Antiulcerogenic Activity and Toxicity of Bauhinia holophylla Hydroalcoholic Extract.

Several species of Bauhinia are used in traditional medicine for the treatment of gastrointestinal diseases, diabetes, and inflammation, among other conditions. The aim of this study was to investigate the antiulcer effect of a hydroalcoholic extract from the leaves of B. holophylla. The chemical profile of the extract was determined by HPLC-PAD-ESI-IT-MS. A dose-effect relation was constructed using the ethanol-induced gastric ulcer model in male Wistar rats. Histological analyses and studies of antioxidant and anti-inflammatory activities were performed in stomach samples. The involvement of SH compounds, NO, K(+) ATP channels, and α 2-adrenergic receptors in the gastroprotective effect was evaluated. A toxicity study was performed with a single oral dose of 5000 mg/kg. The extract was composed mainly of cyanoglucoside and flavonol-O-glycosides derivatives of quercetin and myricetin. SH compounds, NO release, K(+) ATP channel activation, and presynaptic α 2-adrenergic receptor stimulation each proved to be involved in the antiulcer effect. The levels of GSH and activity of GR and GPx were increased, and the levels of TNF-α, IL-6 and IL-10 were modulated. There was an antidiarrheal effect and there were no signs of toxicity. B. holophylla presents antiulcer activity mainly by decreasing oxidative stress and attenuating the inflammatory response, without inducing side effects.

Abarema cochliacarpos reduces LPS-induced inflammatory response in murine peritoneal macrophages regulating ROS-MAPK signal pathway.

ETHNOPHARMACOLOGICAL RELEVANCE: Abarema cochliacarpos (Gomes) Barneby and Grimes (Fabaceae), known by the vulgar name of Babatenã, has been traditionally used in Northeast Brazil, as an anti-inflammatory remedy. Previous studies have demonstrated its anti-inflammatory and antiulcer effects in skin lesion, alcohol gastric ulcer and acute and chronic colitis. AIMS: The present study was designed to evaluate the antioxidant and anti-inflammatory effects of the butanolic fraction from A. cochliacarpos (BFAC) and its major flavonoid, (+)-catechin, in LPS-stimulated murine peritoneal macrophages. Moreover, we studied the role of mitogen-activated protein kinase (MAPK)s and NF-kB signaling pathways possibly involved in the beneficial effects. MATERIALS AND METHODS: The quantification of the extract was carried out by ultra-performance liquid chromatography analysis. Cell viability was determined using SRB assay. Nitric oxide (NO) production was analyzed by Griess method and intracellular reactive oxygen species (ROS) by fluorescence analysis. In addition, cyclooxygenase (COX-2) and inducible nitric oxide synthase (iNOS) expression, MAPK activation and IkappaBalpha (IKBα) degradation, were determined by Western blot. RESULTS: After BFAC characterization, (+)-catechin was revealed as its major constituent. Both BFAC and (+)-catechin, exerted significant anti-oxidant and anti-inflammatory effects inhibiting LPS-induced intracellular ROS and NO production in peritoneal macrophages. Additionally, the extract but also its major component reduced pro-inflammatory proteins expression probably through c-Jun N-terminal kinase and p38 MAPK signaling pathways. CONCLUSION: These data suggest that the beneficial effects of BFAC might be mediated, at least in part, by the presence of (+)-catechin. Conclusively our findings confirm the potential of A. cochliacarpos as a new therapeutic strategy for the management of inflammatory and oxidative stress-related diseases.

Antimicrobial activity of some medicinal plants of the Cerrado, Brazil.

In order to determine the potential of Cerrado plants as sources of antimicrobial activity, the phytochemical screening of ethanol extracts from Virola surinamensis, Qualea grandiflora, Alchornea castaneifolia, Hancornia speciosa and Curatella americana traditionally used in folk medicine are reported.

The gastroprotective effect of the essential oil of Croton cajucara is different in normal rats than in malnourished rats.

It has been shown previously that malnourished rats are resistant to acute gastric lesions but not to subchronic gastric ulceration. It also has been demonstrated that the essential oil obtained from the bark of Croton cajucara (Sacaca) has antiulcer properties. In the present study, the ability of this essential oil to prevent the formation of gastric ulcers in rats fed a diet with 17% protein (normoproteic rats) or 6% protein (malnourished rats) was investigated. At a dose of 100 mg/kg body weight, orally, the essential oil significantly reduced the gastric injury caused by indomethacin (25% after 2 h and 70% after 4 h) only in normoproteic rats. In the pylorus ligature model, the essential oil increased the pH and gastric volume, but decreased the total acid concentration in both groups when compared to the respective control group. The essential oil significantly increased prostaglandin E2 production in glandular cells by 50% compared to the controls in both groups of rats. In addition, the amount of gastric mucus was two-fold higher in malnourished rats than in normoproteic rats. The present results show that the enhanced protective effect of essential oil in malnourished rats involved an increase in prostaglandin E2 production and mucus secretion, which are both factors that protect the gastric mucosa against damage. In agreement with this, malnourished rats always had a lower number of acute gastric ulcers.

Strychnos L. da América do Sul e Central / Strychnos L. of South America and Central

Uma revisão do perfil químico e farmacológico é apresentada de espécies de Strychnos (Loganiaceae) ocorrentes na América do Sul e Central, incluindo o uso popular, as substâncias isoladas e suas atividades biológicas.

A review of the chemical and pharmacological profile of Strychnos species (Loganiaceae) found in South and in Central America is presented. It includes the folk uses, the isolated compounds as well as the pharmacological activities as reported in the literature.

Is gastric ulceration different in normal and malnourished rats?

Protein malnutrition can adversely affect all tissues. The aim of the present study was to test the hypothesis that protein deprivation influences gastric ulcer formation, as well as metabolism and organ growth, in rats. In the present study, there was a significant reduction in the body and organ weight of rats fed a low-protein diet (P<0.001). Malnourished rats were less susceptible to ulceration of the gastric mucosa in ethanol and indomethacin models of acute gastric ulcers when compared with rats fed a normoproteic diet (17 % protein). Mucus production and prostaglandin E2 formation increased in malnourished rats, possibly explaining the lower number of acute ulcers in these animals. Pylorus ligature altered gastric juice composition (increased pH and gastric volume, and decreased total acid concentration) in the animal group fed a low-protein diet compared with the group fed a diet containing 17 % protein (P<0.05). The gastric mucosa was more damaged in malnourished rats than in normal rats evaluated for 14 d after acetic acid injection (P<0.001). Malnourished rats exhibited resistance to acute gastric lesions, owing to an increase in prostaglandin GE2 release and mucus secretion, which protected their gastric mucosa. This phenomenon was not seen in subchronic gastric ulceration.

Flavonoids and antiulcerogenic activity from Byrsonima crassa leaves extracts.

Byrsonima crassa Niedenzu (IK) (Malpighiaceae) is used in Brazilian folk medicine for the treatment of diseases related mainly to gastric ulcers. In this study, we evaluated the potential antiulcerogenic effect of three different extracts obtained from the leaves of Byrsonima crassa namely hydromethanolic (80% MeOH), methanolic (MeOH) and chloroformic extracts (CHCl(3)). The oral administration (250, 500 and 1000 mg/kg) of all the extracts reduced the formation of lesions associated with HCl/ethanol administration in mice. The 80% MeOH extract significantly reduced the incidence of gastric lesions by 74, 78 and 92% at doses of 250, 500 and 1000 mg/kg, respectively (P<0.01). The MeOH extract reduced the ulceration by 93 and 99% only at the doses of 500 and 1000 mg/kg (P<0.01). The lower gastroprotective action (69%) was observed when animals were treated with CHCl(3) extract at the dose of 1000 mg/kg (P<0.01). Phytochemical investigation of Byrsonima crassa afforded five known substances: quercetin-3-O-beta-d-galactopyranoside, quercetin-3-O-alpha-l-arabinopyranoside, the biflavonoid amentoflavone, (+)-catechin and (-)-epicatechin. The presence of these phenolic compounds may probably explain the antiulcerogenic effect of the extracts of Byrsonima crassa leaves.

Trypanocidal activity of 2-propen-1-amine derivatives on trypomastigotes culture and in animal model.

The cis and trans isomers (either E or Z isomers) of the unsubstituted and bromo-2-propen-1-amine derivatives were evaluated in vitro on Trypanosoma cruzi. The results showed that cis is the most active isomeric form against trypomastigote forms of T. cruzi, indicating that it may contribute most to the trypanocidal effect. All mice which received 5 mg kg(-1) daily for 9 consecutive days, or 200 mg kg(-1) in a single dose of the bromo derivative of 2-propen-1-amine, survived after an infection with 10(4) trypomastigotes/ml of the Y-strain of T. cruzi. They also had a significantly lower parasitemia than the controls. However, with 100 mg kg(-1) of benznidazol for 9 consecutive days, 25% of the animals died by the end of the evaluation 40 days after infection. The involvement of the biosynthesis of ergosterol in the trypanocidal effect of the unsubstituted 2-propen-1-amine derivative was investigated on proliferative epimastigote forms of the parasite. The chromatographic analyses of the lipid extracts obtained from parasites treated with 2-propen-1-amine derivatives and controls (not treated) revealed that growth inhibition is correlated with the accumulation of squalene and the decrease of ergosterol levels. These results suggest that inhibition of the biosynthesis of ergosterol is an important target for the action of the 2-propen-1-amine derivative on T. cruzi through the inhibition of the enzyme squalene epoxidase.

Evaluation of the analgesic and antiedematogenic activities of Quassia amara bark extract.

We evaluated the possible antiedematogenic, antinociceptive and/or sedative effects of four different extracts obtained from the bark of Quassia amara namely, 70% ethanol (70EtOH), 100% ethanol (100EtOH), dichloromethane (DCM) and hexane extracts (HEX). The oral administration (100, 250 and 500 mg/kg) of these extracts did not show significant effects in any experiment. However, when administered intraperitoneally, the HEX extract decreased the paw edema induced by carrageenan, showed antinociceptive effects on the hot-plate test and on acetic acid-induced writhing, and showed sedative effects on pentobarbital-induced sleep. Naloxone did not reverse the antinociceptive effect of this extract. In conclusion, although the mechanisms are uncertain, the results demonstrated that these effects are apparently related to sedative and muscle relaxant or psychomimetic activities of the HEX extract of the plant.

Avaliação toxicológica aguda e screening hipocrático da epiisopilosina, alcalóide secundário de Pilocarpus microphyllus Stapf / Toxicological screening failure and the Hippocratic epiisopilosina, alkali secondary Pilocarpus microphyllus Stapf

A espécie Pilocarpus microphyllus Stapf. recebe a designação geral de jaborandi, fonte industrial de pilocarpina, utilizada no tratamento do glaucoma. O jaborandi contém vários alcalóides secundários. A epiisopilosina foi submetida a testes farmacológicos para determinação da DL50’ screening hipocrático e determinação do peso corporal dos animais sobreviventes da DL50. A análise dos resultados revelou que a epiisopilosina apresentou DL50 duas vezes maior que a pilocarpina. Os animais que sobreviveram à determinação da DL50 ganharam peso no período de 14 dias de observação. A eplisopilosina demonstrou ser um estimulante periférico do sistema nervoso parassimpático, semelhante à pilocarpina, somente em altas doses.

Pilocarpus microphyllus Stapf. (Rutaceae) is a source for industrial isolation of pilocarpine, alkaloid used in the treatment of glaucoma. It contains several secondary alkaloids; one of them being eplisopilosine. Pharmacological evaluation showed DL50 value of epiisopilosine two times higher than of pilocarpine. Epiisopilosine also showed to be a pilocarpine-like peripheric stimulant of parasympatic nervous system, although in higher dosis.

Avaliaçäo toxicológica aguda e "screening" hipocrático da Anchietae St. Hill. - Violaceae / Acute toxicology assay and hipocratic screening of Anchietae salutaris St. Hill

O uso indiscriminado de plantas medicinais pode levar a intoxicaçöes, mesmo aquelas que possuem grande emprego na medicina popular. Neste trabalho avaliou-se a toxicidade aguda da Anchietae salutaris St. Hill, através da determinaçäo da DL50 e "screening" hipocrático. Em ambos os experimentos, foram utilizados camundongos que receberam o extrato por via oral e intraperetoneal, em diferentes níveis de dose. Vários parâmetros foram monitorados durante o período de observaçäo (14 dias). A análise dos resultados revelou que esta espécie, quando administrada por via oral, näo apresenta sinais de toxicidade; entretanto, quando a administraçäo é feita por via intraperitoneal, observa-se depressao do sistema motor e de alguns parâmetros relacionados aos sistemas nervosos central e periférico.