Evaluation of the Antioxidant Activity and Phenolic Composition of Different Monofloral and Polyfloral Brazilian Honey Extracts.

This study aimed to evaluate the chemical composition and antioxidant activity of phenolic extracts from monofloral and polyfloral honey samples obtained from different Brazilian regions. The chemical composition (total content of phenolic compounds and flavonoids) of extracts were measured by using colorimetric assays and analyzed by high performance liquid chromatographic (HPLC-DAD). The antioxidant activity was evaluated by chemical and biochemical assays (reducing power assay, 1,1-diphenyl-2-picrylhydrazyl (DPPH⋅) and 2,2-azino-bis(3-ethylbenzothiazoline-6-sulphonic) acid (ABTS⋅+) scavenger assays. It was also investigated the ability of extracts in attenuate lipid peroxidation induced by Fe2+ in phospholipids. The obtained results clearly demonstrated that the botanical origin and geographical region of honey collection influenced the chemical composition and antioxidant activity of extracts. Furthermore, the samples were constituted by phenolic acids and flavonoids, which p-coumaric acid was predominant among the compounds identified. All samples were able to scavenge free radicals and inhibit lipid peroxidation, and good correlations were obtained between the flavonoid content and honey color. In conclusion, the obtained extracts were constituted by antioxidant compounds, which reinforce the usage of honey in human diets, and demonstrated that the region of honey collection strong influenced in the chemical composition and, consequently, its biological effect.

Effects of Gender and Geographical Origin on the Chemical Composition and Antiradical Activity of Baccharis myriocephala and Baccharis trimera.

This study aimed to characterize and compare essential oils and ethyl acetate fractions obtained in basic and acidic conditions from both male and female Baccharis species (Baccharis myriocephala and Baccharis trimera) from two different Brazilian regions. Samples were characterized according to their chemical compositions and antiradical activity by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays. Principal component analysis (PCA) provided a clear separation regarding the chemical composition of essential oils from the samples obtained from different regions by using gas chromatography-mass spectrometry with flame-ionization detection (GC-MS-FID). PCA also revealed that gender and region of plant collections did not influence the chemical composition and antiradical activity of ethyl acetate fractions, which was corroborated with hierarchical cluster analysis (HCA) data. High performance liquid chromatography with diode-array detector (HPLC-DAD) identified significant quantities of flavonoids and phenolic acids in the fractions obtained in basic and acidic fractions, respectively. The obtained results clearly demonstrated that the geographical region of plant collection influenced the chemical composition of essential oils from the studied Baccharis species. Moreover, the obtained fractions were constituted by several antiradical compounds, which reinforced the usage of these species in folk medicine.

Effects of different levels of exploration on the ecological processes of Dimorphandra gardneriana, a tropical savanna tree.

The exploitation of forest resources, especially non-timber forest products, has effects on different biological levels, from the biochemical level of an organism to the ecosystem level. The present study addresses the effects of different management strategies (protected area, managed area, and an area where the species is cultivated in agroforestry systems) in reproductive phenology, fruit features, and phytochemical profiles of Dimorphandra gardneriana (Leguminosae), a tree species, pioneer, and socioeconomically important plant of the Brazilian Savanna. Its fruits are exploited by extractivist communities to obtain rutin and quercetin, which are internationally traded bioflavonoids (two of the ten most exported phytochemicals in Brazil). The results showed that the effects on these parameters were characterized as positive, increasing according to the level of exploitation. The agroforestry system had higher yields of flavonoids of economic interest, viable fruits and seeds, followed by the management area and the protected area. Finally, knowledge about the planting effects on fava d'anta fruit production can be a great ally for effectively managing forest resources. A varied system of exploitation implies greater and more stable economic returns for extractive communities, favoring the conservation of the species in protected areas.

Croton campestris A. St.-Hill Methanolic Fraction in a Chlorpyrifos-Induced Toxicity Model in Drosophila melanogaster: Protective Role of Gallic Acid.

Croton campestris A. St-Hill popularly known as "velame do campo" is a native species of the savannah from northeastern Brazil, being used in folk medicine due to its beneficial effects in the treatment of many diseases, inflammation, detoxification, gastritis, and syphilis; however, its potential use as an antidote against organophosphorus compound poisoning has not yet been shown. Here, the protective effect of the methanolic fraction of C. campestris A. St.-Hill (MFCC) in Drosophila melanogaster exposed to chlorpyrifos (CP) was investigated. Flies were exposed to CP and MFCC during 48 h through the diet. Following the treatments, parameters such as mortality, locomotor behavior, and oxidative stress markers were evaluated. Exposure of flies to CP induced significant impairments in survival and locomotor performance. In parallel, increased reactive oxygen species and lipoperoxidation occurred. In addition, the activity of acetylcholinesterase was inhibited by CP, and superoxide dismutase and glutathione S-transferase activity was induced. Treatment with MFCC resulted in a blockage of all CP-induced effects, with the exception of glutathione S-transferase. Among the major compounds found in MFCC, only gallic acid (GA) showed a protective role against CP while quercetin and caffeic acid alone were ineffective. When in combination, these compounds avoided the toxicity of CP at the same level as GA. As far as we know, this is the first study reporting the protective effect of MFCC against organophosphate toxicity in vivo and highlights the biotechnological potential of this fraction attributing a major role in mediating the observed effects to GA. Therefore, MFCC may be considered a promising source for the development of new therapeutic agents for the treatment of organophosphate intoxications.

Ilex paraguariensis Attenuates Changes in Mortality, Behavioral and Biochemical Parameters Associated to Methyl Malonate or Malonate Exposure in Drosophila melanogaster.

Methylmalonic acidemia is a genetic disease characterized by accumulation of organic acids, such as methylmalonic (MMA) and malonic (MA) acids. Considering that the accumulation of MMA and MA causes several damages due to oxidative stress, antioxidants are thought to play a pivotal role in preventing deleterious effects associated with exposure to such compounds. Ilex paraguariensis (IP) was used here to test the hypothesis that supplementation with the aqueous extract of this plant could exert protective effect against MMA or MA induced mortality, behavioral and/or biochemical changes in Drosophila melanogaster (DM). Initially, a curve time- and dose-response to MMA (1-10 mM), MA (1-10 mM) and IP (63-500 µM) was performed. Thereafter, flies were concomitantly exposed to MA (5 mM), MMA (5 mM) and/or IP (250 µg/mL) during 15 days for survival assay, and for 48 hs to MA (1 or 5 mM), MMA (1 or 5 mM) and/or IP (250 µg/mL) for subsequent investigations. Both MMA and MA exposure resulted in higher incidence of mortality, a worse performance in the negative geotaxis assay and increased locomotion in open-field test as compared with control group. Furthermore, a marked increase in non-protein thiol (NPSH) and in thiobarbituric acid reactive substances (TBARS) levels, decrease in superoxide dismutase (SOD), catalase and acetylcholinesterase (AChE) activities, and decrease in MTT and resazurin reduction were noted in MMA or MA treated groups. IP treatment offered significant protection against all alterations associated to MMA or MA exposure. This study confirm the hypothesis that supplementation with IP offers protection against changes associated to MMA or MA exposure in DM, due, at least in part, to its antioxidant effect.

Anti-inflammatory activity of herb products from Licania rigida Benth.

PURPOSE: The objective of the present study was to evaluate the systemic anti-inflammatory activity of the hydroalcoholic extract of the leaves of Licania rigida Benth (EHFLR) on models of systemic inflammation in mice. METHODS: The quantitative chemical profiles of phenolic acids and flavonoids were performed by High-Performance Liquid Chromatography (HPLC). Systemic anti-inflammatory activity was determined from carrageenan and dextran-induced paw edema models and the animals were orally treated (p.o.) with EHFLR at doses of 25, 50, 100 mg/kg, indomethacin (10 mg/kg) for carrageenan-induced paw edema and promethazine (6 mg/kg) for dextran-induced paw edema. The possible mechanisms involved in the anti-inflammatory action of the extract were evaluated by the paw edema models induced by histamine and arachidonic acid, and by the model of carrageenan-induced peritonitis, where vascular permeability and leukocyte migration to the peritoneal cavity were evaluated. RESULTS: The results of the HPLC identified the presence of phenolic acids and flavonoids, with chlorogenic acid (1.16%) and Caempferol (0.81%) as the main constituents. From the results, it was concluded that the extract has an LD50 ≥5000 mg/kg when administered orally in mice as this dose did not trigger deaths in any of the observed groups. EHFLR (25 mg/kg) showed a significant antiderematogenic effect on histamine and arachidonic acid-induced paw edema at the third hour of the tests, with a percentage of inhibition of 46.64% and 18.33%, respectively. The extract (25 mg/kg, p.o.) also significantly reduced vascular permeability and leukocyte migration in the peritoneal cavity. CONCLUSIONS: It is concluded that EHFLR exerts a systemic anti-inflammatory action, which seems to depend, at least in part, on the inhibition of arachidonic acid metabolism and the action of vasoactive amines. In addition, the extract reduced the leukocyte migration in the peritoneal cavity, indicating that its action may be linked to the inhibition of pro-inflammatory cytokines.

Chemical composition and anti-Candida potencial of the extracts of Tarenaya spinosa (Jacq.) Raf. (Cleomaceae).

Phytochemical prospecting was performed by HPLC-DAD. The Inhibitory Concentration of 50% of mortality the microorganisms (IC50) was determined and a cell viability curve was obtained. Minimum Fungicidal Concentration (MFC) was determined by subculture in Sabourad Dextrose Agar. The effect of the combination extract/fluconazole was verified by microdilution, with the extracts in subinhibitory concentrations (MFC/16). Caffeic acid was the major compound of both extracts, representing 6.08% in the aqueous extract and 7.62% in the ethanolic extract. The extracts showed a fungistatic effect (MFC ≥ 16,384 µg/mL). The IC50 results demonstrated that the combination of the extracts with fluconazole were more significant than the products tested alone, with values from 4.9 to 34.8 µg/mL for the ethanolic extract/fluconazole and 5 to 84.7 µg/mL for the aqueous extract/fluconazole. The potentiating effect of fluconazole action was observed against C. albicans and C. tropicalis. In C. krusei the aqueous extract had an antagonistic effect.

GC-MS Chemical Characterization and In Vitro Evaluation of Antioxidant and Toxic Effects Using Drosophila melanogaster Model of the Essential Oil of Lantana montevidensis (Spreng) Briq.

Background and objectives: Natural products such as essential oils with antioxidant potential can reduce the level of oxidative stress and prevent the oxidation of biomolecules. In the present study, we investigated the antioxidant potential of Lantana montevidensis leaf essential oil (EOLM) in chemical and biological models using Drosophila melanogaster. Materials and methods: in addition, the chemical components of the oil were identified and quantified by gas chromatography coupled to mass spectrometry (GC-MS), and the percentage compositions were obtained from electronic integration measurements using flame ionization detection (FID). Results: our results demonstrated that EOLM is rich in terpenes with Germacrene-D (31.27%) and ß-caryophyllene (28.15%) as the major components. EOLM (0.12-0.48 g/mL) was ineffective in scavenging DPPH radical, and chelating Fe(II), but showed reducing activity at 0.24 g/mL and 0.48 g/mL. In in vivo studies, exposure of D. melanogaster to EOLM (0.12-0.48 g/mL) for 5 h resulted in 10% mortality; no change in oxidative stress parameters such as total thiol, non-protein thiol, and malondialdehyde contents, in comparison to control (p > 0.05). Conclusions: taken together, our results indicate EOLM may not be toxic at the concentrations tested, and thus may not be suitable for the development of new botanical insecticides, such as fumigants or spray-type control agents against Drosophila melanogaster.

Antinociceptive activity of Copaifera officinalis Jacq. L oil and kaurenoic acid in mice.

Copaifera officinalis L. possesses traditional uses as an analgesic, anti-inflammatory, and antiseptic. However, until now the antinociceptive effect and the mechanism of action were not described for Copaifera officinalis L. oil and no compound present in this oil was identified to be responsible for its biological effects. The goal of this study was to identify the presence of kaurenoic acid in Copaifera officinalis oil and investigate its antinociceptive effect, mechanism of action, and possible adverse effects in mice. The quantification of kaurenoic acid in Copaifera officinalis oil was done by HPLC-DAD technique. Male and female albino Swiss mice (25-35 g) were used to test the antinociceptive effect of Copaifera officinalis (10 mg/kg, intragastric) or kaurenoic acid (1 mg/kg) in the tail-flick test, intraplantar injection of capsaicin, allyl isothiocyanate (AITC) or complete Freund's adjuvant (CFA). Copaifera officinalis oil and kaurenoic acid caused the antinociceptive effect in the tail-flick test in a dose-dependent manner, and their effect was reversed by naloxone (an opioid antagonist). Copaifera officinalis oil or kaurenoic acid reduced the nociception caused by capsaicin or AITC and produced an anti-allodynic effect in the CFA model (after acute or repeated administration for 7 days). Possible adverse effects were also observed, and non-detectable adverse effect was observed for the intragastric administration of Copaiba officinalis oil or kaurenoic acid and in the same way, the treatments were neither genotoxic nor mutagenic at the doses tested. Thus, Copaiba officinalis oil, and kaurenoic acid possess antinociceptive action without adverse effects.

In vitro activities of Ceiba speciosa (A.St.-Hil) Ravenna aqueous stem bark extract.

Several species of the genus Ceiba (Malvaceae) are ethnopharmacologically used. Thus, this study aimed to investigate the in vitro beneficial properties of the aqueous stem bark extract of Ceiba speciosa. The extract presented a great amount of phenolic compounds (117.4 ± 6.2 mg GAE/g). The antioxidant activity was assessed by DPPH (IC50 = 42.87 µg/mL), ORAC (2351.17 µmol TE/g) and FRAP (235.94 µM FeSO4/g) methods. In addition, the extract reduced MCF-7 cell viability as assessed by MTT. However, it prevented mitochondrial membrane depolarization and reduced caspase-9 activity induced by hydrogen peroxide. In conclusion, these findings indicate the extract is an excellent source of natural antioxidants and is able to protect ROS-induced cell death. Therefore, C. speciosa extract may possess beneficial properties for application in pharmaceutical industry as an antioxidant. However, further studies to better elucidate its mechanisms and to isolate its active compounds are required.

Chemical analysis and evaluation of antioxidant and antimicrobial activities of fruit fractions of Mauritia flexuosa L. f. (Arecaceae).

BACKGROUND: Fruit consumption is currently considered beyond the nutritional aspects because of the important roles in disease prevention and benefits to health. The objective of this study was to characterize the chemical profile and evaluate the antioxidant and antimicrobial properties of different fractions obtained from fruit pulps of Mauritia flexuosa (MFFs). METHODS: Initially, chloroform, ethyl acetate and ethanol fractions were obtained from the pulps. Quantifications of total phenols and flavonoids were performed using the methods of Folin-Ciocalteu and complexation with aluminum chloride, respectively. Standard samples were used to identify and quantify phenolic acids and flavonoids using high-performance liquid chromatography with a diode-array detector (HPLC-DAD). The antioxidant capacity of the fractions was verified by sequestration of the free radical 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid (ABTS) and iron chelating activity. The antimicrobial activity was determined using the microdilution method and the modulating activity was determined using sub-inhibitory concentrations of the fractions in association with antibiotics. RESULTS: The chemical analyzes revealed the presence of catechin, caffeic acid, rutin, orientin, quercetin, apigenin, luteolin and kaempferol, where all are present in the ethyl acetate fraction. The fractions exhibited moderate antioxidant and antimicrobial activities against Gram-positive and Candida strains in addition to modulating the activity of conventional antibiotics. The most expressive result was obtained from the association of the chloroform fraction with cefotaxime, which produced a synergistic effect, reducing the minimum inhibitory concentration (MIC) of the antibiotic from 1,024 to 256 µg/mL. DISCUSSION: The fractions presented a constitution rich in phenolic compounds, especially flavonoids. The data obtained demonstrated that the fractions presented moderate antioxidant activity by acting both as primary and secondary antioxidants. The fractions presented antimicrobial and antibiotic potentiating activities, being the first record of modulating effect of fractions of this species against the studied microbial strains, but failed in modulating the activity of antifungal drugs, indicating that this plant has the potential to be used in the development of therapeutic alternatives against resistant bacteria. The constitution phenolic the fractions may be responsible for their pharmacological properties in vitro.

Immunotoxicological Evaluation of Schinus molle L. (Anacardiaceae) Essential Oil in Lymphocytes and Macrophages.

Schinus molle L. is used to treat various diseases; however, the literature lacks information regarding its possible immunotoxic effects. The aim of the study was to investigate the immunotoxic effects of essential oil from leaves of Schinus molle L. in cultures of human lymphocytes and macrophages. The cultures were treated with essential oil (EO) of Schinus molle L. and subsequently subjected to genotoxic analysis (comet assay), mutagenic analysis (micronucleus frequency and chromosomal aberration), and cytotoxic (cell viability) and functional parameters (interleukins secretions). Our analyses have determined that the essential oil from leaves of Schinus molle L. presents several compounds with α-pinene being the major compound; in addition, the compound verbenene was firstly identified; genotoxic effects were detected only in macrophages and only at the two highest concentrations tested. An important finding is that Schinus molle L. oil causes an activation of the immune system. This action has its mechanism centered by the cascade nitric oxide-interleukin-10-tumor necrosis factor alpha.

Brazil nut improves the oxidative metabolism of superoxide-hydrogen peroxide chemically-imbalanced human fibroblasts in a nutrigenomic manner.

There are some genes associated to the risk of chronic diseases that present potential nutrigenetic response, such as the human manganese-dependent superoxide dismutase gene (Val16Ala-SOD2, rs4880) for which homozygous genotypes (VV and AA) are associated with higher basal superoxide (S) and hydrogen peroxide (HP) levels, respectively. It is possible that the VV- and AA-imbalance could be attenuated by selenium(Se)-rich foods such as Brazil nut (BN). To test this hypothesis, we conducted an in vitro protocol triggering a chemical S-HP imbalance by exposure of dermal fibroblast cells (HFF-1) to paraquat, which generates high S levels (VV-like treatment) and porphyrin (MnTBAP), which generates high HP levels (AA-like treatment). Modulation of cell growth and pro-oxidative and antioxidant markers were evaluated. BN aqueous extract (BNAE) most effective concentration which increased cell growth and decreased oxidative metabolism indicators of imbalanced cells was 75 ng Se/mL. However, this effect was not directly affected by the S-HP imbalance: in AA-SOD2-like cells, thioredoxin reductase (TrxR-1) gene was upregulated and in VV-SOD2-like cells an upregulation of glutathione peroxidase (GPx-1) gene expression was observed, however, this regulation occured in a homeostatic manner. These results suggest that BNAE was able to minimize negative effects in both directions of the S-HP imbalance, by modulation of different oxidative-metabolic pathways.

Antioxidant activity and physicochemical characteristics of honeys from the eastern Amazon region, Brazil / Atividade antioxidante e características físico-químicas de méis da Amazônia Oriental, Brasil

Honey is a natural product that has several beneficial properties for health, such as anti-inflammatory, antioxidant and antimicrobial activities, which depend on its composition. In this context, physicochemical properties (colour, pH, ash, moisture, sugars, and total phenolic contents) and antioxidant activity (DPPH radical scavenging ability) of Apis mellifera honeys from Santarém, the main honey production area in the eastern Amazon region, were evaluated. Most samples were dark in colour and acidic. The ash and moisture contents ranged from 0.112 to 0.318 and from 14.751 to 17.514, respectively. The reducing sugars content was 62.873-91.563%. The total amount of phenolic compounds was higher than normally reported, ranging between 15.22 and 16.51 mg g1 and 17.70 and 18.94 mg g1, for honey after and before exposure to light, respectively. Quercetin was found only in honey that had been protected from light, with values ranging from 0.24 to 0.43 mg g-1. The absence of quercetin in the samples of honey exposed to light suggests that UV radiation has degraded this compound. All samples presented maximum radical scavenging capacity close to 50%. Our results showed inverse correlations between the colour and pH, ash, reducing sugars, and moisture content, and positive correlations between the colour and the concentration of phenolic compounds, and antioxidant activity.(AU)

O mel é um produto natural que apresenta várias propriedades benéficas para a saúde, tais como atividade antinflamatória, antioxidante e antimicrobiana, as quais dependem de sua composição. Neste contexto, as propriedades físico-químicas (cor, pH, conteúdo de cinzas, umidade, açúcares e compostos fenólicos totais) e a atividade antioxidadente (capacidade de remoção do radical DPPH) de méis de abelhas Apis mellifera de Santarém, na principal região de produção de mel na Amazônia Oriental, Brasil, foram avaliadas. A maioria das amostras teve cor escura e apresentaram-se ácidas. Os teores de cinzas e a umidade variaram de 0,112 a 0,318 e de 14,751 a 17,514, respectivamente. O teor de açúcares redutores vairou entre 62,873 e 91,563%. O teor total de compostos fenólicos foi mais elevado que os já reportados na literatura, variando entre 15,22 e 16,51 mg g1 e 17,70 e 18,94 mg g1 para amostras de mel protegidas e expostas à radiação UV, respectivamente. A quercetina foi encontrada apenas no mel que foi protegido da luz, com teores variando entre 0,24 e 0,43 mg g1. A ausência de quercetina nas amostras de mel expostas à luz sugere que a radiação UV pode ter degradado esse composto. Todas as amostras apresentaram máxima capacidade de remover o radical DPPH próxima a 50%. Houve correlação inversa entre a cor e o pH, cinzas, açúcares redutores e teor de umidade, e correlação positiva entre a cor e o teor de composto fenólicos e a atividade antioxidante.(AU)

Antioxidant activity and physicochemical characteristics of honeys from the eastern Amazon region, Brazil / Atividade antioxidante e características físico-químicas de méis da Amazônia Oriental, Brasil / Antioxidant activity and physicochemical characteristics of honeys from the eastern Amazon region, Brazil

RESUMO O mel é um produto natural que apresenta várias propriedades benéficas para a saúde, tais como atividade antinflamatória, antioxidante e antimicrobiana, as quais dependem de sua composição. Neste contexto, as propriedades físico-químicas (cor, pH, conteúdo de cinzas, umidade, açúcares e compostos fenólicos totais) e a atividade antioxidadente (capacidade de remoção do radical DPPH) de méis de abelhas Apis mellifera de Santarém, na principal região de produção de mel na Amazônia Oriental, Brasil, foram avaliadas. A maioria das amostras teve cor escura e apresentaram-se ácidas. Os teores de cinzas e a umidade variaram de 0,112 a 0,318 e de 14,751 a 17,514, respectivamente. O teor de açúcares redutores vairou entre 62,873 e 91,563%. O teor total de compostos fenólicos foi mais elevado que os já reportados na literatura, variando entre 15,22 e 16,51 mg g−1 e 17,70 e 18,94 mg g−1 para amostras de mel protegidas e expostas à radiação UV, respectivamente. A quercetina foi encontrada apenas no mel que foi protegido da luz, com teores variando entre 0,24 e 0,43 mg g−1. A ausência de quercetina nas amostras de mel expostas à luz sugere que a radiação UV pode ter degradado esse composto. Todas as amostras apresentaram máxima capacidade de remover o radical DPPH próxima a 50%. Houve correlação inversa entre a cor e o pH, cinzas, açúcares redutores e teor de umidade, e correlação positiva entre a cor e o teor de composto fenólicos e a atividade antioxidante.

ABSTRACT Honey is a natural product that has several beneficial properties for health, such as anti-inflammatory, antioxidant and antimicrobial activities, which depend on its composition. In this context, physicochemical properties (colour, pH, ash, moisture, sugars, and total phenolic contents) and antioxidant activity (DPPH radical scavenging ability) of Apis mellifera honeys from Santarém, the main honey production area in the eastern Amazon region, were evaluated. Most samples were dark in colour and acidic. The ash and moisture contents ranged from 0.112 to 0.318 and from 14.751 to 17.514, respectively. The reducing sugars content was 62.873-91.563%. The total amount of phenolic compounds was higher than normally reported, ranging between 15.22 and 16.51 mg g−1 and 17.70 and 18.94 mg g−1, for honey after and before exposure to light, respectively. Quercetin was found only in honey that had been protected from light, with values ranging from 0.24 to 0.43 mg g-1. The absence of quercetin in the samples of honey exposed to light suggests that UV radiation has degraded this compound. All samples presented maximum radical scavenging capacity close to 50%. Our results showed inverse correlations between the colour and pH, ash, reducing sugars, and moisture content, and positive correlations between the colour and the concentration of phenolic compounds, and antioxidant activity.

Phytochemical profile and mechanisms involved in the anti-nociception caused by the hydroethanolic extract obtained from Tocoyena formosa (Cham. & Schltdl.) K. Schum (Jenipapo-bravo) leaves in mice.

Tocoyena formosa, a small ornamental tree growing in the dry regions of central Brazil, is commonly known as 'genipapo do bravo'. This is a medicinal plant traditionally used as an analgesic for rheumatic pain, lower back pain and myalgia, however its use is carried out without scientific evidence, which thus justifies the development of studies to investigate and prove its therapeutic potential. Therefore, the objective of this study was to evaluate the phytochemical profile of Tocoyena formosa (Cham. & Schlecht.) K. Schum (TFLHE) and the mechanisms involved in its anti-nociceptive effect. The TFLHE revealed the presence of gallic acid, catechin, chlorogenic acid, caffeic acid, ellagic acid, rutin, quercetin and luteolin. The TFLHE at doses of 200 and 400mg/kg significantly decreased acetic acid-induced abdominal contortions, the reaction time for the formalin test in both phases and increased the paw withdrawal time in the hot plate thermal stimulus test. The 200mg/kg dose also significantly inhibited the plantar mechanical hyperalgesia intensity induced by formalin within 24h. TREATMENT: with the TFLHE did not cause significant changes in motor performance and coordination in the Rota Rod test. The investigation on the possible mechanism of antinociceptive action of TFLHE indicates the involvement of opioid, glutamatergic, nitric oxide/cGMP and vanilloid systems. It is concluded that the TFLHE has an antinociceptive effect promoted by the aforementioned mechanisms.

Toxicity against Drosophila melanogaster and antiedematogenic and antimicrobial activities of Alternanthera brasiliana (L.) Kuntze (Amaranthaceae).

Bioactive phytocompounds are studied by several bioactivities demonstrated, as their cytotoxic effects. The aim of this work was to evaluate the phytochemical profile, the toxic effect using the Drosophila melanogaster animal model and the anti-inflammatory and antimicrobial effect of the Alternanthera brasiliana (EEAB) ethanol extract. The phytochemical profile was performed using HPLC. The cytotoxic effect was evaluated in vivo using D. melanogaster. The anti-inflammatory effect was determined by neurogenic and antiedematogenic assays, and the antimicrobial activity was assayed using a microdilution method to determine the minimum inhibitory concentration (MIC) of the EEAB alone and in association with antibiotics. The main compound identified on the EEAB was luteolin (1.93%). Its cytotoxic effect was demonstrated after 24 h in the concentrations of 10, 20 and 40 mg/mL. The extract demonstrated an antiedematogenic effect, with a reduction of the edema between 35.57 and 64.17%. The MIC of the extract was ≥1.024 µg/mL, thus being considered clinically irrelevant. However, when the EEAB was associated with gentamicin, a synergism against all bacterial strains assayed was observed: Staphylococcus aureus (SA10), Escherichia coli (EC06) and Pseudomonas aeruginosa (PA24). Due to these results, the EEAB demonstrated a low toxicity in vivo and anti-inflammatory and synergistic activities. These are promising results, mainly against microbial pathogens, and the compounds identified can be a source of carbon backbones for the discovery and creation of new drugs.

Antioxidant and mercury chelating activity of Psidium guajava var. pomifera L. leaves hydroalcoholic extract.

Mercury (Hg) is widely distributed in the environment and is known to produce several adverse effects in organisms. The aim of the present study was to examine the in vitro antioxidant activity and Hg chelating ability of the hydroalcoholic extract of Psidium guajava leaves (HEPG). In addition, the potential protective effects of HEPG against Hg(II) were evaluated using a yeast model (Saccharomyces cerevisiae). HEPG was found to exert significant antioxidant activity in 2,2-diphenyl-1-picrylhydrazyl scavenger and inhibition of lipid peroxidation induced by Fe(II) assays in a concentration-dependent manner. The extract also exhibited significant Hg(II) chelating activity. In yeast, Hg(II) induced a significant decrease in cell viability. In contrast, HEPG partially prevented the fall in cell viability induced by Hg(II). In conclusion, HEPG exhibited protective effects against Hg(II)-mediated toxicity, which may be related to both antioxidant and Hg(II)-chelating activities.

Safety evaluation of supratherapeutic dose of Maytenus ilicifolia Mart. ex Reissek extracts on fertility and neurobehavioral status of male and pregnant rats.

Maytenus ilicifolia Mart. ex Reissek is a plant commonly used in folklore medicine in the management of gastric diseases in South America. This study explores the effects of a supratherapeutic dose of aqueous and ethanol extracts of M. ilicifolia (1360 mg/kg) on fertility and neurobehavioral status in male and pregnant rats. A battery of sensory-motor developmental endpoints was carried out to assess impairments on pups of dams orally treated with the aqueous extract of M. ilicifolia during the organogenesis period of pregnancy (GD 9 through GD 14). The neuromotor maturation reflexes and physical developments of the offspring were not significantly different between the groups (p < 0.05). Also, the hippocampal morphology revealed no indices of cell loss in the CA1, CA2, CA3 and CA4 areas. As second protocol, some fertility aspects were investigated in young post pubertal male Wistar rats treated with the ethanol extract for 30 days. The semen quality and testicular tissue morphology of male rats treated with the ethanol extract of M. ilicifolia remained unaffected upon treatment. Thus, the results indicate that the high-dose of M. ilicifolia extracts have no neurotoxic potential on offspring and seem not to affect the sperm quality of male rats.

Buddleja thyrsoides Lam. crude extract presents antinociceptive effect on an arthritic pain model in mice.

Arthritis is a chronic inflammatory disease which reduces the life quality of affected individuals. Therapeutic tools used for treating inflammatory pain are associated with several undesirable effects. Buddleja thyrsoides Lam., known as 'Barbasco' or 'Cambara', is mostly used in several disorders and possesses antirheumatic, anti-inflammatory, and analgesic properties. Here, we investigated the antinociceptive and anti-inflammatory effects of the B. thyrsoides crude extract applied orally and topically in acute pain models and an arthritic pain model induced by complete Freund's adjuvant (CFA) paw injection in male mice (25-30 g). The high-performance liquid chromatography (HPLC) of the B. thyrsoides extract crude revealed the presence of the lupeol, stigmasterol, and ß-sitosterol. The stability study of the B. thyrsoides gel did not show relevant changes at low temperatures. The oral treatment with the B. thrysoides extract prevented the capsaicin-induced spontaneous nociception and the acetic acid-induced abdominal writhing, but did not alter the thermal threshold in the tail immersion test. The B. thyrsoides antinociceptive effect was not reversed by naloxone in the capsaicin test. The B. thyrsoides oral or topical treatment reversed the CFA-induced mechanical allodynia and thermal hyperalgesia with maximum inhibition (Imax) of 69 ± 6 and 68 ± 5% as well as 78 ± 15 and 87 ± 12%, respectively. Moreover, the topical but not oral treatment inhibited the CFA-induced cell infiltration, but did not reduce the paw edema significantly. The oral treatment with B. thyrsoides did not cause adverse effects. These findings suggest that the oral or topical treatment with B. thyrsoides presents antinociceptive actions in an arthritic pain model without causing adverse effects.