RESUMEN
Chronic pain is a continuous or recurring pain which exceeds the normal course of recovery to an injury or disease. According to the origin of the chronic pain, it can be classified as inflammatory or neuropathic. This study aimed to evaluate the antinociceptive and anti-inflammatory effect of (-)-α-bisabolol (BIS) alone and complexed with ß-cyclodextrin (ßCD) in preclinical models of chronic pain. Chronic pain was induced by Freund's Complete Adjuvant (FCA) or partial lesion of the sciatic nerve (PLSN). Swiss mice were treated with BIS, BIS-ßCD (50â¯mg/kg, p.o) or vehicle (control) and mechanical hyperalgesia, thermal hyperalgesia, muscle strength and motor coordination were evaluated. In addition, levels of TNF-α and IL-10 and expression of the ionized calcium-binding adapter protein (IBA-1) were assessed in the spinal cord of the mice. The complexation efficiency of BIS in ßCD was evaluated by High-Performance Liquid Chromatography. BIS and BIS-ßCD reduced (pâ¯<â¯0.001) mechanical and thermal hyperalgesia. No alterations were found in force and motor coordination. In addition, BIS and BIS-ßCD inhibited (pâ¯<â¯0.05) TNF-α production in the spinal cord and stimulated (pâ¯<â¯0.05) the release of IL-10 in the spinal cord in PLSN-mice. Further, BIS and BIS-ßCD reduced IBA-1 immunostaining. Therefore, BIS and BIS-ßCD attenuated hyperalgesia, deregulated cytokine release and inhibited IBA-1 expression in the spinal cord in the PLSN model. Moreover, our results show that the complexation of BIS in ßCD reduced the therapeutic dose of BIS. We conclude that BIS is a promising molecule for the treatment of chronic pain.
Asunto(s)
Citocinas/metabolismo , Gliosis/tratamiento farmacológico , Hiperalgesia/inducido químicamente , Inflamación/tratamiento farmacológico , Sesquiterpenos Monocíclicos/uso terapéutico , Neuralgia/tratamiento farmacológico , beta-Ciclodextrinas/uso terapéutico , Animales , Proteínas de Unión al Calcio/biosíntesis , Adyuvante de Freund , Calor , Hiperalgesia/metabolismo , Inflamación/metabolismo , Masculino , Ratones , Proteínas de Microfilamentos/biosíntesis , Fuerza Muscular/efectos de los fármacos , Neuralgia/inducido químicamente , Neuralgia/metabolismo , Desempeño Psicomotor/efectos de los fármacos , Neuropatía Ciática/tratamiento farmacológico , Médula Espinal/metabolismo , EstereoisomerismoRESUMEN
Ocimum basilicum L. is an aromatic herb used in Brazil to treat illnesses such as respiratory and rheumatic problems, vomiting, and pain. In the present study, the chemical composition, acute toxicity, and antinociceptive effects of the essential oil (EO) of the cultivar "Maria Bonita" obtained from O. basilicum L. PI 197442 genotype were evaluated in Swiss mice (20-35 g each). Lethal dose to cause 50 % death (LD50) was calculated from a dose-response curve (100-5000 mg/kg body wt.; n = 6) as 532 mg/kg body wt. In the acetic acid-induced writhing test (0.6 % i. p.), EO (50, 100, and 200 mg/kg body wt., n = 8, s. c.) was effective in reducing the abdominal contractions at all doses (48-78 %). In the hot-plate test, EO significantly increased the latency at 50 mg/kg body wt. at all times (37-52 %, n = 8, s. c.). However, the effects of morphine and EO at 50 mg/kg were reverted in the presence of naloxone, an opioid antagonist. In the formalin test, EO significantly reduced paw licking time in the first and second phases of pain at 200 mg/kg body wt. (38 and 75 %, respectively, n = 8, s. c.). The results suggested that the peripheral and central antinociceptive effects of EO are related to the inhibition of the biosynthesis of pain mediators, such as prostaglandins and prostacyclins, and its ability to interact with opioid receptors.
Asunto(s)
Analgésicos/farmacología , Ocimum basilicum/química , Aceites Volátiles/química , Aceites Volátiles/farmacología , Analgésicos/química , Analgésicos/toxicidad , Analgésicos Opioides/farmacología , Animales , Brasil , Femenino , Dosificación Letal Mediana , Masculino , Ratones , Morfina/farmacología , Naloxona/farmacología , Antagonistas de Narcóticos/farmacología , Nociceptores/metabolismo , Aceites Volátiles/toxicidad , Dolor/tratamiento farmacológico , Dimensión del Dolor/efectos de los fármacos , Hojas de la Planta/química , Plantas Medicinales/químicaRESUMEN
Cladonia clathrata Ahti & L. Xavier-Filho (Cladoniaceae) is a lichen; several Cladonia species extracts have been used for various remedies in folk medicine. In order to evaluate the actions of this lichen, studies were performed on antinociceptive, anti-inflammatory, and antioxidant activities. The hydroalcoholic extract (HE) of C. clathrata stems was used in the following experiments. Oral treatment with the HE of C. clathrata elicited inhibitory activity (p < 0.001) on acetic acid-induced abdominal writhes at 100 (47.2%), 200 (47.2%), and 400 mg/kg (86.4%), and reduced the formalin-induced nociception on both the neurogenic (400 mg/kg, p < 0.01) and inflammatory phases (200 and 400 mg/kg, p < 0.01). It was not associated with non-specific effects, such as muscle relaxation or sedation. The HE reduced the carrageenan-induced edema formation at 100, 200, and 400 mg/kg (p < 0.05) and inhibited neutrophil migration into the peritoneal cavity at 400 mg/kg (p < 0.001). The HE of C. clathrata reacted with the DPPH radical and reduced the same by 50.19%, and exhibited an IC(50) value of 69.25 +/- 0.65 mug/mL. The HE of C. clathrata stems shows antinociceptive and anti-inflammatory activities, with a moderate antioxidant potential.
Asunto(s)
Analgésicos/farmacología , Antiinflamatorios/farmacología , Antioxidantes/farmacología , Ascomicetos , Líquenes , Analgésicos/química , Animales , Antiinflamatorios/química , Antioxidantes/química , Benzofuranos/metabolismo , Compuestos de Bifenilo/metabolismo , Carragenina , Evaluación Preclínica de Medicamentos , Ratones , Actividad Motora/efectos de los fármacos , Infiltración Neutrófila/efectos de los fármacos , Dimensión del Dolor , Picratos/metabolismo , Ratas , Ratas WistarRESUMEN
OBJECTIVES: This study has investigated the cardiovascular effects of the Cymbopogon winterianus essential oil (EOCW) in rats. C. winterianus is a plant used in folk medicine for the treatment of hypertension. METHODS: For the measurement of haemodynamic and ECG parameters, male Wistar rats under anaesthesia were cannulated in the abdominal aorta and lower vena cava and electrodes were subcutaneously implanted in their paws. For an in-vitro approach, the rats were killed and the superior mesenteric artery was removed and cut into rings (1-2 mm). These rings were then mounted in organ baths containing Tyrode's solution at 37 degrees C and gassed with carbogen. KEY FINDINGS: In rats, EOCW (1-20 mg/kg, i.v.) induced dose-dependent hypotension and tachycardia. These effects were not affected by L-NAME or indometacin, but were partially reduced after atropine administration. EOCW (20 mg/kg only) also induced bradycardia-associated sinoatrial blockade, junctional rhythm, and first-degree atrioventricular block, which was abolished after atropine administration or vagotomy. In arterial rings, EOCW (0.1-3000 microg/ml) induced relaxation of phenylephrine tonus that was not affected by removal of the endothelium. These relaxations were similar to those observed in rings without endothelium precontracted with KCl 80 mm. EOCW was able to antagonize the CaCl(2) (30-300 mum) induced contractions in depolarizing solution (KCl 60 mm). CONCLUSIONS: These results demonstrated that EOCW induced hypotension and vasorelaxation. These effects appeared to be mainly mediated by Ca(+2)-channel blocking. Furthermore, the higher dose of EOCW induced transient bradycardia and arrhythmias due to a cardiac muscarinic activation secondary to a vagal discharge.
Asunto(s)
Canales de Calcio/metabolismo , Cymbopogon/química , Corazón/efectos de los fármacos , Hemodinámica/efectos de los fármacos , Aceites Volátiles/farmacología , Nervio Vago/efectos de los fármacos , Animales , Presión Sanguínea/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Electroencefalografía , Corazón/inervación , Corazón/fisiología , Frecuencia Cardíaca/efectos de los fármacos , Técnicas In Vitro , Contracción Isotónica/efectos de los fármacos , Masculino , Arteria Mesentérica Superior/efectos de los fármacos , Músculo Liso Vascular/efectos de los fármacos , Aceites Volátiles/aislamiento & purificación , Ratas , Ratas Wistar , Vagotomía , Nervio Vago/fisiología , Vasodilatación/efectos de los fármacosRESUMEN
PURPOSE: This study was carried out to assess the effects of the aqueous extract of Hyptis pectinata leaves on liver regeneration and on serum enzymes (AST, ALT and gamma-GT) after 67% partial hepatectomy in rats. METHODS: AST, ALT and gamma-GT, were determined by conventional procedures using a spectrophotometer (Model E2250-CELM). Liver regeneration was evaluated by immunohistochemical staining for proliferating cell nuclear antigen (PCNA). RESULTS: Oral pretreatment during 4 days at 100 mg/kg increased liver regeneration index. At 200 mg/kg, AST level was statistically decreased in comparison to the group submitted to distilled water administration. The other enzymes assessed disclosed no difference when all groups were compared. CONCLUSION: The present study shows that the aqueous extract of Hyptis pectinata leaves contains some biological active principles that stimulate liver regeneration at 100 mg/kg and cause slight hepatic protection at 200 mg/kg.
Asunto(s)
Hyptis , Regeneración Hepática/efectos de los fármacos , Fitoterapia , Hojas de la Planta , Preparaciones de Plantas/uso terapéutico , Animales , Modelos Animales de Enfermedad , Hepatectomía , Masculino , Extractos Vegetales/uso terapéutico , Antígeno Nuclear de Célula en Proliferación , Ratas , Ratas Wistar , Espectrofotometría , Estadísticas no Paramétricas , Transaminasas/sangre , gamma-Glutamiltransferasa/sangreRESUMEN
PURPOSE: The use of medicinal plants for the treatment of human diseases has increased worldwide. Many of them are used by oral administration and, after absorption, may affect many organs. Therefore, this study aimed at assessing the effects of the aqueous extract of Sida cordifolia leaves, popularly known in Brazil as "malva-branca", on liver regeneration. METHODS: Twenty rats were divided into four groups: control, Sida100, Sida200 and Sida400 groups. All animals were submitted to oral administration of distilled water, 100, 200 and 400 mg/kg of the aqueous extract of Sida cordifolia, respectively. Immediately after this, they underwent 67% partial hepatectomy. Twenty four hours later, their livers were removed. Hepatic regeneration was assessed by immunohistochemical staining for proliferating cell nuclear antigen (PCNA) using the PC-10 monoclonal antibody. RESULTS: Sida100 and Sida200 groups disclosed higher liver regeneration indices than control group (p<0.001 and p<0.05, respectively). CONCLUSION: The aqueous extract of Sida cordifolia stimulates liver regeneration after 67% partial hepatectomy in rats.
Asunto(s)
Regeneración Hepática/efectos de los fármacos , Malvaceae , Fitoterapia , Hojas de la Planta , Preparaciones de Plantas/uso terapéutico , Animales , Modelos Animales de Enfermedad , Hepatectomía , Masculino , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Preparaciones de Plantas/farmacología , Antígeno Nuclear de Célula en Proliferación , Ratas , Ratas Wistar , Estadísticas no ParamétricasRESUMEN
PURPOSE: This study was carried out to assess the effects of the aqueous extract of Hyptis pectinata leaves on liver regeneration and on serum enzymes (AST, ALT and gamma-GT) after 67 percent partial hepatectomy in rats. METHODS: AST, ALT and gamma-GT, were determined by conventional procedures using a spectrophotometer (Model E2250-CELM). Liver regeneration was evaluated by immunohistochemical staining for proliferating cell nuclear antigen (PCNA). RESULTS:Oral pretreatment during 4 days at 100 mg/kg increased liver regeneration index. At 200 mg/kg, AST level was statistically decreased in comparison to the group submited to distilled water administration. The other enzymes assessed disclosed no difference when all groups were compared. CONCLUSION: The present study shows that the aqueous extract of Hyptis pectinata leaves contains some biological active principles that stimulate liver regeneration at 100 mg/kg and cause slight hepatic protection at 200 mg/kg.
OBJETIVO: Este estudo foi realizado com o objetivo de verificar o efeito do extrato aquoso da Hyptis pectinata na regeneração hepática bem como nos níveis das enzimas séricas (AST, ALT e gama-GT) após hepatectomia parcial de 67 por cento em ratos. MÉTODOS: AST, ALT e gama-GT, foram determinadas pelo método cinético utilizando um espectrofotômetro (Modelo E2250-CELM). A regeneração hepática foi avaliada por imunohistoquímica (PCNA). RESULTADOS: O pré-tratamento oral de 100 mg/kg foi realizado durante 4 dias e causou aumento na regeneração hepática O pré-tratamento oral com 200 mg/kg diminuiu significativamente os níveis de AST quando comparado com o grupo submetido ao pré-tratamento com água destilada. As demais enzimas avaliadas não apresentaram diferenças quando comparadas entre os grupos estudados. CONCLUSÃO: O presente estudo mostra que o extrato aquoso da Hyptis pectinata, numa concentração de 100 mg/kg possui alguma atividade biológica estimulando a regeneração hepática e causando também um leve efeito hepatoprotetor numa concentração de 200 mg/kg.
Asunto(s)
Animales , Masculino , Ratas , Hyptis , Regeneración Hepática/efectos de los fármacos , Fitoterapia , Hojas de la Planta , Extractos Vegetales/uso terapéutico , Preparaciones de Plantas/uso terapéutico , Modelos Animales de Enfermedad , Hepatectomía , Antígeno Nuclear de Célula en Proliferación , Extractos Vegetales/farmacología , Preparaciones de Plantas/farmacología , Ratas Wistar , Espectrofotometría , Estadísticas no Paramétricas , Transaminasas/sangre , gamma-Glutamiltransferasa/sangreRESUMEN
PURPOSE: The use of medicinal plants for the treatment of human diseases has increased worldwide. Many of them are used by oral administration and, after absorption, may affect many organs. Therefore, this study aimed at assessing the effects of the aqueous extract of Sida cordifolia leaves, popularly known in Brazil as "malva-branca", on liver regeneration. METHODS: Twenty rats were divided into four groups: control, Sida100, Sida200 and Sida400 groups. All animals were submitted to oral administration of distilled water, 100, 200 and 400 mg/kg of the aqueous extract of Sida cordifolia, respectively. Immediately after this, they underwent 67 percent partial hepatectomy. Twenty four hours later, their livers were removed. Hepatic regeneration was assessed by immunohistochemical staining for proliferating cell nuclear antigen (PCNA) using the PC-10 monoclonal antibody. RESULTS: Sida100 and Sida200 groups disclosed higher liver regeneration indices than control group (p<0.001 and p<0.05, respectively). CONCLUSION: The aqueous extract of Sida cordifolia stimulates liver regeneration after 67 percent partial hepatectomy in rats.
INTRODUÇÃO: O uso de plantas medicinais para o tratamento de patologias humanas tem aumentado em todo mundo. Muitas delas são usadas por administração oral, e após a absorção podem afetar muitos órgãos. OBJETIVO: Esse estudo, tem como objetivo verificar o efeito do extrato aquoso de Sida cordifolia, popularmente conhecida no Brasil como "malva-branca", na regeneração hepática. MÉTODOS: Vinte ratos foram divididos em 4 grupos: controle, Sida 100, Sida 200 e Sida 400. Os animais foram submetidos a administração oral de água destilada, 100, 200 e 400 mg/kg de extrato aquoso de Sida cordifolia, respectivamente. Imediatamente após, foi realizada hepatectomia parcial 67 por cento. Vinte quatro horas após, os fígados foram removidos. A regeneração hepática foi avaliada por imunohistoquímica (PCNA), usando o anticorpo monoclonal PC-10. RESULTADOS: Os grupos Sida100 e Sida200 mostraram índices de regeneração hepática maiores que o grupo controle (p<0.001 e p<0.05, respectivamente). CONCLUSÃO: O extrato aquoso de Sida cordifolia estimula a regeneração hepática após hepatectomia parcial a 67 por cento em ratos.
Asunto(s)
Animales , Masculino , Ratas , Regeneración Hepática/efectos de los fármacos , Malvaceae , Fitoterapia , Hojas de la Planta , Extractos Vegetales/uso terapéutico , Preparaciones de Plantas/uso terapéutico , Modelos Animales de Enfermedad , Hepatectomía , Antígeno Nuclear de Célula en Proliferación , Extractos Vegetales/farmacología , Preparaciones de Plantas/farmacología , Ratas Wistar , Estadísticas no ParamétricasRESUMEN
Anti-nociceptive and anti-oedematogenic effects of the aqueous extract from the leaves of Erythrina velutina were tested through experimental models of nociception in mice and paw oedema induced by carrageenin in rats. The extract (300 and 600 mg/kg) did not change the carrageenin-induced paw oedema. In the hot plate test the extract also did not alter the latency time for mice liking the rear paws. Moreover, the extract (600 mg/kg) decreased by 96.5% the paw liking time in the second phase of the formalin test. This effect was antagonized by naloxone (5 mg/kg). In the acetic acid-induced writhing test, the extract (300 and 600 mg/kg) reduced the number of writhing by 88.8% and 96.4%, respectively. Our present results demonstrated that the crude extract from the leaves of E. velutina has anti-nociceptive but not anti-oedematogenic properties.
Asunto(s)
Analgésicos/farmacología , Antiinflamatorios/farmacología , Erythrina , Extractos Vegetales/farmacología , Animales , Femenino , Masculino , Ratones , Nociceptores/efectos de los fármacos , Dimensión del Dolor , Hojas de la Planta , Ratas , Ratas WistarRESUMEN
An aqueous extract of the aerial part of Peperomia pellucida (L.) HBK (Piperaceae) was tested for anti-inflammatory (paw edema induced by carrageenin and arachidonic acid) and analgesic activity (abdominal writhes and hot plate) in rats and mice, respectively. Oral administration of 200 and 400 mg/kg of the aqueous extract exhibited an anti-inflammatory activity in the carrageenin test, which was based on interference with prostaglandin synthesis, as confirmed by the arachidonic acid test. In the abdominal writhing test induced by acetic acid, 400 mg/kg of the plant extract had the highest analgesic activity, whereas in the hot-plate test the best dose was 100 mg/kg. The LD(50) showed that Peperomia pellucida (5000 mg/kg) presented low toxicity.
Asunto(s)
Analgésicos/farmacología , Antiinflamatorios/farmacología , Edema/prevención & control , Dolor/prevención & control , Peperomia , Fitoterapia , Extractos Vegetales/farmacología , Ácido Acético , Analgésicos/administración & dosificación , Analgésicos/uso terapéutico , Animales , Antiinflamatorios/administración & dosificación , Antiinflamatorios/uso terapéutico , Ácido Araquidónico , Carragenina , Relación Dosis-Respuesta a Droga , Edema/inducido químicamente , Femenino , Calor , Masculino , Dolor/inducido químicamente , Componentes Aéreos de las Plantas , Extractos Vegetales/administración & dosificación , Extractos Vegetales/uso terapéutico , Ratas , Ratas WistarRESUMEN
BACKGROUND: Peperomia pellucida is popularly known as coraçãozinho in the Brazilian northeast and is used in the treatment of abscesses, furuncles, and conjunctivitis. Our work aimed to determine the term of the development stages and the species cycle in the four seasons of the year (complete development, beginning of bloom, complete bloom, and seed set), verifying the plant's therapeutic profile during the four distinct development phases in order to detect differences in its potency. Pharmacological tests were performed to observe the anti-inflammatory activity. RESULTS: Phenological observations were accessed for a 12 month-period, from the Brazilian summer of 1999/2000 to fall 2000. On average the plantules' emergence occurred 15 days after seeding. All plantules grew in a similar manner up to 25 days after transplantation in all seasons. Starting on the 25th day, we observed faster growth during spring, with plants reaching a height of about 60 cm after 100 days of transplantation, unlike other seasons, in which plants reached heights of 40, 40, and 35 cm during winter, summer, and fall, respectively. The P. pellucida aqueous extract showed significant anti-inflammatory activity during phenophases 1 and 2 of winter and spring. Depending on the plant's phenophase there was variation in the potency of edema inhibition. CONCLUSION: P. pellucida has a phenological cycle of approximately 100 days. It is recommended that the P. pellucida aqueous extract is used as an antiedematogenic only during phenophases 1 and 2 of winter and spring.
Asunto(s)
Antiinflamatorios/uso terapéutico , Edema/tratamiento farmacológico , Peperomia/química , Peperomia/fisiología , Estaciones del Año , Animales , Antiinflamatorios/farmacología , Modelos Animales de Enfermedad , Femenino , Germinación/fisiología , Masculino , Medicina Tradicional , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Ratas , Ratas Wistar , Semillas/fisiologíaRESUMEN
Objetivo: O uso de plantas medicinais tem aumentado mundialmente. Então, é necessário saber seus possíveis efeitos a fim de estabelecer seu uso correto em seres humanos. Dessa forma, neste trabalho se propôs a estudar os efeitos do extrato aquoso das folhas da Hyptis pectinata, popularmente conhecida como "sambacaitá" ou "canudinho", sobre a regeneração hepática após hepatectomia parcial em ratos. Métodos: Dez ratos foram divididos em 2 grupos: grupos HP, que foi submetido à hepatectomia de 67 por cento após 4 dias de administração de água destilada; e o grupo HP100, que foi submetido à hepatectomia parcial e administração oral de 100 mg/kg do extrato aquoso da Hyptis pectinata pelo mesmo período de tempo. Todos os animais foram sacrificados 24 horas após o procedimento cirúrgico. A regeneração foi analisada através do método de imuno-histoquímica PCNA, usando o anticorpo monoclonal PC-10. Resultados: O índice de regeneração hepática estava significativamente elevado no grupo HP100 (p<0,05). Conclusões: O presente estudo mostra que o extrato aquoso das folhas da Hyptis pectinata pode estimular a regeneração de 100mg/kg.