Anti-ulcerogenic and antisecretory effects of Celtis iguanaea (Jacq. ) Sargent hexane leaf extract / Efeito anti-ulcerogênico e antisecretório do extrato hexânico das folhas de Celtis iguanaea (Jacq. ) Sargent

The Celtis iguanaea (Jacq.) Sargent (Cannabaceae) is one of the native species of the Cerrado region of Brazil widely used in folk medicine to treat dyspepsia. The objective of the present study was to evaluate the gastroprotective effect of the Celtis iguanaea (Jacq.) Sargent (HE) hexane leaf extract in the lesion and gastric secretion models.Antiulcerogenic activity of the Celtis iguanaea (HE) hexane leaf extract was observed with the experimental models, such as indomethacin and pyloric ligation-induced gastric ulcers. In order to evaluate the antisecretory activity of this extract, isolated Rana catesbeiana mucosa and pyloric ligation in mice were used. The HE treatment reduced the lesion index of indomethacin and pyloric ligation-induced ulcer. This extract also reduced the gastric acid secretion and total acidity (increasing the gastric pH) in mice. The secretion of H+ was reduced in the basal values (15.58 ± 1.99 µEq H+/g/15 min) when isolated Rana catesbeiana mucosa was incubated with HE. Intraduodenal administration of HE reduced the gastric secretion produced by bethanecol or histamine. The antiulcerogenic and antisecretory efficacy of HE in this study suggest anticholinergic and antihistaminergic mechanism or interruption of intracellular events that are linked to acid secretion.

Celtis iguanaea (Jacq.) Sargent (Cannabaceae) é uma das espécies nativas do cerrado brasileiro, sendo amplamente utilizada na medicina popular para o tratamento de dispepsia. O objetivo do presente trabalho foi avaliar o efeito gastroprotetor do extrato hexânico das folhas de Celtis iguanaea (Jacq.) Sargent (EH) em modelos de secreção e de lesões gástricas. A atividade antisecretória do extrato hexânico das folhas de Celtis iguanaea (EH) foi avaliada no modelo de mucosa isolada de Rana catesbeiana e pelo modelo de ligadura pilórica em camundongos. A avaliação da atividade anti-ulcerogênica do EH foi determinada no modelo de úlceras gástricas induzidas por indometacina e ligadura pilórica. Quando a mucosa de Rana catesbeiana isolada foi incubada com o EH, a secreção de H+ foi reduzida em comparação com o valor basal (15,58 ± 1,99 µEq H+/g/15 min). O tratamento com o EH reduziu o índice de lesões na úlcera induzida por indometacina e ligadura pilórica. O EH também reduziu o volume de secreção, a acidez total, e aumentou o pH gástrico. A administração intraduodenal reduziu a secreção gástrica produzida por betanecol ou histamina. A eficácia anti-ulcerogênica e antisecretória do EH neste estudo, sugere um mecanismo anticolinérgico e antihistaminérgico ou interrupção de eventos intracelulares que estão ligados à secreção ácida.

Estudo farmacognóstico de folhas e raízes da Spiranthera odoratissima A. St. -Hil. (Rutaceae) / Pharmacognostic study of the leaves and roots of Spiranthera odoratissima A. St. -Hil. (Rutaceae)

A Spiranthera odoratissima A. St.-Hil. (manacá) é um arbusto cujas raízes são utilizadas popularmente contra dores musculares, de estômago e de cabeça, disfunções hepáticas, reumatismo, e como estimulante do apetite. As folhas são empregadas como depurativo do sangue, nas afecções renais e hepáticas. O objetivo deste trabalho foi realizar o estudo morfo-anatômico de S. odoratissima, bem como a triagem fitoquímica, a determinação dos teores de água, cinzas totais e insolúveis em ácido. O material vegetal foi coletado em Leopoldo de Bulhões/ Goiás e os estudos morfo-anatômicos e a triagem fitoquímica foram realizados utilizando as técnicas convencionais. Verificou-se que a folha é hipoestomática, com estômatos anomocíticos e a epiderme apresenta papilas na face abaxial. O mesofilo é dorsiventral e a nervura principal possui drusas de oxalato de cálcio e cavidades secretoras. O pecíolo apresenta sistema vascular em forma circular. Na raiz, em crescimento primário, observou-se cilindro vascular com organização diarca. Na prospecção fitoquímica detectaram-se fenóis, taninos, cumarinas, flavonoides, triterpernos/esteróis, antraquinonas e antocianinas nas folhas e alcaloides, cumarinas, amido e saponinas nas raízes. Esses resultados são parâmetros importantes para o controle de qualidade dessa matéria-prima vegetal.

Spiranthera odoratissima A. St.-Hil. (manacá) is a shrub whose roots are popularly used against stomach pains, headache, muscle pain, liver disorders, rheumatism and as an appetite stimulant. The leaves are used as a blood depurative and for liver and kidney disease. The purpose of this work was to perform the morphological and anatomical study, the phytochemical screening and determine the water content and the levels of total and acid of S. odoratissima. The plant material was collected in Leopoldo de Bulhões/ Goiás and the morpho-anatomical studies and the phytochemical screening were performed using conventional techniques. It was verified that the leaf is hypostomatic, with anomocytic stomata and the epidermis has papillae on the abaxial surface. The mesophyll is dorsiventral and the midrib presents druses of calcium oxalate and secretory cavities. The petiole has a circular vascular system. The root in primary growth presents vascular cylinder with diarchic organization. Phenols, tannins, coumarins, flavonoids, triterpenes/sterols, anthraquinones and anthocyanins were detected in the phytochemical screening of the leaves, and alkaloids, coumarins, saponins and starch were detected in the roots. These results are important parameters for the quality control of the vegetal raw material.

Anti-inflammatory and antinociceptive activities of LQFM002 - A 4-nerolidylcatechol derivative.

AIMS: The current study describes the synthesis and pharmacological evaluation of (E)-N-(3,7-dimethylocta-2,6-dienyl)-1,3-dimethyl-1H-pyrazol-5-amine (LQFM002), a compound originally designed through a molecular simplification strategy from 4-nerolidylcatechol. LQFM002 was evaluated for preservation of the PLA(2) enzyme inhibitory effects of the lead compound, 4-nerolidylcatechol, using in vitro and in vivo models. MAIN METHODS: Rota-rod, open field and pentobarbital-induced sleeping tests were used to evaluate the effects of LQFM002 on the central nervous system. A gel plate assay of PLA(2) activity, carrageenan-induced pleurisy and TNF-α levels was used to assay anti-inflammatory activity. Antinociceptive activities of LQFM002 were evaluated with acetic acid-induced writhing, formalin and hot-plate tests, while involvement of the opioid pathway in the LQFM002 antinociceptive effect was investigated with naloxone pre-treatment. KEY FINDINGS: LQFM002 inhibited PLA(2) activity, cell migration into the pleural cavity, and capillary permeability (Evan's blue concentration) and reduced TNF-α levels in pleural exudates. LQFM002 also reduced acetic acid-induced writhing and the licking time in both phases of the formalin test and increased latency in the hot-plate test. Pre-treatment with 8.25 µmol/kg naloxone (3mg/kg) reversed the analgesic effects of LQFM002 in the early phase of the formalin test. SIGNIFICANCE: LQFM002 showed anti-inflammatory activity, which possibly involved reduction of leukocyte migration and TNF-α levels. LQFM002 also demonstrated inhibition of PLA(2) activity in vitro. LQFM002 had an antinociceptive effect that involved the opioidergic system.

Effect of extender supplementation with various antimicrobial agents on viability of Brucella ovis and Actinobacillus seminis in cryopreserved ovine semen.

The objective was to determine the effectiveness of various antimicrobial agents added to semen extender for inactivation of B. ovis or A. seminis in ovine semen after cryopreservation. In Experiment 1, 20 ejaculates from a crossbred ram infected with B. ovis were cryopreserved in Tris-based extenders with various antimicrobial agents: (I) control without antibiotics, (II) with penicillin and streptomycin (1000 IU/mL and 1 mg/mL, respectively), (III) lincomycin (0.15 mg/mL), (IV) sulphadiazine (0.60 mg/mL), and (V) gentamicin sulphate (0.25 mg/mL). Semen was stored in 0.25 mL straws at a final concentration of 150 × 10(6) spermatozoa/mL. After thawing (37 °C for 30 s), sperm total motility (TM), sperm morphology, integrity of sperm membranes, and bacterial growth were assessed. In Experiment 2, six B. ovis isolates were separately inoculated into aliquots of a fresh ejaculate from a B. ovis-free ram. Mock inoculated semen was processed for cryopreservation using the five extenders described above, and bacteriologically evaluated after thawing. In Experiment 3, sensitivity of A. seminis to the same antimicrobial agents was evaluated by inoculating an ejaculate from an A. seminis and B. ovis-free ram. There were no significant differences among treatments in post-thawing sperm parameters. B. ovis was isolated from 100% (20/20), 0% (0/20), 95% (19/20), 100% (20/20), and 5% (1/20) of semen samples diluted in tris-based extender of untreated (I) and treated semen samples with antimicrobial agents II, III, IV, and V, respectively. Frequencies of isolation from samples treated with antimicrobial agent II and V were significantly lower than untreated ones (P < 0.05). There were no significant differences in the profile of antimicrobial resistance of different B. ovis isolates. A. seminis had a similar sensitivity to the antimicrobial agents. We concluded that addition of a combination of penicillin and streptomycin or gentamicin alone to ram semen cryo-extenders inactivated B. ovis and A. seminis.

Antidepressant-like effect of Lafoensia pacari A. St.-Hil. ethanolic extract and fractions in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Lafoensia pacari A. St.-Hil. (Lythraceae) has been referred in Brazilian traditional medicine for the treatment of different diseases, among them depression. Nevertheless, there are not studies about this possible effect on the central nervous system (CNS). AIM OF THE STUDY: To evaluate the antidepressant-like effects of the ethanolic extract of Lafoensia pacari (PEtExt) and its fractions on the performance of male mice. MATERIALS AND METHODS: Antidepressant activity was studied using forced swimming (FST) and tail suspension (TST) tests, and motor activity in the open-field test. The ethanolic extract of Lafoensia pacari (PEtExt) were administered acutely (1.0 g/kg, p.o.), for 21 days (100, 300 mg, and 1.0 g/(kg day), p.o.), three administration in a 24-h period (1.0 g/kg, p.o.), and the fractions for 21 days. Imipramine (15 mg/(kg day), p.o.) was used as the control positive. RESULTS: The PEtExt significantly reduced immobility time in FST and TST, without affecting the motor activity. Only the chloroformic fraction (50 mg/(kg day), p.o.) increase the latency to immobility and decrease the immobility time in the FST. CONCLUSIONS: These data indicate that the extract of Lafoensia pacari A. St.-Hil. possesses antidepressant-like properties in mice.

Analgesic and anti-inflammatory activity of the ethanolic extract from Spiranthera odoratissima A. St. Hillaire (Manacá) roots.

Acetic acid-induced abdominal writhing, the tail flick test and carrageenan-induced peritonitis were used to study the analgesic and anti-inflammatory activity of the crude ethanolic extract from Spiranthera odoratissima roots. Pentobarbital-induced sleeping time was used to study the central depressant effect of the extract. The ethanolic extract caused a dose dependent inhibition of acetic acid-induced abdominal writhing and leukocyte migration, and produced a significant, dose-related increase in the duration of sleep. The results suggest that Spiranthera odoratissima roots contain compounds with anti-inflammatory and central depressant actions.

Anti-inflammatory effect of Solanum lycocarpum fruits.

The croton oil-induced mouse ear oedema test, acetic acid-induced abdominal writhing, and carrageenan-induced peritonitis were used to study the anti-inflammatory effects of the crude ethanol extract and its alkaloid fraction from Solanum lycocarpum fruits. The alkaloid fraction induced a dose-dependent reduction in ear oedema formation and leukocyte migration, suggesting that S. lycocarpum fruits may contain steroidal alkaloids accounting for the anti-inflammatory effect of the crude ethanol extract.