Obtaining Hexoses from Chitosan through Depolymerization with Nitrous Acid.

BACKGROUND AND OBJECTIVE: Residues from shrimp farming have a great potential for sugar production and the production of derivatives for the low-carbon chemical industry. Obtainment of bioactives from chitosan has been extensively investigated using different methodologies. The purpose of this work was to study the chitosan depolymerization reaction aiming at the production of monomers without the use of additional enzymes or mineral acids. MATERIALS AND METHODS: In this work, we systematically study the effect of sodium nitrite concentration and reaction conditions (pH and temperature ranges) with acetic acid as the solvent on the chitosan depolymerization reaction aiming at the production of monomers, specifically 2,5- anhydromannose, without the use of additional enzymes or mineral acids. RESULTS: The results indicate that only a small range of reaction conditions and nitrite concentrations allow for obtaining the monomer, while in most combinations of these parameters, oligomers are obtained. We found that the temperature decisively affects the reaction yield, with the attainment of 2,5-anhydromannose favored at lower temperatures. CONCLUSION: The method proved to be simple and easy to perform allowing to obtain 2,5- anhydromannose with the use of low-cost reagents. This monomer can be converted into several derivatives for industrial application (5-Hydroxymethylfurfural, ethanol, etc.).

Preliminary Report on the Effect of Savanna Plants Leucaena leucocephala, Parkia platycephala and Senna alata against Eggs and Immature Stages of Trichostrongylid Nematodes In Vitro.

The current study evaluated the anthelmintic effect of different extracts of Leucaena leucocephala, Parkia platycephala, and Senna alata on trichostrongylid eggs and infective larvae and determined the potential active components of each plant. Dried and macerated plant material was concentrated using rotaevaporation to obtain the crude extract (CE), followed by solvent partitioning to obtain hexanic (HexE), acetatic (AcE), and butanolic (BuE) extracts used for phytochemical analysis and anthelmintic efficacy testing in vitro. All the crude and partitioned extracts tested showed inhibition activity in the hatching of trichostrongylid eggs. Larvicidal efficacy was observed at CE concentrations of 2.5, 5.0, and 7.5 mg/mL for P. platycephala and S. alata. However, L. leucocephala CE did not significantly reduce the number of living larvae in the tested concentrations. Chromatographic analysis revealed several active metabolites; gallic acid, ellagic acid, naringin, morin, and kaempferol on AcE of P. platycephala; gallic acid, rutin, and ellagic acid on BuE of P. platycephala; and gallic acid and naringin on BuE of L. leucocephala. The extracts of P. platycephala, L. leucocephala, and S. alata leaves showed egg hatching inhibition and larvicidal activity, probably produced by tannins and flavonoids, which may act alone or by synergism.

Cochlospermum regium (Mart. ex Schrank) Pilg.: Evaluation of chemical profile, gastroprotective activity and mechanism of action of hydroethanolic extract of its xylopodium in acute and chronic experimental models.

ETHNOPHARMACOLOGICAL RELEVANCE: Cochlospermum regium (Bixaceae) is a native shrub of Brazil and its xylopodium (infusion/decoction) is being used for the treatment of gastritis, ulcers, arthritis, intestinal infections, gynaecological infections, skin diseases, among others. The aim of the present study was to evaluate the gastroprotective/antiulcer activity and the mechanism of action of hydroethanolic extract of C. regium xylopodium (HECr), using in vitro and in vivo models. Additionally, phytochemical constituents were identified by high-performance liquid chromatography (HPLC). MATERIALS AND METHODS: C. regium xylopodium was macerated with ethanol/water to obtain the HECr. The phytochemical characterisation was carried out by HPLC. The antiulcer efficacy of HECr (25, 100 and 400 mg/kg, p.o.) was evaluated using acute acidified ethanol (HCl/EtOH), piroxicam and water immersion-induced experimental ulcer models. Chronic gastric ulcer healing activity of HECr was evaluated through acetic acid (99.8%) - induced model. Histological analysis and myeloperoxidase (MPO), glutathione (GSH), catalase (CAT) activities were also evaluated in chronic ulcer induced gastric tissues. The plausible mode of action of the HECr was assessed by estimation of gastric wall mucus production and the role of gastric secretion in pylorus ligature. The animals were also pre-treated with various inhibitors which includes indomethacin (10 mg/kg, p.o.) a selective inhibitor of cyclooxygenase, L-NAME (10 mg/kg, i.p.), an inhibitor of nitric oxide synthase, glibenclamide, a ATP-sensitive potassium channels (K+ATP) blocker (5 mg/kg, p.o.) or yohimbine (2 mg/kg, i.p.), an α2-adrenergic receptor antagonist. In vitro, Helicobacter pylori action was done by broth microdilution method. RESULTS: The HPLC analysis data revealed the presence of gallic acid, rutin, myricetin, morin and kaempferol. HECr promoted protective effect against acute ulcers induced by HCl/EtOH with inhibitions of 47.52% (p < 0.01) and 62.69% (p < 0.001) at 100 and 400 mg/kg, and in piroxicam by 34.11% (p < 0.05), 49.14% (p < 0.01) and 61.34% (p < 0.001), at 25, 100 or 400 mg/kg, respectively, and in water restraint stress by 78.26% inhibition, p < 0.001, at the dose of 400 mg/kg when compared to the vehicle control group respectively. In the chronic gastric ulcer model, HECr (25, 100 and 400 mg/kg p.o.) significantly (p < 0.001) decreased the injured area by 58.80%, 77.87% and 71.10% respectively. Histological examination indicated that oral treatment of HECr promoted healing of gastric lesions by regenerating gastric mucosa layer with less inflammatory cells. HECr augmented the GSH, CAT activities and reduced MPO level. The pre-treatment with HECr increased the gastric wall mucus production. It also significantly altered the gastric secretion parameters by causing the reduction in the gastric juice volume, elevated the pH level and reduced the total acidity at all doses tested when compared with the vehicle group. HECr at the most active dose (100 mg/kg) reversed completely the reduction of PGs, NO production, closure of K+ATP- channels and α2-adrenoreceptor blockage - induced damages. In microdilution assay, the HECr showed good anti-Helicobacter pylori effect with MIC = 100 µg/mL. CONCLUSION: The HECr presented preventive and curative effects in the experimental gastric ulcer models, besides good anti-Helicobacter pylori activity, which supports the traditional medicinal use of the xylopodium of this plant for gastrointestinal diseases. The underlying mechanisms of this antiulcerogenic/antiulcer action involve, at least, augmentation of mucus production, inhibition of gastric secretion, stimulation of PGs and NO synthesis. And that it involves activation of K+ATP channels and α-2-adrenergic receptors, in addition to an antioxidant activity, probably due to the presence of gallic acid and flavonoids in HECr.

Chemical characterization and evaluation of gastric antiulcer properties of the hydroethanolic extract of the stem bark of Virola elongata (Benth.) Warb.

ETHNOPHARMACOLOGICAL RELEVANCE: Virola elongata is a tree species belonging to the Myristicaceae family, distributed in the North and Midwest regions of Brazil, in the phytogeographic domain of the Amazon. The aqueous infusion or the hydroethanolic macerate of the stem bark of V. elongata are used in Brazilian and Ecuadorian indigenous folk medicine for several ethnopharmacological purposes, principally, in the treatment of stomach pain, indigestions, and gastric ulcers. This study was aimed to investigate the gastroprotective activity of this plant in order to support its popular use with scientific evidence. MATERIALS AND METHODS: The stem bark hydroethanolic extract of the plant (HEVe) was prepared by maceration. Its qualitative and quantitative phytochemical constituents were investigated by classical colorimetric techniques, HPLC, and electrospray ionization-multiple stage fragmentation (ESI-MSn). The gastroprotective and antiulcer activity of HEVe at doses of 100, 300 and 900 mg/kg p.o. were tested using three acute (acidified ethanol, piroxicam, and in-water-restrain stress), and one chronic (acetic acid) animal ulcer models. The probable mode of action of the HEVe was evaluated by analyzing gastric acid secretion, mucus content, nitric oxide effect, and its antioxidant properties (on catalase, myeloperoxidase, and GSH content) in experimental rodents. The direct extract's activity on the growth of Helicobacter pylori was also investigated. RESULTS: Total phenolic content in the HEVe was of 146.20 ±â€¯1.07 mg, being flavonoids about 50% (71.79 ±â€¯0.70 mg) of it. Comparative HPLC fingerprint analysis revealed the presence of known phenolic antiulcer compounds, such as gallic acid, catechin, and rutin. Also, methanol/water fractionation and ESI-MSn analysis of the HEVe reveals the presence of quinic acid, 3,3',4-trihydroxystilbene, juruenolid D, one catechin dimer, one C-glycosyl flavonoid, one polyketide and two neolignans as the major components of the extract. The HEVe attenuated gastric ulceration in all the different models of acute gastric ulcer, by enhancing gastroprotection through its antioxidant properties in vivo, and reducing also considerably the gastric secretion and total acidity. The HEVe also presented healing properties against the induced chronic ulceration process. On the other hand, the HEVe did not exhibit direct activity against H. pylori. CONCLUSION: The HEVe exhibited significant gastroprotective/antiulcer effects and contain a relative high proportion of phenolic compounds, especially flavonoids, that could likely account, at least in part, for its pharmacological properties. The results justify its traditional usage and provided scientific evidence for its potential as a new herbal medicine to treat gastric ulcers.

Chemical characterisation and toxicity assessment in vitro and in vivo of the hydroethanolic extract of Terminalia argentea Mart. leaves.

ETHNOPHARMACOLOGICAL RELEVANCE: Terminalia argentea Mart. (Combretaceae), known mainly as "capitão", is a native tree, not endemic, that occurs in the Amazon, Caatinga, Cerrado and Atlantic Forest in Brazil. Leaf infusion is popularly mentioned by riverine communities that inhabit the microregion of Northern Araguaia (Mato Grosso, Brazil) for the treatment of gastric ulcer, bronchitis and haemorrhage. Considering the wide medicinal use, lack of studies that evaluate the safety of use and the scarcity of phytochemical studies of T. argentea leaves, this work was carried out with the objective of evaluating the toxicity of the hydroethanolic extract of the leaves of T. argentea Mart. (HETa) in experimental models in vivo and in vitro, as well as to advance the phytochemical analysis of HETa. MATERIALS AND METHODS: HETa was prepared by macerating the leaf powder in hydroethanolic solution. Phytochemical characterisation was carried out by thin-layer chromatography (TLC), high-performance liquid chromatography (HPLC) and mass spectrometry through direct flow infusion coupled with electrospray ionization and ion-trap analyzer (DFI-ESI-IT-MS analyses) The contents of phenols, flavonoids and phytosterols were analysed by colorimetric methods. Cytotoxicity was assessed by the Alamar blue assay on Chinese hamster ovary epithelial cells (CHO-K1) and human gastric adenocarcinoma cells (AGS). In vitro genotoxicity of HETa (10, 30 or 100 µg/mL) was assessed by micronucleus (MN) and comet tests using CHO-K1 cells. The acute toxicity assessment was performed by oral administration of HETa in single dose Swiss mice (males and females) up to 2000 mg/kg and sub-chronic toxicity by daily oral administration of HETa (50, 200 and 800 mg/kg) in Wistar rats for 30 days. The parameters related to the clinical and toxicological observations were determined every 6 days and at the end of the treatment the blood was collected for biochemical and haematological analysis, and some organs were removed for macroscopic and histopathological analysis. RESULTS: Preliminary phytochemistry and TLC analysis of HETa revealed the presence of phenolic compounds (18.8%), flavonoids (10.8%), saponins, tannins and phytosterols (19%). The HPLC data revealed the presence of gallic acid, rutin, ellagic acid, catechin, quercetin and kaempferol. In the analysis by DFI-ESI-IT-MS, the presence of gallic acid, rutin, ellagic acid and quercetin was confirmed and identified caffeic acid, quinic acid, galloylmucic acid, quercetin xyloside, quercetin rhamnoside, quercetin glucoside, caffeoyl ellagic acid, quercetin galloyl xyloside, terminalin, quercetin galloyl glucose, corilagin, quercetin digalloyl xyloside, quercetin digalloyl glucoside, punicalin and punicalagin. HETa showed no cytotoxic effect on CHO-K1 and AGS cells. In the MN assay, HETa increased the number of MNs and nuclear buds (NBUDs) in binucleate cells at the three concentrations tested and the nucleoplasmic bridges (NPBs) number at 30 µg/mL. In the comet test, HETa (10 and 100 µg/mL) alone showed a genotoxic effect on CHO-K1 cells. In pre-treatment, HETa at all concentrations tested prevented DNA damage induced by H2O2. In co-treatment with H2O2, HETa showed genotoxic effects at the three concentrations, and post-treatment DNA damage in exposed CHO-K1 cells to H2O2 was repaired in 22.5% with 10 µg/mL HETa. In the acute toxicity test, the HETa did not cause death in the mice, being verified only by piloerection and reversible in 2 h in males and in 4 days in females. No macroscopic changes were observed in the analysed organs. In the sub-chronic toxicity test, the HETa did not cause death in the rats after 30 days and the few changes were: absolute (103/mm3) and relative (%) values of basophils increased by 477.8% and 423% (p < 0.001), respectively, with 50 mg/kg; reduction in feed intake (23.6%, p < 0.01) only on day 18; total cholesterol concentration (13.1%, p < 0.05) and relative heart weight (13.2% %, p < 0.05) at a dose of 800 mg/kg. These effects were not dose-dependent nor followed by clinical signs and symptoms of intoxication, nor of macroscopic and histopathological changes in the organs of animals treated with HETa. CONCLUSIONS: The results demonstrated that HETa had no cytotoxic in vitro effects for CHO-K1 and AGS cells. In in vitro genotoxicity assays, the HETa induced different responses, according to concentration and experimental condition. In the MN test the HETa presented genotoxic potential by increasing the number of MNs, NBUDs and NPBs. In the comet assay, HETa was genotoxic by itself and in the co-treatment protocol with H2O2. In pre-treatment or post-treatment protocols with H2O2, HETa presented an antigenotoxic effect by preventing or repairing, respectively, the genotoxicity induced by H2O2. In the in vivo models, HETa was shown to be relatively safe after acute administration in mice [no-observed-adverse effect level (NOAEL) of 2000 mg/kg] and sub-chronic in rats (NOAEL of 800 mg/kg), confirming the riverine information that it is non-toxic in the dosage used. Phytochemical analysis of HETa revealed the presence of phenolic compounds, flavonoids, saponins, tannins and phytosterols. Among the flavonoids and tannins, we highlight gallic acid, rutin, ellagic acid, quercetin, caffeic acid, quinic acid, corilagin, punicalin and punicalagin. Thus, it can be stated that HETa has a good safety margin for therapeutic use.

Assessment of toxicity and differential antimicrobial activity of methanol extract of rhizome of Simaba ferruginea A. St.-Hil. and its isolate canthin-6-one.

ETHNOPHARMACOLOGICAL RELEVANCE: Simaba ferruginea A. St.-Hil., Simaroubaceae, popularly known as "calunga" is a typical subtropical shrub used in Central Brazil mainly for infection, anti-inflammatory, analgesic and gastric duodenal-ulcers. It presents in its composition the alkaloid canthin-6-one, an alkaloid indole ß-carboxylic. AIM: This study aims to investigate the toxicity, antimicrobial activities of methanol extract of Simaba ferruginea (MESf) and canthin-6-one by using different experimental models. METHODS: The present study evaluated the phytochemical analysis by high performance liquid chromatography (HPLC), toxicological potential of MESf and canthin-6-one, using the cytotoxicity, genotoxicity assays with CHO-K1 cells and in vivo acute test in mice. Antimicrobial activity was evaluated by the broth microdilution assays, while the antimicrobial mechanism of action was also assessed using different in vitro bacterial and fungal models. RESULTS: The HPLC analysis of MESf revealed the presence of canthin-6-one, kaempferol and morin. Differential in vitro toxicities were observed between MESf and canthin-6-one. In the cytotoxicity assay, MESf presented toxicity against CHO-K1, while canthin-6-one did not. In the case of in vitro genotoxicity, both showed to be potentially genotoxic. In the in vivo toxicity study, both MESf (up to 1000 mg/kg) and cantin-6-one (up to 100 mg/kg) caused no toxicologically relevant alterations and are thus considered not to be toxic. MESf was shown to be relatively safe with NOAEL (100 mg/kg) when administrate in mice. Both MESf and canthin-6-one also showed differential antimicrobial activities. On one hand, MESf demonstrated good spectrum of antibacterial action against Staphylococcus aureus (MIC 12.5 µg/mL) and Escherichia coli (MIC 25 µg/mL) and moderate activity against Enterococcus faecalis and Shigella flexneri (MIC 200 µg/mL) but no antifungal effect. On the hand, canthin-6-one showed no antibacterial activity, except against Staphylococcus aureus (100 µg/mL), but potent in vitro fungicidal activity against clinically important Aspergillus niger and Candida species at MFC intervals ranging from 3.12 to 25 µg/mL. Both MESf and canthin-6-one were bacteriostatic in action. MESf antimicrobial mechanism of actions are associated with changes in the permeability of bacterial membranes, evidenced by the increased entry of hydrophobic antibiotic in Shigella flexneri, intense K+ efflux (Shigella flexneri, Staphylococcus aureus) and nucleotides leakage (Staphylococcus aureus). In the antifungal mode of action, canthin-6-one inhibited Saccharomyces cerevisiae growth and including alteration in the cell membrane of Neurospora crassa. CONCLUSION: The results of this work demonstrated the differential antimicrobial activities of MESf and its alkaloid isolate, canthin-6-one with antibacterial and antifungal activities, respectively. The present study support the popular use of Simaba ferruginea in combatting afflictions related to bacterial infections, and demonstrate that canthin-6-one as a promising antifungal agent. Both MESf and canthin-6-one are considered non-toxic based on the in vitro toxicological study.

Ocimum gratissimum L. leaf flavonoid-rich fraction suppress LPS-induced inflammatory response in RAW 264.7 macrophages and peritonitis in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Ocimum gratissimum L. is a herbaceous plant that has been reported in several ethnopharmacological surveys as a plant readily accessible to the communities and widely used for the treatment of inflammatory diseases. The main goal of this study was to investigate the in vitro and in vivo anti-inflammatory activity and mechanism of action of the ethylacetate fraction of O. gratissimum leaf (EAFOg) and to chemically characterize this fraction. MATERIALS AND METHODS: EAFOg was obtained from a sequential methanol extract. The safety profile was evaluated on RAW 264.7 cells, using the alamarBlue® assay. Phenolic contents were determined by spectrophotometry, and metabolites quantified by high performance liquid chromatography. The anti-inflammatory activity of EAFOg and its ability to acts on leucocytes infiltration, inflammatory mediators as NO, IL-1ß, TNF-α, and IL-10 in lipopolysaccharide-induced peritonitis in mice and LPS-stimulated RAW 264.7 macrophage were evaluated. In addition, the anti-inflammatory activity of EAFOg was also investigated in arachidonic acid-related enzymes. RESULTS: Total phenolic and flavonoid contents of EAFOg were 139.76±1.07mg GAE/g and 109.95±0.05mg RE/g respectively. HPLC analysis revealed the presence of rutin, ellagic acid, myricetin and morin. The fraction exhibited no cytotoxic effects on the RAW 264.7 cells. The EAFOg (10, 50 and 200mg/kg) significantly reduced (p<0.05) neutrophils (38.8%, 58.9%, and 66.5%) and monocytes (38.9%, 58.0% and 72.8%) in LPS-induced peritonitis. Also, EAFOg (5, 20 and 100µg/mL) produced significant reduction in NO, IL-1ß, and TNF-α in RAW 264.7 cells. However, IL-10 level was not affected by the EAFOg, and it preferentially inhibits COX-2 (IC50 =48.86±0.02µg/mL) than COX-1 and 15-LO (IC50 >100µg/mL). CONCLUSION: The flavonoid-rich fraction of O. gratissimum leaves demonstrated anti-inflammatory activity via mechanisms that involves inhibition of leucocytes influx, NO, IL-1ß, and TNF-α in vivo and in vitro, thus supporting its therapeutic potential in slowing down inflammatory processes in chronic diseases.

Hydroethanolic extract from Echinodorus scaber Rataj leaves inhibits inflammation in ovalbumin-induced allergic asthma.

ETHNOPHARMACOLOGICAL RELEVANCE: Echinodorus scaber, Alismataceae, is popularly known in Brazil as "chapéu-de-couro". The plant leaves are used by the population as decoction, infusion, or maceration in bottled spirits, to treat inflammatory respiratory diseases. AIM OF THE STUDY: To investigate the anti-inflammatory mechanism of the hydroethanolic extract of leaves of Echinodorus scaber (HEEs) in allergic asthma. A phytochemical analysis of the extract was performed as well. MATERIALS AND METHODS: The leaves of Echinodorus scaber were prepared by maceration in 75% ethanol. Preliminary phytochemical analysis was carried out using basic classical methods, and the secondary metabolites detected in HEEs were analyzed and confirmed by high-performance liquid chromatography (HPLC). The in vivo anti-inflammatory activity of HEEs was evaluated in Swiss male albino mice sensitized and challenged by OVA. The HEEs (1, 5 and 30mg/kg, p.o.) was administered to mice twice a day, 1h before the challenge, from days 19 through 24. The mechanism of action of HEEs was studied by evaluating the levels of TH2 cytokines (IL-4, IL-5 and IL-13) in bronchoalveolar lavage fluid (BALF) and IgE production in blood plasma. Histopathological changes triggered by OVA-sensitization/challenge in the lung tissue were also investigated. RESULTS: HEEs reduced total leukocyte, eosinophil, neutrophil, and mononuclear cell counts at all doses tested, with maximum effect at 30mg/kg (73.9%, 75.9%, 75.5%, and 65.2% reduction, p<0.001, respectively). Increases in TH2 cytokine secretion (IL-4, IL-5 and IL-13) and in IgE levels were also attenuated by HEEs. Preliminary phytochemical screening seems to indicated the presence of phenolic compounds, flavonoids and alkaloids. HPLC analyses evidenced the presence of phenolic compounds, such as gallic acid, rutin and vitexin. CONCLUSION: Our findings provided pharmacological preclinical evidence for the popular use of the leaves of Echinodorus scaber in allergic inflammation. Its anti-inflammatory effect was dependent on the decrease in migratory inflammatory cells, and both TH2 cytokines and IgE levels. It is suggested that vitexin, gallic acid and rutin, known anti-inflammatory compounds, may participate in the anti-asthamtic effect of the HEEs, by acting jointly along with other components present in the extract.

Mandevilla longiflora (Desf.) Pichon improves airway inflammation in a murine model of allergic asthma.

ETHNOPHARMACOLOGICAL RELEVANCE: Mandevilla longiflora, popularly known as "velame" in central Brazil, is a subshrub widely distributed in South America. Its xylopodium is used in the form of a decoction or infusion to treat inflammation and other ailments. AIM OF THE STUDY: This study aimed to evaluate the anti-inflammatory potential of M. longiflora in an in vivo model of ovalbumin-induced immediate hypersensitivity, identifying its effects on leukocyte infiltration, IgE and LTB4 levels, and Th2 cytokine production. In addition, HPLC fingerprint of the extract was performed. MATERIAL AND METHODS: The hydroethanolic extract 70% of M. longiflora (HEMI) was obtained by maceration of the plant xylopodium. Swiss mice were sensitized by i.p. injection OVA-aluminium hydroxide on days 1 and 10. Nine days after the last sensitisation animals were challenged for 6 consecutive days with OVA solution for 20min daily in a closed chamber under continuous flow of aerosol. The animals were treated with HEMl (20, 50 and 200mg/kg p.o.), 2 times per day, and euthanized 24h later. Animals treated with vehicle (2% Tween-20) or dexamethasone were used as negative and positive controls, respectively. The recruitment of inflammatory cells into the pulmonary cavity was evaluated by counting cells present in broncho-alveolar lavage fluid (BALF). Lung tissue was also collected for histopathology and infiltration analysis. Quantification of IL-4, IL-5 and IL-13 from the BALF, and IgE, and LTB4 from plasma, were conducted by immunoassay. RESULTS AND CONCLUSIONS: The HEMl attenuated leukocyte migration into the airways, which was evidenced by a decrease in eosinophils, neutrophils and mononuclear cells, both in BALF quantification and by histopathological analysis, as well as decreasing the concentrations of IL-4, IL-5, IL-13, IgE and LTB4. All of these events are typical of air-mucosa inflammatory disease. These findings scientifically evidence for the first time the ethnopharmacological use of M. longiflora to treat chronic inflammatory events, such as asthma, and suggest a potential therapeutic use or complementary therapy for this plant extract.

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.

Physicochemical properties and antioxidant capacity of propolis of stingless bees (Meliponinae) and Apisfrom two regions of Tocantins, Brazil / Propriedades físico-químicas e capacidade antioxidante de própolis de abelhas sem ferrão (Meliponinae) e Apis de duas regiões do Tocantins, Brasil

The composition of propolis depends on time, vegetation and the location of the collection area. The objective of this study was to determine the physicochemical characteristics, the concentration of phenol compounds and the antioxidant capacity of propolis of native stingless bees (Meliponinae) and Apis from the State of Tocantins. Extraction with 80% ethanol (v/v) was performed in order to obtain the extracts. Parameters examined were: propolis mass loss by desiccation at 105 ºC, ashes, wax concentration and pH. Furthermore, the propolis antioxidant activity was measured, as well as the total concentration of phenol compounds. The extracts were also analyzed by high performance liquid chromatography. The total concentration of phenol compounds varied between 121.78 and 631.29 (mg GAE g-1). The antioxidant activity expressed by the value of CE50 varied between 29.81 and 845.38 µg mL-1. High performance liquid chromatography analysis allowed us to infer the existence of phenol compounds. The results indicated that the studied propolis samples constitute good sources of natural antioxidants. The variety of phenol compounds identified in this study, and the diverse biological functions reported in literature for these compounds indicated that this stingless bee propolis (Meliponinae) and Apis has a high pharmacological potential.

A composição da própolis depende do tempo, da vegetação e a localização da área de coleta. Este estudo teve como objetivo determinar as características físicas e químicas, o teor de compostos fenólicos e capacidade antioxidante da própolis de abelhas nativas sem ferrão (Meliponinae) e Apis do Estado do Tocantins. Para a obtenção dos extratos empregou-se extração com etanol 80% (v/v). Os parâmetros analisados foram: perda de peso por dessecação a 105 °C, cinzas, Teor de cera e pH. Além dessas foi mensurada a atividade antioxidante e o teor de compostos fenólicos totais. Adicionalmente os extratos de própolis foram também analisados por cromatografia líquida de alta eficiência. O teor de compostos fenólicos totais variou entre 121,78 e 631,29 (mg GAE g-1). A atividade antioxidante expressa pelo valor de CE50 variou entre 29,81 e 845,38 µg mL-1. As análises por cromatografia líquida de alta eficiência permitiram inferir a existência de compostos fenólicos. Os resultados indicaram que as amostras de própolis estudadas constituem boas fontes de antioxidantes naturais. A variedade de compostos fenólicos identificada neste estudo, e as diversas funções biológicas relatadas na literatura para estes compostos, indicaram que a própolis de abelhas sem ferrão (Meliponinae) e Apis tem um grande potencial farmacológico.

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.

Insecticidal and repellent activity of Siparuna guianensis Aubl. (Negramina) against Aedes aegypti and Culex quinquefasciatus.

This study investigated the toxic effects of essential oils isolated from Siparuna guianensis against Aedes aegypti, Culex quinquefasciatus (eggs, larvae, pupae, and adult) and Aedes albopictus (C6/36) cells. The oviposition-deterring activity, egg viability, and repellence activity in the presence of different essential oils concentrations were determined. The essential oils showed high toxicity to all developmental stages of A. aegypti and C. quinquefasciatus. Furthermore, the oils also showed high repellent activity towards the adult stage of mosquitoes (0.025 to 0.550 µg/cm2 skin conferred 100% repellence up to 120 min) and in contact with cultured insect cells (C6/36) induced death possibly by necrosis. The results presented in this work show the potential of S. guianensis essential oils for the development of an alternative and effective method for the natural control of mosquitoes in homes and urban areas.

Hydroethanolic extract of the inner stem bark of Cedrela odorata has low toxicity and reduces hyperglycemia induced by an overload of sucrose and glucose.

ETHNOPHARMACOLOGICAL RELEVANCE: Cedrela odorata L. (Meliaceae) is a native plant of the Amazon region and its inner stem bark is used in the treatment of diabetes in the form of maceration in Brazilian popular medicine. Until now, there is no scientific study on this activity. The present study was aimed at evaluating the anti-hyperglycemic activity, anti-diabetic, toxicity, antioxidant and potential mechanism of action of hydroethanolic extract of the inner stem bark of Cedrela odorata. MATERIAL AND METHODS: The inner stem bark extract of Cedrela odorata was prepared by maceration in 70% ethanol for 7 days to obtain hydroethanolic extract of Cedrela odorata (HeECo). The preliminary phytochemical analysis was performed according to procedures described in the literature. Selected secondary metabolites detected were quantified by high performance liquid chromatography (HPLC). Acute toxicity of HeECo was investigated in male and female mice with oral administration of graded doses of HeECo from 10 to 5000 mg/kg. Subchronic oral toxicity study was done by oral administration of HeECo (500 mg/kg) and vehicle for 30 days to both sexes of Wistar rats. Clinical observations and toxicological related parameters were determined. Blood was collected for biochemical and hematological analyses, while histological examinations were performed on selected organs. Anti-hiperglycemic and antidiabetic effects were evaluated in streptozotocin-induced diabetic rats. In acute evaluation, the animals received pretreatment with 250 and 500 mg/kg of HeECo, before carbohydrate overload. For subchronic effect, the antidiabetic activity of HeECo was evaluated using the same doses for 21 days. At the end of the treatments, the levels of triacylglycerols, malondialdehyde, total antioxidant status, superoxide dismutase and glutathione peroxidase activities were evaluated in the plasma. RESULTS: The extract showed low acute toxicity. HeECo exhibited inhibitory activity against α-glucosidase and caused a lowering in the peak levels of blood glucose in animals that received glucose overload by 36.7% and 24.1% in the area under the glucose curve (AUC). When the overload was sucrose, HeECo reduced the blood glucose level by 44.4% without affecting AUC. Treatment with HeECo of the blood glucose of the diabetic animals for 21 days did not lead to improvement in weight gain and regularization of the blood glucose level, but reduced the triacylglycerol and malondialdehyde levels by 36.6% and 48.1%, respectively. The activity of the antioxidant enzymes, superoxide dismutase and glutathione peroxidase were significantly increased when compared to diabetic control rats. HPLC analysis showed the presence of polyphenols, such as gallic acid, (-)- gallocatechin and (+)- catechin, the latter is present in higher quantity. CONCLUSIONS: Collectively, these data showed that HeECo could blunt the postprandial glycemic surge in rats; possibly through inhibition of alpha-glucosidase and positive modulation of antioxidant enzymes. Our findings confirmed the anti-hiperglycemic activity of HeECo in STZ- diabetic rats. Cedrela odorata is effective in diminishing glucose levels in vitro and in vivo and in ameliorating oxidative damage that occurs in diabetes and/or due to hyperglycemia in rats. According to our results, the efficacy of Cedrela odorata preparation could be due to the presence of active principles with different mode of actions at the molecular level, including α-glycosidases and glucose transporter inhibitors and antioxidant property.

Toxicological evaluation of hydroethanolic extract of Helicteres sacarolha A. St.- Hil. et al.

ETHNOPHARMACOLOGICAL RELEVANCE: Helicteres sacarolha, popularly known in Brazil as 'rosquinha', 'sacarolhas', 'semente-de-macaco', is widely distributed in different phytogeographic zones in Brazil. Preparations from its roots and leaves are employed in popular Brazilian medicine in the treatments of ailments such as peptic ulcer, hypertension among others. Cytotoxicity, acute oral and subchronic toxicity of the hydroethanolic extract of Helicteres sacrolha was investigated as well as the classes of phytochemical present in the extract. MATERIALS AND METHODS: Hydroethanolic (70%) extract of Helicteres sacarolha (HEHs) was prepared by maceration. Potential cytotoxicity was evaluated in CHO-k1 cells. Acute administration of HEHs was done in mice as a single dose up to 5000mg/kg and subchronic oral toxicity study for 30 days in Wistar rats at daily oral doses of 0, 250 and 750mg/kg b.w. Clinical observations and toxicological related parameters were determined every 6 days. Blood was collected for biochemical and hematological analyses, while histological examinations were performed on selected organs. Selected secondary metabolites detected were quantified by UV-spectrophotometry and high performance liquid chromatography (HPLC). RESULTS: The extract was non-cytotoxic to CHO-k1 cells. In acute oral toxicity, there was no mortality or clinical alterations in the female mice, at all doses, except for the transient diarrhea observed at 5000mg/kg acute. Doses up to 2000mg/kg caused no mortality or treatment-related clinical manifestations in the male mice, but treatment-related alterations were however observed at 4000mg/kg, with mortalities recorded at 5000mg/kg. During the subchronic oral toxicity study, no mortality or treatment-related clinical signs were observed. Differences in relative organ weight, hematological parameters and histopathology observations between the treated and the control groups were considered not to be treatment-related. Spectrophotometric analysis revealed the presence of relatively high content of phenolics and flavonoids in HEHs. HPLC analysis confirmed the presence of the quantified compounds and demonstrated the presence of ellagic acid, morin and naringin. CONCLUSION: Our results confirmed that HEHs have a broad safety margin for therapeutic use.

Evaluation of anti-inflammatory activity of hydroethanolic extract of Dilodendron bipinnatum Radlk.

ETHNOPHARMACOLOGICAL RELEVANCE: Dilodendron bipinnatum Radlk. (Sapindaceae), popularly known as "mulher-pobre", is a native tree of the Pantanal of Mato Grosso, Brazil. The stem bark of Dilodendron bipinnatum is used by the population, in the forms of decoction and maceration in the treatment of inflammatory conditions. There is no information in the literature demonstrating the anti-inflammatory activity of Dilodendron bipinnatum and its respective mechanism of action. This study aimed to evaluate the anti-inflammatory activity and mechanism of action of the hydroethanolic extract of the stem bark of Dilodendron bipinnatum (HEDb) using in vivo and in vitro experimental models. MATERIALS AND METHODS: The stem bark of Dilodendron bipinnatum was macerated in 70% hydroethanolic solution (1:3, w/v) for 7 days, filtered, concentrated on a rotary evaporator and the residual solvent removed in oven at 40°C, thus obtaining HEDb. Cytotoxicity of HEDb in RAW 264.7 was assessed by the Alamar blue assay. in vivo anti-inflammatory activity of HEDb was evaluated with carrageenan and dextran-induced paw edemas and lipopolysaccharide (LPS)-induced peritonitis in mice. Effects of HEDb on the inflammatory cytokines (TNF-α, IL-1ß and IL-10) concentrations in the peritoneal fluid were evaluated using commercial ELISA kits. The in vitro anti-inflammatory activity was evaluated using RAW 264.7 cells stimulated with LPS and/or INF-γ, while a Griess method was employed to determine nitric oxide (NO) concentrations in the peritoneal lavage and in the supernatants of RAW 264.7 cells. Preliminary phytochemical analysis was carried out using classical methods and secondary metabolites detected on HEDb were analyzed and confirmed by high performance liquid chromatography (HPLC). RESULTS: HEDb showed very low cytotoxicity with IC50>200±0.38 µg/mL. HEDb effectively inhibited paw edema by carrageenan in the 2nd hour at 20 mg/kg (36%, p<0.001), and by dextran in the 1st hour at 100 mg/kg (46%, p<0.01), after induction with the phlogistic agents. Furthermore, HEDb reduced total leukocytes and neutrophils migration at all doses tested producing maximum effect at 20 mg/kg (45% and 64%, p<0.001 respectively). HEDb also attenuated increases in the concentrations of the pro-inflammatory cytokines (IL-1ß and TNF-α) and increased the level of the anti-inflammatory cytokine IL-10 in the peritonitis model. However, it had no effect on NO production in activated RAW 264.7 cells. Preliminary phytochemical analysis revealed the presence of phenolic compounds, chalcones, flavones, flavonones, flavonoids, saponins and coumarins. HPLC analyses identified some tannins, with epigallocatechin gallate being the major compound. CONCLUSIONS: Our findings provide evidence for the popular use of the stem bark of Dilodendrum bipinnatum in inflammation. Its anti-inflammatory action was due, at least in part, to the inhibition of cell migration, of the inflammatory mediators and Th1 cytokines and an increase in Th2 cytokines, without affecting NO pathway. It can be suggested that tannins account at least in part for the anti-inflammatory activity of HEDb.

Evaluation of anti-inflammatory and mechanism of action of extract of Macrosiphonia longiflora (Desf.) Müll. Arg.

ETHNOPHARMACOLOGICAL RELEVANCE: Macrosiphonia longiflora (Desf.) Müll. Arg (Apocynaceae), popularly known as 'velame' and 'velame branco', is a native subshrub that grows in the Brazilian Cerrado. This plant is widely used in traditional medicine in the form of decoction and infusion, particularly as anti-inflammatory, depurative, anti-rheumatic, antisyphilitic and antiulcer remedy. There is no available information in the literature that has addressed its pharmacological activity and phytochemical analysis. AIM OF THE STUDY: This study aimed to evaluate the anti-inflammatory pharmacological profile of the hydroethanolic extract of Macrosiphonia longiflora, using in vivo and in vitro acute inflammation experimental models, as well as investigate the roles of cytokines and nitric oxide in its mechanism of action, and including phytochemical analysis constitution of its hydroethanolic extract. MATERIALS AND METHODS: Hydroethanolic (70%) extract of Macrosiphonia longiflora (HEMl) was prepared by maceration. The preliminary phytochemical analysis was performed according to procedures described in the literature. Selected secondary metabolites detected were quantified by spectrophotometry and high performance liquid chromatography (HPLC). Its cytotoxic potential in Chinese hamster ovary (CHO-k1) epithelial cell lines was evaluated using Alamar Blue. in vivo anti-inflammatory activity was evaluated with carrageenan- and dextran-induced paw edemas, carrageenan-induced pleurisy in rats and lipopolysaccharide (LPS)-induced peritonitis in mice. The in vitro anti-inflammatory activity was evaluated using RAW 264.7 cells stimulated with LPS and interferon (INF)-γ. Effects of HEMl on the inflammatory cytokines (IL-1ß, IL-10, IL-17, INF-γ and TNF-α) concentrations in the peritoneal lavage were evaluated using commercial ELISA kits, while the Griess method was employed to determine nitric oxide (NO) concentrations in the peritoneal lavage, as well as in the supernatants of RAW 264.7 cells. RESULTS: Preliminary phytochemical analysis, revealed the presence of phenolics compounds, terpenoids, alkaloids and flavonoids. Spectrophotometric analysis revealed the presence of relatively high content of phenolics and flavonoids in HEMl. HPLC analysis confirmed the presence of the quantified compounds and demonstrated the presence of ellagic acid in the detected matrix of compounds. HEMl appeared to be non-cytotoxic. It effectively inhibited (p<0.05) paw edema induced by carrageenan and dextran. Furthermore, HEMl also significantly reduced exudates volume and leukocyte migration in the carrageenan-induced pleurisy and LPS-induced peritonitis, neutrophils counts in LPS-induced peritonitis. HEMl also acts by effectively inhibiting the following inflammatory cytokines: IL-1ß and IL-10 levels in the peritoneal lavage, but had no effect on IL-17 level in the peritonitis model. In addition, HEMl had no effect on the levels of tumor necrosis factor alpha (TNF-α) present in the peritoneal lavage and cells supernatants. The concentration of NO, as assessed by measurement of nitrite (NO2(-)), showed that pretreatment with HEMl reduced NO significantly in the peritoneal lavage and in RAW 264.7 cells co-stimulated with LPS and INF-γ. CONCLUSION: The results obtained in this study indicate that HEMl possesses very low cytotoxic potential. In addition, it demonstrated a potent anti-inflammatory activity in both the in vivo and in vitro models of acute inflammation. The anti-inflammatory effect is partly related to the inhibition of IL-1ß, IL-10, and nitric oxide releases, but independent of TNF-α and IL-17 modulation. Phytochemical analysis revealed the predominant presence of the flavonoids (naringin, rutin, myricetin, morin, quercetin, (±)-naringenin, and luteolin) and phenols (ellagic acid), which are possibly involved in the anti-inflammatory effect of HEMl. The current study provided supportive evidence for the popular use of HEMl in the treatment of inflammatory conditions, and shed more light on the possible roles of the inflammatory cytokines in its mechanisms of action as anti-inflammatory agent.

Fumigant antifungal activity of Corymbia citriodora and Cymbopogon nardus essential oils and citronellal against three fungal species.

Corymbia citriodora and Cymbopogon nardus essential oils samples were analyzed by GC and GC-MS and their qualitative and quantitative compositions established. The main component of essential oils of C. citriodora and C. nardus was citronellal, at 61.78% and 36.6%, respectively. The essential oils and citronellal were tested for their fumigant antifungal activity against Pyricularia (Magnaporthe) grisea, Aspergillus spp., and Colletotrichum musae. The minimum inhibitory concentration (MIC) ranged from 100 to 200 ppm for the essential oils and 25 to 50 mg · mL(-1) for citronellal. The contact assay using the essential oils and citronellal showed growth inhibition of the three fungal species. However, a concentration of 1.47 mg · mL(-1) only reduced the inhibition of Aspergillus growth to 90% at 14 days of exposure. For the fumigant assay, 0.05, 0.11, and 0.23 mg · mL(-1) of essential oils and citronellal drastically affected growth of P. grisea, Aspergillus spp., and C. musae. Harmful effects on the sporulation and germination of the three fungi were seen, and there was complete inhibition at 0.15 mg · mL(-1) with both oils and citronellal. This showed that the crude component of essential oils of C. citriodora and C. nardus markedly suppressed spore production, germination, and growth inhibition of P. grisea, Aspergillus spp., and Colletotrichum musae.

Chemical Assessment and Antimicrobial and Antioxidant Activities of Endophytic Fungi Extracts Isolated from Costus spiralis (Jacq.) Roscoe (Costaceae).

Costus spiralis (Costaceae) is a species native to the Amazon region and is used in traditional medicine. The endophytic fungi used in this study were obtained from leaves of this plant. 13 strains were selected to obtain hydroethanolic extracts and were submitted to hydroalcoholic extraction and evaluated for antioxidant activity by DPPH (2,2-difenil-1-picrilhidrazil) and FRAP (ferric reducing antioxidant power), and all of the fungi had positive results. The antimicrobial action of crude extracts had a good range of activities. All extracts had inhibitory activities against the yeasts of Candida albicans and C. parapsilosis, with 125 to 500 µg/mL MIC. Eight extracts had antimicrobial activities against Bacillus subtilis (MIC from 62.4 to 125 µg/mL), 5 against Pseudomonas aeruginosa (MIC from 125 to 500 µg/mL), 2 against Salmonella enterica (MIC from 125 to 62.5 µg/mL), and 2 against Enterococcus faecalis (MIC from 500 to 125 µg/mL). The presence of secondary metabolites, including coumarins, was observed during chemical evaluation by thin layer chromatography. Total phenol content was estimated, and a strong positive correlation to antioxidant activity was observed, according to its Pearson coefficient. This is the first report of the bioactive potential of endophytic fungi isolated from the Costaceae family in Brazilian ecosystems.