RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Lafoensia pacari A. St.-Hil. (Lythraceae), known popularly as "pacari" or "mangaba-brava" is popularly used in the state of Goiás, Brazil. The stem bark or leaves are used to treat cancer, gastric disorders, inflammation and as a tonic to treat loss of enthusiasm. AIM OF THE STUDY: Previous results suggest that the ethanol:water 7:3 extract of the stem bark of L. pacari (PEx) has antidepressant-like activity in male mice. Our aim was to perform the PEx׳s bioguided fractionation and evaluate the monoaminergic system involvement in the antidepressant effect as well as progress in the study of L. pacari mechanism of action. MATERIAL AND METHODS: Mice (30-35g) orally treated (24, 5 and 1h) with PEx (100, 300 or 1000mg/kg), chloroform (ChloF-70mg/kg), ethyl acetate (180mg/kg), n-butanol (370mg/kg) and aqueous (1g/kg) fractions were submitted to the forced swimming test. To assess the mechanism of action, different groups of mice were pretreated with p-chlorophenylalanine (PCPA-100mg/kg, 4 days, i.p.) and alpha-methyl-p-tyrosine (AMPT-100mg/kg, 4h, i.p.) to assess the involvement of serotoninergic and catecholaminergic systems in the ChloF effects, respectively. A putative in vitro inhibition of monoamine oxidase (MAO) activity as well as the ex vivo hippocampal brain-derived neurotrophic factor (BDNF) quantification were carried out. Phytochemical screening, spectroscopy and chromatography analysis were used for identification of compounds present in ChloF. RESULTS AND DISCUSSION: After the fractionation, the ChloF 70mg/kg was the most active fraction, reducing the immobility time by 22%. Pre-treatments with both PCPA and AMPT abolished the ChloF effects, suggesting that ChloF antidepressant-like effect is dependent on serotonergic and catecholaminergic systems. ChloF did not inhibited MAO-A or MAO-B activity, excluding this as possible mechanism of action. ChloF augmented hippocampal BDNF level, which could be accounted for its antidepressant-like effect. Phytochemical screening showed the presence of saponins, tannins, steroids and triterpene in the PEx, and the presence of triterpene and steroids in ChloF. The spectroscopy and chromatography analysis identified lupeol, ß-sitosterol and stigmasterol in ChloF. CONCLUSION: ChloF is the fraction that better retained the crude extract active constituents. ChloF presents antidepressant-like effect that involves both serotonergic and catecholaminergic systems without inhibiting MAO enzymatic activity; this fraction also increases the hippocampal BDNF levels.
Assuntos
Antidepressivos/farmacologia , Depressão/tratamento farmacológico , Lythraceae/química , Extratos Vegetais/farmacologia , Animais , Antidepressivos/administração & dosagem , Antidepressivos/isolamento & purificação , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Brasil , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Hipocampo/efeitos dos fármacos , Hipocampo/metabolismo , Masculino , Camundongos , Monoaminoxidase/metabolismo , Extratos Vegetais/administração & dosagem , Serotonina/metabolismo , NataçãoRESUMO
Peptic and/or duodenal ulcers are characterized by diverse acute and chronic ulcerative lesions that commonly arise in any portion of the gastric mucosa that is exposed to the aggressive action of gastric acid. The pathophysiology of peptic ulcers has been attributed to an imbalance between aggressive and protective factors. In Brazil, medicinal plants are commonly used to treat this ailment. A country with great biodiversity, Brazil is considered a rich source of therapeutic products. There have been popular and pharmacological reports on the medicinal relevance of the Brazilian cerrado plant species, including Ananas ananassoides, Celtis iguanaea, Encholirium spectabile, Hymenaea stigonocarpa, Lafoensia pacari, Qualea grandiflora, Qualea parvifora, Mouriri pusa, Solanum lycocarpum, Solanum paniculatum, Serjania erecta, and Vochysia tucanorum, in the treatment of stomach disorders. The aim of the present review was to report on some of the Brazilian cerrado plants that are used in folk medicine because of their gastroprotective potential and to encourage novel studies in the search and preservation of plants with this therapeutic potential.
RESUMO
Our study sought to evaluate the anxiolytic and antidepressant activities of oleanolic acid as well as the neural mechanisms involved. Animal models such as barbiturate sleep-induction, light-dark box, elevated plus maze, forced swimming test, tail suspension test and open field test were conducted. Male Albino Swiss mice were treated orally with vehicle 10 mL/kg, fluoxetine 20 mg/kg, imipramine 15 mg/kg, diazepam 1 mg/kg or oleanolic acid 5-40 mg/kg. Pretreatment (intraperitoneal) of animals with pentylenetetrazole (PTZ) 20 mg/kg, 1-(2-methoxyphenyl)-4-[4- (2-phthalimido) butyl]piperazine hydrobromide (NAN-190) 0.5 mg/kg, p-chlorophenylalanine methyl ester (PCPA) 100 mg/kg or α-methyl-p-tyrosine (AMPT) 100 mg/kg, WAY100635 (WAY) 0.3 mg/kg, prazosin (PRAZ) 1 mg/kg, yohimbine 2 mg/kg as well as monoamine oxidase assay and hippocampal brain-derived neurotrophic factor (BDNF) quantification were carried out. Oleanolic acid potentiated the hypnotic effect of barbiturate and demonstrated an anxiolytic effect in both the light-dark box and elevated plus maze. This effect was not reversed by PTZ. Acute and/or chronic oral treatment of mice with oleanolic acid (5-20 mg/kg) elicited an antidepressant effect in the forced swimming test and the tail suspension test without interfering with the locomotor activity. The antidepressant effect of oleanolic acid was attenuated by NAN-190, AMPT, PCPA, WAY and PRAZ. Although monoamine oxidase activity remained unaltered by oleanolic acid, chronic administration of oleanolic acid augmented hippocampal BDNF level. These findings demonstrate multiple mechanisms of the anxiolytic and antidepressant effect of oleanolic acid.
Assuntos
Ansiolíticos/farmacologia , Antidepressivos/farmacologia , Ácido Oleanólico/farmacologia , Animais , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Diazepam/farmacologia , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Fenclonina/análogos & derivados , Fenclonina/farmacologia , Fluoxetina/farmacologia , Hipocampo/efeitos dos fármacos , Hipocampo/metabolismo , Imipramina/farmacologia , Masculino , Camundongos , Monoaminoxidase/metabolismo , Atividade Motora/efeitos dos fármacos , Ácido Oleanólico/antagonistas & inibidores , Pentilenotetrazol/farmacologia , Piperazinas/farmacologia , Piridinas/farmacologia , alfa-Metiltirosina/farmacologiaRESUMO
The Hydrocotyle umbellata L. is a specimen of the Araliaceae family popularly known as acariçoba. Its indications in folk medicine include treatment of skin ulcers, and rheumatism. The aim of this study was to evaluate the antinociceptive and anti-inflammatory activities of the ethanolic extract from acariçoba's underground parts (EEA). EEA reduced the nociceptive response of the animals as evaluated in the acetic acid-induced writhing test and in both phases of formalin test. EEA also presented a supraspinal analgesic activity by increasing the pain latency in the hot plate test. Moreover, EEA reduced the leukocytes migration and plasma extravasation to pleural cavity in the carrageenan-induced pleurisy, besides reducing the edema induced by carrageenan until the second hour and also the edema induced by dextran. In conclusion our results showed that EEA of H. umbellata L. presents analgesic and anti-inflammatory activities, and that a blockade of activity or reduction in the release of different mediators, such as histamine and serotonin, could be involved in these pharmacologic effects.
Assuntos
Analgésicos/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Araliaceae/química , Edema/tratamento farmacológico , Dor/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Analgésicos/isolamento & purificação , Animais , Anti-Inflamatórios/isolamento & purificação , Carragenina , Edema/induzido quimicamente , Masculino , Camundongos , Dor/induzido quimicamenteRESUMO
The Streptoverticillium sp. Z1 is an actinomycete isolated from the soil under Cerrado vegetation, the extract of this strain was investigated in nociceptive and inflammatory models. The Streptoverticillium extract (ExS) 50 and 100 mg/kg (s.c.) produced a significant inhibition of acetic acid-induced abdominal writhings thereby demonstrating an anti-nociceptive effect. In the tail flick test the ExS (s.c.) was inactive. This result implited that ExS does not contain opioid-like compounds with central analgesic properties. In the inflammatory models, ExS 100 and 200 mg/kg (s.c.) were able to inhibit the croton oil-induced ear edema and, ExS 200 and 500 mg/kg (s.c.) inhibited the leukocyte migration on the carrageenan-induced peritonitis. The phospholipase A2 enzymatic assay showed that the anti-inflammatory activity of ExS was not due to direct effect on phospholipase A2 activity. These data suggest that Streptoverticillium sp. produces metabolites with anti-inflammatory effect and that these metabolites are unable to directly inhibit phospholipase A2 enzyme.
Assuntos
Acetona/uso terapêutico , Analgésicos/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Edema/tratamento farmacológico , Dor/tratamento farmacológico , Streptomycetaceae/química , Acetona/isolamento & purificação , Analgésicos/isolamento & purificação , Animais , Anti-Inflamatórios/isolamento & purificação , Carragenina , Óleo de Cróton , Edema/induzido quimicamente , Masculino , Camundongos , Dor/induzido quimicamente , Microbiologia do SoloRESUMO
Acetic acid-induced writhing, hot-plate, carrageenan-induced pleurisy, formalin-induced pain, croton oil-induced ear edema, vascular permeability tests and phospholipase A2 activity assay were used to study the analgesic and/or anti-inflammatory activity of the hydromethanolic fraction of ethanolic extract from Spiranthera odoratissima A. St.-Hil., Rutaceae, leaves (HMF) and its subfraction (sub-Fr10-28). HMF and sub-Fr10-28 reduced the leukocyte migration on the carrageenan-induced pleurisy test; sub-Fr10-28 reduced the pain reaction time in the second phase of formalin-induced pain, as well as the ear edema and vascular permeability. Both HMF and sub-Fr10-28 inhibited the phospholipase A2 activity. These results suggest that the analgesic effect of this plant could be, in part, due to an anti-inflammatory action produced by the inhibition of phospholipase A2 activity.
RESUMO
The antinociceptive and antiinflammatory properties of the neolignan, grandisin, isolated from Virola surinamensis (Myristicaceae) were investigated. Grandisin (GRA) is present in several plant species from Brazil used in popular medicine for the treatment of disorders such as colic, inflammation, rheumatism, dyspepsia and liver dysfunction. These studies demonstrated that GRA is able to inhibit the acetic acid-induced writhing in mice dose-dependently, and that this effect is not caused by motor incoordination or sedation due to depressant effect in the CNS. Through the formalin test the antiinflammatory activity of GRA was characterized, this substance reduced the time licking the paw by 60.5% (only in the second phase (inflammatory pain). This activity was also verified by the oil-induced ear oedema test, where GRA 10.0 mg/kg reduced the oedema by 36.4%. The results suggest that GRA has antinociceptive effects arising from antiinflammatory activity.