16 research outputs found

    Involvement of Opioid System, TRPM8, and ASIC Receptors in Antinociceptive Effect of Arrabidaea brachypoda (DC) Bureau

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    Arrabidaea brachypoda (DC) Bureau is a medicinal plant found in Brazil. Known as "cipó-una", it is popularly used as a natural therapeutic agent against pain and inflammation. This study evaluated the chemical composition and antinociceptive activity of the dichloromethane fraction from the roots of A. brachypoda (DEAB) and its mechanism of action. The chemical composition was characterized by high-performance liquid chromatography, and this fraction is composed only of dimeric flavonoids. The antinociceptive effect was evaluated in formalin and hot plate tests after oral administration (10-100 mg/kg) in male Swiss mice. We also investigated the involvement of TRPV1 (transient receptor potential vanilloid 1), TRPA1 (transient receptor potential ankyrin 1), TRPM8 (transient receptor potential melastatin 8), and ASIC (acid-sensing ion channel), as well as the opioidergic, glutamatergic, and supraspinal pathways. Moreover, the nociceptive response was reduced (30 mg/kg) in the early and late phase of the formalin test. DEAB activity appears to involve the opioid system, TRPM8, and ASIC receptors, clearly showing that the DEAB alleviates acute pain in mice and suggesting the involvement of the TRPM8 and ASIC receptors and the opioid system in acute pain relief

    The Anti-Inflammatory Effects of the Methanolic Extract and Fractions from Davilla elliptica St. Hil. (Dilleniaceae) on Bothrops jararaca Envenomation

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    Inflammation and haemorrhage are the main characteristics of tissue injury in botropic envenomation. Although some studies have shown that anti-venom prevents systemic reactions, it is not efficient in preventing tissue injury at the site of the bite. Therefore, this work was undertaken to investigate the anti-inflammatory effects of the methanolic extract and fractions from D. elliptica and to evaluate the role of matrix metalloproteinases (MMPs) in this process. Effects of the extract and fractions from D. elliptica were evaluated using a carrageenan-induced paw oedema model in rats, and leukocyte rolling was visualized by intravital. The quantification of MMPs activities (MMP-2 and MMP-9) extracted from the dermis of mice treated with extract and fractions alone or incubated with venom was determined by zymographic analyses. Our results show that intraperitoneal (i.p.) injection of fractions significantly reduced paw oedema after the carrageenan challenge. Treatment with the tannins fraction also resulted in considerable inhibition of the rolling of leukocytes and this fraction was able to decrease the activation of MMP-9. These results confirmed the anti-inflammatory activity of the methanolic extract and tannins fraction of D. elliptica and showed that the dermonecrosis properties of B. jararaca venom might be mediated through the inhibition of MMP-9 activity.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq

    Gastroprotective effect of Cissus sicyoides (Vitaceae): Involvement of microcirculation, endogenous sulfhydryls and nitric oxide

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    Aim of the study: Cissus sicyoides L. is a medicinal plant popularly known in Brazil against various diseases and the research interest in this plant is justifiable because of its potential medicinal value in stomachache and gastric ulcer.Materials and methods: The methanolic extract obtained from the leaves of Cissus sicyoides (Cc) was evaluated for the ability to protect the gastric mucosa against injuries caused by necrotizing agents (0.3 M HCl/60% EtOH, absolute ethanol, piroxicam and pylorus ligature) in rodents. We also evaluated microcirculation, antioxidant action and participation of NO (nitric oxide) and sulfhydryls (SH) groups in the Cc gastroprotective action.Results: Administration of Cc significantly reduced gastric lesions induced by different ulcerogenic agents in rodents. This extract administered by oral route significantly increased gastric volume without exerting antisecretory effect. The Cc effect involved an increase of the defense mechanism of the gastrointestinal mucosa such as NO and SH groups that prevent and attenuate the ulcer process. The Cc also has antioxidant property against oxidative stress but does not modify microcirculation response in gastric mucosa.Conclusions: These results confirmed the traditional use of Cissus sicyoides for the treatment of gastric ulcer. (C) 2008 Elsevier B.V. All rights reserved

    Caracteriza√ß√£o do efeito anti-inflamat√≥rio e anti-hemorr√°gico dos extratos e fra√ß√Ķes enriquecidas de esp√©cies do projeto tem√°tico BIOTA/FAPESP

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    Acidente of√≠dico √© um s√©rio problema de sa√ļde p√ļblica no Brasil. Embora a neutraliza√ß√£o do efeito t√≥xico sist√™mico seja alcan√ßada pela administra√ß√£o do soro antiof√≠dico, a inj√ļria tecidual local n√£o √© evitada. Em muitos pa√≠ses, plantas medicinais s√£o tradicionalmente usadas no tratamento de envenenamento por picada de cobra. Nesse trabalho, foi investigado o potencial efeito anti-inflamat√≥rio de algumas esp√©cies vegetais da flora brasileira que apresentaram capacidade de neutraliza√ß√£o total contra a hemorragia causada por Bothrops jararaca como: Byrsonima crassa Niedenzu, Mouriri pusa Gardn., Rhamnidium elaeocarpum Reiss. e Davilla elliptica St. Hill. Os resultados obtidos nesse trabalho demonstraram uma importante a√ß√£o anti-inflamat√≥ria de algumas esp√©cies, com destaque para o extrato metan√≥lico das cascas de R. elaeocarpum, que inibiu a produ√ß√£o de NO e TNF-őĪ in vitro. Essa esp√©cie possui ainda a√ß√£o anti-nociceptiva modulada pelos receptores seroton√©rgicos e opi√≥ides. J√° o extrato metan√≥lico das folhas de B. crassa n√£o apresentou atividade anti-nociceptiva na indu√ß√£o da nocicep√ß√£o no modelo da formalina. O extrato metan√≥lico das folhas de M. pusa possui a√ß√£o anti-nociceptiva tanto na dor neurog√™nica como na dor inflamat√≥ria na dose de 500 mg/kg (p.o). Extratos metan√≥licos de B. crassa (folhas), R. elaeocarpum (cascas) e D. elliptica apresentaram importante a√ß√£o anti-edematog√™nica nas doses de 15.62 mg/kg (i.p) e 31.24 mg/kg (i.p). Adicionalmente, a fra√ß√£o de taninos de D. elliptica (30 mg/kg, i.p) foram capazes de diminuir em 50 % o rolamento de leuc√≥citos em vasos (¬ī¬īrolling¬ī¬ī) durante o processo inflamat√≥rio induzido pela administra√ß√£o t√≥pica de LPS. A fra√ß√£o de taninos e o extrato de D. elliptica diminu√≠ram da atividade de MMP-9 ativa frente a inocula√ß√£o de veneno de B. jararaca e apresentaram efeito anti-edematog√™nico...Funda√ß√£o de Amparo √† Pesquisa do Estado de S√£o Paulo (FAPESP

    Davilla elliptica and Davilla nitida: Gastroprotective, anti-inflammatory immunomodulatory and anti-Helicobacter pylori action

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    Ethnopharmacological relevance: Davilla elliptica and Davilla nitida are species commonly found in the Brazilian Cerrado biome.Aim of the study: Based on ethnopharmacological and phytochemical analyses, methanolic extracts from leaves of Davilla elliptica (EDE) and Davilla nitida (EDN) were evaluated for their anti-ulcer, anti-inflammatory, immunological and anti-Helicobacter pylori activities.Materials and methods: The gastroprotective action of both extracts was evaluated in rodent experimental models (HCl/ethanol, ethanol or NSAID). We also evaluated anti-inflammatory (carrageenin-induced rat hind paw edema), immunomodulatory (murine peritoneal macrophages) and antibacterial action of both extracts against a standard strain of Helicobacter pylori.Results: EDE and EDN (500 mg/kg) were able to protect gastric mucosa against HCl/ethanol solution (EDE 63%; EDN 59%), absolute ethanol (EDE 95%; EDN 88%), and also against injurious effect of NSAID (EDE 77%: EDN 67%). When EDE and EDN were challenged with sulfhydryl depleter compound, the gastroprotective action of both extracts was completely abolished. EDE had gastroprotective effect related to increase of glutathione bioavailability and stimulated higher levels of NO, H(2)O(2) and TNF-alpha production. Otherwise EDN showed better anti-Helicobacter pylori action than EDE. Neither extracts presented anti-inflammatory activity by oral route.Conclusion:The phytochemical investigation showed that both extracts possess phenolic acid derivatives, acylglycoflavonoids and condensed tannins with evident quantitative variations that probably influenced the pharmacological differences between extracts. Published by Elsevier B.V.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq

    Citral: A monoterpene with prophylactic and therapeutic anti-nociceptive effects in experimental models of acute and chronic pain

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    Citral (3,7-dimethy1-2,6-octadienal) is an open-chain monoterpenoid present in the essential oils of several medicinal plants. The aim of this work was to evaluate the effects of orally administered citral in experimental models of acute and chronic nociception, inflammation, and gastric ulcers caused by nonsteroidal anti-inflammatory drugs (NSAIDs). Oral treatment with citral significantly inhibited the neurogenic and inflammatory pain responses induced by intra-plantar injection of formalin. Citral also had prophylactic and therapeutic anti-nociceptive effects against mechanical hyperalgesia in plantar incision surgery, chronic regional pain syndrome, and partial ligation of sciatic nerve models, without producing any significant motor dysfunction. In addition, citral markedly attenuated the pain response induced by intra-plantar injection of glutamate and phorbol 12-myristate 13-acetate (PMA, a protein kinase C activator), as well as by intrathecal (i.t.) injection of ionotropic and metabotropic glutamate receptor agonists (N-methyl-D-aspartic acid [NMDA] and 1-amino-1,3-dicarboxycyclopentane [trans-ACPD], respectively), substance P, and cytokine tumour necrosis factor-alpha. However, citral potentiated behaviours indicative of pain caused by i.t, but not intra-plantar, injection of a transient receptor potential vanilloid receptor type 1 (TRPV1) agonist. Finally, the anti-nociceptive action of citral was found to involve significant activation of the 5-HT2A serotonin receptor. The effect of citral was accompanied by a gastro-protective effect against NSAID-induced ulcers. Together, these results show the potential of citral as a new drug for the treatment of pain. (C) 2014 Elsevier B.V. All rights reserved.Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP