RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Buddleja globosa, known as "matico", is employed in Chile for wound healing. AIM OF THE STUDY: To validate the traditional use of the crude drug through in vivo and in vitro evaluation of the anti-inflammatory, analgesic and antioxidant properties of its extracts. MATERIALS AND METHODS: Sequential hexane, dichloromethane, methanol and total methanol extracts were studied using bioguided fractionation. The following activities were investigated: analgesic (writhing test), oral and topic anti-inflammatory (paw- and ear-induced edema), free radical scavenging and antioxidant activities (1,1-diphenyl-2-picrylhydrazyl, DPPH, superoxide anion, lipid peroxidation and xanthine oxidase inhibition). Sodium naproxen, nimesulide, indomethacin were used as reference drugs for in vivo, quercetin and allopurinol for in vitro assays. RESULTS: A mixture of alpha- and beta-amyrins was isolated from the hexane extract that showed 41.2% of analgesic effect at 600 mg/kg, inhibited by 47.7 and 79.0% the arachidonic acid (AA) and 12-deoxyphorbol-13-decanoate (TPA)-induced inflammation at 3mg/20 microL/ear, respectively. A mixture of beta-sitosterol, stigmasterol, stigmastenol, stigmastanol and campesterol was isolated from the fraction CD4-N and beta-sitosterol-glycoside from the fraction CD5-N, reducing TPA-induced inflammation by 78.2 and 83.7% at 1mg/20 microL/ear, respectively. The fraction CD4-N at 300 mg/kg also showed analgesic activity (38.7%). The methanol extract at 600mg/kg per os showed anti-inflammatory effect (61.4%), topic anti-inflammatory (56.7% on TPA) and analgesic activity (38.5%). Verbascoside and luteolin-7-O-glucoside were the major components of the methanol extract; apigenin 7-O-glucoside was also detected. Inhibition of superoxide anion, lipoperoxidation, and DPPH bleaching effect was found in the methanol serial and global extracts. CONCLUSIONS: The present report demonstrate the analgesic and anti-inflammatory properties of Buddleja globosa and validate its use in Chilean traditional medicine.
Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Buddleja/química , Extratos Vegetais/farmacologia , Animais , Feminino , Masculino , Camundongos , Análise EspectralRESUMO
The addition of antioxidants to broiler diets has been shown to enhance their antioxidant status. Since boldo (Peumus boldus Mol.) leaves contain highly antioxidant molecules, a dried extract of boldo (DEB) was added to broiler diets to improve "in vivo" antioxidant tissue status and to favor animal growth. A DEB standardized for antioxidant content was prepared and added to poultry diets at three different levels (low-DELB, medium-DEMB, and high-DEHB) for a period of 6 weeks. A single negative control (no added antioxidant) and one positive control (supplementation with 200 mg/kg vitamin E) were used. Plasma antioxidant capacity (PAC), thiol content (GHS), and basal and induced lipoperoxidation of liver, leg and breast tissues were determined in birds at 2, 4, and 6 weeks of age. PAC increased with chicken age until week 6, but was unaffected by DEB addition at any level. However, DEB increased hepatic GSH content. No data indicated that DEB improved the resistance against induced lipoperoxidation in the assayed tissues. DEB contains compounds exhibiting high antioxidant activity "in vivo", as evidenced by the increase in liver thiol content. Regarding broiler performance, no differences in poultry body weight and feed consumption were detected during the assay.
RESUMO
The addition of antioxidants to broiler diets has been shown to enhance their antioxidant status. Since boldo (Peumus boldus Mol.) leaves contain highly antioxidant molecules, a dried extract of boldo (DEB) was added to broiler diets to improve "in vivo" antioxidant tissue status and to favor animal growth. A DEB standardized for antioxidant content was prepared and added to poultry diets at three different levels (low-DELB, medium-DEMB, and high-DEHB) for a period of 6 weeks. A single negative control (no added antioxidant) and one positive control (supplementation with 200 mg/kg vitamin E) were used. Plasma antioxidant capacity (PAC), thiol content (GHS), and basal and induced lipoperoxidation of liver, leg and breast tissues were determined in birds at 2, 4, and 6 weeks of age. PAC increased with chicken age until week 6, but was unaffected by DEB addition at any level. However, DEB increased hepatic GSH content. No data indicated that DEB improved the resistance against induced lipoperoxidation in the assayed tissues. DEB contains compounds exhibiting high antioxidant activity "in vivo", as evidenced by the increase in liver thiol content. Regarding broiler performance, no differences in poultry body weight and feed consumption were detected during the assay.
RESUMO
A standard aqueous extract of Mangifera indica L., used in Cuba as antioxidant under the brand name VIMANG, was tested in vivo for its anti-inflammatory activity, using commonly accepted assays. The standard extract of M. indica, administered orally (50-200mg/kg body wt.), reduced ear edema induced by arachidonic acid (AA) and phorbol myristate acetate (PMA) in mice. In the PMA model, M. indica extract also reduced myeloperoxidase (MPO) activity. In vitro studies were performed using macrophage cell line J774 stimulated with pro-inflammatory stimuli lipopolysaccharide-interferon gamma (LPS-IFNgamma) or calcium ionophore A23187 to determine prostaglandin PGE(2) or leukotriene LTB(4) release, respectively. The extract inhibited the induction of PGE(2) and LTB(4) with IC(50) values of 21.7 and 26.0microg/ml, respectively. Mangiferin (a glucosylxanthone isolated from the extract) also inhibited these AA metabolites (PGE(2), IC(50) value=17.2microg/ml and LTB(4), IC(50) value=2.1microg/ml). These results represent an important contribution to the elucidation of the mechanism involved in the anti-inflammatory and anti-nociceptive effects reported for the standard extract of M. indica VIMANG.
Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Edema/prevenção & controle , Mangifera , Fitoterapia , Extratos Vegetais/farmacologia , Administração Oral , Analgésicos/administração & dosagem , Analgésicos/uso terapêutico , Animais , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/uso terapêutico , Ácido Araquidônico , Dinoprostona/biossíntese , Relação Dose-Resposta a Droga , Edema/induzido quimicamente , Eicosanoides/biossíntese , Interferon gama , Ionóforos , Leucotrieno B4/biossíntese , Lipopolissacarídeos , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos , Casca de Planta , Extratos Vegetais/administração & dosagem , Extratos Vegetais/uso terapêutico , Acetato de TetradecanoilforbolRESUMO
The antiinflammatory (per os and topic) and analgesic (per os) properties of the aerial part of Proustia pyrifolia a species in danger of extinction were investigated, and the major compounds of two of its active extracts were isolated. In addition, the evaluation of cytotoxicity in three tumoral cell lines and the acute toxicity of the crude methanol extract were also assayed, together with the antioxidant activity for the different extracts of this species. The results of the evaluation of the topic antiinflammatory activities induced by arachidonic acid, and phorbol 12-myristate 13-acetate of the different extracts showed that this species possesses active constituents that could diminish cyclo-oxygenase and lipoxygenases activities, the enzymes that allow the synthesis of proinflammatory endogenous substances as prostaglandin E(2) and leukotrienes, respectively. Our results corroborate the antiinflammatory and analgesic effects of Proustia pyrifolia, and could justify its use in folk medicine for the treatment of rheumatic and gout illnesses. From bio-active extracts beta-sitosterol, quercetin and dihydroquercetin were obtained, and these compounds could explain in part the antiinflammatory, analgesic and antioxidant activities of this species. The crude methanol extract did not present acute toxicity or cytotoxic activity, however only this extract exhibited antioxidant activity.
Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Asteraceae/química , Animais , Anti-Inflamatórios/farmacologia , Antineoplásicos Fitogênicos , Antioxidantes/farmacologia , Carragenina , Fenômenos Químicos , Físico-Química , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Edema/induzido quimicamente , Edema/prevenção & controle , Feminino , Cobaias , Dose Letal Mediana , Espectroscopia de Ressonância Magnética , Masculino , Camundongos , Medição da Dor/efeitos dos fármacos , Extratos Vegetais/farmacologia , Extratos Vegetais/toxicidade , Solventes , Espanha , Células Tumorais Cultivadas , Xantina Oxidase/antagonistas & inibidoresRESUMO
Acaena splendens H. et A. has been used in Chilean folk medicine for the treatment of fever and inflammation. A description of the in vivo reduction of bacterial pyrogen-induced fever in rabbits and carrageenan-induced paw oedema in guinea pigs is presented. The methanol extract named ME-1, obtained after succesive extractions with petroleum ether and dichloromethane, showed a strong antipyretic action (45.7% of effect), though the antiinflammatory activity was only observed after submitting this extract to column fractionation, giving a crude mixture of flavonoids named C4 with both activities (55.7% and 98.9% of antiinflammatory and antipyretic effect respectively at a dose of 600 mg/kg). The bioassay-guided fractionation by column chromatography afforded the active fraction, which contained (-,-)-epicatechin, tiliroside, 7-O-acetyl-3-O-beta-D-glucosyl-kaempferol and 7-beta-D-glucosyloxy-5-hydroxy-chromone.
Assuntos
Quempferóis , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Rosaceae , Analgésicos não Narcóticos/química , Analgésicos não Narcóticos/farmacologia , Analgésicos não Narcóticos/uso terapêutico , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Anti-Inflamatórios não Esteroides/uso terapêutico , Benzopiranos/química , Benzopiranos/isolamento & purificação , Carragenina/farmacologia , Catequina/química , Catequina/isolamento & purificação , Cromonas/química , Cromonas/isolamento & purificação , Edema/induzido quimicamente , Edema/tratamento farmacológico , Feminino , Febre/tratamento farmacológico , Flavonoides/química , Flavonoides/isolamento & purificação , Glucosídeos/química , Glucosídeos/isolamento & purificação , Cobaias , Membro Posterior/efeitos dos fármacos , Inflamação/tratamento farmacológico , Espectroscopia de Ressonância Magnética , Masculino , Medicina Tradicional , Estrutura Molecular , Naproxeno/farmacologia , Fenóis/química , Fenóis/isolamento & purificação , Fenóis/uso terapêutico , Fitoterapia , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , CoelhosRESUMO
The antiinflammatory and antipyretic activities of the petroleum ether extract (PEE), dichloromethane extract (DME) and methanol extract (ME1) of the aerial part of Psoralea glandulosa L. (Papilionaceae) were studied. The bioactivity-guided fractionation of the active extracts yielded the isolation of bakuchiol (Bk) from the petroleum ether as the active compound, cyclobakuchiols A and B (Cbk), and angelicin (Ang) from DME.
Assuntos
Analgésicos não Narcóticos/química , Analgésicos não Narcóticos/farmacologia , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Plantas Medicinais/química , Psoralea/química , Analgésicos não Narcóticos/isolamento & purificação , Animais , Anti-Inflamatórios não Esteroides/isolamento & purificação , Edema/induzido quimicamente , Edema/prevenção & controle , Éteres , Feminino , Cobaias , Espectroscopia de Ressonância Magnética , Masculino , Metanol , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Coelhos , SolventesRESUMO
Vimang is an aqueous extract of Mangifera indica used in Cuba to improve the quality of life in patients suffering from elevated stress. To assess its possible analgesic and antiinflammatory effects, the results of a standard extract evaluation are presented. Analgesia was determined using acetic acid-induced abdominal constriction and formalin-induced licking. Antiinflammatory effects were evaluated using carrageenan- and formalin-induced oedema. Vimang (50-1000 mg/kg, p.o.) exhibited a potent and dose-dependent antinociceptive effect against acetic acid test in mice. The mean potency (DE(50)) was 54.5 mg/kg and the maximal inhibition attained was 94.4%. Vimang (20-1000 mg/kg, p.o.) dose-dependently inhibited the second phase of formalin-induced pain but not the first phase. The DE(50) of the second phase was 8.4 mg/kg and the maximal inhibition was 99.5%, being more potent than indomethacin at doses of 20 mg/kg. Vimang (20-1000 mg/kg, p.o.) significantly inhibited oedema formation (p < 0.01 or p < 0.05) of both carrageenan- and formalin-induced oedema in rat, guinea-pigs and mice (maximal inhibitions: 39.5, 45.0 and 48.6, respectively). The inhibitions were similar to those produced by indomethacin and sodium naproxen, p.o. The different polyphenols found in Vimang could account for the antinociceptive and antiinflammatory actions reported here for the first time for M. indica bark aqueous extract.
Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Edema/prevenção & controle , Dor/prevenção & controle , Plantas Medicinais , Rosales , Ácido Acético , Animais , Carragenina , Relação Dose-Resposta a Droga , Edema/induzido quimicamente , Feminino , Formaldeído , Cobaias , Masculino , Camundongos , Camundongos Endogâmicos , Dor/induzido quimicamente , Medição da Dor/efeitos dos fármacos , Extratos Vegetais/farmacologia , Ratos , Ratos Sprague-DawleyRESUMO
Two previously undescribed elemanolide esters, the 2-methylpropanoate and 2-methyl-2-propenoate of 11,13-dehydromelitensin, were isolated in the course of a bioassay-guided fractionation from the aerial parts of Centaurea chilensis Hook. et Arn., used traditionally to treat 'gout and rheumatism'. The mixture of both substances exhibits anti-inflammatory activity in the carrageenan-induced paw edema assay.