Topical Antiedematogenic Activity of the Essential Oil of Psidium brownianum Mart. (OEPB) in Murine Ear Edema Models.

Psidium brownianum Mart is reported in the literature by antinociceptive and antioxidant activities, indicating that this species' secondary metabolites might be used to control inflammatory processes. The present study aimed to characterize the topical antiedematogenic activity of the essential oil of Psidium brownianum Mart. (OEPB) in ear edema models by different inflammatory agents. Female Swiss mice (25-35 g) and Wistar albino rats (200-300 g) were used throughout tests (n=6/group) on acute or chronic edema models induced by single and multiple topical applications. The OEPB is administered topically pure or at a concentration of 100 or 200 mg/mL. The antiedematogenic mechanism of OEPB was analyzed by administering capsaicin, arachidonic acid, histamine, and phenol at the best effective dose (200 mg/mL). The results showed a significant reduction of edema-induced single (28.87 %) and multiple (50.13 %) applications of croton oil compared to the negative control group. Regarding potential mechanisms of action, OEPB (200 mg/mL) inhibited the development of edema triggered by capsaicin (29.95 %), arachidonic acid (22.66 %), phenol (23.35 %), and histamine (75.46 %), suggesting an interference with the histaminergic pathway. These results indicate that OEPB presents a topical antiedematogenic effect in acute and chronic murine models, possibly interfering with inflammatory pathways triggered by mediators such as histamine.

Hypoglycemic, Hypolipidemic, and Anti-Inflammatory Effects of Beta-Pinene in Diabetic Rats.

Background: Diabetes is a metabolic disease linked to multiple comorbidities, such as low-grade inflammation. ß-pinene, a monoterpene commonly found in aromatic plants, is endowed with anti-inflammatory effect and this fact lead us to investigate the possible hypoglycemic, hypolipidemic and anti-inflammatory effects of the monoterpene in the alloxan-induced diabetes experimental model. Methods: Male Wistar rats (200-250 g) were treated orally with ß-pinene (25, 50, 100, and 200 mg/kg) or glibenclamide (5 mg/kg), for seven consecutive days. Diabetes was induced by alloxan (40 mg/kg) through the penile vein. On the seventh day of treatment, blood samples were collected for biochemical analysis. The anti-inflammatory effect of ß-pinene was evaluated using the carrageenan-induced paw edema model, followed by the carrageenan-induced peritonitis. Results: The treatment with ß-pinene decreased plasma glucose, triglyceride, VLDL, LDL, and HDL levels, when compared to those of the control group. In addition, the association ß-pinene 10 mg/kg + glibenclamide 2 mg/kg significantly decreased blood glucose, total cholesterol, and triglyceride level. Finally, oral treatment with ß-pinene reduced carrageenan-induced paw edema and leukocyte migration in the peritoneum. Taken together, our results indicate that ß-pinene shows hypoglycemic and hypolipemic effects, which may involve some common mechanisms of glibenclamide. Besides, the monoterpene presented an anti-inflammatory action in diabetic rats that needs further investigation in order to clarify such effect and its correlation with the alterations observed in plasma parameters of ß-pinene-treated diabetic rats.

Comparative analysis of chemical profiles and antioxidant activities of essential oils obtained from species of Lippia L. by chemometrics.

Due to the importance of diseases associated with oxidative stress, the search for natural antioxidants proves to be essential. This work aimed to compare the chemical composition and antioxidant potential of essential oils from the genus Lippia L. through chemometric analysis. The essential oils were characterized by gas chromatography coupled with mass spectrometry. Antioxidant potentials were determined by DPPH, ABTS, Deoxyribose and ß-carotene protection, Iron chelation and reduction methods. All data were related by multivariate analyzes. Essential oils showed low similar chemical compositions and no statistically significant relationship. These showed relevant antioxidant activity, especially for L. sidoides that obtained IC50 of 5.22 ± 0.08 µg/mL in ABTS capture. Multivariate analyzes showed the effectiveness of L. alba compounds to DPPH scavenging, Fe3+ reduction and ß-carotene protection, and L. gracilis components to deoxyribose protect. Thus, studies proving the antioxidant potential of Lippia compounds against oxidative stress and their use in food conservation are fundamental.

Pharmacological screening of the phenolic compound caffeic acid using rat aorta, uterus and ileum smooth muscle.

Caffeic acid is a phenolic compound widely found in commonly consumed foods such as pears, apples and coffee, and is pharmacologically known for its antioxidant, anti-inflammatory and anti-asthmatic properties. However, its relaxant activity in the aorta, uterus and ileum smooth muscle has not been investigated. This study aimed to comparatively evaluate the effect of caffeic acid on smooth muscle from different organs (aorta, uterus and ileum), and the contractions of this different organ were induced by different agonists. The organ bath technique was used, where the organs were placed in different cuvettes with 10 mL of Tyrode solution for 1 h to stabilize, then, myometrial, intestinal strip and aortic ring contractions were evoked using different contractile agonists (KCl 60 mM, PHE 0.1 µM, OT 10-2 IU/mL, CCh 10-6 M and BaCl2 0.1-30 mM); increasing concentrations of caffeic acid (0.03-7 mM) were administered in the experimental preparations. In the presence of KCl (60 mM), caffeic acid caused relaxations with the following EC50 values: 2.7 ± 0.26 mM/mL (aorta), 5.7 ± 0.71 mM/mL (uterus) and 2.1 ± 0.39 mM/mL (ileum). When in the presence of different agonists, PHE (0.1 µM) for the aorta, OT (10-2 IU/mL) for the uterus and CCh (10-6 M) for the ileum, caffeic acid caused relaxations with EC50 values of: 2.7 ± 0.31 mM/mL; 2.2 ± 0.34 mM/mL and 2.0 ± 0.28 mM/mL, respectively. The inhibitory effect of caffeic acid on serotonergic (aorta and uterus) and muscarinic receptors (uterus and ileum), as well as its possible involvement with L-type Ca2+ channels, was also observed. This study reports the pharmacological characterization of caffeic acid on smooth muscle from different organs, for which caffeic acid was more potent in the ileum. A diverse understanding of its performance as a possible therapeutic product is attributed to its relaxant effect.

Antinociceptive activity of the Psidium brownianum Mart ex DC. leaf essential oil in mice.

Chronic pain management has several adverse effects and research looking for new and effective pain management drugs posing lower undesirable effects is necessary. Given the above, the pharmacological investigation of medicinal plants significantly contributes to the dissemination of plant-derived therapeutics. The aim of this study was to evaluate the antinociceptive activity of the Psidium brownianum Mart ex DC. leaf essential oil (PBEO) and the participation of the opioid pathway in this effect in mice. Swiss Mus musculus male mice were tested using acute nociception models (acetic acid induced abdominal contortions, formalin, capsaicin and hot plate tests). The possible myorelaxant action of the PBEO was tested using the rotarod test. The essential oil reduced animal nociception in chemical and heat models, with this action being devoid of a myorelaxant effect. Naloxone (2 mg/kg, intraperitoneally - i.p.) partially antagonized the PBEO activity, possibly acting via opioid receptors. The results obtained provide evidence that the traditional Psidium brownianum use may be effective for pain treatment.

Anxiolytic and antidepressant-like effects of Annona coriacea (Mart.) and caffeic acid in mice.

This research evaluated the anxiolytic and antidepressant-like effects of a hydroethanolic extract from the leaves of Annona coriacea (EHFAC) and caffeic acid (CA). Mice were intraperitoneally treated with saline, EHFAC (1, 10, 20 mg/kg) or CA (0.15 mg/kg) and subject to the elevated plus-maze, open field, rota-rod, forced swimming and reserpine-induced akinesia tests. Pro-convulsant and anticholinergic effects were also evaluated. EHFAC presented anxiolytic-like effect on the elevated plus-maze, which was partially reversed by flumazenil. A similar effect was observed with CA. In the forced swimming test, EHFAC and CA reduced the immobility time of mice; such effect was potentiated when EHFAC or CA were associated with imipramine, bupropion and fluoxetine. The antidepressant-like effect was reinforced as EHFAC partially reversed the reserpine-induced akinesia. In addition, a pre-treatment with EHFAC and CA did not decrease the latency to 1st seizure of animals that received a sub-convulsive dose of PTZ, nor reduced the intensity of oxotremorine-induced tremors. Taken together, the results indicate that EHFAC and CA have anxiolytic and antidepressant-like effects, which involve important neurotransmitter systems, such as GABAergic and monoaminergic ones, being devoid of side effects, commonly associated with classical psychotropic drugs.

Phytochemical Analysis and Central Effects of Annona Muricata Linnaeus: Possible Involvement of the Gabaergic and Monoaminergic Systems.

Annona muricata Linnaeus (Annonaceae), popularly known as graviola, is used in folk medicine as both sedative and anticonvulsant. This study correlates the neurochemical profile with the behavioral effects of the hydroalcoholic extract from the leaves of Annona muricata (HLEAM) in mice, proposing to elucidate their mechanism of action on the central nervous system. Flavonoids and phenolic compounds were identified and quantified by High Performance Liquid Chromatography (HPLC) method. The acute toxicity (median lethal dose - LD50) was determined by probitos method using the percentage of mortality based on the Hippocratic screen. HLEAM (25, 50 and 100 mg/kg) was tested, intraperitoneally (i.p.), in models of sedation, anxiety, motor coordination, and seizures. The endogenous levels of dopamine, norepinephrine and DOPAC were assayed by reverse-phase HPLC with electrochemical detection. The HPLC analysis of the extract revealed the presence of flavonoids (quercetin, isoquercitrin, quercitrin, rutin, and kaempferol) and phenolics acids (gallic, chlorogenic, ellagic and caffeic acids). The LD50 was 1091.7 mg/kg and Hippocratic screening indicated central nervous system depressant effect. HLEAM presented sedative effects at doses of 25, 50, and 100 mg/kg, as well as anxiolytic and anticonvulsant effects at a dose of 100 mg/kg. In addition, these effects were partially reversed by flumazenil. The monoamines analysis by HPLC showed that HLEAM decreased the level of norepinefrine and dopamine in the mouse brain striatum. Thus, the results indicate a possible interaction of HLEAM with the GABAergic and monoaminergic systems, adding medicinal value to the popular use of the plant for the treatment of behavioral and neurological disorders.

Caffeine-supplemented diet modulates oxidative stress markers and improves locomotor behavior in the lobster cockroach Nauphoeta cinerea.

The effects of caffeine supplementation is well documented in conventional animal models, however, in the lobster cockroaches Nauphoeta cinerea, they have not been reported. Thus, the aim of this study was to investigate the locomotor behavior and biochemical endpoints in the head of the nymphs of N. cinerea following 60 days exposure to food supplemented with 0, 0.5, 1.0, 2.5, 5.0 and 10.0 mg of caffeine/g of diet. The analysis of the locomotor behavior using the video-tracking software, Any-maze, for 12 min revealed that caffeine supplementation caused significant behavioral improvement. There was increase in distance travelled, velocity, frequency of rotation and turn angle (stereotypical behavior such as circling movements), and this was supported by the representative track plots of the path travelled by cockroaches in the open-field arena. In addition, caffeine supplementation markedly increased total thiol and non-protein thiol glutathione (GSH) levels in the heads of cockroaches, and this was in parallel with significant reduction of lipid peroxidation and free Fe(II) content. Taking together, our results indicate that long-term caffeine supplementation may exert preventive effects against oxidative stress and support the use of N. cinerea as an efficient alternative model to assess the efficacy of food molecules.

Evaluation of the antioxidant and gastroprotective activity and HPLC analysis of the hydroalcoholic extract of Tocoyena formosa leaves (Cham. & Schlecht) K. Schum.

The peptic ulcer is a gastric disorder that affects millions of people and yet they cause many side effects. In this sense, natural products represent an important alternative to the discovery of compounds with gastroprotective activity. The present work has as its objective to evaluate the antioxidant and gastroprotective activity of the Hydroalcoholic Extract of Leaves from Tocoyena formosa (Cham. & Schlecht.) K. Schum (HELTF), this being much emphasized in traditional medicine for inflammatory morbidities and gastric symptoms. For the evaluation of the antioxidant activity, FRAP and DPPH tests were carried out, and for the evaluation of the gastroprotective activity, gastric lesion induction by ethanol, acidified ethanol, indomethacin and physical barrier tests were used. Antioxidant assay of HELTF revealed an EC50 of 558.66 µM FeSO4/g and IC50 of 189.78 µg/ml for FRAP and DPPH respectively. In gastroprotective, in ethanol model, all the doses presented significant activity in comparison to controls, however, in the gastric lesion induction test by acidified ethanol and indomethacin, only the dose of 200 mg/kg presented with significance. In the physical barrier test presented evidence that protection by the formation of a protective layer associated with mucus. Concluded, therefore, that HELTF possesses antioxidant and significate gastroprotective activity.

Modulação in vitro da atividade antibiótica pelo óleo essencial dos frutos de Piper tuberculatum Jacq / Modulación in vitro de la actividad antibiótica por el aceite esencial de frutos de Piper tuberculatum Jacq / In vitro modulation of the antibiotic activity of essential oil from fruits of Piper tuberculatum Jacq

Introdução: Piper tuberculatum Jacq., popularmente conhecida como pimenta-longaou pimenta-d'Arda, é utilizada empiricamente no tratamento de doenças respiratórias (asma, bronquite e tosse) e digestivas (dores abdominais e diarreias). Na literatura é descrita com importantes atividades anti-inflamatória, antimicrobiana, antileucêmico e anti-helmíntica. Objetivos: avaliar a atividade moduladora do óleo essencial dos frutos de P. tuberculatum (OEPT) em associação com diferentes antibióticos frente à Staphylococcus aureus, Escherichia coli e Pseudomona aeruginosa. Metodos: Os frutos (frescos) de P. tuberculatum foram coletados em Barbalha/CE e submetidos à hidrodestilação em aparelho tipo Clevenger para ser extraído o óleo essencial, após a extração o óleo essencial foi tratado com sulfato de sódio anidro para eliminação da umidade residual. A avaliação da atividade antibacteriana e modulação (em resistência bacteriana) frente às cepas de S. aureus (SA358), E. coli (EC27) e P. aeruginosa (PA03) foram determinadas pelo método de microdiluição para identificar a concentração inibitória mínima (CIM), realizada em triplicata. CIM de ≤ 256 µg/mL foi considerado clinicamente relevante. Resultados: a atividade antibacteriana do OEPT exibiu um CIM de ≥ 1024 µg/mL contra as cepas de bactérias de padrão resistente a múltiplas drogas. Na avaliação da atividade moduladora, o OEPT antagonizou o efeito da amicacina contra E. coli e S. aureus, mas teve efeito sinérgico contra P. aeruginosa. Combinado com a getamicina o óleo exibiu antagonismo frente a E. coli, no entanto não apresentou resultado relevante contra S. aureas e P. aeruginosa. A associação do OEPT com o antibiótico imipenem resultou efeito mais relevante, apresentando sinergismo para todas as bactérias avaliadas, por outro lado, em associação com ciprofloxacino não apresentou efeito significante em relação ao controle. Conclusão: O OEPT apresentou uma melhor atividade quando associado ao imipenem frente todas as bactérias avaliadas, mostrando ser uma possível alternativa no desenvolvimento de novos fármacos com atividade antibacteriana advindos de produtos fitoterápicos(AU)

Introducción: Piper tuberculatum Jacq. popularmente conocida como pimenta-longa o pimenta-d'Arda, se utiliza empíricamente en el tratamiento de enfermedades respiratorias (asma, bronquitis y tos) y digestivas (dolor abdominal y diarrea). En la literatura es describe con importantes actividades antiinflamatorias, antimicrobianas, antileucémicas y antihelmínticas. Objetivo: evaluar la actividad moduladora de los aceites esenciales de frutos de P. tuberculatum (AEPT) en asociación con diferentes antibióticos contra Staphylococcus aureus, Escherichia coli y Pseudomona aeruginosa. Metodología: los frutos (frescos) de P. tuberculatum fueron recolectados en Barbalha/CE y sometidos a hidrodestilación en un equipo Clevenger, para extraer el aceite essencial (AEPT), el cual, una vez extraído, fue tratado con sulfato de sodio anhidro para eliminar la humedad residual. Se evaluó su actividad antibacteriana contra las cepas de S. aureus (SA358), E. coli (EC27) y P. aeruginosas (PA03). Empleando el método de microdilución se determinó la concentración inhibitoria mínima (CIM), con tres réplicas por cada tratamiento. Un valor de CIM ≤ 256 µg/mL se considera clínicamente relevante. Resultados: la actividad antibacteriana del AEPT exhibió una CIM ≥ 1024 µg/mL contra las cepas estándar de bacterias resistentes a múltiples fármacos. En efecto, la actividad AEPT antagoniza el efecto de amikacina contra E. coli y S. aureus, pero tenía un efecto sinérgico contra P. aeruginosa. Combinado con la getamicina el aceite exhibió antagonismo contra E. coli, sin embargo no presentó resultado relevante ante S. aureus y P. aeruginosa. La asociación de AEPT con el antibiótico imipenem resultó el efecto más relevante, mostrando sinergismo frente a todas las bacterias evaluadas. Por el contrario, en asociación con ciprofloxacina no mostró ningún efecto significativo con respecto al control. Conclusión: el AEPT presentó una mejor actividad cuando se asoció a imipenem, frente todas las bacterias evaluadas, demostrando ser una posible alternativa en el desarrollo de nuevos fármacos con actividad antimicrobiana, a partir de productos herbarios(AU)

Introduction: Piper tuberculatum Jacq., commonly known as pimenta-longa or pimenta-d'Arda, is empirically used to treat respiratory conditions (asthma, bronchitis and coughing) and digestive disorders (abdominal pain and diarrhea). Reference may be found in the literature to outstanding antiinflammatory, antimicrobial, antileukemic and antihelmintic activity. Objective: Evaluate the modulatory activity of essential oils from fruits of P. tuberculatum (AEPT) combined with various antibiotics againstStaphylococcus aureus, Escherichia coli and Pseudomona aeruginosa. Methods: Fresh fruits of P. tuberculatum were collected in Barbalha, CE, and subjected to hydrodistillation in a Clevenger set to extract the essential oil (AEPT). The oil extracted was then treated with anhydrous sodium sulfate to eliminate residual humidity. Antibacterial activity was evaluated against strains of S. aureus (SA358), E. coli (EC27) and P. aeruginosas (PA03). Minimum inhibitory concentration (MIC) was determined by the microdilution method, with three replications for each treatment. A MIC ≤ 256 µg/mL was considered to be clinically relevant. Results: Antibacterial activity of AEPT displayed a MIC of ≥1024 µg/mL against standard strains of multi-drug resistant bacteria. In fact, activity of AEPT antagonized the effect of amikacin against E. coli and S. aureus, but had a synergic effect against P. aeruginosa. Combined with gentamicin, the oil exhibited antagonism against E. coli, but no relevant result was obtained against S. aureus and P. aeruginosa. Combination of AEPT with the antibiotic imipenem had the most relevant effect, displaying synergism against all the bacteria evaluated. However, in combination with ciprofloxacin it did not show any significant effect with respect to the control. Conclusion: AEPT displayed better activity against all the bacteria evaluated when combined with imipenem, proving to be a possible alternative for the development of new herbal drugs with antimicrobial activity(AU)

Modulação in vitro da atividade antibiótica pelo óleo essencial dos frutos de Piper tuberculatum Jacq / In vitro modulation of the antibiotic activity of essential oil from fruits of Piper tuberculatum Jacq

Introdução: Piper tuberculatum Jacq., popularmente conhecida como pimenta-longa ou pimenta-d'Arda, é utilizada empiricamente no tratamento de doenças respiratórias (asma, bronquite e tosse) e digestivas (dores abdominais e diarreias). Na literatura é descrita com importantes atividades anti-inflamatória, antimicrobiana, antileucêmico e anti-helmíntica. Objetivos: avaliar a atividade moduladora do óleo essencial dos frutos de P. tuberculatum (OEPT) em associação com diferentes antibióticos frente à Staphylococcus aureus, Escherichia coli e Pseudomona aeruginosa. Metodos: Os frutos (frescos) de P. tuberculatum foram coletados em Barbalha/CE e submetidos à hidrodestilação em aparelho tipo Clevenger para ser extraído o óleo essencial, após a extração o óleo essencial foi tratado com sulfato de sódio anidro para eliminação da umidade residual. A avaliação da atividade antibacteriana e modulação (em resistência bacteriana) frente às cepas de S. aureus (SA358), E. coli (EC27) e P. aeruginosa (PA03) foram determinadas pelo método de microdiluição para identificar a concentração inibitória mínima (CIM), realizada em triplicata. CIM de ≤ 256 µg/mL foi considerado clinicamente relevante. Resultados: a atividade antibacteriana do OEPT exibiu um CIM de ≥ 1024 µg/mL contra as cepas de bactérias de padrão resistente...(AU)

Introducción: Piper tuberculatum Jacq. popularmente conocida como pimenta-longa o pimenta-d'Arda, se utiliza empíricamente en el tratamiento de enfermedades respiratorias (asma, bronquitis y tos) y digestivas (dolor abdominal y diarrea). En la literatura es describe con importantes actividades antiinflamatorias, antimicrobianas, antileucémicas y antihelmínticas. Objetivo: evaluar la actividad moduladora de los aceites esenciales de frutos de P. tuberculatum (AEPT) en asociación con diferentes antibióticos contra Staphylococcus aureus, Escherichia coli y Pseudomona aeruginosa. Metodología: los frutos (frescos) de P. tuberculatum fueron recolectados en Barbalha/CE y sometidos a hidrodestilación en un equipo Clevenger, para extraer el aceite essencial (AEPT), el cual, una vez extraído, fue tratado con sulfato de sodio anhidro para eliminar la humedad residual. Se evaluó su actividad antibacteriana contra las cepas de S. aureus (SA358), E. coli (EC27) y P. aeruginosas (PA03). Empleando el método de microdilución se determinó la concentración inhibitoria mínima (CIM), con tres réplicas por cada tratamiento. Un valor de CIM ≤ 256 µg/mL se considera clínicamente...(AU)

Introduction: Piper tuberculatum Jacq., commonly known as pimenta-longa or pimenta-d'Arda, is empirically used to treat respiratory conditions (asthma, bronchitis and coughing) and digestive disorders (abdominal pain and diarrhea). Reference may be found in the literature to outstanding antiinflammatory, antimicrobial, antileukemic and antihelmintic activity. Objective: Evaluate the modulatory activity of essential oils from fruits of P. tuberculatum (AEPT) combined with various antibiotics againstStaphylococcus aureus, Escherichia coli and Pseudomona aeruginosa. Methods: Fresh fruits of P. tuberculatum were collected in Barbalha, CE, and subjected to hydrodistillation in a Clevenger set to extract the essential oil (AEPT). The oil extracted was then treated with anhydrous sodium sulfate to eliminate residual humidity. Antibacterial activity was evaluated against strains of S. aureus (SA358), E. coli (EC27) and P. aeruginosas (PA03). Minimum inhibitory concentration (MIC) was determined by the microdilution method, with three replications for each treatment. A MIC ≤ 256 µg/mL was considered to be clinically relevant. Results: Antibacterial activity of AEPT displayed a MIC of ≥1024 µg/mL against standard strains of multi-drug resistant bacteria. In fact, activity of AEPT antagonized the effect of amikacin against...(AU)

Avaliação da atividade anti-Leishmania e anti-Trypanosoma do extrato etanólico das folhas de Annona squamosa L / Evaluation of the anti-leishmania and anti-trypanosoma activity of ethanolic extract from the leaves of Annona squamosa L

As doenças parasitárias, também chamadas de “doenças negligenciadas”, continuam sendo uma grande dificuldade para o desenvolvimento social e econômico dos países mais pobres. Podemos citar como exemplo dessas doenças, a leishmaniose e a doença de Chagas. A leishmaniose é causada por parasitas do gênero Leishmania e afeta cerca de 12 milhões de pessoas. A doença de Chagas, causada pelo protozoário Trypanosoma cruzi, causa aproximadamente 50.000 mortes por ano. Os fármacos disponíveis para o tratamento dessas doenças são altamente tóxicos, sendo este um dos motivos que leva à busca por drogas eficazes e seguras para seus tratamentos. As folhas da Annona squamosa, espécie da família Annonaceae, já foram descritas na literatura por suas atividades hepatoprotetora, antiparasitária, pesticida e antimicrobiana. Nesse estudo avaliamos a atividade anti-leishmania e tripanocida do extrato etanólico das folhas de Annona squamosa L. (EEAS) em formas promastigota do parasita Leishmania braziliensis e Leishmania infantum e epimastigota de Trypanosoma cruzi, além de avaliar a atividade citotóxica em fibroblasto. Os resultados demonstram que o extrato apresentou uma melhor atividade contra Leishmania infantum e Leishmania brasiliensis quando comparados com Trypanosoma cruzi; e que apresentou uma maior toxicidade nas concentrações de 500 e 1000 μg/ml, com mortalidade dos fibroblastos de aproximadamente 85% e 100%, respectivamente. Esse estudo aponta para uma perspectiva terapêutica alternativa que se mostrou eficaz frente aos parasitas aqui estudados, exceto a forma epimastigota de Trypanosoma cruzi. Com relação aos testes de citotoxicidade fazem-se necessários novos testes, uma vez que apresentou um alto nível de toxicidade, viabilizando assim futuros ensaios in vivo.

The parasitic diseases, also calls by “neglected diseases”, continue being a major difficulty for the social and economic development of the poorest countries. We can cite as an example of these diseases, the leishmaniasis and the Chagas disease. Leishmaniasis is caused by parasites of the genus Leishmania and affects about 12 million people. The Chagas disease, caused by the protozoan Trypanosoma cruzi, causes approximately 50,000 deaths per year. The drugs available for the treatment of these diseases are highly toxic, being this one of the reasons that leads to the search for effective and safe drugs for their treatments. The leaves of the Annona squamosa, species of the family Annonaceae, have already been described in the literature by their hepatoprotective activities, antiparasitic, pesticide and antimicrobial. In this study we assessed the activity tripanocidal and antileishmania of ethanolic extract from the leaves of Annona squamosa L. (EEAS) in promastigota forms of the parasite Leishmania braziliensis and Leishmania infantum and epimastigota of Trypanosoma cruzi, in addition to evaluating the cytotoxic activity in fibroblasts. The results demonstrate that the extract presented a better activity against Leishmania infantum and Leishmania brasiliensis when compared with Trypanosoma cruzi; and which presented a greater toxicity at concentrations of 500 and 1000 μg/ml, with mortality of fibroblasts of approximately 85% and 100%, respectively. This study points to an alternative therapeutic perspective that showed effective against the parasites here studied, except the epimastigota form of Trypanosoma cruzi. With relation to cytotoxicity tests are required new tests, once presented a high level of toxicity, thus enabling future in vivo assays.

Atividade moduladora sobre antibióticos pelo extrato aquoso das folhas de Bauhinia ungulata L / Actividad modulador acerca de antibióticos por el extracto acuoso de las hojas de Bauhinia ungulata l / Modulatory activity about antibiotics by aqueous extract of the leaves of Bauhinia ungulata l

Introdução: cepas de Staphylococcus aureus, Escherichia coli e Pseudomonas aeruginosa são caracterizadas como importantes causadores de infeções bacterianas e destacam-se como um preocupante problema de saúde pública. A atividade antibacteriana de várias plantas tem sido estudada com a finalidade de diminuir a resistência microbiana existente com relação aos fármacos já industrializados. O gênero Bauhinia compreende cerca de 300 espécies que são conhecidas no Brasil como pata-de-vaca. A espécie Bauhinia ungulata Lin é bastante utilizada no controle glicêmico, mas, também, apresenta outras atividades, dentre elas é relatado uma ação antibacteriana. Objetivo: verificar o potencial modulador da espécie B. ungulata em associação a outros medicamentos já testados contra cepas de S. aureus, E. coli e P. aeruginosa. Métodos: as folhas da B. ungulata Lin foram coletadas no distrito de Arajara, Chapada do Araripe, estado do Ceará, Brasil. Foi utilizado o extrato aquoso das folhas de Bauhinia ungulata em associação aos antibióticos Amicacina, Gentamicina, Imipenem e Ciprofloxacino, esperando que o extrato agisse com antagonismo ou sinergismo frente ao efeito dos antibióticos. Resultados: o extrato das folhas de B. ungulata Lin apresentou relevante atividade sinérgica sobre os antibióticos utilizados (amicacina, gentamicina, imipenem e ciprofloxacino). Conclusão: portanto, o extrato em associação com os fármacos potencializou o efeito destes, revelando uma atividade antibacteriana significante(AU)

Introducción: las cepas de Staphylococcus aureus, Escherichia coli e Pseudomonas aeruginosa son causa importante de infecciones bacterianas y se destacan como un problema de salud pública. La actividad antibacteriana de varias plantas se ha estudiado con el fin de reducir la resistencia microbiana existente con respecto a los medicamentos ya industrializados. El género Bauhinia comprende alrededor de 300 especies que se les conoce en Brasil como pata-de-vaca. La especie Bauhinia ungulata Lin es ampliamente utilizada en control de la glucemia, pero también ofrece otras actividades, entre ellas es divulgado una acción antibacteriana. Objetivo: verificar el potencial modulador de las especies B. ungulata en asociación con otros fármacos probados contra cepas de S. aureus, E. coli y P. aeruginosa. Métodos: las hojas de B. ungulata Lin fueron recolectados en el distrito de Arajara, Chapada do Araripe, estado de Ceará, Brasil. Se utilizó el extracto acuoso de hojas de B. ungulata en asociación con antibióticos amikacina, gentamicina imipinem y ciprofloxacina, con la esperanza de que el extracto actúa con antagonismo o sinergismo, delantero de los efectos de los antibióticos. Resultados: el extracto de las hojas de B. ungulata Lin presenta relevante actividad sinérgica de los antibióticos utilizados (amikacina, gentamicina, ciprofloxacina y imipinem). Conclusión: el extracto en asociación con las drogas aumentó el efecto de estos, revelando una significativa actividad antibacteriana(AU)

Introduction: strains of Staphylococcus aureus, Escherichia coli e Pseudomonas aeruginosa are characterized as important causes of bacterial infections and stand out as a worrying public health problem. The antibacterial activity of several plants has been studied for the purpose of reducing the existing microbial resistance with respect to drugs already industrialized. The genus Bauhinia it comprises about 300 species they are known in Brazil as pata-de-vaca. The specie Bauhinia ungulata Lin is widely used in glycemic control, but also features other activities, among them is reported an antibacterial action. Objective: to verify the potential modulator of the species B. ungulata in association with other drugs tested against strains of S. aureus, E. coli and P. aeruginosa. Methods: The leaves of B. ungulata Lin were collected in the District of Arajara, Chapada do Araripe, Ceará state, Brazil. We used the water extract of leaves of B. ungulata in association with antibiotics amikacin, gentamicin, imipinem and ciprofloxacin, hoping that the extract acted with antagonism or synergism, front of the effects of antibiotics. Results: the extract of the leaves of B. ungulata Lin presented relevant synergistic activity about the antibiotics used (amikacin, gentamicin, ciprofloxacin and imipinem). Conclusion: therefore, the extract in association with the drugs increased the effect of these, revealing a significant antibacterial activity(AU)

Anti-inflammatory and antiedematogenic activity of the Ocimum basilicum essential oil and its main compound estragole: In vivo mouse models.

The genus Ocimum are used in cooking, however, their essential oils are utilized in traditional medicine as aromatherapy. The present study was carried out to investigate the chemical composition and systemic anti-inflammatory activity of the Ocimum basilicum essential oil (EOOB) and its major component estragole, as well as its possible mechanisms of action. The Ocimum basilicum essential oil was obtained by hydrodistillation and analyzed by GC-MS. The anti-inflammatory action was verified using acute and chronic in vivo tests as paw edema, peritonitis, and vascular permeability and granulomatous inflammation model. The anti-inflammatory mechanism of action was analyzed by the participation of histamine and arachidonic acid pathways. The chemical profile analysis identified fourteen components present in the essential oil, within them: estragole (60.96%). The in vivo test results show that treatment with EOOB (100 and 50 mg/kg) and estragole (60 and 30 mg/kg) significantly reduced paw edema induced by carrageenan and dextran. The smallest doses of EOOB (50 mg/kg) and estragole (30 mg/kg) showed efficacy in the reduction of paw edema induced by histamine and arachidonic acid, vascular permeability inhibition and leukocyte emigration in the peritoneal fluid. Theses doses were capable of reducing the chronic inflammatory process. The results observed between the EOOB and estragole demonstrate efficacy in anti-inflammatory activity, however, the essential oil is more efficacious in the acute and chronic anti-inflammatory action. This study confirms the therapeutic potential of this plant and reinforces the validity of its use in popular medicine.

Estudo etnofarmacológico comparativo na região do Araripe da Annona muricata L. (Graviola) / Estudio etnofarmacológico comparativo en la región del Araripe de la Annona muricata L. (Graviola) / Ethnopharmacological comparative study in the region of the Araripe of Annona muricata L. (Graviola)

Introdução: a utilização de plantas medicinais na prevenção e na terapêutica de diversas doenças é habitual em todos os períodos históricos da civilização humana. No Brasil, das espécies de plantas identificadas, cerca de dez mil possui alguma propriedade medicinal conhecida. Na Chapada do Araripe destaca-se o uso da Annona muricata L. (Graviola), pertencente à família Annonaceae. Na medicina tradicional, as folhas, os frutos e as raízes da A. muricata são utilizadas sob a forma de chá para o tratamento de diversas doenças. Objetivo: realizar uma investigação dos diversos usos etnofarmacológicos da espécie em três Municípios da Biorregião do Araripe, no contexto de suas comunidades tradicionais. Métodos: aplicou-se um estudo randomizado, desenvolvido na área rural dos municípios de Crato e Santana do Cariri, no estado do Ceará, e Exu, no estado de Pernambuco. A amostra contou com 41 informantes que atribuíram valor de uso medicinal para a espécie. A análise dos dados sucedeu através do Fidelity Level (FL) e da Relative Frequency of Citation (RFC). Resultados: os resultados da presente pesquisa relatam o uso da espécie para uma gama de enfermidades, dentre as quais, destacaram-se: doenças pulmonares, processos inflamatórios, patologias infecciosas, dor e câncer. Conclusões: este estudo ressalta a importância do conhecimento empírico das comunidades tradicionais, pois acreditamos na relevância em investigar o potencial farmacológico de diferentes espécies, com a finalidade de melhorar o acesso aos medicamentos para aquelas populações que apresentam dificuldades na disponibilidade de recursos de saúde de alto custo(AU)

Introducción: el uso de plantas medicinales para la prevención y tratamiento de diversas enfermedades es común en todos los períodos históricos de la civilización humana. En Brasil, de acuerdo a las especies de plantas identificadas, cerca de diez mil ha conocida propiedad medicinal. En el Chapada del Araripe destaca el uso de Annona muricata L. (Guanábana), perteneciente a la familia Annonaceae. En la medicina tradicional, hojas, frutos y raíces de A. muricata se utilizan en forma de té para el tratamiento de enfermedades. Objectivo: realizar una investigación de los diversos usos etnofarmacológicas de esta especie en tres municipios de la bioregión del Araripe, en el contexto de sus comunidades tradicionales. Métodos: un estudio aleatorio fue desarrollado en las zonas rurales de los municipios de Crato y Santana do Cariri en el estado de Ceará, y Exú en el estado de Pernambuco. La muestra fue de 41 entrevistados que atribuyeron valor de uso medicinal para la especie. Se realizó el análisis de datos mediante el Fidelity Level (FL) y Relative Frequency of Citation (RFC). Resultados: los resultados de esta investigación muestran el uso de las especies para enfermedades pulmonares, procesos inflamatorios, infecciones, dolor y cáncer. Conclusiones: este estudio destacó la importancia del conocimiento empírico de las comunidades tradicionales, ya que se cree en la importancia de investigar el potencial farmacológico de diferentes especies a fin de mejorar el acceso a los medicamentos para las poblaciones que tienen dificultades en la disponibilidad de servicios de salud más costosos(AU)

Introduction: the use of medicinal plants in the prevention and therapy of various diseases is typical of all historical periods of human civilization. In Brazil, among the plant species identified, nearly ten thousand has any known medicinal property. In the Araripe Plateau highlights the use of Annona muricata Linnaeus (Soursop), belonging to the Annonaceae family. In traditional medicine, leaves, fruits and roots of A. muricata are used in the form of tea for the treatment of various diseases. Objective: to conduct an investigation of the ethnopharmacological uses of A. muricata in three municipalities of the bioregion Araripe, in the context of their traditional communities. Methods: a randomized study was developed in rural areas of the municipalities of Crato and Santana Cariri in the state of Ceará, and Exu in the state of Pernambuco. The sample had a number of 41 informants who attributed value of medicinal use for the specie. Data analysis occurred through Fidelity Level (FL) and Relative Frequency of Citation (RFC). Results: the results of this research reported the use of the species for various diseases, including: lung diseases, inflammatory processes infectious diseases, cancer and pain. Conclusions: this study emphasizes the importance of empirical knowledge of traditional communities, because we believe in the relevance of investigating the pharmacological potential of different species, with the purpose of optimize access to medications for those people who have difficulties in the availability of Health Resources expensive(AU)

Atividade antibacteriana e moduladora de Cecropia pachystachya Trécul sobre a ação de aminoglicosídeos / Antibacterial and modulatory activity of Cecropia pachystachya Trécul on the action of aminoglycosides / Actividad antibacteriana y moduladora de Cecropia pachystachya Trécul en la acción de los aminoglucósidos

Introdução: a Cecropia pachystachya Trécul., é conhecida como toré (Urticaceae), com ocorrência em todo o território brasileiro, usada na medicina popular no tratamento de infecções respiratórias e gonorreia. Objetivo: avaliar a atividade antibacteriana e moduladora sobre antibióticos, do extrato etanólico e frações metanólicas das folhas e caule de C. pachystachya T., contra linhagens bacterianas padrões e multirresistentes. Métodos: o material vegetal (folhas e caule), coletado na Chapada do Araripe, foi triturado e submerso em solvente etanol PA, e submetido à destilação do solvente no aparelho evaporador rotativo para a produção dos extratos, que foi particionado e submetido ao solvente metanólico, fornecendo as frações metanólicas. Um ensaio de microdiluição foi realizado para verificar a atividade antibacteriana e as possíveis interações dos aminoglicosídeos associados às amostras estudadas, utilizando uma concentração sub-inibitória de 128 µg/mL (CIM/8). Resultados: o efeito mais representativo a associação da neomicina com o EEFCP (Extrato Etanólico das Folhas de C. pachystachya T) e sua fração com redução da CIM de 312.5 para 39,06 µg/mL e redução de 312,50 para 78,13 µg/mL, respectivamente ambos contra Staphylococcus aureus 358. Quando frente a E. coli 27, foi observado antagonismo. Conclusões: os dados obtidos indicam que o extrato e as frações metanólicas de C. pachystachya, podem ser uma alternativa relevante na pesquisa de substâncias que tenham ação contra as bactérias Staphylococcus multirresistentes. Entretanto, o mesmo também pode interferir negativamente na ação das drogas testadas. Contudo são necessários novos teste in vivo para melhor comprovar essa ação.

Introduction: Cecropia pachystachya Trécul, commonly known as 'toré' (Urticaceae) and distributed throughout Brazil, is used in folk medicine to treat respiratory and sexually transmitted infections such as gonorrhea. Objective: evaluate the antibacterial and modulatory activity on antibiotics of the ethanolic extract and methanolic fractions of C. pachystachya T. leaves and stems against standard and multiresistant bacterial strains. Methods: the plant material (leaves and stems) was collected in Araripe, crushed and put into ethanol PA as solvent. Distillation of the solvent was then performed in a rotary evaporator to produce the extracts, which were divided and subjected to the methanolic solvent to obtain the fractions. A microdilution assay was conducted to verify antibacterial activity and the possible interactions of aminoglycosides associated with the study samples. A sub-inhibitory concentration of 128 ?g/mL (MIC/8) was used. Results: the most representative effect was the association of neomycin with EEFCP (ethanolic extract of leaves of C. pachystachya T.) and its fraction, with a MIC reduction of 312.5 for 39.06 µg/mL and 312.50 for 78.13 µg/mL, respectively, against Staphylococcus aureus 358. An antagonistic effect was observed against E. coli 27. Conclusions: the data obtained indicate that C. pachystachya methanolic fractions and extract may be an important alternative in the search for substances with an action against multiresistant Staphylococcus bacteria. However, such a substance may also negatively affect the action of the drugs studied. It is necessary to conduct new experiments in vivo to verify such an action.

Introducción: Cecropia pachystachya Trécul., es conocida como "toré" (Urticaceae), presente en todo el territorio brasileño, utilizada en la medicina popular para el tratamiento de infecciones respiratorias y de transmisión sexual (gonorrea). Objetivo: evaluar la actividad antibacteriana y moduladora sobre antibióticos del extracto etanólico y fracciones metanólicas de las hojas y tallo de C. pachystachya T. contra cepas bacterianas estándar y multirresistentes. Métodos: el material vegetal (hojas y tallos), colectado en el Araripe, fue triturado y sumergido en etanol PA como solvente. Seguidamente, fue sometido a destilación del solvente en un evaporador rotativo para la producción de los extractos, que fueron divididos y sometidos al solvente metanólico, formando así las fracciones. Se llevó a cabo un ensayo de microdilución para verificar la actividad antibacteriana y las posibles interacciones de aminoglucósidos asociados con las muestras estudiadas, se utilizó una concentración sub-inhibitoria de 128 µg/mL (CIM/8). Resultados: el efecto más representativo resultó el de la asociación de neomicina con el EEFCP (Extrato Etanólico de hojas de C. pachystachya T) y su fracción con disminución de la CIM de 312,5 para 39,06 µg/mL y 312,50 para 78,13 µg/mL, respectivamente contra Staphylococcus aureus 358. Se observó un efecto antagónico contra E. coli 27. Conclusiones: los datos obtenidos indican que el extracto y fracciones metanólicas de C. pachystachya, pueden ser una alternativa importante en la búsqueda de sustancias que tienen acción contra las bacterias Staphylococcus multirresistentes. Sin embargo, puede afectar negativamente a la acción de las drogas estudiadas. No obstante, es necesario realizar nuevos experimentos in vivo para comprobar esta acción.