-type calcium channels, or both in mediating the anti-inflammatory effects of MgSO(4). METHODS: RAW264.7 cells, an immortalized murine macrophage-like cell line, were treated with phosphate buffered saline, MgSO(4), lipopolysaccharide (LPS), LPS plus MgSO(4), LPS plus MgSO(4) plus extra-cellular supplement with calcium chloride (CaCl(2)), or LPS plus MgSO(4) plus the L-type calcium channel activator BAY-K8644. After harvesting, the production of inflammatory molecules was evaluated. Because the production of endotoxin-induced inflammatory molecules is regulated by the crucial transcription factor nuclear factor (NF)-kappaB, we also evaluated the expression of NF-kappaB. RESULTS: LPS significantly induced the production of inflammatory molecules, including macrophage inflammatory protein-2, tumour necrosis factor-alpha, interleukin (IL)-1beta, IL-6, nitric oxide/inducible nitric oxide synthase, and prostaglandin E(2)/cyclo-oxygenase-2. LPS also induced NF-kappaB activation, as inhibitor-kappaB degradation, NF-kappaB nuclear translocation, and NF-kappaB-DNA binding activity were significantly increased in LPS-treated RAW264.7 cells. MgSO(4), in contrast, significantly inhibited the LPS-induced inflammatory molecules production and NF-kappaB activation. Moreover, the effects of MgSO(4) on inflammatory molecules and NF-kappaB were reversed by extra-cellular calcium supplement with CaCl(2) and L-type calcium channel activator BAY-K8644. CONCLUSIONS: MgSO(4) significantly inhibited endotoxin-induced up-regulation of inflammatory molecules and NF-kappaB activation in activated RAW264.7 cells. The effects of MgSO(4) on inflammatory molecules and NF-kappaB may involve antagonizing calcium, inhibiting the L-type calcium channels, or both.
Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Bloqueadores dos Canais de Cálcio/farmacologia , Canais de Cálcio Tipo L/efeitos dos fármacos , Sulfato de Magnésio/farmacologia , Animais , Linhagem Celular Transformada , Mediadores da Inflamação/metabolismo , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , NF-kappa B/metabolismo , RNA Mensageiro/genética , Regulação para Cima/efeitos dos fármacosRESUMO
The protective activity of melanin derived from tea (MDFT) was studied using hydrazine as a DNA-reactive chemical agent. Intra-peritoneal administration of MDFT at the doses of 5 or 20 mg/kg dose-dependently prevented liver toxicity induced by hydrazine in rats. It normalized rises in serum alanine transferase activity and a decrease in the glutathione level in the liver. It also reduced the hepatic malondialdehyde concentration. Monitoring the intensity of chemiluminescence showed that MDFT could prevent the production of free radicals that are generated owing to metabolic transformation of hydrazine. It also prevented the formation 8-hydroxy-deoxyguanosine (8-OH-dG) DNA adducts. The results obtained in vivo and in vitro suggest that MDFT confers marked protection of the liver against hydrazine-induced oxidative toxicity.
Assuntos
Antioxidantes/uso terapêutico , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Desoxiguanosina/análogos & derivados , Melaninas/uso terapêutico , Extratos Vegetais/uso terapêutico , Chá/química , 8-Hidroxi-2'-Desoxiguanosina , Alanina Transaminase/sangue , Animais , Antioxidantes/administração & dosagem , Antioxidantes/isolamento & purificação , Doença Hepática Induzida por Substâncias e Drogas/sangue , Doença Hepática Induzida por Substâncias e Drogas/patologia , Adutos de DNA/efeitos dos fármacos , Dano ao DNA , Desoxiguanosina/metabolismo , Relação Dose-Resposta a Droga , Radicais Livres/metabolismo , Glutationa/metabolismo , Hidrazinas/toxicidade , Injeções Intraperitoneais , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Malondialdeído/metabolismo , Melaninas/administração & dosagem , Melaninas/isolamento & purificação , Extratos Vegetais/administração & dosagem , Extratos Vegetais/isolamento & purificação , Ratos , Ratos WistarRESUMO
Some chemical and physical properties of bambara groundnut seed were determined. The proximate composition of the bambara groundnut seed was found to be 9.7% moisture, 16.6% protein, 5.9% fat, 2.9% ash, 4.9% crude fibre and 64.9% carbohydrate. Maximum water absorption was attained after soaking for 11, 9, 6, and 4 h at 25, 40, 50, and 60 degrees C, respectively. Maximum dehulling efficiency was attained when the seeds absorbed 54.7% water and drying for 9 h at 60 degrees C. Study of the microstructure of the raw flour and seed showed that they contained differently shaped and sized starch granules and protein materials within the cell wall in the cotyledon. Milling disorganised the arrangement of these components in the cotyledons. In the steamed moin-moin ('okpa'), all components in the seed had lost their identity and integrity.
Assuntos
Fabaceae/química , Manipulação de Alimentos/métodos , Plantas Medicinais , Sementes/química , Carboidratos da Dieta/análise , Gorduras na Dieta/análise , Fibras na Dieta/análise , Proteínas Alimentares/análise , Análise de Alimentos , Nigéria , Sementes/ultraestruturaRESUMO
Phytochemical analysis of the fruits of Annona squamosa yielded 12 known kaurane derivatives (1-11, 13) and two new kaurane diterpenoids, which have been named annosquamosin A (16 beta-hydroxy-17-acetoxy-ent-kauran-19-al) (12) and annosquamosin B (19-nor-ent-kaurane-4 alpha,16 beta,-17-triol) (14). The structures of the new compounds were established by spectral analyses and chemical evidence. Among these 14 compounds, 16 beta, 17-dihydroxy-ent-kauran-19-oic acid (2) showed significant activity against HIV replication in H9 lymphocyte cells with an EC50 value of 0.8 microgram/mL (therapeutic index > 5).
Assuntos
Antivirais/isolamento & purificação , Diterpenos do Tipo Caurano , Diterpenos/isolamento & purificação , HIV-1/efeitos dos fármacos , Plantas Medicinais/química , Antivirais/farmacologia , Diterpenos/farmacologia , Humanos , Linfócitos/virologia , Espectroscopia de Ressonância Magnética , Replicação Viral/efeitos dos fármacosRESUMO
The treatment effect of "ryu-wei-ti-huang-wan', a Chinese prescription composed of extracts from six plants, on diabetic impotence was evaluated in the present study. Adult male Wistar rats were divided into three groups: (1) rats rendered diabetic with a single intraperitoneal injection of streptozotocin (60 mg/kg body weight); (2) rats with streptozotocin-induced diabetes treated with a ryu-wei-ti-huang-wan powder preparation at a dose of 30 mg powder/kg body weight twice a day, and (3) control rats. A male rat was caged with an adult ovariectomized female rat during the dark cycle. Infra-red-light-illuminated video recording was utilized to evaluate the sexual performance. The diabetic rats exhibited depressed mounting activity and no intromission or ejaculation. After ryu-wei-ti-huang-wan treatment either for 1 day or 2 weeks, the diabetic rats showed significant improvement in mounting performance with preservation of intromission and ejaculation. No significant difference in the blood sugar level was noted between the treatment and non-treatment groups. In conclusion, the diabetic rats showed impairment in sexual arousal, erectile as well as ejaculatory functions. Ryu-wei-ti-huang-wan was effective in preserving these functions with a rapid onset. It is evident that the extracts exert the therapeutic effects not through a lowering of blood sugar. These substances are potentially useful in the clinical treatment of male diabetic impotence.
Assuntos
Diabetes Mellitus Experimental/complicações , Medicamentos de Ervas Chinesas/uso terapêutico , Disfunção Erétil/tratamento farmacológico , Animais , Medicamentos de Ervas Chinesas/efeitos adversos , Disfunção Erétil/etiologia , Masculino , Ratos , Ratos Wistar , Comportamento Sexual Animal/efeitos dos fármacos , EstreptozocinaRESUMO
Heat-pasteurized cassava root, cowpeas, partially defatted peanuts, rice and soybeans were evaluated for their suitability to support growth and sporulation of the tempeh mold, Rhizopus microsporus var. oligosporus, and the oncom mold, Neurospora intermedia, at 25, 30 and 37 degrees C. The molds grew best and sporulated most luxuriantly on cassava and rice incubated at 37 degrees C. Viability of molds remained high for up to 30 weeks when dried (a(w) 0.48), powdered substrates on which the molds had been cultured, were stored at 5, 25 and 37 degrees C. Survival was best when powders were stored at 5 degrees C, although storage at 25 degrees C did not cause a marked decline in CFU/g. R. microsporus var. oligosporus starter cultures produced on rice and then stored for 20 weeks at these temperatures compared most favorably with commercial starter cultures for preparing high-quality soybean tempeh. The simple technology required to prepare these starter cultures enhances the potential for their application in developing countries where the introduction of nontraditional fermented legume foods to low-protein diets could help to ameliorate malnutrition.