RESUMEN

To evaluate the antibacterial, antibiofilm and antivirulence potential of the main diterpenes from Copaifera spp. oleoresins against multidrug-resistant (MDR) bacteria. Antimicrobial assays included determination of the Minimum Inhibitory Concentration (MIC), Minimum Bactericidal Concentration (MBC), Minimum Inhibitory Concentration of Biofilm (MICB50), as well as synergistic and antivirulence assays for eight diterpenes against MDR. The tests revealed that two diterpenes (named 1 and 5) showed the best results, with MIC and MBC between 12.5 and 50 µg/mL against most MDR bacteria. These diterpenes exhibited promising MICB50 in concentration between 3.12-25 µg/mL but showed no synergistic antimicrobial activity. In the assessment of antivirulence activity, diterpenes 1 and 5 inhibited only one of the virulence factors evaluated (Dnase) produced by some strains of S. aureus at subinhibitory concentration (6.25 µg/mL). Results obtained indicated that diterpenes isolated from Copaifera oleoresin plays an important part in the search of new antibacterial and antibiofilm agents that can act against MDR bacteria.

Asunto(s)

Antibacterianos , Biopelículas , Diterpenos , Farmacorresistencia Bacteriana Múltiple , Fabaceae , Pruebas de Sensibilidad Microbiana , Extractos Vegetales , Biopelículas/efectos de los fármacos , Diterpenos/farmacología , Diterpenos/aislamiento & purificación , Antibacterianos/farmacología , Antibacterianos/aislamiento & purificación , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Fabaceae/química , Extractos Vegetales/farmacología , Extractos Vegetales/aislamiento & purificación , Virulencia/efectos de los fármacos

RESUMEN

The concern regarding the harm caused by biocides to human health has been increasing over the years, making the natural products an alternative to less toxic and more efficient biocides. Therefore, this paper reports the investigation of the disinfectant potential of extracts and isolated compounds from Baccharis dracunculifolia. For this purpose, extracts of aerial parts (BD-C), tricomial wash (BD-L) and roots (BD-R) of B. dracunculifolia were obtained by maceration. The extracts were submitted to different chromatographic techniques, including high-speedy countercurrent chromatography (HSCCC) furnishing nine isolated compounds. The extracts and isolated compounds were evaluated regarding their antimicrobial activity by the broth microdilution method, according to the Clinical and Laboratory Standards Institute, and regarding their sanitizing activity according to Standard Operating Procedure No. 65·3210·007 (INCQS, 2011), developed by the National Institute for Quality Control in Health (INCQS) - Oswaldo Cruz Foundation (FIOCRUZ). In the antimicrobial evaluation the BD-C extract showed minimum inhibitory concentration (MIC) values of 200 and 100 µg/ml against Staphylococcus aureus and Tricophyton mentagrophytes, respectively. BD-L extract showed MIC value of 200 µg/ml against S. aureus. The isolated compounds caffeic acid (MBC 2·22 µmol l-1 ), ferulic acid (MBC 2·06 µmol l-1 ) and baccharin (MBC 0·27 µmol l-1 ) showed significant inhibitory activity against S. aureus. All B. dracunculifolia isolated compounds were active with exception of aromadrendin-4´-O-methyl-ether for T. mentagrophytes. Additionally, isosakuranetin was active against Salmonella choleraesuis (MIC 1·4 µmol l-1 ). Regarding the sanitizing activity, the hydroalcoholic solution containing 0·2% of B. dracunculifolia extract in 40°GL ethanol was effective in eliminating the microbial contamination on all carrier cylinders and against all microorganisms evaluated in the recommended exposure time of 10 min. Therefore, B. dracunculifolia has potential for the development of sanitizing agents to be used in hospitals, food manufactures and homes.

Asunto(s)

Antiinfecciosos , Baccharis , Desinfectantes , Antiinfecciosos/farmacología , Baccharis/química , Desinfectantes/farmacología , Humanos , Pruebas de Sensibilidad Microbiana , Extractos Vegetales/química , Staphylococcus aureus

RESUMEN

Gold nanoparticles (AuNPs) are highlighted due to their low toxicity, compatibility with the human body, high surface area to volume ratio, and surfaces that can be easily modified with ligands. Biosynthesis of AuNPs using plant extract is considered a simple, low-cost, and eco-friendly approach. Brazilian Red Propolis (BRP), a product of bees, exhibits anti-inflammatory, anti-tumor, antioxidant, and antimicrobial activities. Here, we described the biosynthesis of AuNPs using BRP extract (AuNPextract) and its fractions (AuNPhexane, AuNPdichloromethane, AuNPethyl acetate) and evaluated their structural properties and their potential against microorganisms and cancer cells. AuNPs showed a surface plasmon resonance (SPR) band at 535 nm. The sizes and morphologies were influenced by the BRP sample used in the reaction. FTIR and TGA revealed the involvement of bioactive compounds from BRP extract or its fractions in the synthesis and stabilization of AuNPs. AuNPdichloromethane and AuNPhexane exhibited antimicrobial activities against all strains tested, showing their efficacy as antimicrobial agents to treat infectious diseases. AuNPs showed dose-dependent cytotoxic activity both in T24 and PC-3 cells. AuNPdichloromethane and AuNPextract exhibited the highest in vitro cytotoxic effect. Also, the cytotoxicity of biogenic nanoparticles was induced by mechanisms associated with apoptosis. The results highlight a potential low-cost green method using Brazilian red propolis to synthesize AuNPs, which demonstrated significant biological properties.

Asunto(s)

Antiinfecciosos/farmacología , Antineoplásicos/farmacología , Oro/química , Nanopartículas del Metal/química , Própolis/farmacología , Antiinfecciosos/química , Antineoplásicos/química , Bacterias/efectos de los fármacos , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Hongos/efectos de los fármacos , Tecnología Química Verde/métodos , Humanos , Pruebas de Sensibilidad Microbiana , Microscopía Electrónica de Transmisión , Própolis/química , Espectroscopía Infrarroja por Transformada de Fourier , Resonancia por Plasmón de Superficie , Termogravimetría

RESUMEN

Solanum lycocarpum fruits contain two major glycoalkaloids (GAs), solamargine (SM) and solasonine (SS). These compounds are reported as cytotoxic. However, they have poor water solubility and low bioavailability. To overcome these disadvantages and getting an efficient formulation the current study aimed to develop, characterize, and test the effectiveness of a nanotechnology-based strategy using poly(D,L-lactide) (PLA) nanoparticles functionalized with folate as delivery system of glycoalkaloidic extract (AE) for bladder cancer therapy. The strategic of adding folic acid into nanoformulations can increase the selectivity of the compounds to the cancer cells reducing the side effects. Our results revealed the successful preparation of AE-loaded folate-targeted nanoparticles (NP-F-AE) with particle size around 177 nm, negative zeta potential, polydispersity index <0.20, and higher efficiency of encapsulation for both GAs present in the extract (>85 %). To investigate the cellular uptake, the fluorescent dye coumarin-6 was encapsulated into the nanoparticle (NP-F-C6). The cell studies showed high uptake of nanoparticles by breast (MDA-MB-231) and bladder (RT4) cancer cells, but not for normal keratinocytes cells (HaCaT) indicating the target uptake to cancer cells. The cytotoxicity of nanoparticles was evaluated on RT4 2D culture model showing 2.16-fold lower IC50 than the free AE. Furthermore, the IC50 increased on the RT4 spheroids compared to 2D model. The nanoparticles penetrated homogeneously into the urotheliumof porcine bladder. These results showed that folate-conjugated polymeric nanoparticles are potential carriers for targeted glycoalkaloidic extract delivery to bladder cancer cells.

RESUMEN

Two novel compounds bearing heterocyclic nitrogen, 2-pyridone alkaloid (1) and alloxazine derivative (2), along with the known pretenellin B (3), pyridovericin (4) and lumichrome (5) were isolated from a culture of the entomopathogenic fungal strain Beauveria bassiana. The chemical structures of 2-pyridone alkaloid and alloxazine derivative were established on the basis of the interpretation of spectroscopic data. The isolated compounds were evaluated in a panel of five cancer cell lines and pyridovericin exhibited cytotoxicity (IC50, µM) against cancer cell lines: HL-60 (25.9 ± 0.3), HCT8 (34.6 ± 3.6), MDA-MB435 (34.8 ± 3.8) and SF295 (31.1 ± 0.6). Considering that other pyridone compounds display good cytotoxic activity, it would be suggested to obtain new semi synthetic derivatives of pyridovericin, for the development of new cytotoxic chemical entities.

Asunto(s)

Alcaloides/química , Antineoplásicos/farmacología , Beauveria/química , Alcaloides/aislamiento & purificación , Alcaloides/farmacología , Antineoplásicos/química , Beauveria/metabolismo , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Flavinas/química , Flavinas/aislamiento & purificación , Humanos , Estructura Molecular , Monosacáridos/química , Piridonas/química , Piridonas/aislamiento & purificación , Piridonas/farmacología , Metabolismo Secundario

RESUMEN

A possible immunomodulatory/anti-inflammatory effect of Baccharis dracunculifolia (Bd) and its major compound--caffeic acid (Ca)--on cytokines production (IL-1ß, IL-6 and IL-10) by murine macrophages was investigated. Cells were incubated with Bd and Ca, and the inhibitory concentrations were tested before or after macrophages challenge with LPS. Bd and Ca stimulated IL-1ß and inhibited IL-6 and IL-10 production. In LPS-challenge protocols, Bd prevented LPS action either before or after LPS challenge, whereas Ca prevented LPS effects only after LPS addition. Bd modulatory action on cytokines production may be at least in part mediated by Ca, since it has been shown to inhibit the transcription factor NF-κB. Further studies are still needed to evaluate Bd efficacy in inflammatory diseases, in order to explore its antiinflammatory activity in vivo.

Asunto(s)

Antiinflamatorios/química , Antiinflamatorios/farmacología , Baccharis/química , Factores Inmunológicos/química , Factores Inmunológicos/farmacología , Hojas de la Planta/química , Animales , Cromatografía Líquida de Alta Presión , Interleucina-10/metabolismo , Interleucina-1beta/metabolismo , Interleucina-6/metabolismo , Macrófagos Peritoneales/efectos de los fármacos , Ratones , FN-kappa B/metabolismo

RESUMEN

From cultures of thermophilic soil fungus Humicola grisea var thermoidea, a δ-lactam derivative (3-(2-(4-hydroxyphenyl)-2-oxoethyl)-5,6-dihydropyridin-2(1H)-one) that displayed anti-allergic activity was isolated, which was predicted by in silico computational chemistry approaches. The in vitro anti-allergic activity was investigated by ß-hexosaminidase release assay in rat basophilic leukaemia RBL-2H3 cells. The δ-lactam derivative exhibited similar anti-allergic activity (IC(50) = 18.7 ± 6.7 µM) in comparison with ketotifen fumarate (IC(50) = 15.0 ± 1.3 µM) and stronger anti-allergic activity than azelastine (IC(50) = 32.0 µM). Also, the MTT cytotoxicity assay with RBL-2H3 cells showed that δ-lactam does not display cytotoxicity at concentrations lower than 50 µM. This study suggests that the δ-lactam derivative has the potential to be used as a lead compound in the development of anti-allergic drugs for clinical use in humans.

Asunto(s)

Antialérgicos/química , Antialérgicos/farmacología , Ascomicetos/química , Lactamas/química , Piridonas/química , Piridonas/farmacología , Animales , Degranulación de la Célula/efectos de los fármacos , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Simulación por Computador , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos/métodos , Concentración 50 Inhibidora , Cetotifen/farmacología , Espectroscopía de Resonancia Magnética , Estructura Molecular , Ftalazinas/farmacología , Ratas , Microbiología del Suelo , beta-N-Acetilhexosaminidasas/metabolismo

RESUMEN

The aim of this study was to examine the effects of Dorstenia asaroides extracts on cariogenic properties of the most cariogenic bacteria, Streptococcus mutans. Hexane (HFr), ethyl-acetate (EFr) and chloroform (CFr) extracts obtained from D. asaroides rhizomes were submitted to chemical analyses, Minimal Inhibitory Concentrations (MIC), glycolysis assay and S. mutans 12-h-old initial biofilms. Chemical characterization showed that all the extracts present furanocoumarins. The MIC values were 80 (HFr and CFr) and 50 µg/mL (EFr). Acid production by S. mutans cells was significantly disrupted by HFr (12.5 mg/mL), EFr (at 2.5; 6.25 and 12.5 mg/mL) and CFr (at 2.5, 6.25 and 12.5 mg/mL) (p < 0.01). Topical applications of HFr, EFr and CFr significantly reduced the colony forming units of S. mutans biofilms compared with those treated with control group in order to 20, 30 and 25% respectively (p < 0.01). The results of the present study suggest that rhizomes of D. asaroides had inhibitory effects on cariogenic properties of S. mutans.

Asunto(s)

Antibacterianos/farmacología , Moraceae/química , Extractos Vegetales/farmacología , Streptococcus mutans/efectos de los fármacos , Streptococcus mutans/metabolismo , Biopelículas/efectos de los fármacos , Glucólisis/efectos de los fármacos , Pruebas de Sensibilidad Microbiana

RESUMEN

(±)-Licarin A (1) was obtained by oxidative coupling, and its enantiomers, (-)-licarin A (2) and (+)-licarin A (3), were resolved by chiral HPLC. Schistosomicidal and trypanocidal activities of these compounds were evaluated in vitro against Schistosoma mansoni adult worms and trypomastigote forms of Trypanosoma cruzi. The racemic mixture (1) displayed significant schistosomicidal activity with an LC50 value of 53.57 µM and moderate trypanocidal activity with an IC50 value of 127.17 µM. On the other hand, the (-)-enantiomer (2), displaying a LC50 value of 91.71 µM, was more active against S. mansoni than the (+)-enantiomer (3), which did not show activity. For the trypanocidal assay, enantiomer 2 showed more significant activity (IC50 of 23.46 µM) than enantiomer 3, which showed an IC50 value of 87.73 µM. Therefore, these results suggest that (±)-licarin A (1) and (-)-licarin A (2) are promising compounds that could be used for the development of schistosomicidal and trypanocidal agents.

Asunto(s)

Lignanos/farmacología , Schistosoma mansoni/efectos de los fármacos , Esquistosomicidas/química , Tripanocidas/química , Trypanosoma cruzi/efectos de los fármacos , Animales , Chlorocebus aethiops , Cromatografía Líquida de Alta Presión/métodos , Femenino , Concentración 50 Inhibidora , Lignanos/química , Masculino , Ratones , Ratones Endogámicos BALB C , Estructura Molecular , Acoplamiento Oxidativo , Esquistosomicidas/farmacología , Relación Estructura-Actividad , Tripanocidas/farmacología , Células Vero

RESUMEN

The dibenzylbutyrolactolic lignan (-)-cubebin was isolated from dry seeds of Piper cubeba L. (Piperaceae). (-)-Cubebin possesses anti-inflammatory, analgesic and antimicrobial activities. Doxorubicin (DXR) is a topoisomerase-interactive agent that may induce single- and double-strand breaks, intercalate into the DNA and generate oxygen free radicals. Here, we examine the mutagenicity and recombinogenicity of different concentrations of (-)-cubebin alone or in combination with DXR using standard (ST) and high bioactivation (HB) crosses of the wing Somatic Mutation And Recombination Test in Drosophila melanogaster. The results from both crosses were rather similar. (-)-Cubebin alone did not induce mutation or recombination. At lower concentrations, (-)-cubebin statistically reduced the frequencies of DXR-induced mutant spots. At higher concentrations, however, (-)-cubebin was found to potentiate the effects of DXR, leading to either an increase in the production of mutant spots or a reduction, due to toxicity. These results suggest that depending on the concentration, (-)-cubebin may interact with the enzymatic system that catalyzes the metabolic detoxification of DXR, inhibiting the activity of mitochondrial complex I and thereby scavenging free radicals. Recombination was found to be the major effect of the treatments with DXR alone. The combined treatments reduced DXR mutagenicity but did not affect DXR recombinogenicity.

Asunto(s)

Antimutagênicos/farmacología , Doxorrubicina/toxicidad , Furanos/farmacología , Lignanos/farmacología , Mutágenos/toxicidad , Recombinación Genética/efectos de los fármacos , Alas de Animales/efectos de los fármacos , Animales , Drosophila melanogaster/genética , Interacciones Farmacológicas , Femenino , Larva/efectos de los fármacos , Masculino , Pruebas de Mutagenicidad , Piper/química , Extractos Vegetales/farmacología , Alas de Animales/citología

RESUMEN

The reactive oxygen species (ROS) produced by neutrophils are involved in the pathogenesis of several diseases, for which the intake of antioxidants could benefit patients either as a prophylactic or therapeutic treatment. Propolis is among the known antioxidants, and its chemical composition may vary under the influence of seasonality, which may interfere in its biological properties. This work evaluates the role of seasonality on the production of some important compounds of propolis samples produced monthly from November 2001 through October 2002 as well as the effect of these samples on the oxidative metabolism of stimulated neutrophils, by using both luminol and lucigenin to produce chemiluminescence (CLlum and CLluc, respectively). The cytotoxicity of the most active extracts to neutrophils was also investigated. The inhibitory effect of the propolis samples varied significantly during the studied period for both assays (3.4 ± 1.1 to 16.0 ± 1.1 µg/mL for CLlum and 6.2 ± 2.0 to 30.0 ± 5.0 µg/mL for CLluc), which was also observed in the quantitative profile of the main analyzed compounds (aromadendrin-4'-methyl ether, artepillin C, and baccharin). This effect started to become more prominent during the fall and, among all the studied extracts, the one obtained in May displayed the highest inhibitory effect on CL production (3.4 ± 1.1 µg/mL for CLlum and 6.2 ± 2.0 µg/mL for CLluc). The HPLC qualitative profiles of the extracts of propolis samples were quite similar, but there was a huge variation in terms of quantitative profile. It seems that aromadendrin-4'-methyl ether and baccharin play an essential role in the antioxidant activity, while artepillin C is not very important for this effect. The extracts presenting the highest antioxidant activity were produced in May, June, and August, and they did not display cytotoxicity at 25 µg/mL; quercetin, used as control, was not toxic to neutrophils at 8.5 µg/mL.

Asunto(s)

Neutrófilos/metabolismo , Própolis/farmacología , Animales , Baccharis/química , Baccharis/metabolismo , Abejas , Brasil , Células Cultivadas , Relación Dosis-Respuesta a Droga , Femenino , Própolis/química , Conejos , Estaciones del Año , Zimosan

RESUMEN

Baccharis dracunculifolia is the most important vegetal source of propolis in southeast Brazil, and researchers have been investigating its biological properties. Propolis is a complex resinous hive product collected by bees from several plants, showing a very complex chemical composition. It has been employed since ancient times due to its therapeutic properties, such as antimicrobial, anti-inflammatory, antioxidant, immunomodulatory and antitumour activities, among others. The goal of this work was to compare the cytotoxic action of B. dracunculifolia, propolis and two isolated compounds (caffeic and cinnamic acids) on human laryngeal epidermoid carcinoma (HEp-2) cells in vitro. These cells were incubated with different concentrations of each variable, and cell viability was assessed by the crystal violet method. Lower concentrations of B. dracunculifolia (extract and essential oil), propolis, as well as caffeic and cinnamic acids, showed no cytotoxic activity against HEp-2 cells. On the other hand, elevated concentrations (50 and 100 µg per 100 µL) exerted a cytotoxic action, and propolis showed a more efficient action than its vegetal source and isolated compounds. Further investigation is still needed in order to explore the potential of these variables as antitumour agents and to understand their mechanisms of action.

Asunto(s)

Baccharis/química , Aceites Volátiles/toxicidad , Extractos Vegetales/toxicidad , Hojas de la Planta/química , Própolis/toxicidad , Brasil , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Violeta de Genciana , Humanos , Técnicas In Vitro , Aceites Volátiles/análisis , Extractos Vegetales/análisis , Própolis/análisis , Estadísticas no Paramétricas

RESUMEN

The genotoxic effect of the Austroplenckia populnea chloroform fraction from barkwood extract was tested in vivo on peripheral blood cells of Swiss mice with the comet assay (SCGE), and the clastogenic effect was investigated on peripheral blood cells of Swiss mice and bone marrow cells of Wistar rats, with the micronucleus and chromosome aberrations tests. The animals were treated by gavage with 3 concentrations of the extract: 300, 600 and 900 mg.kg-1. Peripheral blood cells of Swiss mice were collected 4 and 24 hours after the treatment to the SCGE assay and 48 and 72 hours to the micronucleus test. Bone marrow cells of Wistar rats were collected 24 hours after the treatment to the micronucleus and chromosome aberration tests. The results showed that the A. populnea chloroform fraction induced an increase in the average number of DNA damage in peripheral blood cells at the three concentrations tested, but this increase was not statistically significant. In the micronucleus and chromosome aberrations test, no significant increase was observed in the mean number of micronucleated polychromatic erythrocytes (MNPCE) of Swiss mice or MNPCE or chromosome aberrations for the rat bone marrow cells, for any of the tested doses. Our findings enable us to conclude that by the comet assay, A. populnea chloroform fraction from barkwood extract showed no genotoxic effects, and by the micronucleus and chromosome aberration tests, the extract fraction showed no clastogenic/aneugenic effects on the rodent cells tested.

Asunto(s)

Celastraceae/química , Cloroformo/toxicidad , Extractos Vegetales/toxicidad , Animales , Células Cultivadas , Cloroformo/aislamiento & purificación , Relación Dosis-Respuesta a Droga , Ratones , Pruebas de Mutagenicidad/métodos , Extractos Vegetales/aislamiento & purificación , Ratas , Ratas Wistar

RESUMEN

Cymbopogon citratus has been widely recognised for its ethnobotanical and medicinal usefulness. Its insecticidal, antimicrobial and therapeutic properties have been reported, but little is known about its effect on the immune system. This work aimed to investigate the in vivo effect of a water extract of lemongrass on pro-inflammatory cytokine (IL-1beta and IL-6) production by macrophages of BALB/c mice. The action of lemongrass essential oil on cytokine production by macrophages was also analysed in vitro. The chemical composition of the extract and the oil was also investigated. Treatment of mice with water extract of lemongrass inhibited macrophages to produce IL-1beta but induced IL-6 production by these cells. Lemongrass essential oil inhibited the cytokine production in vitro. Linalool oxide and epoxy-linalool oxide were found to be the major components of lemongrass water extract, and neral and geranial were the major compounds of its essential oil. Taken together, these data suggest an anti-inflammatory action of this natural product.

Asunto(s)

Antiinflamatorios/farmacología , Cymbopogon/química , Regulación de la Expresión Génica/efectos de los fármacos , Interleucina-1beta/metabolismo , Interleucina-6/metabolismo , Macrófagos Peritoneales/efectos de los fármacos , Extractos Vegetales/farmacología , Animales , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Células Cultivadas , Cromatografía de Gases , Ensayo de Inmunoadsorción Enzimática , Macrófagos Peritoneales/metabolismo , Masculino , Ratones , Ratones Endogámicos BALB C , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación

RESUMEN

Baccharis dracunculifolia (Asteraceae), the most important plant source of the Brazilian green propolis (GPE), displayed in vitro activity against Leishmania donovani, with an IC(50) value of 45 microg/mL, while GPE presented an IC(50) value of 49 microg/mL. Among the isolated compounds of B. dracunculifolia, ursolic acid, and hautriwaic acid lactone showed IC(50) values of 3.7 microg/mL and 7.0 microg/mL, respectively. Uvaol, acacetin, and ermanin displayed moderate antileishmanial activity. Regarding the antiplasmodial assay against Plasmodium falciparum, BdE and GPE gave similar IC(50) values (about 20 microg/mL), while Hautriwaic acid lactone led to an IC(50) value of 0.8 microg/mL (D6 clone).

Asunto(s)

Antimaláricos/farmacología , Baccharis/química , Fenoles/farmacología , Extractos Vegetales/farmacología , Triterpenos/farmacología , Tripanocidas/farmacología , Animales , Antimaláricos/efectos adversos , Antimaláricos/aislamiento & purificación , Chlorocebus aethiops , Leishmania donovani/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Pruebas de Sensibilidad Parasitaria , Fenoles/efectos adversos , Fenoles/aislamiento & purificación , Extractos Vegetales/efectos adversos , Extractos Vegetales/química , Hojas de la Planta , Plasmodium falciparum/efectos de los fármacos , Própolis , Triterpenos/efectos adversos , Triterpenos/aislamiento & purificación , Tripanocidas/efectos adversos , Tripanocidas/aislamiento & purificación , Células Vero

RESUMEN

We examined the antibacterial activities of several types of propolis, including Africanized honey bee green propolis and propolis produced by meliponini bees. The antibacterial activity of green propolis against Micrococcus luteus and Staphylococcus aureus was superior to that of Melipona quadrifasciata and Scaptotrigona sp propolis. Only two samples of propolis (green propolis and Scaptotrigona sp propolis) were efficient against Escherichia coli. Melipona quadrifasciata propolis was better than green propolis and Scaptotrigona sp propolis against Pseudomonas aeruginosa. We concluded that these resins have potential for human and veterinary medicine.

Asunto(s)

Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Abejas/química , Própolis/farmacología , Animales , Escherichia coli/efectos de los fármacos , Pseudomonas aeruginosa/efectos de los fármacos

RESUMEN

AIMS: The aim of this work was to evaluate the antiviral activities of Baccharis dracunculifolia (extract and essential oil), propolis and some isolated compounds (caffeic and cinnamic acids) against poliovirus type 1 (PV1) replication in HEp-2 cells. METHOD: Three different protocols (pre-, simultaneous and post-treatments) were used to verify the effect of addition time of the variables on PV1 replication by crystal violet method and relative viral RNA quantification by real-time PCR for analysing in which step of virus replication the variables could interfere. CONCLUSIONS: Data revealed that the B. dracunculifolia showed the best antiviral activity percentage in the simultaneous treatment, as well as lower relative viral quantification by real-time PCR. Variables might block partially the viral entry within cells, affect the steps of viral cycle replication into cells, or lead to RNA degradation before the virus entry into cells or after their release to the supernatant. SIGNIFICANCE AND IMPACT OF THE STUDY: Baccharis dracunculifolia is the most important botanical source of the south-eastern Brazilian propolis, and its potential for the development of new phytotherapeutic medicines has been investigated. Propolis is commonly used for its antimicrobial and immunomodulatory activities. Nevertheless, B. dracunculifolia and propolis effects on PV1 have not been investigated yet.

Asunto(s)

Antivirales/farmacología , Baccharis/química , Poliovirus/efectos de los fármacos , Poliovirus/crecimiento & desarrollo , Própolis/farmacología , Baccharis/fisiología , Línea Celular Tumoral/virología , Supervivencia Celular , Violeta de Genciana , Humanos , Extractos Vegetales/farmacología , Aceites de Plantas/farmacología , Reacción en Cadena de la Polimerasa/métodos , ARN Viral/análisis

RESUMEN

Biological properties of clove have been reported, but little is known about its effect on the immune system. This work was aimed to investigate the effect in vivo of a water-soluble part of hydroalcoholic extract of clove on pro-inflammatory cytokines (IL-1beta and IL-6) production by macrophages of BALB/c mice. The action of the essential oil of clove on the production of these cytokines macrophages was also investigated in vitro. The chemical compositions of the extract and of the oil were also investigated. Treatment of mice with water extract of clove was found to inhibit macrophages to produce both IL-1beta and IL-6. The essential oil of clove also inhibited the production of these cytokines in vitro. Eugenol was found to be the major component of the clove extract and essential oil, and probably is the causative agent of cytokine inhibition. Taken together, these data suggest an anti-inflammatory action of this spice.

Asunto(s)

Citocinas/metabolismo , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Extractos Vegetales/farmacología , Syzygium/química , Animales , Células Cultivadas , Ensayo de Inmunoadsorción Enzimática , Eugenol/química , Eugenol/farmacología , Interleucina-1beta/metabolismo , Interleucina-6/metabolismo , Lipopolisacáridos/farmacología , Masculino , Ratones , Ratones Endogámicos BALB C , Aceites Volátiles/química , Aceites Volátiles/farmacología , Extractos Vegetales/química

RESUMEN

The trypanocidal activity of racemic mixtures of cis- and trans-methylpluviatolides was evaluated in vitro against trypomastigote forms of two strains of Trypanosoma cruzi, and in the enzymatic assay of T. cruzi gGAPDH. The cytotoxicity of the compounds was assessed by the MTT method using LLC-MK2 cells. The effect of the compounds on peroxide and NO production were also investigated. The mixture of the trans stereoisomers displayed trypanocidal activity (IC50 approximately 89.3 microM). Therefore, it was separated by chiral HPLC, furnishing the (+) and (-)-enantiomers. Only the (-)-enantiomer was active against the parasite (IC50 approximately 18.7 microM). Despite being inactive, the (+)-enantiomer acted as an antagonistic competitor. Trans-methylpluviatolide displayed low toxicity for LLC-MK2 cells, with an IC50 of 6.53 mM. Furthermore, methylpluviatolide neither inhibited gGAPDH activity nor hindered peroxide and NO production at the evaluated concentrations.

Asunto(s)

Lactonas/química , Lactonas/farmacología , Lignanos/química , Lignanos/farmacología , Tripanocidas/química , Tripanocidas/farmacología , Trypanosoma cruzi/efectos de los fármacos , Animales , Línea Celular , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Ratones , Estructura Molecular , Óxido Nítrico/biosíntesis , Relación Estructura-Actividad

RESUMEN

The effect of spray drying conditions on the chemical composition of Brazilian green propolis extract was investigated using a factorial design and high performance liquid chromatography. The raw and dried extract contents of caffeic acid, p-coumaric acid, drupanin, isosakuranetin, artepillin C, baccharin and 2,2-dimethyl-6-carboxyethenyl-2H-1-benzopyran were quantified using veratraldehyde (3,4-dimethoxybenzaldehyde) as internal standard. The baccharin content in spray-dried propolis was affected by the drying temperature with a 5% significance level, while the coumaric acid and drupanin contents were dependent on drying temperature at a 15% significance level. The other chemical markers, caffeic acid, isosakuranetin, artepillin C and 2,2-dimethyl-6-carboxyethenyl-2H-1-benzopyran, showed to be independent of drying conditions. However, all the chemical markers showed some loss on drying, which varied from 30 to 50%. The results showed that prenylated compounds are sensitive to drying, but their losses may be considerably reduced under low temperatures, around 40 degrees C. The antioxidant activity of the spray dried propolis was determined by the diphenylpicrylhydrazyl (DPPH) method and showed a quadratic dependency on the temperature; extract feed rate and the interaction between them. However, spray dried propolis extracts presented antioxidant activities similar to the original propolis tincturae.

Asunto(s)

Antioxidantes/análisis , Própolis/análisis , Algoritmos , Antioxidantes/química , Compuestos de Bifenilo , Cromatografía Líquida de Alta Presión , Desecación , Etanol , Picratos/química , Própolis/química , Estándares de Referencia , Solventes , Temperatura