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Background/Objectives: Acute lung injury (ALI) is an inflammatory disorder affecting patients in intensive care with high mortality. No specific pharmacological treatment is available. Musa paradisiaca L. (banana) is a cosmopolitan plant, and homemade syrup from its inflorescence is used in many countries to treat pulmonary inflammation. Therefore, this study analyzed the hydroalcoholic extract (HEM) of the inflorescence on the ALI experimental model. Methods: Swiss mice were challenged with lipopolysaccharide and treated with HEM after 1, 24, and 48 h (five animals/group, three times). Results: The HEM-treated ALI mice presented a decrease in neutrophil migration in the bronchoalveolar lavage fluid (BALF), in the alveolar region, and in the blood, correlating to downregulation of CD18 expression. The HEM treatment also reduced the protein concentration in the BALF, caused lung edema formation, impaired NF-κB activation via inhibition of TLR4 signaling pathway, and decreased IL-1β, TNF-α production, free DNA release, and myeloperoxidase (MPO) activity. However, the extract induced an increased IL-10 in the BALF. Conclusions: Therefore, HEM’s anti-inflammatory and immunomodulatory activities in ALI mice are by deactivating neutrophils by decreasing CD18 receptor, free DNA release, and MPO activity and inducing IL-10 production. Thus, this study supports the use of banana inflorescence in folk medicine and suggests its rational use to develop a phytomedicine to treat pulmonary inflammation.

Background: (-)-Fenchone is a bicyclic monoterpene present in the plant species Foeniculum vulgare Mill, Thuja occidentalis L. (tuja), and Lavandula stoechas (lavender). These plants have therapeutic value in the treatment of intestinal disorders. Aim: To evaluate intestinal anti-inflammatory activity in an acute and chronic trinitrobenzene sulphonic acid (TNBS)-induced colitis model in rats. Methods: Intestinal anti-inflammatory effects were assessed using the acute and chronic TNBS-induced colitis model in rats. The mechanisms were evaluated from colonic tissue fragments of the acute and chronic models. Results: Oral administration of the (-)-fenchone (37.5–300 mg/kg) acute phase or (150 mg/kg) (p < 0.001) chronic phase reduced the macroscopic lesion score, ulcerative area, intestinal weight/length ratio, and diarrheal index in TNBS-treated animals. At a dose of 150 mg/kg, the acute and chronic phase decreased malondialdehyde (MDA) and myeloperoxidase (MPO) (p < 0.001), restored glutathione (GSH) levels and superoxide dismutase (SOD) (p < 0.001), decreased immunomarking for factor nuclear kappa B (NF-κB) and levels of interleukin (IL)-1 and tumor necrosis factor α (TNF-α), and maintained IL-10 and TGF-β basal levels. Furthermore, increased immunostaining for zonula occludens 1 (ZO-1) was observed. Conclusions: (-)-fenchone has intestinal anti-inflammatory activity related to cytoprotection of the intestinal barrier, as well as antioxidant and immunomodulatory effects.

Probiotics have been shown to have a beneficial effect on allergic diseases. Anti-allergic effect of Lacticaseibacillus paracasei was demonstrated in asthma, however, its effect in combined allergic rhinitis and asthma syndrome (CARAS) is still unclear. This study evaluated the Lacticaseibacillus paracasei (LPc-G110) supplementation in CARAS mice model. BALB/c mice were ovalbumin-sensitized and challenged after being supplemented with LPc-G110. Supplemented animals showed reduced allergic rhinitis signs, eosinophilic infiltration, mucus, extracellular matrix deposition into airway tissues, and lung smooth muscle hypertrophy. LPc-G110 supplementation also reduced eosinophilia, serum levels of allergen-specific IgE, IL-4, IL-13, and IL-5, and favored the production of IFN-γ, IL-10, and short-chain fatty acids. Additionally, LPc-G110 supplementation preserved the gut tissue integrity and epithelial barrier by increasing the tight junction protein ZO-1. Therefore, LPc-G110 improves the gut-airway axis in CARAS by ameliorating inflammatory parameters in both compartments and is a promising candidate for preventing allergic airway diseases.

Background: (-)-Fenchone is a naturally occurring monoterpene found in the essential oils of Foeniculum vulgare Mill., Thuja occidentalis L., and Peumus boldus Molina. Pharmacological studies have reported its antinociceptive, antimicrobial, anti-inflammatory, antidiarrheal, and antioxidant activities. Methods: The preventive antiulcer effects of (-)-Fenchone were assessed through oral pretreatment in cysteamine-induced duodenal lesion models. Gastric healing, the underlying mechanisms, and toxicity after repeated doses were evaluated using the acetic acid-induced gastric ulcer rat model with oral treatment administered for 14 days. Results: In the cysteamine-induced duodenal ulcer model, fenchone (37.5–300 mg/kg) significantly decreased the ulcer area and prevented lesion formation. In the acetic acid-induced ulcer model, fenchone (150 mg/kg) reduced (p < 0.001) ulcerative injury. These effects were associated with increased levels of reduced glutathione (GSH), superoxide dismutase (SOD), interleukin (IL)-10, and transforming growth factor-beta (TGF-β). Furthermore, treatment with (-)-Fenchone (150 mg/kg) significantly reduced (p < 0.001) malondialdehyde (MDA), myeloperoxidase (MPO), interleukin-1 beta (IL-1β), tumor necrosis factor-alpha (TNF-α), and nuclear transcription factor kappa B (NF-κB). A 14-day oral toxicity investigation revealed no alterations in heart, liver, spleen, or kidney weight, nor in the biochemical and hematological parameters assessed. (-)-Fenchone protected animals from body weight loss while maintaining feed and water intake. Conclusion: (-)-Fenchone exhibits low toxicity, prevents duodenal ulcers, and enhances gastric healing activities. Antioxidant and immunomodulatory properties appear to be involved in its therapeutic effects.

Obesity is characterized by an energy imbalance caused by caloric intake and expenditure, being a risk factor associated with a wide range of pathophysiological conditions including gastrointestinal diseases. In recent years, it has been shown that overexpression of oxidative stress and pro-inflammatory cytokines is a mechanistic link between obesity and cellular functions in animals and humans. Some natural products are reported to be effective in counteracting the adverse effects of oxidative stress. Thus, Arthorpira platensis (AP) stands out, an alga with anti-inflammatory and antioxidant activities. Thus, the objective is to evaluate the preventive effects of AP supplementation on oxidative stress and interleukin-1β (IL-1β) levels in the ileum of rats fed a hypercaloric diet. The rats were divided into a group fed a standard diet (SD), a hypercaloric diet (HCD) and/or fed a hypercaloric diet and supplemented simultaneously with AP 25 mg/Kg (HCD + AP25), after 8 weeks of treatment the ileum was collected for The analyses. It was observed that in the DHC group there was underproduction of antioxidant enzymes as well as overexpression of oxidative stress in the ileum of rats, interestingly this damage was prevented by the alga. Furthermore, the DHC group showed high levels of IL-1β (940.6 ± 34.5) such an increase was prevented in the HCD + AP25 group (597.2 ± 33.3). It is evident, therefore, that AP prevents the increase in oxidative stress and the inflammatory profile in the ileum of obese rats, making it a promising therapeutic alternative in the treatment of inflammatory bowel diseases aggravated by obesity.

Background: (-)-Carveol (p-Mentha-6,8-dien-2-ol) is a monocyclic monoterpenic alcohol, present in essential oils of plant species such as Cymbopogon giganteus, Illicium pachyphyllum and in spices such as Carum carvi (cumin). Pharmacological studies report its antitumor, antimicrobial, neuroprotective, vasorelaxant, antioxidant and anti-inflammatory activity.Hypothesis/Purpose: The objective of this study was to evaluate the acute non-clinical oral toxicity, gastroprotective activity of monoterpene (-)-Carveol in animal models and the related mechanisms of action.Methods: Acute toxicity was assessed according to OECD guide 423 in mice. Ethanol, stress, NSAIDs and pylorus ligation-induced gastric ulcer models were used to investigate antiulcer properties. The related mechanisms of action were using the ethanol-gastric lesions protocol.Results: (-)-Carveol has low toxicity, with a lethal dose 50% (LD50) equal to or greater than 2,500 mg/kg according to OECD guide nº 423. In all gastric ulcer induction methods evaluated, (-)-Carveol (25, 50, 100 and 200 mg/kg, p.o.) significantly reduced the ulcerative lesion in comparison with the respective control groups. To investigate the mechanisms involved in the gastroprotective activity, the antisecretory or neutralizing of gastric secretion, cytoprotective, antioxidant and immunoregulatory effects were evaluated. In the experimental protocol of pylorus ligation-induced gastric ulcer, (-)-Carveol (100 mg/kg) reduced (p < 0.001) the volume of gastric secretion in both routes (oral and intraduodenal). The previous administration of blockers NEM (sulfhydryl groups blocker), L-NAME (nitric oxide synthesis inhibitor), glibenclamide (KATP channel blocker) and indomethacin (cyclo-oxygenase inhibitor), significantly reduced the gastroprotection exercised by (-)-Carveol, suggesting the participation of these pathways in its gastroprotective activity. In addition, treatment with (-)-Carveol (100 mg/kg) increased (p < 0.001) mucus adhered to the gastric wall. Treatment also increased (p < 0.001) levels of reduced glutathione (GSH), superoxide dismutase (SOD) and interleukin-10 (IL-10). It also reduced (p < 0.001) malondialdehyde (MDA), myeloperoxidase (MPO), interleukin-1 beta (IL-1β) and tumor necrosis factor-alpha (TNF-α) levels.Conclusion: Thus, it is possible to infer that (-)-Carveol presents gastroprotective activity related to antisecretory, cytoprotective, antioxidant and immunomodulatory mechanisms.

Abstract Background The essential oil from Mesosphaerum sidifolium (L’Hérit.) Harley & J.F.B.Pastore (syn. Hyptis umbrosa), Lamiaceae (EOM), and its major component, have been tested for toxicity and antitumor activity. Methods EOM was obtained from aerial parts of M. sidifolium subjected to hydro distillation, and gas chromatography-mass spectrometry was used to characterize the EOM chemical composition. The toxicity was evaluated using haemolysis assay, and acute toxicity and micronucleus tests. Ehrlich ascites carcinoma model was used to evaluate the in vivo antitumor activity and toxicity of EOM (50, 100 and 150 mg/kg), and fenchone (30 and 60 mg/kg) after 9 d of treatment. Results The EOM major components were fenchone (24.8%), cubebol (6.9%), limonene (5.4%), spathulenol (4.5%), β-caryophyllene (4.6%) and α-cadinol (4.7%). The HC50 (concentration producing 50% haemolysis) was 494.9 μg/mL for EOM and higher than 3000 μg/mL for fenchone. The LD50 for EOM was approximately 500 mg/kg in mice. The essential oil induced increase of micronucleated erythrocytes only at 300 mg/kg, suggesting moderate genotoxicity. EOM (100 or 150 mg/kg) and fenchone (60 mg/kg) reduced all analyzed parameters (tumor volume and mass, and total viable cancer cells). Survival also increased for the treated animals with EOM and fenchone. For EOM 150 mg/kg and 5-FU treatment, most cells were arrested in the G0/G1 phase, whereas for fenchone, cells arrested in the S phase, which represents a blockage in cell cycle progression. Regarding the toxicological evaluation, EOM induced weight loss, but did not induce hematological, biochemical or histological (liver and kidneys) toxicity. Fenchone induced decrease of AST and ALT, suggesting liver damage. Conclusions The data showed EOM caused in vivo cell growth inhibition on Ehrlich ascites carcinoma model by inducing cell cycle arrest, without major changes in the toxicity parameters evaluated. In addition, this activity was associated with the presence of fenchone, its major component.

Objetivo: O presente estudo objetivou analisar, a partir de prescrições médicas, o perfil dos antimicrobianos prescritos na Unidade de Terapia Intensiva (UTI) de um hospital público de ensino na cidade de João Pessoa - PB, com foco nas potenciais interações medicamentosas envolvendo os mesmos. Métodos: Estudo de caráter descritivo e retrospectivo. Para tanto, selecionou-se 52 prescrições da UTI, sendo estas digitalizadas, de usuários acima de 18 anos, ambos os sexos, aviadas entre os meses de outubro e dezembro de 2011 e que continham dois ou mais medicamentos sendo pelo menos um deles um anti-infeccioso. Para análise das IMs potenciais foram utilizadas a base de dados DrugDex® Evalutions do Micromedex® e a disponível no endereço eletrônico www.drugs.com. Resultados: Constatou-se que é comum a utilização de anti-infecciosos na UTI, sendo ainda observada a freqüente associação entre os mesmos com vistas a obter sucesso terapêutico. Além disso, identificou-se a ocorrência de potenciais IM envolvendo os anti-infecciosos prescritos. Conclusão: Salienta-se a necessidade de maior atenção no que tange a associação de antimicrobianos devido ao risco iminente de surgimento de interações medicamentosas que podem inviabilizar a terapêutica e acarretar sérios danos à saúde dos usuários.

Objetivos: Identificar e avaliar os registros de notificações de farmacovigilância durante cinco anos em um hospital oncológico sentinela da Paraíba. Métodos: Estudo de caráter documental, transversal e retrospectivo que utilizou como fonte de dados a ficha de notificação de suspeita de reação adversa a medicamento (RAM) e de queixa técnica sobre medicamentos do serviço de Gerência de Risco do hospital no período de 01 de janeiro de 2008 a 31 de dezembro de 2012. Resultados: Foram processadas 34 notificações, sendo 61,8% referente à queixas técnicas sobre medicamentos e 38,2% à suspeitas de RAM. Sobre os profissionais envolvidos, destacaram-se farmacêuticos (73,5%), enfermeiros (11,8%), técnicos de enfermagem (8,8%) e médicos (5,9%). Das notificações de suspeitas de RAM, constatou-se que os medicamentos mais frequentes eram agentes antineoplásicos (84,7%). Os órgãos e sistemas acometidos foram: sistema tegumentar (37,5%), sistema respiratório (31,5%), distúrbios do estado geral (15,5%), sistema gastrintestinal (9,3%) e sistema nervoso central e periférico (6,2%). Das notificações de queixas técnicas sobre medicamentos, os tipos mais relevantes foram: alterações gerais (57%), alterações de cor (19%), inefetividade (14%), e alterações físico-químicas (10%). Conclusões: Constatou-se a necessidade de mais investimento nessa área, principalmente em relação à sensibilização da importância da notificação para obtenção de dados para fins de regulamentação sanitária e garantia da segurança do usuário.

Peptic ulcer is a common disease characterized by lesions that affect the mucosa of the esophagus, stomach and/or duodenum, and may extend into the muscular layer of the mucosa. Natural products have played an important role in the process of development and discovery of new drugs, due to their wide structural diversity and present, mostly specific and selective biological activities. Among natural products the alkaloids, biologically active secondary metabolites, that can be found in plants, animals or microorganisms stand out. The alkaloids are compounds consisting of a basic nitrogen atom that may or may not be part of a heterocyclic ring. This review will describe 15 alkaloids with antiulcer activity in animal models and in vitro studies.

Peptic ulcer disease (PUD) is a multifactorial and complex disease caused by an imbalance of protective and aggressive factors (endogenous and exogenous). Despite advances in recent years, it is still responsible for substantial mortality and triggering clinical problems. Over the last decades, the understanding of PUD has changed a lot with the discovery of Helicobacter pylori infection. However, this disease continues to be a challenge due to side-effects, incidence of relapse from use of various anti-ulcer medicines, and the rapid appearance of antimicrobial resistance with current H. pylori therapies. Consequently, there is the need to identify more effective and safe anti-ulcer agents. The search for new therapies with natural products is a viable alternative and has been encouraged. The literature reports the importance of monoterpenes based on the extensive pharmacological action of this class, including wound healing and anti-ulcerogenic agents. In the present study, 20 monoterpenes with anti-ulcerogenic properties were evaluated by assessing recent in vitro and in vivo studies. Here, we review the anti-ulcer effects of monoterpenes against ulcerogenic factors such as ethanol, nonsteroidal anti-inflammatory drugs (NSAIDs), and Helicobacter pylori, highlighting challenges in the field.

The Combretaceae is a large family of herbs, shrubs and trees, comprising about 20 genera and 600 species with tropical distribution around the globe and centers of diversity in Africa and Asia. Some Combretum species are extensively used in traditional medicine against inflammation, infections, diabetes, malaria, bleeding, diarrhea and digestive disorders and others as a diuretic. The present work is a literature survey of Combretum species that have been evaluated for their ability to exert biological activities. A total number of 36 Combretum species are discussed with regard to plant parts used, component tested and bioassay models. This review is of fundamental importance to promoting studies on Combretum species, thereby contributing to the development of new therapeutic alternatives that may improve the health of people suffering from various health problems.

Leaves and bark infusions Anacardium humile St. Hil. (Anacardiaceae), known as in Brazil as “cajuzinho do cerrado”, have been used in folk medicine as an alternative treatment for ulcers and gastritis. This study evaluated the gastroprotective activity of an ethyl acetate extract of the leaves of A. humile (AcF) and the mechanism involved in this gastroprotection. Pretreatment concentrations (50, 100, 200 mg.kg−1) were administered by gavage. Following a 60 min. period, all the rats were orally administered 1 mL of absolute ethanol. One hour after the administration of ethanol, all groups were sacrificed, and the gastric ulcer index was calculated. Prostaglandin PGE2 concentration, gastric adherent mucous, and the participation of nitric oxide (NO) and sulfhydryl compounds in the gastroprotection process were also analyzed using the most effective tested dose (50 mg·kg−1). A histological study of the glandular stomach for the evaluation of the epithelial damage and mucus content was also performed. AcF significantly reduced the gastric damage produced by ethanol. This effect was statistically significant for the 50 mg·kg−1 group compared to control. Also, it significantly increased the PGE2 (by 10-fold) and mucous production, while pretreatment with NG-nitro-L-arginine methyl ester (L-NAME) or N-ethylmaleimide (NEM) completely abolished the gastroprotection. AcF has a protective effect against ethanol, and this effect, might be due to the augmentation of the protective mechanisms of mucosa.

Peptic ulcers are a common disorder of the entire gastrointestinal tract that occurs mainly in the stomach and the proximal duodenum. This disease is multifactorial and its treatment faces great difficulties due to the limited effectiveness and severe side effects of the currently available drugs. The use of natural products for the prevention and treatment of different pathologies is continuously expanding throughout the world. This is particularly true with regards to flavonoids, which represent a highly diverse class of secondary metabolites with potentially beneficial human health effects that is widely distributed in the plant kingdom and currently consumed in large amounts in the diet. They display several pharmacological properties in the gastroprotective area, acting as anti-secretory, cytoprotective and antioxidant agents. Besides their action as gastroprotectives, flavonoids also act in healing of gastric ulcers and additionally these polyphenolic compounds can be new alternatives for suppression or modulation of peptic ulcers associated with H. pylori. In this review, we have summarized the literature on ninety-five flavonoids with varying degrees of antiulcerogenic activity, confirming that flavonoids have a therapeutic potential for the more effective treatment of peptic ulcers.

The phytochemical investigation of Herissantia crispa led to the isolation of seven compounds, identified as: sitosterol 3-O-β-D-glucopyranoside, stigmasterol 3-O-β-D-glucopyranoside, 3,5,7,4'-tetrahydroxyflavone (kaempferol), 3,5,7,3',4'-pentahydroxyflavone (quercetin), unpublished in the genus Herissantia, besides β-sitosterol, kaempferol 3-O-β-D-(6''-E-p-coumaroil) (tiliroside) glucopyranoside and kaempferol 3,7-di-O-α-L-ramnopyranoside (lespedin), described for the first time in the species. The structural determination of the compounds was made by means of spectroscopy methods such as Infrared Spectroscopy, ¹H and 13C Nuclear Magnetic Resonance, with the aid of two dimensional techniques, and by comparison with literature data. The toxicity activity of the MeOH extract and lespedin on Artemia salina Leach. was also carried out.