Attenuation of capsaicin-induced acute and visceral nociceptive pain by α- and β-amyrin, a triterpene mixture isolated from Protium heptaphyllum resin

Abstract The triterpene mixture, a-and h-amyrin, isolated from Protium heptaphyllum resin was evaluated on capsaicinevoked nociception in mice. Orally administered a-and h-amyrin (3 to 100 mg/kg) significantly suppressed the nociceptive behaviors-evoked by either subplantar (1.6 Ag) or intracolonic (149 Ag) application of capsaicin. The antinociception produced by a-and h-amyrin against subplantar capsaicin-induced paw-licking behavior was neither potentiated nor attenuated by ruthenium red (1.5 mg/kg, s.c.), a non-specific antagonist of vanilloid receptor (TRPV1), but was greatly abolished in animals pretreated with naloxone (2 mg/kg, s.c.), suggesting an opioid mechanism. However, participation of a 2 -adrenoceptor involvement was unlikely since yohimbine (2 mg/ kg, i.p.) pretreatment failed to block the antinociceptive effect of a-and h-amyrin in the experimental model of visceral nociception evoked by intracolonic capsaicin. The triterpene mixture (3 to 30 mg/kg, p.o.) neither altered significantly the pentobarbital sleeping time, nor impaired the ambulation or motor coordination in open-field and rota-rod tests, respectively, indicating the absence of sedative or motor abnormality that could account for its antinociception. Nevertheless, a-and h-amyrin could significantly block the capsaicin (10 mg/kg, s.c.)-induce

Anti-inflammatory, antinociceptive, and antipyretic effects of methanol extract of Cariniana rubra stem bark in animal models

Cariniana rubra Miers (Lecythidaceae), popularly known as "jequitibá-vermelho'', is a large Brazilian tree whose bark is used in infusion and decoction for the treatment of inflammatory conditions. This study aims to assess the anti-inflammatory, antinociceptive, and antipyretic effects of Cariniana rubra methanolic stem bark extract (EM Cr) using experimental animals. Anti-inflammatory activity of EM Cr was tested on carrageenan and dextran-induced rat paw edema, carrageenan-induced pleurisy in rats and acetic acid-increase vascular permeability in mice. Antinociceptive and antipyretic activities were evaluated using acetic acid-induced writhing, formalin and hot-plate tests in mice, as well as brewer's yeast-induced pyrexia in rats. The extract inhibitied carrageenan and dextran-induced edema, reduced exudate volume and leukocyte migration on the carrageenan-induced pleurisy and on the vascular permeability increase induced by acetic acid. The EM Cr inhibited nociception on the acetic acid-induced writhing and in the second phase of formalin test, and decreased rectal temperature. It was, however, inactive against thermal nociception.Phytochemical analysis with EM Cr showed the occurrence of saponins, triterpenes, sterols and phenolic compounds. Phytosterols (&#946;-sitosterol, stigmasterol), pentacyclic triterpenes (&#945;- and &#946;-amyrin as a mixture), arjunolic acid, a phytosterol glycoside (sitosterol 3-O-&#946;-D-glucopyranoside), and triterpenoid saponins (28-&#946;-glucopyranosyl-23-O-acetyl arjunolic acid; 3-O-&#946;-glucopyranosyl arjunolic acid and 28-O-[&#945;-L-Rhamnopyranosyl-(1&#8594;2)-&#946;-glucopyranosyl]-23- O-acetyl arjunolic acid) were the main identified compounds. It can be presumed that EM Cr caused their effects by inhibiting the liberation and/or action of different inflammatory mediators. These findings support the traditional use of Cariniana rubra preparations to treat inflammation.<br>Cariniana rubra Miers (Lecythidaceae), popularmente conhecido como "jequitibá-vermelho'', é uma árvore brasileira de grande porte, cuja casca é utilizada nas formas de infusão e decocção para o tratamento de condições inflamatórias. Os efeitos antiinflamatório, antinociceptivo e antipirético do extrato metanólico da casca do caule de Cariniana rubra (EM Cr) foram avaliados em animais experimentais. A atividade antiinflamatória do EM Cr foi testada nos modelos de edema depata induzido por carragenina e dextrana em ratos, pleurisia induzida por carragenina em ratos e permeabilidade vascular aumentada por ácido acético em ratos. As atividades antinociceptiva e antipirética foram avaliadas utilizando os modelos de nocicepções induzidos por ácido acético e formalina, placa quente em camundongos e de pirexia, pela injeção de levedura de cerveja em ratos. O extrato inibiu o edema induzido porcarragenina e dextrana, reduziu o volume de exsudato e a migração de leucócitos na pleurisia induzida por carragenina eo aumento da permeabilidade vascular induzida por ácidoacético. O EM Cr inibiu a nocicepção nas contorções induzidas por ácido acético e na segunda fase do teste de formalina e diminuiu a temperatura retal. No entanto, foi inefetivo no teste da placa quente. A análise química por via úmida deu resultados positivos para saponinas, triterpenos, esteroides e compostos fenólicos. Fitosteróis e triterpenóides pentacíclicos (&#946;-sitosterol, estigmasterol, &#945; and &#946;-amirinas em mistura e ácido arjunólico) e as saponinas triterpenoidais: 3-O-&#946;-D-glucopiranosideo de sitosterol; ácido arjunólico 28-&#946;-glucopiranosila-23-O-acetila; ácido arjunólico 3-O-&#946;-glucopiranosila e ácido arjunólico 28-O-[&#945;-L-rhamnopiranosil-(1&#8594;2)-&#946;-D-glucopiranosila]-23-O-acetila. Pode-se presumir que os efeitos do EM Cr foram causados pela inibição da liberação e/ou ação de diversos mediadores inflamatórios. Estes resultados validam o uso tradicional das preparações caseiras de Cariniana rubra para tratar a inflamação

1,8-cineole protects against liver failure in an in-vivo murine model of endotoxemic shock

Freitas, Luiz Antônio Rodrigues de “Documento produzido em parceria ou por autor vinculado à Fiocruz, mas não consta à informação no documento”.Submitted by Ana Maria Fiscina Sampaio ([email protected]) on 2017-08-11T17:34:03Z No. of bitstreams: 1 Santos FA 1,8-cineole protects....pdf: 313163 bytes, checksum: 4b7a5a588d0cf5796c69e4c36104b90e (MD5)Approved for entry into archive by Ana Maria Fiscina Sampaio ([email protected]) on 2017-08-11T17:51:35Z (GMT) No. of bitstreams: 1 Santos FA 1,8-cineole protects....pdf: 313163 bytes, checksum: 4b7a5a588d0cf5796c69e4c36104b90e (MD5)Made available in DSpace on 2017-08-11T17:51:35Z (GMT). No. of bitstreams: 1 Santos FA 1,8-cineole protects....pdf: 313163 bytes, checksum: 4b7a5a588d0cf5796c69e4c36104b90e (MD5) Previous issue date: 2001Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq, 300870/98-1).Federal University of Ceará. Department of Physiology and Pharmacology. Fortaleza, CE, BrasilFederal University of Ceará. Department of Physiology and Pharmacology. Fortaleza, CE, BrasilFederal University of Ceará. Department of Physiology and Pharmacology. Fortaleza, CE, BrasilFederal University of Ceará. Department of Physiology and Pharmacology. Fortaleza, CE, BrasilFederal University of Ceará. Department of Pathology and Legal Medicine. Fortaleza,Federal University of Ceará. Department of Pathology and Legal Medicine. Fortaleza,Fundação Oswaldo Cruz. Laboratório de Patologia e Biologia Celular. Rio de Janeiro, RJ, BrasilFundação Oswaldo Cruz. Laboratório de Patologia e Biologia Celular. Rio de Janeiro, RJ, BrasilThe effects of 1,8-cineole on D-galactosamine/lipopolysaccharide (GalN/LPS)-induced shock model of liver injury was investigated in mice. The co-administration of GalN (700 mg kg−1, i.p.) and LPS (5 lgkg−1, i.p.) greatly elevated serum concentrations of tumour necrosis factor-a (TNFa), alanine aminotransferase and aspartate aminotransferase, and induced massive hepatic necrosis and lethality in 100% of control mice. Pretreatment with 1,8-cineole (400 mg kg−1, p.o.) and dexamethasone (1 mgkg−1, s.c.), 60 min before GalN/LPS, offered complete protection (100%) against the lethal shock and acute elevation in serum TNF-a and serum transaminases. Hepatic necrosis induced by GalN/LPS was also greatly reduced by both 1,8-cineole and dexamethasone treatment. The results indicate that 1,8-cineole protects mice against GalN/LPSinduced liver injury through the inhibition of TNF-a production, and suggest that 1,8-cineole may be a promising agent to combat septic-shock-associated pathologies

Anti-inflammatory effect of the ethanolic extract from Bowdichia virgilioides H.B.K stem bark

Bowdichia virgilioides H.B.K stem bark (Fabaceae), locally known as "sucupira-preta", is a reputed folk-remedy to treat some inflammatory disorders. To validate its traditional claim, the ethanolic extract from B. virgilioides was evaluated in several animal models of inflammation and nociception. The extract at oral doses of 100 to 1000 mg/kg body weight caused a significant inhibition of carrageenan-induced hind paw oedema, suppression of exudate volume and leukocyte immigration in rat pleurisy induced by carrageenan, and reduction of granuloma weights in the model of subcutaneous granulomas promoted by cotton pellets. In addition, the plant extract significantly inhibited the vascular permeability increase induced by intraperitoneal acetic acid. It also showed marked antinociceptive effect in acetic acid-induced writhing test and in the second phase of formalin test in mice. These findings evidence the anti-inflammatory potential of Bowdichia virgilioides bark and supports its traditional use in inflammatory conditions.<br>A casca do caule de Bowdichia virgilioides H.B.K (Fabaceae), conhecida localmente como sucupira-preta, é um remédio popular muito utilizado para tratar inflamações. Com o objetivo de validar sua crença popular, o extrato etanólico de B. virgilioides foi avaliado em vários modelos experimentais de inflamação e nocicepção. O extrato administrado, via oral, em doses de 100 a 1000 mg/kg de peso corporal produziu inibição significativa no edema de pata induzido por carragenina, no aumento na permeabilidade vascular induzido por acido acético, no volume de exudato e na migração leucocitária no teste de pleurisia induzida por carragenina, bem como no peso de granulomas induzidos por pelotas de algodão, em ratos. Em camundongos, o EE Bv reduziu o número de contorções abdominais induzidas por ácido acético e a lambedura da pata na segunda fase do teste da formalina. Esses resultados validam o potencial anti-inflamatório da casca de Bowdichia virgilioides e referendam seu uso tradicional em condições inflamatórias