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1.
Food Chem ; 337: 127771, 2021 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-32777564

RESUMO

Faveleira (Cnidoscolus quercifolius) is an emerging Brazilian plant, with seeds rich in edible oil. This study investigates physicochemical properties, chemical composition, thermal and oxidative stability, in vitro and in vivo toxicity, antioxidant, antinociceptive and anti-inflammatory activities of faveleira seed oil. It was observed that the oil has low acidity, value of peroxide, chlorophyll, carotenoids, ß-carotene and high concentrations of unsaturated fatty acids. In addition to presenting thermal and oxidative stability and high total phenolic content, with vanillin, eugenol and quercetin were predominating. The oil showed no toxicity in vitro and in vivo, and presented antioxidant, anti-inflammatory and antinociceptive activities. These findings provide relevant and appropriate conditions for processing of faveleira seed oil as functional food.

2.
Chem Biodivers ; 2020 Sep 07.
Artigo em Inglês | MEDLINE | ID: mdl-32894822

RESUMO

The Croton argyrophyllus leaf essential oil has anti-inflammatory, antioxidant, cytotoxic among other activities. However, there are chemical composition variations in the literature. This work reports the first study of the intraspecific chemical variation of C. argyrophyllus population from Pernambuco state, Brazil. The essential oils of nine specimens (OCA1 to OCA9) were analyzed by GC/MS and NIR to identify the chemical compositions and to verify the similarities between the analyzed samples. These analyses resulted in the identification of bicyclogermacrene (mean 38.42 %), (Z)-caryophyllene (mean of 14.06 %), epi-longipinanol (mean of 9.78 %) and germacrene B (mean of 9.1 %) as the major constituents, as well as the same chemical markers for all oil samples. However, these are different to those that were previously registered in the literature for C. argyrophyllus essential oil. The data obtained from the analysis by NIR spectroscopy were treated by PCA and HCA and showed similarities in the chemical samples' profile. By statistical analyses three clusters were obtained: OCA1-6, OCA7-8 and OCA9. All these groups were potentially active against Staphylococcus aureus. However, the OCA7-8 group was the most active.

3.
Molecules ; 25(17)2020 Aug 23.
Artigo em Inglês | MEDLINE | ID: mdl-32842529

RESUMO

Caesalpinia ferrea C. Mart., popularly known as "Jucá" or "Pau-ferro", belongs to the Fabaceae family, and is classified as a native and endemic species in Brazil. Numerous studies that portray its ethnobotany, chemical composition, and biological activities exist in the literature. The present study aimed to systematically review publications addressing the botanical aspects, uses in popular medicine, phytochemical composition, and bioactivities of C. ferrea. The searches focused on publications from 2015 to March 2020 using the Scopus, Periódicos Capes, PubMed, Google Scholar, and ScienceDirect databases. The leaves, fruits, seeds, and bark from C. ferrea are used in popular medicine to treat disorders affecting several systems, including the circulatory, immune, cardiovascular, digestive, respiratory, genitourinary, musculoskeletal, and conjunctive systems. The most commonly found chemical classes in phytochemical studies are flavonoids, polyphenols, terpenoids, tannins, saponins, steroids, and other phenolic compounds. The biological properties of the extracts and isolated compounds of C. ferrea most cited in the literature were antibacterial, antifungal, antioxidant, antiproliferative, anti-inflammatory, and healing potential. However, further studies are still needed to clarify a link between its traditional uses, the active compounds, and the reported pharmacological activities, as well as detailed research to determine the toxicological profile of C. ferrea.

4.
J Ethnopharmacol ; 265: 113248, 2020 Aug 14.
Artigo em Inglês | MEDLINE | ID: mdl-32805356

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Verbesina macrophylla (Cass.) S.F.Blake is a medicinal plant from South America, popularly known as "asa de peixe", "asa de peixe branco", "cambará branco" or "cambará guaçu", being used by traditional communities for its healing powers in the form of teas, infusions, liqueurs and extracts, for the treatment of bacterial and fungal infections of the urinary and respiratory tracts, such as kidney problems, bronchitis, inflammation and fever. However, none of the ethnopharmacological properties has been scientifically evaluated. AIM OF THE STUDY: Based on the ethnopharmacological use of the species, this study investigated the chemical composition, and for the first time acute toxicity, hemolytic, antimicrobial, anti-inflammatory and antipyretic activities of the essential oil from leaves of V. macrophylla. MATERIAL AND METHODS: The essential oil was obtained from the leaves by hydrodistillation (HD), being characterized by gas chromatography coupled to mass spectrometry (GC-MS) and gas chromatography coupled to flame ionization detection (GC-FID). The antimicrobial activity was evaluated by the broth microdilution technique in bacteria and fungi that cause infections of the respiratory and urinary tract, and toxicological safety regarding hemolytic activity on human red blood cells (hRBCs), and acute toxicity in mice. The anti-inflammatory activity was evaluated by the model carrageenan-induced peritonitis with quantification of the levels of TNF-α and IL-1ß in the intraperitoneal fluid, and ear edema induced by croton oil. The antipyretic activity evaluated in mice with pyrexia induced by yeast. RESULTS: The extraction of essential oil by hydrodistillation (HD) showed a yield of 0.33 ±â€¯0.04%, with its composition constituted mainly by sesquiterpenes of hydrocarbons (94.00%). The essential oil demonstrated antibacterial and antifungal activity, with a low rate of hemolysis in human red blood cells (hRBCs) and no clinical signs of toxicity were observed in animals after acute treatment, which suggested that the LD50 is greater than 5000 mg/kg; p.o. The essential oil demonstrated anti-inflammatory activity reducing levels of pro-inflammatory cytokines TNF-α (38.83%, 72.42% and 73.52%) and IL-1ß (37.70%, 75.92% and 87.71%), and ear edema by 49.53%, 85.04% and 94.39% at concentrations of 4, 40 and 400 mg/kg, respectively. The antipyretic activity presented by the essential oil is statistically similar to dipyrone. CONCLUSION: The set of results obtained, validates the main activities attributed to the traditional use of Verbesina macrophylla (Cass.) S.F.Blake. These data add industrial value to the species, considering that the antimicrobial, anti-inflammatory and antipyretic activities present results similar to the drugs already used also presenting safety. The results suggest that essential oil from V. macrophylla may be used by industry for the development of drugs with natural antimicrobial, anti-inflammatory and antipyretic effect.

5.
Chem Biol Interact ; 320: 109028, 2020 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-32119865

RESUMO

Reactive oxygen species (ROS) cause cell damage and death. To reverse these effects, cells produce substances such as reduced glutathione (GSH) that serve as substrates for antioxidant enzymes. One way to combat microbial resistance includes nullifying the effect of glutathione in microbial cells, causing them to die from oxidative stress. The compound 2-((5-nitrothiophen-2-yl)methylene)-N-(pyridin-3-yl) hydrazine carbothioamide (L10) is a new thiophene-thiosemicarbazone derivative with promising antifungal activity. The aim of this study was to evaluate its mechanism of action against Candida albicans using assays that evaluate its effects on redox balance. Treatment with L10 promoted significant changes in the minimum inhibitory concentration (MIC) values in ascorbic acid and GSH protection tests, the latter increasing up to 64-fold of the MIC. Using nuclear magnetic resonance, we demonstrated interaction of L10 and GSH. At concentrations of 4.0 and 8.0 µg/mL, significant changes were observed in ROS production and mitochondrial membrane potential. The cell death profile showed characteristics of initial apoptosis at inhibitory concentrations (4.0 µg/mL). Transmission electron microscopy data corroborated these results and indicated signs of apoptosis, damage to plasma and nuclear membranes, and to mitochondria. Taken together, these results suggest a possible mechanism of action for L10 antifungal activity, involving changes in cellular redox balance, ROS production, and apoptosis-compatible cellular changes.


Assuntos
Antifúngicos/farmacologia , Apoptose/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Tiofenos/farmacologia , Tiossemicarbazonas/farmacologia , Antifúngicos/química , Humanos , Estrutura Molecular , Tiofenos/química , Tiossemicarbazonas/química
6.
Nat Prod Res ; : 1-5, 2020 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-32081039

RESUMO

This work aimed to investigate the chemical composition, antimicrobial activity, synergistic effect, and structure changes of the essential oil of Hymenaea rubriflora (EOHr). Forty-five constituents were identified in the essential oil, corresponding to 94.43% of the compounds present, being the main components E-Caryophyllene (36.72 ± 1.05%), Germacrene D (16.13 ± 0.31%), α-Humulene (6.06 ± 0.16%), ß-elemene (5.61 ± 0.14%) and δ-Cadinene (3.76 ± 0.07%). Antimicrobial activity was evaluated, presenting antibacterial and antifungal activity with MIC ranging from 0.62 to 40 µL/mL. The essential oil had a synergistic effect when combined with gentamicin and fluconazole. Structural changes were also evaluated and it was possible to observe that EOHr action was related to changes in membrane permeability. The findings obtained here suggest that the use of the essential oil of H. rubriflora in the treatment of infectious diseases presents a potential for the future development of pharmaceutical products.

7.
J Ethnopharmacol ; 253: 112567, 2020 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-32027999

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Himatanthus drasticus is a tree popularly known as janaguba. Endemic to Brazil, it is found in the Cerrado and Caatinga biomes, rock fields, and rainforests. Janaguba latex has been used in folk medicine for its antineoplastic, anti-inflammatory, analgesic, and antiallergic activities. However, studies investigating the safety of its use for medicinal purposes are limited. AIM OF THE STUDY: This study aimed to evaluate the toxicity of the latex extracted from H. drasticus. MATERIALS AND METHODS: The latex was extracted from H. drasticus specimens by removing a small area of bark (5 × 30 cm) and then dissolving the exudate in water and lyophilizing it. Phytochemical screening was performed by TLC and GC-MS, protein, and carbohydrate levels. Cell viability was performed by the MTT method. Acute oral toxicity, genotoxicity, and mutagenicity assays were performed in mice. RESULTS: TLC showed the presence of saponins and reducing sugars, as well as steroids and terpenes. The GC-MS analysis of the nonpolar fraction identified lupeol acetate, betulin, and α/ß-amyrin derivatives as the major compounds. The latex was toxic to S-180 cells at 50 and 100 µg/mL. No signals of toxicity or mutagenicity was found in mice treated with 2000 mg/kg of the latex, but genotoxicity was observed in the Comet assay. CONCLUSIONS: H. drasticus latex showed toxicity signals at high doses (2000 mg/kg). Although the latex was not mutagenic to mice, it was genotoxic in the Comet assay in our experimental conditions. Even testing a limit dose of 2000 mg/kg, which is between 10 to 35-fold the amount used in folk medicine, caution must be taken since there is no safe level for genotoxic compounds exposure. Further studies on the toxicological aspects of H. drasticus latex are necessary to elucidate its possible mechanisms of genotoxicity.

8.
Microb Drug Resist ; 26(7): 802-814, 2020 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31916896

RESUMO

Acinetobacter baumannii and Pseudomonas aeruginosa are the most relevant Gram-negative bacteria associated with hospital and opportunistic infections. This study aimed to evaluate the dynamics of drug-resistant A. baumannii and P. aeruginosa and biofilm formers from two public hospitals in northeastern Brazil. One hundred isolates (35 from A. baumannii and 65 from P. aeruginosa) were identified using the automated Vitek®2 Compact method (bioMérieux) and confirmed using the MALDI-TOF (MS) mass spectrometry technique. Molecular experiments were performed by polymerase chain reaction (PCR) to detect the frequency of blaKPC, blaIMP, blaVIM, and blaSHV genes. The biofilm formation potential was evaluated using crystal violet in Luria Bertani Miller and trypticase soy broth culture media under the following conditions: at standard concentration, one quarter (25%) of the standard concentration and supplemented with 1% glucose. In addition, the genetic diversity of the isolates was verified by the ERIC-PCR technique. Isolates presented distinct resistance profiles with a high level of beta-lactam resistance. The highest index of genes detected was blaKPC (60%), followed by blaSHV (39%), blaVIM (8%), and blaIMP (1%). All the isolates were sensitive to the polymyxins tested and formed biofilms at different intensities. Twelve clones of A. baumannii and eight of P. aeruginosa were identified, of which few were indicative of intra- and interhospital dissemination. This study reveals the dispersion dynamics of these isolates in the hospital environment. The results demonstrate the importance of monitoring programs to combat the spread of these pathogens.

9.
Comp Immunol Microbiol Infect Dis ; 65: 226-233, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31300118

RESUMO

The aim of this study is to verify the action of the aqueous leaf extract Ziziphus joazeiro in the eradication of bacterial and fungal biofilms, and to compare these effects with the stem bark extracts, as well as with conventional standard drugs. The presence of secondary metabolites was observed through phytochemical prospection assays. The effect of the aqueous extract on microbial biofilm formation was observed by OD600 nm absorbance and the crystal violet assay. For bacterial and fungal biofilms, chlorhexidine gluconate and fluconazole, respectively, were used as positive controls. Phytochemical characterization showed the presence of secondary metabolite classes common to both extracts such as flavonoids, steroids and saponins. In particular, in the aqueous leaf extract phenols, condensed tannins and alkaloids were observed. Eradication results using the aqueous leaf extract showed an inhibition of the microbial biofilm mass, moreover the biofilms were more sensitive to the bark extract, which presented a greater inhibition number and an action similar to standard drugs. It is important to highlight the leaf extract showed significant eradication at the lowest concentrations for mature yeast biofilms, thus demonstrating its potential to modify microbial resistance susceptibility. Bacterial and fungal biofilm eradication results using the Ziziphus joazeiro aqueous extracts presented a biofilm inhibition effect for both, moreover the results support the ethnopharmacological knowledge surrounding the use of Ziziphus joazeiro stems in the community. In comparison, the bark extract presented a more effective treatment than the leaf extract against biofilms, presenting inhibition levels similar to the used standard drugs.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Bactérias/efeitos dos fármacos , Biofilmes/efeitos dos fármacos , Fungos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Ziziphus/química , Antibacterianos/química , Antifúngicos/química , Clorexidina/análogos & derivados , Clorexidina/farmacologia , Fluconazol/farmacologia , Testes de Sensibilidade Microbiana , Casca de Planta/química , Extratos Vegetais/química , Folhas de Planta/química
10.
Nat Prod Res ; : 1-5, 2019 Jul 22.
Artigo em Inglês | MEDLINE | ID: mdl-31328548

RESUMO

This work evaluated the volatile composition, antioxidant and antiprotozoal activities of the essential oil obtained from leaves of Eugenia gracillima Kiaersk. (EGEO) grown in Brazilian Northeast area (Araripe, Brazil). The volatile compounds of EGEO were analyzed by GC and GC-MS and its chemical composition is mainly composed of sesquiterpene hydrocarbons (91.22%), oxygenated sesquiterpenes (7.45%) and monoterpene (1.01%). The most abundant volatile constituents of the EGEO were germacrene D (16.10%), γ-muurolene (15.60%), bicyclogermacrene (8.53%), germacrene B (7.43%), and Δ-elemene (6.06%). The oil showed weak to moderate antioxidant activity. EGEO was highly selective to Leishmania braziliensis and Leishmania infantum promastigotes with selective indexes of 73.66 and 71.41, respectively. EGEO did not inhibit Trypanosoma cruzi. These data suggest that the E. gracillima essential oil is a relevant source of lead compounds for development of anti-Leishmania drugs.

11.
Environ Sci Pollut Res Int ; 26(26): 27112-27127, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31317435

RESUMO

In this study, we screened for the antifouling activity of 15 species plant extracts from Brazilian the Brazilian Caatinga Fabaceae against the initial colonization of natural marine bacterial biofilm. We also investigated the potential toxicity of extracts against planktonic and benthic non-target organisms. Aqueous extracts of plants collected in the Caatinga biome (PE, Brazil) were prepared and tested at different concentration levels (0, 0.5, 1, 2, 4, and 8 mg mL-1). Natural marine bacterial consortium was inoculated in multi-well plates and incubated with the different treatments for 48 h. The biofilm and planktonic bacterial density and biomass inhibition were evaluated along with biofilm biomass eradication. The extracts that showed the highest bacterial biofilm inhibition were evaluated for toxicity against microalgae and crustaceans. The biofilm and planktonic bacterial inhibition potential were evaluated through flow cytometry and spectrophotometry. The selected treatments were evaluated for their toxicity using the microalgae Chaetoceros calcitrans, the copepod Nitokra sp., and the brine shrimp Artemia salina as bioindicators. Our work demonstrates the biotechnological potential of Fabaceae plant compounds as a safe antifouling alternative. Anadenanthera colubrina var. cebil fruits and Apuleia leiocarpa leaf extracts showed antibiofilm activity (≥ 80%), while Myroxylon peruiferum and Dioclea grandiflora leaf extracts showed antibiotic activity. These extracts were safe to planktonic and benthic non-target organisms. The results of this study point to potential substitutes to highly toxic antifouling paints and shed light on the prospect of a yet to be explored biome for more sustainable alternatives in biofouling research.


Assuntos
Incrustação Biológica/prevenção & controle , Desinfetantes/farmacologia , Fabaceae/química , Extratos Vegetais/farmacologia , Animais , Antibacterianos/farmacologia , Antibacterianos/toxicidade , Artemia/efeitos dos fármacos , Biofilmes/efeitos dos fármacos , Brasil , Copépodes/efeitos dos fármacos , Diatomáceas/efeitos dos fármacos , Desinfetantes/toxicidade , Ecotoxicologia/métodos , Microalgas/efeitos dos fármacos , Pintura , Plâncton/efeitos dos fármacos , Plâncton/microbiologia , Extratos Vegetais/toxicidade
12.
Nat Prod Res ; : 1-5, 2019 Apr 23.
Artigo em Inglês | MEDLINE | ID: mdl-31014086

RESUMO

This work aimed to investigate the chemical composition, antimicrobial, antinociceptive, acute toxicity and antioxidant activity of the essential oil of Algrizea minor (EOAm). The essential oil presented as the major constituents ß-Pinene (56.99%), α-Pinene (16.57%), Germacrene D (4.67%), Bicyclogermacrene (4.66%), (E)-Caryophyllene (3.76%) and Limonene (1.71%). It was verified that the essential oil did not show acute toxicity in the maximum dose of 5,000 mg/kg. In the evaluation of the antinociceptive activity it was verified that the essential oil reduced in 65.84% the number of writhing in the mice, reducing the pain in 59.17%, and the mechanism of action in pain reduction was opioid, similar to morphine. The essential oil also presented significant antimicrobial against Gram positive and Gram-negative bacteria and fungi, and the antioxidant activity was relevant. Therefore, these results demonstrate the great potential for the future development of pharmaceutical products with the essential oil of Algrizea minor (EOAm).

13.
Ecotoxicol Environ Saf ; 169: 669-677, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30500736

RESUMO

The increase in urbanization and industrialization has contributed to the contamination of different environments by means of xenobiotic compounds, such as heavy metals, causing changes in microbial communities. Among these metals, the Mercury (Hg2+) is one the most prevalent toxic metals for the environment The present study aimed to evaluate the effect of mercury on the formation of biofilm by environmental (collected from urban stream water) and clinical isolates of Klebsiella pneumoniae. In addition, antibiotic resistance, virulence factors, and genetic diversity were investigated. Taxonomic identity of eight isolates (one reference, two clinical, and five environmental isolates) was performed by MALDI-TOF-MS, while the antibiotic susceptibility profile was assessed by the disc diffusion method. The ability to form biofilms was evaluated by culture on Congo red agar and by crystal violet staining. Biofilm structure was analyzed by scanning electron microscopy. The hydrophobicity profile and the presence of the virulence genes cps, fimH, and mrkD was investigated. The presence of merA and its relationship with antimicrobial resistance were also assessed. The identity of all isolates was confirmed by MALDI-TOF-MS, and different profiles of resistance to mercury and antibiotics as well as of biofilm formation were identified for the clinical and environmental isolates. All isolates were hydrophilic and positive for the virulence genes cps, fimH, and mrkD; only the clinical isolate K36-A2 was positive for merA. The diversity of the isolates was confirmed by ERIC-PCR, which revealed high heterogeneity among the isolates. In conclusion, the data demonstrate that the investigated isolates present different responses to exposure to Hg2+ and correspond to distinct populations of K. pneumoniae disseminated in the investigated environment. The data obtained in this work will aid in understanding the mechanisms of survival of this pathogen under adverse conditions.


Assuntos
Biofilmes/efeitos dos fármacos , Poluentes Ambientais/toxicidade , Klebsiella pneumoniae/efeitos dos fármacos , Mercúrio/toxicidade , Antibacterianos/farmacologia , Biofilmes/crescimento & desenvolvimento , Farmacorresistência Bacteriana/efeitos dos fármacos , Farmacorresistência Bacteriana/genética , Hospitais , Humanos , Klebsiella pneumoniae/genética , Klebsiella pneumoniae/patogenicidade , Testes de Sensibilidade Microbiana , Fatores de Virulência/genética
14.
BMC Complement Altern Med ; 18(1): 284, 2018 Oct 19.
Artigo em Inglês | MEDLINE | ID: mdl-30340567

RESUMO

BACKGROUND: Spondias tuberosa is a plant that produces a fruit crop with high economic relevance at Brazilian Caatinga. Its roots and leaves are used in folk medicine. METHODS: Chemical composition of a hexane extract from S. tuberosa leaves was evaluated by thin-layer chromatography (TLC), high-performance liquid chromatography (HPLC) and 1H nuclear magnetic resonance (NMR). Antioxidant potential was investigated by DPPH and ABTS assays. Antifungal action on Candida species was evaluated determining the minimal inhibitory concentration (MIC50) and putative mechanisms were determined by flow cytometry analysis. In addition, hemolytic activity on human erythrocytes was assessed and the concentration required to promote 50% hemolysis (EC50) was determined. RESULTS: Phytochemical analysis by TLC showed the presence of flavonoids, hydrolysable tannins, saponins and terpenes. The HPLC profile of the extract suggested the presence of gallic acid (0.28 ± 0.01 g%) and hyperoside (1.27 ± 0.01 g%). The representative 1H NMR spectrum showed saturated and unsaturated fatty acids among the main components. The extract showed weak and moderate antioxidant activity in DPPH (IC50: 234.00 µg/mL) and ABTS (IC50: 123.33 µg/mL) assays, respectively. It was able to inhibit the growth of C. albicans and C. glabrata with MIC50 of 2.0 and 0.078 mg/mL, respectively. The treatment of C. glabrata cells with the extract increased levels of mitochondrial superoxide anion, caused hyperpolarization of mitochondrial membrane, and compromised the lysosomal membrane. Weak hemolytic activity (EC50: 740.8 µg/mL) was detected. CONCLUSION: The results demonstrate the pharmacological potential of the extract as antioxidant and antifungal agent, aggregating biotechnological value to this plant and stimulating its conservation.


Assuntos
Anacardiaceae/química , Antifúngicos/farmacologia , Antioxidantes/farmacologia , Membranas Mitocondriais/efeitos dos fármacos , Extratos Vegetais/farmacologia , Candida/citologia , Candida/efeitos dos fármacos , Hexanos , Lisossomos/efeitos dos fármacos
15.
Oxid Med Cell Longev ; 2018: 1731459, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29854075

RESUMO

Spondias mombin L. is used in folk medicine for the treatment of inflammation and gastrointestinal diseases. Our study investigated the antiulcer activity of S. mombin ethanolic extract (SmEE) and its majority compounds gallic acid (GA) and ellagic acid (EA). Phytochemical characterization was performed by HPLC. The SmEE was screened for in vitro antioxidant activities using phosphomolybdenum, ABTS, DPPH, and FRAP assays. The antiulcer activity of SmEE, GA, EA, or GA + EA was evaluated by gastric lesion models induced by absolute ethanol and indomethacin. Following this, it is capable of stimulating mucus production, antisecretory capacity, and the influence of -SH groups and NO in the effect of SmEE. Its healing activity was demonstrated by acetic acid-induced chronic ulcer model. Anti-Helicobacter pylori activity was assessed by determining the MIC of the SmEE (64-1024 µg/mL). The HPLC results identified the presence of gallic acid and ellagic acid in SmEE. The extract showed antioxidant activity in vitro. SmEE (50, 100, and 200 mg/kg) reduced the area of ulcerative lesions induced by ethanol in 23.8, 90.3, and 90.2%, respectively. In NSAID model, the SmEE induced protection of 36.8, 49.4, and 49.9%, respectively. GA (10 mg/kg) or EA (7 mg/kg) or the association of GA + EA (10 + 7 mg/kg) inhibited the ethanol-induced lesions in 71.8, 70.9, and 94.9%, respectively, indicating synergistic action. SmEE (100 mg/kg) decreased acid secretion and H+ concentration in the gastric contents, increased levels of mucus, and showed to be dependent of -SH groups and NO on the protection of the gastric mucosa. In chronic ulcer model, SmEE reduced the gastric area lesion. SmEE showed anti-H. pylori activity. In conclusion, our study showed that SmEE has antiulcerogenic activity. GA and EA are isolated gastric protectors and, when associated, acted synergistically to protect the gastric mucosa.


Assuntos
Anacardiaceae/química , Medicina Herbária/métodos , Fitoterapia/métodos , Folhas de Planta/química , Úlcera Gástrica/tratamento farmacológico , Animais , Camundongos , Ratos , Ratos Wistar
16.
Oxid Med Cell Longev ; 2017: 6593073, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29213351

RESUMO

Spondias purpurea is used in folk medicine to treat diarrhea and diuresis. The objective of this study was to evaluate the phytochemical profile and antioxidant and antiulcer activities of the hexane extract of the leaves of S. purpurea (SpHE). Phytochemical profile was evaluated via thin layer chromatography (TLC) and HPLC. SpHE was screened for antioxidant activities using DPPH, ABTS, FRAP, and phosphomolybdenum assays. To determine its antiulcer properties, animals were pretreated with injured control, lansoprazole, ranitidine, carbenoxolone, or SpHE (12.5, 25, and 50 mg/kg) and were screened; acute ulcers were induced by HCl/ethanol, absolute ethanol, and nonsteroidal anti-inflammatory drug (NSAID). TLC revealed the presence of flavonoids, whereas HPLC analysis showed the presence of caffeic acid and epigallocatechin. The phenolic compounds and in vitro assays showed antioxidant activity. After gastric ulcer induction by using HCl/ethanol, SpHE reduced the area of ulcerative lesions by 82, 91, and 88%, respectively. In ethanol, SpHE reduced the area of ulcerative lesions by 77, 93, and 92%, respectively. In the NSAID, the percentages of protection were 70, 76, and 78%, respectively. SpHE promoted the minimization of ulcers, increased the levels of reduced glutathione, and decreased tumor necrosis factor. S. purpurea has antioxidant and antiulcer properties.


Assuntos
Anacardiaceae/química , Antiulcerosos/química , Antioxidantes/química , Extratos Vegetais/química , Anacardiaceae/metabolismo , Animais , Antiulcerosos/isolamento & purificação , Antiulcerosos/uso terapêutico , Antioxidantes/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Cromatografia em Camada Delgada , Etanol/toxicidade , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/metabolismo , Mucosa Gástrica/patologia , Glutationa/metabolismo , Hexanos/química , Camundongos , Óxido Nítrico/metabolismo , Folhas de Planta/química , Folhas de Planta/metabolismo , Ratos , Ratos Wistar , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/tratamento farmacológico , Fator de Necrose Tumoral alfa/metabolismo
17.
PLoS One ; 12(11): e0188531, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-29190689

RESUMO

The infection caused by Trichomonas vaginalis is the most common but overlooked non-viral sexually transmitted disease worldwide. Treatment relies on one class of drugs, the 5-nitroimidazoles, but resistance is widespread. New drugs are urgently needed. We reported the effect of crude and purified saponin fractions of Manilkara rufula against Trichomonas vaginalis. The compound responsible for antitrichomonal activity was isolated and identified as an uncommon bidesmosic saponin, Mi-saponin C. This saponin eliminated parasite viability without toxicity against the human vaginal epithelial line (HMVII). In addition, the isolated saponin fraction improved the metronidazole effect against a metronidazole-resistant isolate and dramatically reduced the cytoadherence of T. vaginalis to human cells. Investigation of the mechanism of death showed that the saponin fraction induced the parasite death due to profound membrane damage, inducing a disturbance of intracellular content without nuclear damage. To the best of our knowledge, this is the first report of antitrichomonal activity in the bidesmosic saponins of Manilkara rufula.


Assuntos
Manilkara/química , Saponinas/farmacologia , Trichomonas vaginalis/efeitos dos fármacos , Linhagem Celular , Membrana Celular/efeitos dos fármacos , Cromatografia Líquida , Feminino , Humanos , Espectrometria de Massas/métodos , Microscopia Eletrônica/métodos , Saponinas/isolamento & purificação , Trichomonas vaginalis/ultraestrutura , Vagina/parasitologia
18.
Biomed Pharmacother ; 96: 1055-1064, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29217159

RESUMO

Essential/volatile oils (EOs) from plants used in the traditional medicine are known as a rich source of chemically diverse compounds with relevant biological activities. In this work we analysed the chemical composition and the in vitro effects of EOs from leaves of Eugenia brejoensis (EBEO), Hyptis pectinata (HPEO), Hypenia salzmannii (HSEO), Lippia macrophylla (LMEO) and seeds of Syagrus coronata (SCEO) on Trypanosoma cruzi, the etiological agent of Chagas disease. The EOs were extracted through hydrodistillation and its chemical composition analysed by GC/MS. The trypanocidal activity against epi- and trypomastigotes was evaluated by optical microscopy and the cytotoxicity to mammalian cells by MTT. The effects of EOs on parasite infection in macrophages were estimated by determining the survival index and the percentage of infection inhibition. The cytotoxicity against mammalian cells was compared to those of parasite by determining the Selectivity Index (SI). Overall, 114 compounds were identified: The main constituents of EOS were: δ-cadinene (15.88%), trans-caryophyllene (9.77%) e α-Muurolol (9.42%) for EBEO; trans-caryophyllene (15.24%), bicyclogermacrene (7.33%) e cis-calamenene (7.15%) for HFEO; trans-caryophyllene (30.91%), caryophyllene oxide (13.19%) and spathulenol (5.68%) for HPEO; Xanthoxylin (17.20%) trans-caryophyllene (14.34%) and methyl-eugenol (5.60%) for HSEO; Thymol (49.81%), carvacrol (31.6%) and σ-cimene (10.27%) for LMEO and octanoic acid (38.83%) dodecanoic acid (38.45%) and decanoic acid (20.51%) for SCEO. All the tested oils showed an inhibitory effect on the growth and survival of all forms of T. cruzi and moderate cytotoxicity towards the mammalian cells (100 < CC50 < 500 µg/mL). The EO of E. brejoensis was the most effective against the parasite presenting higher Selectivity Index for trypo- (SI = 14.45) and amastigote forms (SI = 20.11). Except for SCEO, which was the most cytotoxic for both parasite and mammalian cells, all the oils demonstrated to be more selective for the parasite than the reference drug benznidazole. Taken together our results point the essential oils from Caatinga plants, especially Eugenia brejoensis, as promissory agents for the development of new drugs against Chagas disease.


Assuntos
Óleos Voláteis/química , Óleos Voláteis/farmacologia , Plantas Medicinais , Tripanossomicidas/química , Tripanossomicidas/farmacologia , Trypanosoma cruzi/efeitos dos fármacos , Animais , Brasil , Células Cultivadas , Eugenia , Lippia , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Óleos Voláteis/isolamento & purificação , Folhas de Planta , Óleos Vegetais/química , Óleos Vegetais/isolamento & purificação , Óleos Vegetais/farmacologia , Sementes , Tripanossomicidas/isolamento & purificação , Trypanosoma cruzi/fisiologia
19.
Exp Parasitol ; 173: 18-28, 2017 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-27956086

RESUMO

Tritrichomonas foetus infects the bovine urogenital tract, causing bovine trichomoniasis. Significant economic losses may occur due to infertility and abortion among cattle. Trichomonas vaginalis is the causative agent of trichomoniasis; the most common but overlooked non-viral sexually transmitted disease worldwide. Human and bovine trichomoniasis present treatment restrictions and efforts to identify new alternatives are essential. The present study evaluated the anti-trichomonads activities of seven fractions from northwest endemic plant Manilkara rufula. Flavonoids and condensed tannins were identified from these fractions by LC-DAD-MS/MS and MALDI-MS/MS. Altogether, the results demonstrated for the first time the structural description of tannins from leaves of M. rufula and the relation of these compounds with anti-T. vaginalis and anti-T. foetus activities. Overall, this report reveals the potential of M. rufula fractions against both parasites and shows new alternatives to treat the infection caused by trichomonads.


Assuntos
Antitricômonas/farmacologia , Flavonoides/farmacologia , Manilkara/química , Extratos Vegetais/farmacologia , Taninos/farmacologia , Trichomonas vaginalis/efeitos dos fármacos , Tritrichomonas foetus/efeitos dos fármacos , Antitricômonas/química , Antitricômonas/isolamento & purificação , Brasil , Linhagem Celular , Sobrevivência Celular , Cromatografia Líquida , Células Epiteliais/efeitos dos fármacos , Flavonoides/química , Flavonoides/isolamento & purificação , Células HeLa , Humanos , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Espectrometria de Massas por Ionização e Dessorção a Laser Assistida por Matriz , Taninos/química , Taninos/isolamento & purificação , Trichomonas vaginalis/fisiologia , Tritrichomonas foetus/fisiologia
20.
Bioorg Med Chem Lett ; 26(9): 2229-36, 2016 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-27020521

RESUMO

Trichomonas vaginalis causes trichomoniasis; the most common but overlooked non-viral sexually transmitted disease worldwide. The treatment is based at 5'-nitroimidazoles, however, failure are related to resistance of T. vaginalis to chemotherapy. Caatinga is a uniquely Brazilian region representing a biome with type desert vegetation and plants present diverse biological activity, however, with few studies. The aim of this study was to investigate the activity against T. vaginalis of different plants from Caatinga and identify the compounds responsible by the activity. A bioguided fractionation of Manilkara rufula was performed and four major compounds were identified: caproate of α-amyrin (1b), acetate of ß-amyrin (2a), caproate of ß-amyrin (2b), and acetate of lupeol (3a). In addition, six derivatives of α-amyrin (1), ß-amyrin (2) and lupeol (3) were synthesized and tested against the parasite. Ursolic acid (5) reduced about 98% of parasite viability after 2h of incubation and drastic ultrastructural alterations were observed by scanning electron microscopy. Moreover, 5 presented high cytotoxicity to HMVII and HeLa cell line and low cytotoxicity against Vero line at 50 µM (MIC against the parasite). Metronidazole effect against T. vaginalis resistant isolate was improved when in association with 5.


Assuntos
Extratos Vegetais/farmacologia , Plantas Medicinais/química , Trichomonas vaginalis/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Plantas Medicinais/classificação
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