Atividade antiinflamatória e anti-nociceptiva de extratos e lignanas isolados de Phyllanthus amarus

Tese (doutorado) - Universidade Federal de Santa Catarina, Centro de Ciências Biológicas. Programa de Pós-Graduação em FarmacologiaO extrato hexânico (EH) obtido do Phyllanthus amarus reduziu a nocicepção em modelos experimentais de dor aguda e crônica em camundongos, sendo que o mecanismo analgésico poderia estar relacionado possivelmente com a modulação do receptor TRPV1. Este estudo demonstrou que o EH, a fração rica em lignanas, e as lignanas filtetralina, nirtetralina ou nirantina foram efetivos em inibir o edema, a migração celular e/ou a produção de IL-1 . O mecanismo de ação da nirantina parece envolver o receptor para fator de ativação plaquetário, enquanto que para a nirtetralina o perfil farmacológico parece envolver a interação com receptor para endotelina-1. Apesar deste trabalho ainda não ter caracterizado o princípio ativo responsável pelas ações anti-nociceptivas, a filtetralina, a nirtetralina e a nirantina parecem ser as responsáveis pelas ações antiinflamatórias do P. amarus

Anxiolytic-like effects of acute and chronic treatment with Achillea millefolium L. extract

AbstractEthnopharmacological relevanceAchillea millefolium L. (Asteraceae), known as yarrow (“mil folhas”), has been used as folk medicine for gastrointestinal disorders, inflammation, anxiety, and insomnia.AimTo evaluate the potential anxiolytic-like effect of hydroalcoholic extract of Achillea millefolium L. in animal models.MethodsThe present study evaluated the effects of the hydroalcoholic extract from the aerial parts of Achillea millefolium L. in mice subjected to the elevated plus-maze, marble-burying, and open-field tests. Additionally, the GABAA/benzodiazepine (BDZ) mediation of the effects of Achillea millefolium was evaluated by pretreatment with the noncompetitive GABAA receptor antagonist picrotoxin and the BDZ antagonist flumazenil and by [3H]-flunitrazepam binding to the BDZ site on the GABAA receptor.ResultsAchillea millefolium exerted anxiolytic-like effects in the elevated plus-maze and marble-burying test after acute and chronic (25 days) administration at doses that did not alter locomotor activity. This behavioral profile was similar to diazepam. The effects of Achillea millefolium in the elevated plus-maze were not altered by picrotoxin pretreatment but were partially blocked by flumazenil. Furthermore, Achillea millefolium did not induce any changes in [3H]-flunitrazepam binding.ConclusionThe results indicate that the orally administered hydroalcoholic extract of Achillea millefolium L. exerted anxiolytic-like effects that likely were not mediated by GABAA/BDZ neurotransmission and did not present tolerance after short-term, repeated administration

GENOTOXIC AND MUTAGENIC EFFECTS OF DIFLUBENZURON, AN INSECT GROWTH REGULATOR, ON MICE

This study assessed the genotoxic and mutagenic potential of diflubenzuron (DFB) insecticide in mice. Mice were divided into five groups: group I: negative control; group II: positive control; group III: 0.3 mg/kg of DFB; group IV: 1 mg/kg of DFB; group V: 3 mg/kg DFB. Peripheral blood was collected for the comet assay and the micronucleus (MN) test. DFB increased incidence of comet formation at all doses tested. A rise in the frequency of MN in mouse peripheral blood was observed 24, 48, and 72 h postexposure at all doses tested. Data demonstrate that DFB exerts genotoxic and mutagenic effects in a dose-dependent manner.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES

Anti-hyperalgesic and anti-inflammatory activity of alternanthera maritima extract and 2 ''-o-alpha-l-rhamnopyranosylvitexin in mice

Alternanthera maritima are used in Brazilian popular medicine for the treatment of inflammatory and infectious diseases. Species of Alternanthera have demonstrated biological activities in previous scientific studies. The aim of this study was to determine whether the ethanol extract of the aerial parts of A. maritima (EEAM) and the isolated compound 2aEuro(3)-O-alpha-l-rhamnopyranosyl-vitexin inhibit mechanical hyperalgesia and parameters of inflammation in mice. The oral administration of EEAM significantly inhibited carrageenan (Cg)-induced paw edema and reduced leukocyte migration into the pleural cavity. 2aEuro(3)-O-alpha-l-rhamnopyranosylvitexin significantly inhibited paw edema and reduced both leukocyte migration and the leakage of protein into the pleural cavity. Both EEAM and 2aEuro(3)-O-alpha-l-rhamnopyranosylvitexin significantly prevented the Cg-induced hyperalgesia. Local administration of 2aEuro(3)-O-alpha-l-rhamnopyranosylvitexin significantly prevented the Cg- and tumor necrosis factor (TNF)-induced hyperalgesia. In conclusion, this study demonstrated that EEAM is an anti-inflammatory and anti-hyperalgesic agent, and the results suggested that 2aEuro(3)-O-alpha-l-rhamnopyranosylvitexin is responsible for the effects of EEAM and the mechanism involves the TNF pathway38620572066CONSELHO NACIONAL DE DESENVOLVIMENTO CIENTÍFICO E TECNOLÓGICO - CNPQCOORDENAÇÃO DE APERFEIÇOAMENTO DE PESSOAL DE NÍVEL SUPERIOR - CAPESFUNDAÇÃO DE AMPARO À PESQUISA DO ESTADO DE SÃO PAULO - FAPESPFUNDAÇÃO DE APOIO AO DESENVOLVIMENTO DO ENSINO, CIÊNCIA E TECNOLOGIA DO ESTADO DE MATO GROSSO DO SUL - FUNDEC

Safety evaluation of the oils extracted from edible insects (tenebrio molitor and pachymerus nucleorum) as novel food for humans

Increased concerns about ensuring food safety motivated the exploration of insects as an alternative protein source. It has been reported that Tenebrio molitor (TM) and Pachymerus nucleorum (PN) larvae are great protein and lipid sources with considerable concentrations of unsaturated fatty acids. Nevertheless, little attention has been given to the safety of using these edible insects. This study presents the acute and subacute (28 days) toxicological profile of the oil extracted from TM and PN larvae. The TM and PN larvae have all essential amino acids and the oils extracted from them fostered a considerable reduction in cholesterol and glucose levels of the treated rats. The experiments suggested that the TM and PN oils have low toxicity since it did not cause any lethality as well as no changes in hematological parameters1029094CONSELHO NACIONAL DE DESENVOLVIMENTO CIENTÍFICO E TECNOLÓGICO - CNPQCOORDENAÇÃO DE APERFEIÇOAMENTO DE PESSOAL DE NÍVEL SUPERIOR - CAPESFUNDAÇÃO DE APOIO AO DESENVOLVIMENTO DO ENSINO, CIÊNCIA E TECNOLOGIA DO ESTADO DE MATO GROSSO DO SUL - FUNDECTnão temnão temnão te

Anti-hyperalgesic and anti-inflammatory activity of Alternanthera maritima extract and 2″-O-α-L-rhamnopyranosylvitexin in mice

Alternanthera maritima are used in Brazilian popular medicine for the treatment of inflammatory and infectious diseases. Species of Alternanthera have demonstrated biological activities in previous scientific studies. The aim of this study was to determine whether the ethanol extract of the aerial parts of A. maritima (EEAM) and the isolated compound 2″-O-α-L-rhamnopyranosyl-vitexin inhibit mechanical hyperalgesia and parameters of inflammation in mice. The oral administration of EEAM significantly inhibited carrageenan (Cg)-induced paw edema and reduced leukocyte migration into the pleural cavity. 2″-O-α-L-rhamnopyranosylvitexin significantly inhibited paw edema and reduced both leukocyte migration and the leakage of protein into the pleural cavity. Both EEAM and 2″-O-α-L-rhamnopyranosylvitexin significantly prevented the Cg-induced hyperalgesia. Local administration of 2″-O-α-L-rhamnopyranosylvitexin significantly prevented the Cg- and tumor necrosis factor (TNF)-induced hyperalgesia. In conclusion, this study demonstrated that EEAM is an anti-inflammatory and anti-hyperalgesic agent, and the results suggested that 2″-O-α-L-rhamnopyranosylvitexin is responsible for the effects of EEAM and the mechanism involves the TNF pathway

Antipyretic and anti-inflammatory properties of the ethanolic extract, dichloromethane fraction and costunolide from Magnolia ovata (Magnoliaceae)

Aim of the study: Magnolia ovata (A.St.-Hil.) Spreng (formerly Talauma ovata), known as ""pinha-do-brejo"" or ""baguacu"", is a large tree widely distributed in Brazil. Its trunk bark has been used in folk medicine against fever. However, no data have been published to support the antipyretic ethnopharmacological use. This study investigated the antipyretic and anti-inflammatory effects of the ethanolic extract (EEMO). dichloromethane fraction (DCM), and the isolated compound costunolide. Materials and methods: The antipyretic and anti-inflammatory activities were evaluated in experimental models of fever and inflammation in mice. Results: The oral administration of EEMO, DCM and costunolide inhibited carrageenan (Cg)-induced paw oedema (ID(50) 72.35 (38.64-135.46) mg/kg, 5.8 (2.41-14.04) mg/kg and 0.18 (0.12-0.27) mg/kg, respectively) and was effective in abolishing lipopolysaccharide (LPS)-induced fever (30 mg/kg, 4.5 mg/kg and 0.15 mg/kg, respectively). EEMO was also effective in reducing cell migration in the pleurisy model. Intraplantar injection of costunolide also reduced the paw oedema, myeloperoxidase and N-acetyl-glucosaminidase activity induced by Cg in mice. Conclusions: Collectively, these results show, for the first time, that extracts obtained from Magnolia ovata possess antipyretic and anti-inflammatory properties, and costunolide appears to be the compound responsible for these effects. (C) 2009 Elsevier Ireland Ltd. All rights reserved.Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)CAPES (PRODOC