RESUMO
Thirteen fucosterol derivatives were prepared by structural modification at the hydroxyl group in C-3 and catalytic hydrogenation at the carbon-carbon double bond in C-5(6) and C-24(28). The structures of all compounds were established based on their spectral data (IR, MS, and NMR). Fucosterol (1) and its derivatives (2-12, and a mixture of 13a and 13b) were evaluated for their in vitro antibacterial activity against Klebsiella pneumoniae (ATCC 10031), Escherichia coli (ATCC 10536), Pseudomonas aeruginosa (ATCC 15442), Streptococcus mutans (ATCC 0046) and Staphylococcus aureus using the microdilution method. Among them, 1, 8, 9, 10, and a mixture of 13a and 13b exhibited the best antibacterial activity. The derivative 7 was inactive against all bacterial strains evaluated (MIC ≥ 2.327 mM). In addition, the investigation of binding interactions of more active compounds (1, 8, 9, 10, and mixture of 13a and 13b) to appropriate proteins was performed using molecular docking. This paper registers for the first time the in silico studies on the antibacterial activity of compounds 1, 8, 9, 10, and mixture of 13a/13b, and the spectral data of compounds 4, 6, and 7.
Assuntos
Antibacterianos , Bactérias , Simulação de Acoplamento Molecular , Testes de Sensibilidade Microbiana , Antibacterianos/químicaRESUMO
The increase in antibiotic resistance and the emergence of new bacterial infections have intensified the research for natural products from plants with associated therapy. This study aimed to verify the antibacterial and antioxidant activity of crude extracts of the genus Plectranthus species, being the first report on the modulation of aminoglycosides antibiotic activity by Plectranthus amboinicus extracts. The chemical composition was obtained by chemical prospecting and High-Performance Liquid Chromatography with diode arrangement detector (HPLC/DAD). The antibacterial activities of the extracts alone or in association with aminoglycosides were analyzed using the microdilution test. The antioxidant activity was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging. The phytochemical prospection allowed the flavonoids, saponins, tannins and triterpenoids to be identified. Quercetin, rutin, gallic acid, chlorogenic acid, caffeic acid, catechin, kaempferol, glycosylated kaempferol, quercitrin, and isoquercitrin were identified and quantified. The principal component analysis (PCA) observed the influence of flavonoids and phenolic acids from Plectranthus species on studied activities. Phytochemical tests with the extracts indicated, especially, the presence of flavonoids, confirmed by quantitative analysis by HPLC. The results revealed antibacterial activities, and synergistic effects combined with aminoglycosides, as well as antioxidant potential, especially for P. ornatus species, with IC50 of 32.21 µg/mL. Multivariate analyzes show that the inclusion of data from the antioxidant and antibacterial activity suggests that the antioxidant effect of these species presents a significant contribution to the synergistic effect of phytoconstituents, especially based on the flavonoid contents. The results of this study suggest the antibacterial activity of Plectranthus extracts, as well as their potential in modifying the resistance of the analyzed aminoglycosides.
Assuntos
Antibacterianos/química , Antioxidantes/química , Quimiometria , Extratos Vegetais/química , Plectranthus/químicaRESUMO
Resistance to antibiotics has made diseases that previously healed easily become more difficult to treat. Staphylococcus aureus is an important cause of hospital-acquired infections and multi-drug resistant. NorA efflux pump, present in bacteria S. aureus, is synthesized by the expression of the norA gene. Menadione, also known as vitamin K3, is one of the synthetic forms of vitamin K. Therefore, the aim of this study is to verify the menadione effect on efflux inhibition through NorA pump gene expression inhibition and assess the effects of menadione in bacterial membrane. The effect of menadione as an efflux pump inhibitor (EPI) was evaluated by the microdilution method, fluorimetry, electron microscopy, and by RT-qPCR to evaluate gene expression. In the molecular docking, association with menadione induces increased fluorescence intensity. Menadione was observed (100% of the clusters) interacting with residues ILE12, ILE15, PHE16, ILE19, PHE47, GLN51, ALA105, and MET109 from NorA. The results showed the norA gene had its expression significantly diminished in the presence of menadione. The simulation showed that several menadione molecules were able to go through the bilayer and allow the entry of water molecules into the hydrophobic regions of the bilayer. When present within membranes, menadione may have caused membrane structural changes resulting in a decline of the signaling pathways involved in norA expression. Menadione demonstrated to be an efflux pump inhibitor with dual mechanism: affecting the efflux pump by direct interaction with protein NorA and indirectly inhibiting the norA gene expression, possibly by affecting regulators present in the membrane altered by menadione.
RESUMO
Species from the Annona (Anonaceae) genus are used in traditional medicine for the treatment of various diseases. Ethnobotanical studies provide information regarding the plant part and the preparation method being used, while scientific studies such as in vitro, in vivo, and clinical tests can provide evidence supporting ethnopharmacological reports, directing studies towards the isolation of compounds which may be active for specific pathologies. Annona muricata and Annona squamosa were the most commonly reported species from those studied, with Annona cherimola and Annona classiflora also standing out. Acetogenins were the most commonly isolated metabolite class due to their cytotoxic properties, with flavonoids, alkaloids, steroids, and peptides also being reported. Many species from the Annona genus have proven biological activities, such as antitumor, antioxidant, antimicrobial and antifungal. The present review had as its objective to facilitate access to ethnobotanical, chemical and biological information in order to direct future researches.
Assuntos
Annona , Etnobotânica , Etnofarmacologia , Humanos , Medicina Tradicional , Fitoterapia , Extratos Vegetais/farmacologiaRESUMO
In this study the physicochemical characterization of the pulp and almond fixed oil was carried out; their antibacterial activity and aminoglycoside antibiotic modifying action against standard and multiresistant Gram-positive and -negative bacteria were investigated using the broth microdilution assay. Physical properties such as moisture, pH, acidity, peroxide index, relative density and refractive index indicate stability and chemical quality of the oils. In the GC/MS chemical composition analysis, a high unsaturated fatty acid content and the presence of oleic and palmitic acids were observed in the oils. In the antibacterial assay, more significant results were obtained for Escherichia coli, while other standard and multi-resistant strains presented MIC values ≥ 1024 µg/mL. Furthermore, the fixed oils in association with antibiotics were able to significantly improve antibacterial activity against S. aureus with a reduction in MICs.
Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Malpighiales/química , Óleos de Plantas/farmacologia , Aminoglicosídeos/farmacologia , Escherichia coli/efeitos dos fármacos , Ácidos Graxos/análise , Cromatografia Gasosa-Espectrometria de Massas , Testes de Sensibilidade Microbiana , Óleos de Plantas/química , Staphylococcus aureus/efeitos dos fármacosRESUMO
Cissampelos sympodialis Eichler is well studied and investigated for its antiasthmatic properties, but there are no data in the literature describing antibacterial properties of alkaloids isolated from this botanical species. This work reports the isolation and characterization of phanostenine obtained from roots of C. sympodialis and describes for the first time its antimicrobial and antibiotic modulatory properties. Phanostenine was first isolated from Cissampelos sympodialis and its antibacterial activities were determined. Chemical structures of the alkaloid isolate were determined using spectroscopic and chemical analyses. Phanostenine was also tested for its antibacterial activity against standard strains and clinical isolates of Escherichia coli and Staphylococcus aureus. Minimal inhibitory concentration (MIC) was determined in a microdilution assay and for the evaluation of antibiotic resistance-modifying activity. MIC of the antibiotics was determined in the presence or absence of phanostenine at sub-inhibitory concentrations. The evaluation of antibacterial activity by microdilution assay showed activity for all strains with better values against S. aureus ATCC 12692 and E. coli 27 (787.69â mm). The evaluation of aminoglycoside antibiotic resistance-modifying activity showed reduction in the MIC of the aminoglycosides (amikacin, gentamicin and neomycin) when associated with phanostenine, MIC reduction of antibiotics ranging from 21 % to 80 %. The data demonstrated that phanostenine possesses a relevant ability to modify the antibiotic activity inâ vitro. We can suggest that phanostenine presents itself as a promising tool as an adjuvant for novel antibiotics formulations against bacterial resistance.
Assuntos
Alcaloides/química , Antibacterianos/química , Derivados de Benzeno/química , Cissampelos/química , Compostos Heterocíclicos de 4 ou mais Anéis/química , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Derivados de Benzeno/isolamento & purificação , Derivados de Benzeno/farmacologia , Cissampelos/metabolismo , Farmacorresistência Bacteriana/efeitos dos fármacos , Compostos de Anéis Fundidos , Compostos Heterocíclicos de 4 ou mais Anéis/isolamento & purificação , Compostos Heterocíclicos de 4 ou mais Anéis/farmacologia , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Raízes de Plantas/química , Raízes de Plantas/metabolismo , Staphylococcus aureus/efeitos dos fármacosRESUMO
This study aimed to verify the chelating, antioxidant and cytoprotective activities of Psidium brownianum Mart. Ex DC against mercury and aluminum. The ethanolic extract, as well as the tannic and flavonoid fractions, were prepared and subjected to liquid chromatography-mass spectrometry analysis. Ferric ion reduction and antioxidant activity measurement using the FRAP method were performed with P. brownianum. After determining the sub-allelopathic doses, germination tests using Lactuca sativa (lettuce) seeds were performed. The main compounds identified in the extract and fractions were: quercetin and its derivatives; myricetin and its derivatives; gallic acid; ellagic acid; quinic acid and gallocatechin. The Minimum Inhibitory Concentration (MIC) for all samples wereâ¯≥â¯1024⯵g/mL. The flavonoid fraction in association with mercury chloride demonstrated cytoprotection (pâ¯<â¯0.001). The sub-allelopathic concentration used was 64⯵g/mL. The extract and fractions were cytoprotective for radicles and caulicles when assayed in association with mercury and against aluminum for radicles. This suggests that the P. brownianum extract and its fractions present cytoprotective activity, possibly related to the antioxidant effect of secondary metabolites, especially flavonoids.
Assuntos
Cloreto de Alumínio/toxicidade , Antioxidantes/farmacologia , Quelantes/farmacologia , Cloreto de Mercúrio/toxicidade , Extratos Vegetais/farmacologia , Psidium , Alelopatia , Antioxidantes/química , Candida albicans/efeitos dos fármacos , Candida albicans/crescimento & desenvolvimento , Quelantes/química , Cromatografia Líquida , Citoproteção , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Flavonoides/análise , Flavonoides/farmacologia , Germinação/efeitos dos fármacos , Ferro/química , Lactuca/efeitos dos fármacos , Lactuca/crescimento & desenvolvimento , Espectrometria de Massas , Extratos Vegetais/químicaRESUMO
The present study had as its objective to verify the Psidium guajava var. Pomifera L. chelating, antioxidant and cytoprotective effects against mercury and aluminum. The ethanolic extract, tannic and flavonoid fractions were subjected to LC-MS analysis. The Ferric Reducing Antioxidant Power (FRAP) and ferric ion reduction demonstrated a present antioxidant activity. The fungicidal and bactericidal activity of these metals were established. After determining the sub-allelopathic doses, germination tests using Lactuca sativa were performed. Quercetin and its derivatives were the main compounds identified in the extract and the fractions. Mercury chloride significantly reduced the bactericidal effect of the flavonoid fraction (pâ¯<â¯0.001). None of the fractions were cytoprotective against mercury or aluminum in the fungal model assays. Using a sub-allelopathic concentration (64⯵g/mL), the ethanolic extract, flavonoid and tannic fractions were found to be cytoprotective against aluminum for radicles, however only the tannic fraction was cytoprotective for caulicles. These data suggest that natural P. guajava products are promising cytoprotective compound sources. This activity may be related to the antioxidant effect of secondary metabolites, mainly flavonoids. Our results point to a potential for environmental intervention product and technique development aimed at mitigating contamination by toxic metals such as mercury and aluminum.
Assuntos
Antioxidantes/química , Flavonoides/química , Metais Pesados/toxicidade , Psidium/química , Antioxidantes/análise , Metais Pesados/análiseRESUMO
The objective of this work was to evaluate the antioxidant, metal chelating and cytoprotective activity of the Eugenia jambolana Lam. extract, as well as of its flavonoid and tannic fractions, against the action of Mercury Chloride (HgCl2). Flavonoids were quantified and an LC-MS chromatographic analysis was performed to identify secondary metabolites. Fe2+ and Fe3+ chelation tests and antioxidant activity were carried out using the FRAP method. Microbiological tests were performed by microdilution to determine the Minimum Inhibitory Concentration (MIC). From these results the Minimum Bactericidal (MBC) and Minimum Fungicide Concentration (MFC) were evaluated. The allelopathy and cytoprotection assays were performed using eukaryotic and prokaryotic models. The results revealed the presence of phenolic acids and flavonoids in the E. jambolana extract and fractions. The sub-allelopathic concentration (64⯵g/mL) was used and the results demonstrated the E. jambolana potential cytoprotective effect against mercury chloride.
Assuntos
Produtos Biológicos/química , Cloreto de Mercúrio/toxicidade , Syzygium/química , Alelopatia , Anti-Infecciosos/química , Antioxidantes/química , Citoproteção , Flavonoides/química , Lactuca/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Extratos Vegetais/químicaRESUMO
Orbignya speciosa and Mauritia flexuosa are two native palm tree species found in Brazil. Their fruits are rich in edible fixed oils, which are used for many purposes in industry, such as in the manufacture of soaps, surfactants and margarines. The aim of this work was to characterize the chemical profiles and antioxidant properties of the methanol extracts obtained from the fruits of O. speciosa and M. flexuosa. The chemical prospection was carried out using specific qualitative tests to evaluate the presence of phenolic compounds (tannins and flavonoids) in the extracts of both species. The antioxidant properties of the extracts were analyzed by the following methods: production of thiobarbituric acid reactive substances (TBARS) from phospholipids, deoxyribose degradation, radical-scavenging activity-DPPH, iron chelation assay and ferric-reducing antioxidant power (FRAP). The methanolic extracts obtained from M. flexuosa and O. speciosa presented significant antioxidant activities, although M. flexuosa presented higher antioxidant activity than O. speciosa. In conclusion, M. flexuosa and O. speciosa are important sources of antioxidant substances that may be useful in the development of new products to prevent diseases associated with oxidative stress.
Assuntos
Antioxidantes/farmacologia , Arecaceae/química , Frutas/química , Compostos Fitoquímicos/química , Antioxidantes/química , Compostos de Bifenilo/química , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/farmacologia , Quelantes de Ferro , Fosfolipídeos , Picratos/química , Substâncias Reativas com Ácido TiobarbitúricoRESUMO
The Protium heptaphyllum species, also known as Almécega, produces an oily resin, used in folk medicine as an analgesic and anti-inflammatory agent, in healing, and as an expectorant, which is rich in pentacyclic triterpenes and essential oils. In this study, the essential oil obtained by hydrodistillation of Almécega's resin was analyzed by gas chromatography-triple quadrupole mass spectrometry and evaluated for chemical composition and vasorelaxant activity in rat superior mesenteric artery. The main constituents determined by gas chromatography-triple quadrupole mass spectrometry were limonene, p-cineole, and o-cymene. In intact rings precontracted with phenylephrine (Phe 1 µM), EOPh (3-750 µg/mL) induced relaxation, and the essential oil had a concentration-dependent vasorelaxant effect, without involvement of endothelial mediators.
Assuntos
Burseraceae/química , Óleos Voláteis/química , Analgésicos/química , Analgésicos/farmacologia , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Cicloexenos/química , Cicloexenos/farmacologia , Células Endoteliais/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas/métodos , Limoneno , Masculino , Óleos Voláteis/farmacologia , Fenilefrina/química , Fenilefrina/farmacologia , Ratos , Ratos Wistar , Resinas Vegetais/química , Terpenos/química , Terpenos/farmacologia , Vasodilatadores/química , Vasodilatadores/farmacologiaRESUMO
Psidium guajava is a Myrtaceae plant whose medicinal properties are recognized in several locations. The use of teas and tinctures prepared from their leaves has been used to combat infections caused by fungi of the genus Candida. In this study, aqueous extracts of leaves and hydroethanolic were tested to verify the antifungal potential and its chemical composition has been investigated. The microbiological assays were performed by broth microdilution to determine the minimum inhibitory concentration (MIC) and from these the minimum fungicidal concentration was performed (MFC) by subculturing on solid media. A cell viability curve was obtained for demonstration of inhibition of fungal growth of strains of Candida albicans and Candida tropicalis. Tests to check morphological changes by the action of the extracts were performed in microcultive cameras depleted environment at concentrations of MIC/2, MIC and MIC × 2. Extracts analyzed by high performance liquid chromatography demonstrated flavonoids and phenolic acids. The extracts showed fungistatic effect and no fungicide with MIC >8192 µg/mL, MFC above 8192 µg/mL. The IC50 was calculated ranging from 1803.02 to 5623.41 µg/mL. It has been found that the extracts affect the morphological transition capability, preventing the formation of pseudohyphae and hyphae. Teas and tinctures, therefore, have the potential antifungal, by direct contact, causing inhibition of fungal multiplication and its virulence factor, the cell dimorphism, preventing tissue invasion. Further studies are needed to elucidate the biochemical pathways and genes assets involved in these processes.
RESUMO
Evaluations of the therapeutic potential of medicinal plants and their components have been the subject of many studies. Furthermore, the biological activities of various plant species have been reported in various pieces of literature. Hyptis martiusii Benth (Lamiaceae), popularly known as "mad balm" is commonly found in the North, Southeast, and Northeast of Brazil. Its leaves are used ethnobiologically as antiulcerogenic, antimicrobial, antitumor and as insecticide. This study aimed to analyze the chemical composition of the essential oil of H. martiusii Benth (OEHM) by GC/MS as well as its possible topical activity as an antiedematogenic. This is verified by the models of ear edema induced by single (acute edema) and multiple (chronic edema) applications of croton oil topically, and systemically verified through the model of paw edema induced by carrageenan 1%. Doses of 50, 75 and 100 mg/kg OEHM were used in all tests. Chemical analysis of the oil revealed the 1,8-cineole (34.58%) and δ-carene (21:58%) as major components present in the essential oil. On the model of ear edema, acute and chronic OEHM in all the tested doses showed no significant antiedematogenic activity (p < 0.05). The systemic model of paw edema induced by carrageenin showed that a dose of 100 mg/kg effectively reduced swelling by 55.37% in the second hour evaluation when compared to the saline group. The anti-inflammatory systemic effect can give greater bioavailability of the components present in the essential oil and your interference in cytokines and leukotriene, thromboxane and prostaglandin biosynthesis. It is therefore concluded that OEHM presents systemic antiedematogenic activity but not topical activity at these doses.
RESUMO
Medicinal plants are often the only therapeutic resource for many communities and ethnic groups. Cordia verbenacea DC., "Erva-baleeira," is one of the species of plants currently used to produce a phytotherapeutic product extracted from its leaves. The present study aimed to establish its chemical profile, antibacterial activity and resistance-modulating potential. The C. verbenacea extracts were prepared from fresh leaves using solvents as methanol and hexane. Ethyl Acetate was used for the preparation of the fraction. Phytochemical screening was carried out using HPLC-DAD for determination and quantification of the secondary metabolites present in the fractions. Antibacterial and resistance-modulation assays were performed to determine minimum inhibitory concentration (MIC) using a microdilution assay. The data were subjected to statistical analysis with two-way ANOVA and Bonferroni posttests. Results of phytochemical prospecting and HPLC analysis of the fractions were in agreement with the literature. The natural products presented moderate antibacterial activity when considering the clinical relevance of a MIC of 256 µg/mL against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa, and 512 µg/mL against P. aeruginosa. However, when the fractions were combined with antibiotics we observed a synergic effect, as natural products enhanced the antibacterial effect of aminoglycosides, significantly decreasing the MIC of antibiotics at 12.5%-98.4%. We believe that the data obtained from phytochemical analysis and from antibacterial and resistance modulation assays of C. verbenacea extracts new can open perspectives in the search for new alternatives for the treatment of bacterial infections and stimulate the renewed use of antibiotics with reduced effectiveness due to resistance.
Assuntos
Aminoglicosídeos/farmacologia , Antibacterianos/farmacologia , Produtos Biológicos/farmacologia , Cordia/química , Sinergismo Farmacológico , Compostos Fitoquímicos/farmacologia , Antibacterianos/isolamento & purificação , Produtos Biológicos/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Escherichia coli/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/isolamento & purificação , Folhas de Planta/química , Pseudomonas aeruginosa/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacosRESUMO
Biflorin 1 is a biologically active quinone, isolated from Capraria biflora. Five new biflorin-based nitrogen derivatives were synthesized, of which two were mixtures of (E)- and (Z)- isomers: (Z)-2a, (Z)-2b, (Z)-3a, (Z)- and (E)-3b, (Z)- and (E)-3c. The antibacterial activity was investigated using the microdilution method for determining the minimum inhibitory concentration (MIC) against six bacterial strains. Tests have shown that these derivatives have potential against all bacterial strains. The cytotoxic activity was also evaluated against three strains of cancer cells, but none of the derivatives showed activity.
Assuntos
Antibacterianos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Hidrazonas/farmacologia , Naftoquinonas/farmacologia , Oximas/farmacologia , Scrophulariaceae/química , Antibacterianos/síntese química , Antibacterianos/química , Antineoplásicos Fitogênicos/síntese química , Antineoplásicos Fitogênicos/química , Bactérias/efeitos dos fármacos , Infecções Bacterianas/tratamento farmacológico , Linhagem Celular Tumoral , Humanos , Hidrazonas/síntese química , Hidrazonas/química , Testes de Sensibilidade Microbiana , Naftoquinonas/síntese química , Naftoquinonas/química , Neoplasias/tratamento farmacológico , Oximas/síntese química , Oximas/químicaRESUMO
The aim of this work was to evaluate the interactions between gentamicin and the ethanol extract of the fern Lygodium venustum SW (EELV). The ethanol extract of L. venustum was obtained, the phytocompounds were identified and the EELV was assayed by the checkerboard method with gentamicin against two bacterial strains multiresistant to antibiotics. The antibiotic activity of gentamicin, when associated with the extract, was enhanced in an additive manner against both strains. The results indicated that L. venustum can be a source of secondary metabolites to be used in association with antibiotics as aminoglycosides in the antibiotic chemotherapy against resistant bacteria.
Assuntos
Antibacterianos/farmacologia , Gleiquênias/química , Gentamicinas/farmacologia , Extratos Vegetais/farmacologia , Antibacterianos/química , Avaliação Pré-Clínica de Medicamentos/métodos , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Sinergismo Farmacológico , Escherichia coli/efeitos dos fármacos , Etanol/química , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Staphylococcus aureus/efeitos dos fármacosRESUMO
In order to develop bioactive lithocholic acid derivatives, we prepared fifteen semi-synthetic compounds through modification at C-3 and/or C-24. The reactions showed yields ranging from 37% to 100%. The structures of all compounds obtained were identified on the basis of their spectral data (IR, MS, 1D- and 2D-NMR). The activity of lithocholic acid and derivatives was evaluated against the growth of Escherichia coli, Staphylococcus aureus, Bacillus cereus and Pseudomonas aeruginosa. The derivative 3α-formyloxy-5ß-cholan-24-oic acid (LA-06) showed the best activity, with MIC values of 0.0790 mM against E. coli (Ec 27) and B. cereus in both cases, and 0.0395 mM against S. aureus (ATCC 12692). Lithocholic acid and the derivatives with MIC⩽1.2 mM were evaluated on the susceptibility of some bacterial pathogens to the aminoglycoside antibiotics neomycin, amikacin and gentamicin was evaluated. There are no previously reported studies about these compounds as modifiers of the action of antibiotics or any other drugs.
Assuntos
Antibacterianos/farmacologia , Bacillus cereus/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Ácido Litocólico/análogos & derivados , Ácido Litocólico/farmacologia , Pseudomonas aeruginosa/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Antibacterianos/síntese química , Antibacterianos/química , Bacillus cereus/crescimento & desenvolvimento , Relação Dose-Resposta a Droga , Escherichia coli/crescimento & desenvolvimento , Ácido Litocólico/síntese química , Ácido Litocólico/química , Testes de Sensibilidade Microbiana , Conformação Molecular , Pseudomonas aeruginosa/crescimento & desenvolvimento , Staphylococcus aureus/crescimento & desenvolvimento , Relação Estrutura-AtividadeRESUMO
CONTEXT: Murraya paniculata (Linn) JACK (Rutaceae) is used in traditional medicine in the treatment of diabetes, inflammation, and microbial disorders. OBJECTIVE: This study determined the polyphenol composition and antimicrobial and acute toxicological activity of the hydroethanolic extract of M. paniculata leaves (EEMp). MATERIALS AND METHODS: Chemical composition was evaluated by the Folin-Ciocalteu and AlCl3 assays and by HPLC-DAD. Antibacterial and modulatory activity was determined by the microdilution method. Toxicity was assessed with a single dose of EEMp administered orally at doses of 2000 and 5000 mg/kg body weight/day in male and female Swiss mice. RESULTS: Total phenolic content of the EEMp samples varied from 66.5 to 396.8 mg gallic acid equivalent/g of extract and flavonoid content varied from 0.3 to 31.1 mg quercetin equivalent/g of extract. The principal component identified by HPLC-DAD assay was ellagic acid. The results of oral acute toxicity showed no mortality, changes in hematological parameters, or CNS and ANS toxicities in rats. Biochemical analysis showed a significant increase in glucose and glutamic oxaloacetic transaminase activity and reduction in triglycerides and cholesterol for 5000 and 2000 mg/kg doses, respectively, when compared with the control group. Histopathological evaluation showed no significant microscopic changes. EEMp showed essentially no antimicrobial activity, but when aminoglycosides were combined with EEMp their MIC was reduced. CONCLUSIONS: Significant effects were observed in the acute toxicity assay, but they had no clinical relevance. The results suggest that M. paniculata could be used as a source of natural products with antibacterial resistance-modifying activity, with lower toxicity.
Assuntos
Antibacterianos/isolamento & purificação , Farmacorresistência Bacteriana/efeitos dos fármacos , Flavonoides/isolamento & purificação , Murraya/química , Extratos Vegetais/química , Animais , Antibacterianos/farmacologia , Antibacterianos/toxicidade , Brasil , Relação Dose-Resposta a Droga , Feminino , Flavonoides/farmacologia , Flavonoides/toxicidade , Masculino , Medicina Tradicional , Testes de Sensibilidade Microbiana , Folhas de Planta/química , Ratos WistarRESUMO
Psidium guajava (Myrtaceae), a common plant in Cariri region, Ceara, Brazil, as well as in various parts of the world, contains high concentrations of bioactive compounds and in many communities its parts are used for therapeutic purposes. Studies describe antioxidant, antimicrobial and anti-diarrheal actions from extracts obtained from leaves, but information about the activities of the fruits and comparison of these at different maturity stages (immature, partially mature and mature) are scarce. This study aims to evaluate the antioxidant properties by quantifying the levels of phenolic and flavonoid compounds, carotenoids and vitamin C of P. guajava fruits at different stages of maturation. The content of phenolic compounds for the immature fruit, partially mature and mature were: 22.41; 34.61 and 32.92 mg of AG/g fraction. The flavonoid content for immature fruits, intermediate and mature were: 2.83; 5.10 and 5.65 mg RUT/g fraction, respectively. Following the same standards of maturation stages, the ascorbic acid content was determined with values of 0.48; 0.38 and 0.21 mg AA/g fraction, respectively. HPLC analysis identified and quantified the presence of gallic acid, catechin, chlorogenic acid, caffeic acid, epicatechin, rutin, quercitrin, isoquercitrin, quercetin, kaempferol, glycosylated campeferol, tocopherol, ß-carotene and lycopene. The antioxidant activity carried out by DPPH method showed the mature fruits bearing the best results, whereas chelation of Fe2+ ions showed higher percentage for the immature fruit. The results obtained by lipidic peroxidation were not satisfactory.
RESUMO
Objetivo: Estudos recentes apontam a utilização de plantas na forma de sucos ou chás como fontes de agentes antioxidantes naturais que apresentam baixo risco podendo ser utilizado no auxílio do tratamento de várias doenças. Materiais e métodos: Neste contexto, avaliaram-se os potenciais antioxidantes, in vitro, dos extratos de Eugenia uniflora e Psidium sobraleanum, além de quantificar fenóis e flavonoides presentes nos extratos. Resultados: De acordo com os resultados obtidos, observou-se uma melhor atividade antioxidante para o extrato de Eugenia uniflora, para o teste de TBARS com fosfolipídio de ovo, os extratos reduziram os níveis basais no processo de peroxidação lipídica, e quando induzidos por Fe2+ o extrato de Psidium sobraleanum mostrouse mais eficiente. Conclusões: Portanto, através destes ensaios pode-se verificar que os extratos das folhas das espécies, Eugenia uniflora e Psidium sobraleanum, apresentam uma atividade antioxidante, diretamente relacionada com substâncias fenólicas produzidas a partir do seu metabolismo secundário.
Objetivo: Estudios recientes reportan la utilización de plantas en forma de zumos o té como fuente de agentes antioxidantes naturales que presentan bajo riesgo, pudiendo ser utilizados como complemento del tratamiento de diversas enfermedades. Materiales y métodos: En este contexto, se evaluarán in vitro, los potenciales antioxidantes, de los extractos de Eugenia uniflora y Psidium sobraleanum, además de cuantificar fenoles y flavonoides presentes en los extractos. Resultados: De acuerdo con los resultados obtenidos, se observó una mejor actividad antioxidante con el extracto de Eugenia uniflora, en el test de TBARS con fofolípidos de huevo, los extractos redujeron los niveles basales en el proceso de peroxidación lipídica; y cuando fue inducida con Fe+2, el extracto de Psidium sobraleanum se mostró más eficiente. Conclusiones: Por lo tanto, a través de estos ensayos se pudo comprobar que los extractos de las hojas de las especies Eugenia uniflora y Psidium sobraleanum presentan actividad antioxidante, directamente relacionada con sustancias fenólicas producidas a partir de sus metabolitos secundarios.
Objective: Evaluation of antioxidant activity has been an important issue considering its importance in human health. Recent studies show that the use of plants in the form of juices or teas as sources of natural antioxidants with low risk can be used as an aid to the treatment of various diseases. Material and Methods: Evaluation of the antioxidant potential in vitro, extracts of Eugenia uniflora and Psidium sobraleanum, as well as the quantification of phenols and flavonoids present in the extracts. Results: Findings showed a better antioxidant activity for the extract of Eugenia uniflora. In the TBARS test with egg phospholipids, extracts presented a reduction in the basal levels in the lipid peroxidation process; and when the Fe2 + extract was inducted, Psidium sobraleanum proved to be more efficient.. Conclusions: These tests proved that the extracts of leaves of the species Eugenia uniflora and Psidium sobraleanum present antioxidant activity which is directly related to phenolic substances produced in its secondary metabolism.