Potential of the Blue Calm® food supplement in the treatment of alcohol withdrawal-induced anxiety in adult zebrafish (Danio rerio).

Alcohol use disorder (AUD) is characterized by a set of behavioral, cognitive, nutritional, and physiological phenomena derived from the uncontrolled use of alcoholic beverages. There are cases in which AUD is associated with anxiety disorder, and when untreated, it requires careful pharmacotherapy. Blue Calm® (BC) is a food supplement indicated to aid restorative sleep, which has traces of medicinal plant extracts, as well as myo-inositol, magnesium bisglycinate, taurine, and L-tryptophan as its main chemical constituents. In this context, this study aimed to evaluate the potential of the BC in the treatment alcohol withdrawal-induced anxiety in adult zebrafish (aZF). Initially, BC was submitted to antioxidant activity against 2,2-diphenyl-1-picrylhydrazyl radical. Subsequently, the aZF (n = 6/group) were treated with BC (0.1 or 1 or 10 mg/mL; 20 µL; p.o.), and the sedative effect and acute toxicity (96 h) were evaluated. Then, the anxiolytic-like effect and the possible GABAergic mechanism were analyzed through the Light & Dark Test. Finally, BC action was evaluated for treating alcohol withdrawal-induced anxiety in aZF. Molecular docking was performed to evaluate the interaction of the major chemical constituents of BC with the GABAA receptor. BC showed antioxidant potential, a sedative effect, was not toxic, and all doses of BC had an anxiolytic-like effect and showed potential for the treatment of alcohol withdrawal-induced anxiety in aZF. In addition to the anxiolytic action, the main chemical constituents of BC were confirmed in the molecular docking, thus suggesting that BC is an anxiolytic that modulates the GABAergic system and has pharmacological potential for the treatment of alcohol withdrawal-induced anxiety.

Implications of the endocannabinoid system and the therapeutic action of cannabinoids in autism spectrum disorder: A literature review.

Autism spectrum disorder (ASD) is a neurodevelopmental disorder, onset in early childhood and associated with cognitive, social, behavioral, and sensory impairments. The pathophysiology is still unclear, and it is believed that genetic and environmental factors are fully capable of influencing ASD, especially cell signaling and microglial functions. Furthermore, the endocannabinoid system (ECS) participates in the modulation of various brain processes and is also involved in the pathophysiological mechanisms of this condition. Due to the health and quality of life impacts of autism for the patient and his/her family and the lack of effective medications, the literature has elucidated the possibility that Cannabis phytocannabinoids act favorably on ASD symptoms, probably through the modulation of neurotransmitters, in addition to endogenous ligands derived from arachidonic acid, metabolizing enzymes and even transporters of the membrane. These findings support the notion that there are links between key features of ASD and ECS due to the favorable actions of cannabidiol (CBD) and other cannabinoids on symptoms related to behavioral and cognitive disorders, as well as deficits in communication and social interaction, hyperactivity, anxiety and sleep disorders. Thus, phytocannabinoids emerge as therapeutic alternatives for ASD.

Utilization of Agro-Industrial Residues in the Rearing and Nutritional Enrichment of Zophobas atratus Larvae: New Food Raw Materials.

Edible insects are a potential alternative food source of high feed conversion efficiency and protein content. Zophobas atratus is an edible insect that adapts to different diets, enabling sustainable rearing by adding value to by-products and agro-industrial residues. This study aimed to evaluate the performance and nutritional characterization of Zophobas atratus larvae fed with different proportions of grape residue. Physicochemical analysis of the diets and larvae (AOAC procedures), fatty acid profile (chromatographic techniques), metals and non-metals (inductively coupled plasma optical emission spectrometry), larval mass gain, feed conversion efficiency, and mortality rate were assessed. The replacement of 25% of the conventional diet with grape residue increased lipid, ash, and fiber contents and reduced protein, carbohydrates, and energy. It promoted greater mass gain, lower mortality rate, and reduced larval growth time by 51%. Among the replacements, 25% resulted in the second-highest content of calcium, sodium, magnesium, and zinc, and the lowest content of potassium and phosphorus in the larvae. The 100% replacement resulted in the highest amounts of C18:2n6 (27.8%), C18:3n3 (2.2%), and PUFA (30.0%). Replacing 25% of the conventional diet with grape residue is equivalent to the conventional diet in many aspects and improves several larvae performance indices and nutritional values.

Effects of Pilates on the risk of falls, gait, balance and functional mobility in healthy older adults: A randomised controlled trial.

OBJECTIVE: To investigate the effects of Pilates on falls risk, fear of falling, postural balance, functional mobility, spatiotemporal gait parameters, mobility and physical activity in older adults. DESIGN: Randomized Controlled Trial (RCT). METHODS: Sixty-one older adults, mean age 70.08 (SD = 5.51) were randomly allocated into a Pilates group (PG, n = 29) or control group (CG, n = 32). Intervention comprised a 12-week Pilates program, with exercises performed twice a week and supplementary exercises at home. The Montreal Cognitive Assessment (MOCA), was used to screen cognition. PRIMARY OUTCOMES: Fear of falling, postural balance (force platform), gait velocity (electronic walkway). SECONDARY OUTCOMES: Functional mobility, mobility, physical activity, and spatiotemporal parameters of gait. Statistical analysis was carried out using Generalized Estimating Equations (GEE). Covariates were adjusted. RESULTS: Positive effects were found for time effects: Time Up and Go (TUG), anteroposterior (AP) and mediolateral (ML) directions of balance, cadence, (stance, step and double support time). The step and double support time showed significant differences between the two groups (p < 0.05). Interaction between time and groups was found for FRT. Age was a significant factor in TUG, FRT, postural balance for AP under open eyes conditions. Health status was significant for ML in eyes open condition. Gait was significant for age, height and health status. CONCLUSION: Effects of 12 weeks of Pilates intervention on functional mobility, mobility, postural balance and spatiotemporal gait parameters were identified. Further trials of a longer duration are warranted to determine the effectiveness of Pilates on falls prevention.

Six weeks of Pilates improved functional mobility, postural balance and spatiotemporal parameters of gait to decrease the risk of falls in healthy older adults.

OBJECTIVE: To determine the effectiveness of Pilates exercises on falls risk factors. DESIGN: Prospective cohort, pre-test post-test study. Participants were selected using convenience and snowballing sampling. Pilates classes were held twice weekly for six weeks (1-h sessions) with a supplementary home programme. METHODS: A test of cognitive function, the Montreal Cognitive Assessment (MOCA), was employed to determine eligibility for inclusion. The following fall-predictor variable measures were employed: the 16 item Falls Efficacy Scale (FES), the short International Physical Activity Questionnaire (IPAQ), the Functional Reach Test (FRT), the Timed Up and Go (TUG), the GAITRite® system, Platform FOOTWORKpro. Multivariate analysis ANOVA with time as within subject factor was used to test for differences between pre and post-test scores adjusted for the factor Pilates. RESULTS: twenty-seven participants completed the study, mean age = 70.4 (SD = 4.5). After adjusting for the effect of the factor Pilates "previous experience or no previous experience of Pilates", statistically significant differences were identified in the following domains: The TUG (p < 0.001), FRT (p < 0.001), velocity, swing and stance time and the Mediolateral sway (p < 0.05). A significant difference was found between pre and post-test for anteroposterior sway in those with experience of Pilates (p < 0.05) and interaction between time and Pilates experience in Physical Activity (p < 0.05). CONCLUSION: Findings suggest that functional mobility, mobility, spatiotemporal parameters of gait, postural balance and physical activity improved in healthy older adults after 6 weeks of Pilates with a supplementary home programme.

From mango by-product to food packaging: Pectin-phenolic antioxidant films from mango peels.

The objective of the study was to prepare active films based on pectin and polyphenol-rich extracts from Tommy Atkins mango peels. Aqueous and methanolic extracts showed a variety of phenolic compounds that were identified by UPLC-MS analysis, and a high content of total phenolics that were quantified by the Folin-Ciocalteau method. The methanolic extract showed better results in antioxidant tests and was more effective in inhibiting the growth of Gram-positive and Gram-negative bacteria. The pectin extracted from mango peels showed good thermal stability and a degree of methoxylation of 58.3% by 1H NMR. The films containing the phenolic extracts showed lower water vapor permeability when compared to the control film (without any phenolic extracts). The incorporation of the extracts led to an increase in elongation (ε) and a decrease in tensile strength (σ) and modulus of elasticity (Y). The films with aqueous or methanolic extracts showed higher antioxidant activity in terms of inhibition of the DPPH radical. Therefore, the films developed in this work are presented as a promising alternative for food packaging and/or coating applications.

Genomic-based surveillance reveals high ongoing transmission of multi-drug-resistant Mycobacterium tuberculosis in Southern Brazil.

Genomic-based surveillance on the occurrence of drug resistance and its transmission dynamics has emerged as a powerful tool for the control of tuberculosis (TB). A whole-genome sequencing approach, phenotypic testing and clinical-epidemiological investigation were used to undertake a retrospective population-based study on drug-resistant (DR)-TB in Rio Grande do Sul, the largest state in Southern Brazil. The analysis included 305 resistant Mycobacterium tuberculosis strains sampled statewide from 2011 to 2014, and covered 75.7% of all DR-TB cases identified in this period. Lineage 4 was found to be predominant (99.3%), with high sublineage-level diversity composed mainly of 4.3.4.2 [Latin American and Mediterranean (LAM)/RD174], 4.3.3 (LAM/RD115) and 4.1.2.1 (Haarlem/RD182) sublineages. Genomic diversity was also reflected in resistance of the variants to first-line drugs. A large number of distinct resistance-conferring mutations, including variants that have not been reported previously in any other setting worldwide, and 22 isoniazid-monoresistant strains with mutations described as disputed in the rpoB gene but causing rifampicin resistance generally missed by automated phenotypic tests as BACTEC MGIT. Using a cut-off of five single nucleotide polymorphisms, the estimated recent transmission rate was 55.1%, with 168 strains grouped into 28 genomic clusters. The most worrying fact concerns multi-drug-resistant (MDR) strains, of which 73.4% were clustered. Different resistance profiles and acquisition of novel mutations intraclusters revealed important amplification of resistance in the region. This study described the diversity of M. tuberculosis strains, the basis of drug resistance, and ongoing transmission dynamics across the largest state in Southern Brazil, stressing the urgent need for MDR-TB transmission control state-wide.

Phosphoenolpyruvate carboxykinase from T. cruzi magnetic beads affinity-based screening assays on crude plant extracts from Brazilian Cerrado.

In T. cruzi, a causative agent of Chagas disease, phosphoenolpyruvate carboxykinase (TcPEPCK) is associated with carbohydrate catabolism. Due to its importance in the metabolism of the parasite, it has become a promising target for the development of new drugs against Chagas disease. Aiming to investigate different approaches for ligands screening, TcPEPCK was immobilized on amine-terminated magnetic beads (TcPEPCK-MB) and kinetically characterized by liquid chromatography tandem mass spectrometry activity assay with a KMapp value of 10 ± 1 µM to oxaloacetate as substrate. Natural products library affords highly diverse molecular frameworks through their secondary metabolites, herein a ligand fishing TcPEPCK-MB assay is described for prospecting ligands in four ethanolic extracts of Brazilian Cerrado plants: Qualea grandiflora (Vochysiaceae), Diospyros burchellii (Ebenaceae), Anadenanthera falcata (Fabaceae) and Byrsonima coccolobifolia (Malpighiaceae). The chemical characterization of eleven identified ligands was carried out by liquid chromatography tandem high-resolution mass spectrometry experiments. Senecic acid, syneilesinolide A, phytosphingosine and vanillic acid 4-glucopyranoside are herein reported for the first time for Q. grandiflora, D. burchellii, A. falcata, respectively. In addition, the specificity of the assay was observed since only catechin was fished out from the ethanolic extract of B. coccolobifolia leaves, despite the presence of epicatechin epimer.

Larvicidal Activity of Essential Oils Against Aedes aegypti (Diptera: Culicidae).

The Aedes aegypti is responsible for the transmission of arboviruses, which compromise public health. In the search for synthetic product alternatives, essential oils (OEs) have been highlighted by many researchers as natural insecticides. This systematic review (SR) was performed according to PRISMA guidelines (Preferred Reporting Items for Systematic Reviews and Meta-Analyses) and its objective was to evaluate studies addressing OEs with larvicidal properties against Ae. aegypti, through electronic database searches (Pubmed, Science Direct and Scielo), covering an overview of the plant sources OEs, which plant parts were used, the extraction methods, analytical techniques, major and/or secondary constituents with greater percentages, as well as the LC50s responsible for larval mortality. Following study analysis, plants distributed across 32 families, 90 genera and 175 species were identified. The Lamiaceae, Myrtaceae, Piperaceae, Asteraceae, Rutaceae, Euphorbiaceae and Lauraceae families obtained the highest number of species with toxic properties against larvae from this vector. Practically all plant parts were found to be used for OE extraction. Hydrodistillation and steam distillation were the main extraction methods identified, with GC-MS/GC-FID representing the main analytical techniques used to reveal their chemical composition, especially of terpene compounds. In this context, OEs are promising alternatives for the investigation of natural, ecologically correct and biodegradable insecticides with the potential to be used in Ae. aegypti control programs.

In vitro acaricidal activity of Cymbopogon citratus, Cymbopogon nardus and Mentha arvensis against Rhipicephalus microplus (Acari: Ixodidae).

The chemical composition and acaricidal activity of plant-derived essential oils was assessed against Rhipicephalus microplus ticks. The essential oils of Mentha arvensis, Cymbopogon citratus and C. nardus were assessed for acaricidal activity against Rhipicephalus microplus. Essential oils (EO) of plants were separated by hydrodistillation (three times) and analyzed using gas chromatography - mass spectrometer (GC-MS). For bioassays, engorged females of R. microplus were exposed to C. citratus and C. nardus EO at 2%, 3%, 4% and 5% concentrations; and to M. arvensis EO at 1%, 3%, and 5% for 5 min. The weight egg mass, nutrient index (N.I), egg production index (E.P.I), hatching and control rate were evaluated. Non-feed larvae of R. microplus were exposed to essential oils with 0.25%, 0.5%; 1%; 1.5% and 2% concentrations; the mortality rate was measured after 48 h. Only engorged females presented reduced biological activities (oviposition, E.P.I) after exposure to M. arvensis at 3%, when in comparison to both positive and negative controls. The hatchability of R. microplus larvae ranged from 66.9% (after exposure to C. nardus EO at 5%) to 99.2% (positive control). The nutrition index was lower (46.6%) for the exposure to M. arvensis EO at 5%. M. arvensis at 3% and 5% concentrations was significantly efficient for engorged females when compared to control (53.7% and 47.5%, respectively). C. citratus EO at 1%, 1.5% and 2% concentrations yielded better results in the larval packet test, causing 100% mortality. Nonetheless, C. nardus and M. arvensis EO at 2% yielded 66% and 39% mortality, respectively. The study showed that M. arvensis presented potential for the control of R. microplus engorged females while C. citratus and C. nardus presented potential as a larvicide.

Effects of photobiomodulation therapy associated with resistance training in elderly men: a randomized double-blinded placebo-controlled trial.

PURPOSE: The purpose of this study was to investigate the effects of photobiomodulation therapy (PBMT) combined with resistance training on knee extensors muscle mass, strength and functional capacity in elderly men. METHODS: In this randomized double-blinded placebo-controlled trial, healthy elderly men (age 60-80 years) completed 12 weeks of resistance training (2×/week) with application of placebo (n = 13) or active PBMT (n = 11) on quadriceps muscles (850 nm, 240 J per limb) before each training session. Leg press and knee extension one-repetition maximum (1RM) tests, isometric and concentric peak torques, rectus femoris (RF) and vastus lateralis (VL) muscle thickness, timed up-and-go (TUG) and chair rise-to-standing (CRS) tests were performed before and after the intervention period. RESULTS: There were significant improvements in all outcomes for both groups (p < 0.05), except for RF muscle thickness for the placebo group (p = 0.09). Large effect sizes (ES > 0.8) were observed for leg press and leg extension 1RM and CRS tests for both groups, as well as for TUG test for PBMT group. Isokinetic peak torque for both groups and TUG for placebo group had moderate increases (ES > 0.5). Muscle thicknesses and isometric peak torque had small increases (ES > 0.2) in both groups. Both null hypothesis analysis and magnitude-based inference support similar effects of PBMT and placebo treatments. CONCLUSION: Different than previously evidenced in young subjects, PBMT with the parameters used in this study did not provide any additional benefits in comparison to placebo application on muscle mass, strength and functional capacity of healthy elderly men engaged in a resistance training program.

Massage therapy in cortisol circadian rhythm, pain intensity, perceived stress index and quality of life of fibromyalgia syndrome patients.

We investigate the effects of a massage therapy program (MTP) in cortisol concentration (CC), intensity of pain, quality of life and perceived stress index of fibromyalgia patients. Volunteers (n = 24, aged 26-55 years) were treated with MT, twice a week for three months. They answered the Fibromyalgia Impact Questionnaire (FIQ), Perceived Stress Questionnaire (PSQ) and McGill Pain Questionnaire (MPQ-Br), and collected saliva to evaluate CC before and after the end of each month. The MT had improvement in quality of life, according to the FIQ results, and promoted reduction in PSQ values after the second (PSQ2-0.62 ± 0.04vsPSQ0-0.71 ± 0.04) and third month (PSQ3-0.64 ± 0.04vsPSQ0-0.71 ± 0.04). The MTP also promoted reduction in pain after the third month (MQP-Br1-44.50 ± 2.15vsMQP-Br4-35.38 ± 3.71). Despite PSQ reduction, the CC were not affected by the program. This pilot suggests that this treatment improved quality of life, reduced perceived stress index and pain in these volunteers.

Phototherapy for Improvement of Performance and Exercise Recovery: Comparison of 3 Commercially Available Devices.

CONTEXT: Recent studies suggest the prophylactic use of low-powered laser/light has ergogenic effects on athletic performance and postactivity recovery. Manufacturers of high-powered lasers/light devices claim that these can produce the same clinical benefits with increased power and decreased irradiation time; however, research with high-powered lasers is lacking. OBJECTIVE: To evaluate the magnitude of observed phototherapeutic effects with 3 commercially available devices. DESIGN: Randomized double-blind placebo-controlled study. SETTING: Laboratory. PATIENTS OR OTHER PARTICIPANTS: Forty healthy untrained male participants. INTERVENTION(S): Participants were randomized into 4 groups: placebo, high-powered continuous laser/light, low-powered continuous laser/light, or low-powered pulsed laser/light (comprising both lasers and light-emitting diodes). A single dose of 180 J or placebo was applied to the quadriceps. MAIN OUTCOME MEASURE(S): Maximum voluntary contraction, delayed-onset muscle soreness (DOMS), and creatine kinase (CK) activity from baseline to 96 hours after the eccentric exercise protocol. RESULTS: Maximum voluntary contraction was maintained in the low-powered pulsed laser/light group compared with placebo and high-powered continuous laser/light groups in all time points (P < .05). Low-powered pulsed laser/light demonstrated less DOMS than all groups at all time points (P < .05). High-powered continuous laser/light did not demonstrate any positive effects on maximum voluntary contraction, CK activity, or DOMS compared with any group at any time point. Creatine kinase activity was decreased in low-powered pulsed laser/light compared with placebo (P < .05) and high-powered continuous laser/light (P < .05) at all time points. High-powered continuous laser/light resulted in increased CK activity compared with placebo from 1 to 24 hours (P < .05). CONCLUSIONS: Low-powered pulsed laser/light demonstrated better results than either low-powered continuous laser/light or high-powered continuous laser/light in all outcome measures when compared with placebo. The increase in CK activity using the high-powered continuous laser/light compared with placebo warrants further research to investigate its effect on other factors related to muscle damage.

Hybrid organic/inorganic interfaces as reversible label-free platform for direct monitoring of biochemical interactions.

The combination of organic and inorganic materials to create hybrid nanostructures is an effective approach to develop label-free platforms for biosensing as well as to overcome eventual leakage current-related problems in capacitive sensors operating in liquid. In this work, we combine an ultra-thin high-k dielectric layer (Al2O3) with a nanostructured organic functional tail to create a platform capable of monitoring biospecific interactions directly in liquid at very low analyte concentrations. As a proof of concept, a reversible label-free glutathione-S-transferase (GST) biosensor is demonstrated. The sensor can quantify the GST enzyme concentration through its biospecific interaction with tripeptide reduced glutathione (GSH) bioreceptor directly immobilized on the dielectric surface. The enzymatic reaction is monitored by electrical impedance measurements, evaluating variations on the overall capacitance values according to the GST concentration. The biosensor surface can be easily regenerated, allowing the detection of GST with the very same device. The biosensor shows a linear response in the range of 200pmolL-1 to 2µmolL-1, the largest reported in the literature along with the lowest detectable GST concentration (200pmolL-1) for GST label-free sensors. Such a nanostructured hybrid organic-inorganic system represents a powerful tool for the monitoring of biochemical reactions, such as protein-protein interactions, for biosensing and biotechnological applications.

Gallesia integrifolia (Spreng.) Harms: In vitro and in vivo antibacterial activities and mode of action.

ETHNOPHARMACOLOGICAL RELEVANCE: Gallesia integrifolia (Phytolaccaceae) is commonly known as "pau-d'alho" in Brazil or "garlic plant" due to the strong scent of garlic peculiar to all parts of the plant. The bark decoction is used for the treatment of microbial infections among other diseases by different ethnic groups in Brazil, Peruvian Amazonians, Bolivia and Mosetene Indians. This study aimed to advance in the antibacterial activity and characterize the mode of action of the hydroethanolic extract of the inner stem bark of G. integrifolia (HEGi) using in vivo and in vitro experimental models. MATERIALS AND METHODS: The qualitative and quantitative phytochemical analyzes of HEGi were carried out using colorimetric and HPLC technique. The cytotoxic potential of HEGi was evaluated against CHO-K1 cells by Alamar blue assay and its acute toxicity was assessed by the Hippocratic screening test using Swiss-Webster mice. The antibacterial activity was evaluated by micro- dilution method against ten strains of Gram-positive and Gram-negative bacteria. The mode of action of HEGi was investigated by outer membrane permeability, nucleotide leakage and potassium efflux assays. In vivo infection model was established by using Staphylococcus aureus infection model Wistar rats. RESULTS: Qualitative phytochemical analysis of HEGi revealed the presence of saponins, alkaloids, phenolic compounds and flavonoids. Phytochemical quantification of HEGi showed that higher total phenolic (80.10±0.62mg GAE/g) and flavonoid (16.10±0.03mg RE/g) contents. HPLC fingerprint analysis revealed the presence of gallic acid, rutin, and morin. In the Alamar blue assay no cytotoxic effect of HEGi in CHO-K1 cells was observed up to 200µg/mL, and no signs or symptoms of acute toxicity were observed in mice of both sexes at higher doses of up to 2000mg/kg, p.o. HEGi demonstrated bacteriostatic effect against selected Gram positive and Gram negative bacterial pathogens. Its mode of action is associated, at least partly, with changes in the permeability of bacterial membranes, evidenced by the increased entry of hydrophobic antibiotic in Pseudomonas aeruginosa, intense K(+) efflux and nucleotides leakage in Shigella flexneri, Streptococcus pyogenes and S. aureus. HEGi attenuated the experimental blood borne S. aureus infection in rats at all the tested doses levels (10, 50 and 250mg/kg). CONCLUSION: HEGi is safe at the dose tested when used acutely, and it presented broad antibacterial effect, which support its traditional use in the treatment of bacterial infections. It contains well known important phytochemicals, recognized to be active against bacterial pathogens in vitro and might be collectively responsible for the antibacterial activity of HEGi. It is bacteriostatic in nature, with membrane perturbation being one of it mode of action. HEGi represent a potential phytotherapic antibacterial agent.

Evaluation of the safety, gastroprotective activity and mechanism of action of standardised leaves infusion extract of Copaifera malmei Harms.

ETHNOPHARMACOLOGICAL RELEVANCE: Copaifera malmei Harms (Fabaceae) is a plant that occurs in the central region of Brazil, where the plant's leaves infusion is popularly used to treat gastric ulcer and inflammatory diseases. This study was aimed to investigate the gastroprotective activity and mode of action of the plants' leaves infusion in order to establish the scientific basis for such usage, and to assess its potential as a source of an anti-ulcer agent. MATERIALS AND METHODS: Leaves infusion extract of the plant (SIECm) was prepared, freeze dried and lyophilised. Its qualitative and quantitative phytochemical constituents were investigated using TLC and HPLC techniques. The safety profile was evaluated on CHO-k1 epithelial cells viability using the Alamar blue assay, and by acute toxicity test in mice. The gastroprotection and anti-ulcer efficacy of the SIECm (25, 100 and 400mg/kg, p.o.) were tested using acute (acidified ethanol, piroxicam and water restrain stress), and chronic (acetic acid) experimental ulcer models. The plausible mode of action of the SIECm was assessed using gastric secretion, gastric barrier mucus, nitric oxide, and its antioxidant (myeloperoxidase and catalase) effects in mice and rats. The histopathological analyses of the ulcerated tissues as well as the extract's activity on Helicobacter pylori were also investigated. RESULTS: Phytochemical tests indicated the presence of mainly phytosterols, phenolics and flavonoids. The SIECm exhibited no cytotoxic effects on the CHO-k1 cells, and no oral acute toxicity in mice. It prevented against the acute induced ulcerations by enhancing gastroprotection through gastric mucus production, NO modulation, antioxidant, reduced gastric secretion and enhanced chronic ulcers healing process, as shown by reduction/prevention of epithelial and vascular damage, in addition to reduction in leucocyte infiltration. The SIECm however did not exhibit activity against H. pylori. CONCLUSION: The SIECm is safe, contain useful phytochemicals and exhibited significant gastroprotective/anti-ulcer effects. The results justify its folkloric usage, and provided scientific evidence of its potential as a source of new phytodrug to treat gastric ulcers.

Antibacterial mode of action of the hydroethanolic extract of Leonotis nepetifolia (L.) R. Br. involves bacterial membrane perturbations.

ETHNOPHARMACOLOGICAL RELEVANCE: Leonotis nepetifolia (L) R. Br., Lamiaceae, a pantropical shrub, popularly known in Brazil as "cordão-de-frade", "rubim", is reportedly used in Brazilian ethnomedicine as well as in different countries in the treatments of ailments such as infections, inflammations, wounds, stomach disorders, among others. AIM OF THE STUDY: To evaluate its potential cytotoxicity and antibacterial mode of action of the hydroethanolic extract of L. nepetifolia (HELn) leaves, including phytochemical analysis. MATERIALS AND METHODS: The cytotoxicity of HELn was investigated by Alamar blue assay, using CHO-K1 cells. Antibacterial activity of HELn was tested by broth microdilution methods against a panel of bacteria of clinical interest. The mode of action of L. nepetifolia was studied by targeting bacterial membranes. Phytochemical analysis was performed by determining total secondary metabolites with spectrophotometric assays and HPLC. RESULTS: HELn is not cytotoxic in the in vitro evaluation (IC50>200 µg/mL). It demonstrated a good spectrum of antibacterial activity with major activity against Shigella flexneri, Enterococcus faecalis, Staphylococcus aureus and Bacillus subtilis with MIC=6.25 µg/mL, Helicobacter pylori with MIC of 25 µg/mL and Streptococcus pyogenes with MIC of 50 µg/mL. Its mode of action is associated, at least partly, with changes in the permeability of bacterial membranes, as evidenced by the increased entry of hydrophobic antibiotics in Shigella flexneri and intense efflux of K(+) and nucleotide leakage in E. faecalis and Shigella flexneri. In addition, the presence of phenols, flavonoids and carotenoids, described in the literature to possess antibacterial effects, were detected in the composition of HELn, with high phenol content (11.55%), especially the flavonoids (6.47%). CONCLUSION: The results indicate that HELn has low cytotoxicity and potent antibacterial activity. It is bacteriostatic in nature, possibly acting at the level of bacterial membranes, especially on the cytoplasmic membrane and outer membrane, thus supporting its popular use in infectious processes. In addition, the presence of phenols, flavonoids, carotenoids, fatty acids and steroids, described in the literature as possessing antimicrobial activity, were detected in the composition of HELn.

Quantification of bioactive compounds in pulps and by-products of tropical fruits from Brazil.

This study aimed to quantify the levels of resveratrol, coumarin, and other bioactives in pulps and by-products of twelve tropical fruits from Brazil obtained during pulp production process. Pineapple, acerola, monbin, cashew apple, guava, soursop, papaya, mango, passion fruit, surinam cherry, sapodilla, and tamarind pulps were evaluated as well as their by-products (peel, pulp's leftovers, and seed). Total phenolic, anthocyanins, yellow flavonoids, ß-carotene and lycopene levels were also determined. Resveratrol was identified in guava and surinam cherry by-products and coumarin in passion fruit, guava and surinam cherry by-products and mango pulp. These fruit pulp and by-products could be considered a new natural source of both compounds. Overall, fruit by-products presented higher (P<0.05) bioactive content than their respective fruit pulps. This study provides novel information about tropical fruits and their by-products bioactive composition, which is essential for the understanding of their nutraceutical potential and future application in the food industry.