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.

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.

Levantamento etnobotânico de plantas utilizadas como anti-hiperlipidêmicas e anorexígenas pela população de Nova Xavantina-MT, Brasil / Ethnobotanical survey of plants used as anti-hyperlipidemic and anorexigenic by the population of Nova Xavantina-MT, Brazil

O presente trabalho verificou a utilização de plantas medicinais encontradas no Cerrado mato-grossense para o tratamento de hiperlipidemias e obesidade. Entrevistas com 180 pessoas acima de 50 anos foram realizadas em Nova Xavantina-MT. O questionário abordou nome popular, parte utilizada, forma de preparo e uso das espécies citadas, além de informações gerais sobre o uso de plantas. As dez plantas mais citadas foram coletadas, identificadas e estudadas por meio de uma revisão bibliográfica. A maioria dos entrevistados (95,6 por cento) declarou utilizar plantas medicinais regularmente, sendo que 71,5 por cento deles herdaram o conhecimento sobre plantas dos pais e avós e 94,20 por cento relataram aconselhar o uso aos mais jovens. Além disso, 93,6 por cento atestaram que as plantas são mais eficazes que os medicamentos de farmácia e 57 por cento consideraram forte o efeito das mesmas, ou seja, sempre resolvem o problema de saúde. Quanto aos efeitos adversos, 95,9 por cento disseram nunca ter sentido após o uso de plantas. Dos entrevistados, 56,7 por cento conheciam ou já haviam utilizado plantas medicinais no tratamento de hiperlipidemias e obesidade, sendo citadas 54 espécies medicinais diferentes pertencentes a 53 gêneros e 38 famílias, com destaque para Fabaceae (13 por cento). As dez plantas mais citadas foram: guatambu (Aspidosperma tomentosum Mart.), quina-do-cerrado (Strychnos pseudoquina St. Hil.), ipê-roxo [Tabebuia impetiginosa (Mart. Ex DC.) Standl], embaúba (Cecropia pachystachya Trec.), calunga (Simaba sp.), pata-de-vaca [Bauhinia rufa (Bong.) Steud.], mangaba (Hancornia speciosa Gomez), batata-de-tiú [Jatropha elliptica (Pohl.) Muell. Arg.], folha-de-carne (Casearia sylvestris Sw.) e manacá (Spiranthera odoratissima A. St.-Hil.). A folha foi a parte mais utilizada (46 por cento) e o preparo das plantas ocorre principalmente por meio de infusão citado por 36,5 por cento dos entrevistados. Apesar do uso popular destas plantas no combate as hiperlipidemias e obesidade, há necessidade de estudos fitoquímicos e farmacológicos que comprovem estas atividades, com vistas ao desenvolvimento de um fitoterápico.

This study checked the use of medicinal plants found in the Cerrado mato-grossense for the treatment of hyperlipidemia and obesity. Interviews with 180 people over 50 years were held in Nova Xavantina-MT. The questionnaire addressed popular name, part used, type of preparation and use of the species mentioned, beyond general information about the use of plants. The ten plants most cited were collected, identified and studied through a literature review. Most respondents (95.6 percent) said using medicinal plants regularly, while 71.5 percent of them inherited the knowledge of plants of parents and grandparents and 94.20 percent reported the use to advise youngsters. Furthermore, 93.6 percent attested that the plants are more effective than the drugs from pharmacy and 57 percent considered the strong effect of the same, i.e., they always solved health problems. Regarding adverse effects, 95.9 percent said they have never felt them after the use of plants. Of the respondents, 56.7 percent knew or had used medicinal plants in the treatment of hyperlipidemias and obesity, being cited 54 medicinal species belonging to 53 different genera and 38 families, with emphasis on Fabaceae (13 percent). The ten most cited were: guatambu (Aspidosperma tomentosum Mart.), quina-do-cerrado (Strychnos pseudoquina St. Hil.), ipê-roxo [Tabebuia impetiginosa (Mart. Ex DC.) Standl], embaúba (Cecropia pachystachya Trec.), calunga (Simaba sp.), pata-de-vaca [Bauhinia rufa (Bong.) Steud.], mangaba (Hancornia speciosa Gomez), batata-de-tiú [Jatropha elliptica (Pohl.) Muell. Arg.], folha-de-carne (Casearia sylvestris Sw.) and manacá (Spiranthera odoratissima A. St.-Hil.). The leaf was the most used (46 percent) and the preparation of the plants occurs mainly through the infusion cited by 36,5 percent of respondents. Despite the popular use of these plants for treatment of obesity and hyperlipidemia, further chemical and pharmacological studies are required to demonstrate these activities, in order to develop a phytotherapic product.

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.

Triagem da atividade antibacteriana in vitro do látex e extratos de Croton urucurana Baillon / In vitro screening of antibacterial activity of the latex and extracts from Croton urucurana Baillon

Avaliou-se a atividade antibacteriana dos látex e extratos de diferentes polaridades e farmacógenos de Croton urucurana em ensaios antimicrobianos. Os farmacógenos foram coletados em Barão de Melgaço-MT. Os extratos foram obtidos por maceração a frio em hexano, diclorometano, acetato de etila, etanol e clorofórmio, rotaevaporado e seco em estufa. No ensaio de difusão em disco, os látex mostraram potente ação contra todas as bactérias, com exceção da E. coli, não diferindo quanto à potência e espectro antibacterianos. Extratos em hexano, diclorometano e etanol das folhas mostraram atividade contra S. pyogenes, K. pneumoniae, P. aeruginosa, S. typhimurium, S. aureus e S. epidermidis nas maiores doses. Extratos da entrecasca foram ativos contra S. aureus, S. epidermidis, P. aeruginosa, E. faecalis, S. pyogenes, E. coli, K. pneumoniae e S. typhimurium. Os látex apresentaram espectro de ação e potência maiores que os extratos obtidos da entrecasca e folhas. Dos extratos obtidos da entrecasca, o clorofórmico foi o mais potente, seguido pelo etanólico, indicando a presença de diferentes princípios ativos. Na microdiluição em caldo, os látex e extratos foram ativos, porém com maior potência para os primeiros. Os resultados evidenciam atividade antibacteriana para C. urucurana, em diferentes partes da planta e por diferentes metabólitos secundários.

We evaluated the antibacterial activity of the latex and extracts from different polarities and pharmacogens of Croton urucurana using antimicrobial assays. The pharmacogens were collected in Barão de Melgaço-MT. The extracts were obtained by cold maceration in hexane, dichloromethane, ethyl acetate, ethanol and chloroform. They were concentrated in rotatory evaporator and dried in stove. In the disk diffusion assay, the latex showed a potent action against all bacterial strains, excepting E. coli, not differing in the potency and antibacterial spectrum. The hexane, dichloromethane and ethanol extracts of leaves showed activity against S. pyogenes, K. pneumoniae, P. aeruginosa, S. typhimurium, S. aureus and S. epidermidis in the major doses. Extracts obtained of stem bark were actives against S. aureus, S. epidermidis, P. aeruginosa, E. faecalis, S. pyogenes, E. coli, K. pneumoniae and S. typhimurium. The latex showed higher potency and broad-spectrum of action than extracts from stem bark and leaves. Among the stem bark extracts, the chloroform was the most potent one, followed by the ethanol extract. This result suggests the presence of different active principles. In the broth-microdilution, the latex and all extracts showed activity, even though, the latex presented more potency. Our results indicate that C. urucurana presents antibacterial activity, in different parts of the plant and by different secondary metabolites.

Attenuation of visceral nociception by alpha- and beta-amyrin, a triterpenoid mixture isolated from the resin of Protium heptaphyllum, in mice.

In the search for novel natural compounds effective against visceral nociception, the triterpenoid mixture alpha- and beta-amyrin, isolated from Protium heptaphyllum resin, was assessed in two established mouse models of visceral nociception. Mice were pretreated orally with alpha- and beta-amyrin (3, 10, 30, and 100 mg/kg) or vehicle, and the pain-related behavioral responses to intraperitoneal cyclophosphamide or to intracolonic mustard oil were analyzed. The triterpenoid mixture showed a dose-related significant antinociception against the cyclophosphamide-induced bladder pain, and at 100 mg/kg, the nociceptive behavioral expression was almost completely suppressed. Intracolonic mustard oil-induced nociceptive behaviors were maximally inhibited by 10 mg/kg alpha- and beta-amyrin mixture in a naloxone-reversible manner. While pretreatment with ruthenium red (3 mg/kg, s. c.), a non-specific transient receptor potential cation channel V1 (TRPV1) antagonist, also caused significant inhibition, the alpha (2)-adrenoceptor antagonist, yohimbine (2 mg/kg, s. c.), showed no significant effect. The triterpene mixture (10 mg/kg, p. o.) neither altered significantly the pentobarbital sleeping time, nor impaired the ambulation or motor coordination in open-field and rotarod tests, respectively, indicating the absence of sedative or motor abnormalities that could account for its antinociception. These results indicate that the antinociceptive potential of alpha- and beta-amyrin possibly involves the opioid and vanilloid (TRPV1) receptor mechanisms and further suggests that it could be useful to treat visceral pain of intestinal and pelvic origins.

Cardiovascular effects of trans-dehydrocrotonin, a diterpene from Croton cajucara in rats.

Previous studies have established the gastroprotective, hypoglycemic, and hypolipidemic effects of trans-dehydrocrotonin (t-DCTN), a major diterpene isolated from the Amazon medicinal plant Croton cajucara. This study aims to examine the potential effects of t-DCTN on hemodynamic parameters that include resting arterial blood pressure and heart rate in vivo, and on left atrial force, spontaneous beating atria, and aortic rings of rats in vitro. Intravenous bolus injections of t-DCTN (5, 10, or 15 mg/kg) to urethane anesthetized normotensive rats reduced the mean arterial pressure and heart rate in a dose-dependent manner. The hypotensive effect of t-DCTN (10 mg/kg) appears not mediated through effects on the muscarinic cholinergic receptor, beta-adrenoceptor, or ganglionic blockade, for it was not affected by atropine, propranolol, or hexamethonium but was abolished by N(w)-nitro-L-arginine methyl ester (L-NAME), a nitric oxide synthase inhibitor. The diterpene t-DCTN showed no significant influence on inotropism. In isolated rat aortic rings with intact or denuded endothelium, t-DCTN relaxed the tonic contraction induced by phenylephrine (1 microM). Its vasorelaxant effect seen at smaller concentrations in endothelium intact preparations was, however, abolished in endothelium denuded or in l-NAME treated tissues. These data indicate the hypotensive and bradycardia effects of t-DCTN, possibly related in part to the release of nitric oxide and in part to direct effects on vascular smooth muscle, and cardiac pacemaker activity.

Attenuation of capsaicin-induced acute and visceral nociceptive pain by alpha- and beta-amyrin, a triterpene mixture isolated from Protium heptaphyllum resin in mice.

The triterpene mixture, alpha- and beta-amyrin, isolated from Protium heptaphyllum resin was evaluated on capsaicin-evoked nociception in mice. Orally administered alpha- and beta-amyrin (3 to 100 mg/kg) significantly suppressed the nociceptive behaviors--evoked by either subplantar (1.6 microg) or intracolonic (149 microg) application of capsaicin. The antinociception produced by alpha- and beta-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 alpha2-adrenoceptor involvement was unlikely since yohimbine (2 mg/kg, i.p.) pretreatment failed to block the antinociceptive effect of alpha- and beta-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, alpha- and beta-amyrin could significantly block the capsaicin (10 mg/kg, s.c.)-induced hyperthermic response but not the initial hypothermia. These results suggest that the triterpene mixture, alpha- and beta-amyrin has an analgesia inducing effect, possibly involving vanilloid receptor (TRPV1) and an opioid mechanism.

Protective effect of alpha- and beta-amyrin, a triterpene mixture from Protium heptaphyllum (Aubl.) March. trunk wood resin, against acetaminophen-induced liver injury in mice.

In the search of hepatoprotective agents from natural sources, alpha- and beta-amyrin, a triterpene mixture isolated from the trunk wood resin of folk medicinal plant, Protium heptaphyllum was tested against acetaminophen-induced liver injury in mice. Liver injury was analysed by quantifying the serum enzyme activities and by histopathological observations. In mice, acetaminophen (500 mg/kg, p.o.) caused fulminant liver damage characterized by centrilobular necrosis with inflammatory cell infiltration, an increase in serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities, a decrease in hepatic glutathione (GSH) and 50% mortality. Pretreatment with alpha- and beta-amyrin (50 and 100 mg/kg, i.p. at 48, 24, and 2 h before acetaminophen) attenuated the acetaminophen-induced acute increase in serum ALT and AST activities, replenished the depleted hepatic GSH, and considerably reduced the histopathological alterations in a manner similar to N-acetylcysteine, a sulfhydryls donor. Also, the acetaminophen-associated mortality was completely suppressed by terpenoid pretreatment. Further, alpha- and beta-amyrin could potentiate the pentobarbital (50 mg/kg, i.p.) sleeping time, suggesting the possible suppression of liver cytochrome-P450. These findings indicate the hepatoprotective potential of alpha- and beta-amyrin against toxic liver injury and suggest that the diminution in oxidative stress and toxic metabolite formation as likely mechanisms involved in its hepatoprotection. In conclusion, this study supports the traditional use of Protium heptaphyllum resin as a medicinal agent and suggests the feasibility of developing herbal drugs for treatment of liver disorders.

Gastroprotective effect of the mixture of alpha- and beta-amyrin from Protium heptaphyllum: role of capsaicin-sensitive primary afferent neurons.

This investigation evaluated the role of capsaicin-sensitive afferent neurons in the gastroprotective effect of alpha- and beta-amyrin, a triterpenoid mixture isolated from Protium heptaphyllum resin. Gastric mucosai damage was induced in mice by intragastric ethanol and assessed by planimetry. Mice pretreated orally with the amyrin mixture (50 and 100 mg/kg) or capsaicin (2.5 and 5 mg/kg), the pungent principle from red hot peppers, showed a significantly lower intensity of ethanol-associated gastric mucosal damage, in relation to vehicle-treated controls. At higher doses both these agents produced either a diminished protection or no significant effect. The maximal gastroprotection that was observed at the dose of 100 mg/kg amyrin mixture was almost abolished in mice with their sensory afferents chemically ablated by a neurotoxic dose of capsaicin, suggesting that the gastro-protective mechanism of alpha- and beta-amyrin mixture involves at least in part the activation of capsaicin-sensitive primary afferent neurons.

Pentacyclic triterpenoids, alpha,beta-amyrins, suppress the scratching behavior in a mouse model of pruritus.

In the search for natural compounds useful against pruritus, alpha,beta-amyrins, the pentacyclic triterpenes isolated from the resin of popular medicinal plant Protium heptaphyllum were examined on scratching behavior induced by dextran T40 and compound 48/80 in mice. The animals were pretreated orally with alpha,beta-amyrins (50, 100 and 200 mg/kg) or cyproheptadine (10 mg/kg), an antagonist of histamine and serotonin receptors and 2 h later, they were given subcutaneous injections of dextran T40 (75 mg/kg) or compound 48/80 (3 mg/kg) into the rostral back, and scratching was quantified for 20 min. The scratching behavior induced by dextran T40 and compound 48/80 was significantly inhibited in mice pretreated with alpha,beta-amyrins (100 and 200 mg/kg) or cyproheptadine (10 mg/kg), In addition, the compound 48/80-elicited degranulation of rat peritoneal mast cells (ex vivo) was also markedly reduced in animals pretreated with alpha,beta-amyrins (100 mg/kg) or ketotifen (1 mg/kg), a known mast cell stabilizer. In the open-field test, alpha,beta-amyrins (100 and 200 mg/kg)-pretreated mice showed no impairment of spontaneous locomotion, suggesting that these triterpenoids possess no sedative activity that could account for suppression of scratching behavior. These results clearly indicate the antipruritic effect of alpha,beta-amyrins and suggest that this effect may be related to a stabilizing action on mast cell membrane.

Gastroprotective and anti-inflammatory effects of resin from Protium heptaphyllum in mice and rats.

The natural resin collected from the trunk wood of Protium heptaphyllum is used in folk medicine to treat inflammatory conditions and to hasten wound repair. In the search of new potential anti-inflammatory agents with gastroprotective property, the present study evaluated its effects in experimental models of gastric ulcer and inflammation. In mice, the resin (200 and 400 mg/kg) significantly attenuated the gastric damage induced by ethanol or acidified ethanol (HCl/ethanol), in a manner similar to N-acetyl-L-cysteine (NAC), a replenisher of sulfhydryls. Unlike NAC the resin failed to restore the ethanol-induced depletion of non-protein sulfhydryl content, indicating a different mechanism of gastroprotection. However, in 4-h pylorus-ligated rats, the resin significantly reduced the total acidity without much change in gastric secretory volume. In rats, at similar doses the resin did not modify the hind-paw edema induced by carrageenan, but effectively reduced the formation of cotton pellet-induced granuloma, suggesting its inhibitory effect on collagen formation but not on acute edema. Furthermore, the vascular permeability increase induced by acetic acid was significantly reduced in mice that received 400 mg/kg resin. The resin demonstrated no overt toxicity in mice up to an oral dose of 5 g/kg. Phytochemical analysis revealed the presence of alpha- and beta-amyrins as principal triterpenoid constituents of resin, which were previously described to have anti-ulcer property. These findings indicate the potential gastroprotective and anti-inflammatory property of P. heptaphyllum resin and further support its popular use in gastrointestinal disorders.