Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 1.017
Filtrar
1.
Viruses ; 13(2)2021 02 20.
Artículo en Inglés | MEDLINE | ID: mdl-33672561

RESUMEN

In the face of new emerging respiratory viruses, such as SARS-CoV2, vaccines and drug therapies are not immediately available to curb the spread of infection. Non-pharmaceutical interventions, such as mask-wearing and social distance, can slow the transmission. However, both mask and social distance have not prevented the spread of respiratory viruses SARS-CoV2 within the US. There is an urgent need to develop an intervention that could reduce the spread of respiratory viruses. The key to preventing transmission is to eliminate the emission of SARS-CoV2 from an infected person and stop the virus from propagating in the human population. Rhamnolipids are environmentally friendly surfactants that are less toxic than the synthetic surfactants. In this study, rhamnolipid products, 222B, were investigated as disinfectants against enveloped viruses, such as bovine coronavirus and herpes simplex virus 1 (HSV-1). The 222B at 0.009% and 0.0045% completely inactivated 6 and 4 log PFU/mL of HSV-1 in 5-10 min, respectively. 222B at or below 0.005% is also biologically safe. Moreover, 50 µL of 222B at 0.005% on ~1 cm2 mask fabrics or plastic surface can inactivate ~103 PFU HSV-1 in 3-5 min. These results suggest that 222B coated on masks or plastic surface can reduce the emission of SARS-CoV2 from an infected person and stop the spread of SARS-CoV2.


Asunto(s)
Coronavirus Bovino/efectos de los fármacos , Desinfectantes/farmacología , Glucolípidos/farmacología , Herpesvirus Humano 1/efectos de los fármacos , Tensoactivos/farmacología , /prevención & control , Humanos
2.
Curr Microbiol ; 78(5): 1813-1822, 2021 May.
Artículo en Inglés | MEDLINE | ID: mdl-33772618

RESUMEN

In the present investigation, we have evaluated the antibiofilm potential of Bacillus licheniformis SV1 derived glycolipid against C. glabrata biofilm. Impact of isolated glycolipid on the viability of C. glabrata and on inhibiting as well as eradicating ability of its biofilm were studied. Further, morphological alterations, reactive oxygen species generation (ROS) production and transcriptional expression of selected genes (RT-PCR) of C. glabrata in response with isolated glycolipid were studied. The isolated glycolipid (1.0 mg ml-1) inhibited and eradicated C. glabrata biofilm approximately 80% and 60%, respectively. FE-SEM images revealed glycolipid exposure results in architectural alteration and eradication of C. glabrata biofilm and ROS generation. Transcriptional studies of selected genes showed that the expression of AUS1, FKS1 and KRE1 were down-regulated, while that of ergosterol biosynthesis pathway and multidrug transporter increased, in the presence of glycolipid.


Asunto(s)
Bacillus licheniformis , Candida glabrata , Antifúngicos , Biopelículas , Candida glabrata/genética , Glucolípidos/farmacología
3.
Int J Mol Sci ; 22(3)2021 Feb 02.
Artículo en Inglés | MEDLINE | ID: mdl-33540826

RESUMEN

Toll-like receptors (TLRs) are key receptors through which infectious and non-infectious challenges act with consequent activation of the inflammatory cascade that plays a critical function in various acute and chronic diseases, behaving as amplification and chronicization factors of the inflammatory response. Previous studies have shown that synthetic analogues of lipid A based on glucosamine with few chains of unsaturated and saturated fatty acids, bind MD-2 and inhibit TLR4 receptors. These synthetic compounds showed antagonistic activity against TLR4 activation in vitro by LPS, but little or no activity in vivo. This study aimed to show the potential use of N-palmitoyl-D-glucosamine (PGA), a bacterial molecule with structural similarity to the lipid A component of LPS, which could be useful for preventing LPS-induced tissue damage or even peripheral neuropathies. Molecular docking and molecular dynamics simulations showed that PGA stably binds MD-2 with a MD-2/(PGA)3 stoichiometry. Treatment with PGA resulted in the following effects: (i) it prevented the NF-kB activation in LPS stimulated RAW264.7 cells; (ii) it decreased LPS-induced keratitis and corneal pro-inflammatory cytokines, whilst increasing anti-inflammatory cytokines; (iii) it normalized LPS-induced miR-20a-5p and miR-106a-5p upregulation and increased miR-27a-3p levels in the inflamed corneas; (iv) it decreased allodynia in peripheral neuropathy induced by oxaliplatin or formalin, but not following spared nerve injury of the sciatic nerve (SNI); (v) it prevented the formalin- or oxaliplatin-induced myelino-axonal degeneration of sciatic nerve. SIGNIFICANCE STATEMENT We report that PGA acts as a TLR4 antagonist and this may be the basis of its potent anti-inflammatory activity. Being unique because of its potency and stability, as compared to other similar congeners, PGA can represent a tool for the optimization of new TLR4 modulating drugs directed against the cytokine storm and the chronization of inflammation.


Asunto(s)
Analgésicos/uso terapéutico , Antiinflamatorios/uso terapéutico , Glucolípidos/uso terapéutico , Hiperalgesia/prevención & control , Queratitis/tratamiento farmacológico , Neuralgia/tratamiento farmacológico , Receptor Toll-Like 4/antagonistas & inhibidores , Analgésicos/farmacología , Animales , Antiinflamatorios/farmacología , Señalización del Calcio/efectos de los fármacos , Citocinas/metabolismo , Evaluación Preclínica de Medicamentos , Glucolípidos/farmacología , Células HEK293 , Humanos , Hiperalgesia/etiología , Queratitis/inducido químicamente , Queratitis/patología , Lipopolisacáridos/toxicidad , Antígeno 96 de los Linfocitos/metabolismo , Masculino , Ratones , MicroARNs/genética , Modelos Moleculares , Nociceptores/efectos de los fármacos , Nociceptores/fisiología , Conformación Proteica , Células RAW 264.7 , Distribución Aleatoria , Nervio Ciático/lesiones , Canal Catiónico TRPA1/metabolismo
4.
J Dairy Sci ; 104(4): 4002-4011, 2021 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-33589263

RESUMEN

The growth of psychrotolerant aerobic spore-forming bacteria during refrigerated storage often results in the spoilage of fluid milk, leading to off-flavors and curdling. Because of their low toxicity, biodegradability, selectivity, and antimicrobial activity over a range of conditions, glycolipids are a novel and promising intervention to control undesirable microbes. The objective of this study was to determine the efficacy of a commercial glycolipid product to inhibit spore germination, spore outgrowth, and the growth of vegetative cells of Paenibacillus odorifer, Bacillus weihenstephanensis, and Viridibacillus arenosi, which are the predominant spore-forming spoilage bacteria in milk. For spore germination and outgrowth assays, varying concentrations (25-400 mg/L) of the glycolipid product were added to commercial UHT whole and skim milk inoculated with ∼4 log10 spores/mL of each bacteria and incubated at 30°C for 5 d. Inhibition of spore germination in inoculated UHT whole milk was only observed for V. arenosi, and only when glycolipid was added at 400 mg/L. However, concentrations of 400 and 200 mg/L markedly inhibited the outgrowth of vegetative cells from spores of P. odorifer and B. weihenstephanensis, respectively. No inhibition of spore germination or outgrowth was observed in inoculated UHT skim milk for any strain at the concentrations tested (25 and 50 mg/L). The effect of glycolipid addition on vegetative cell growth in UHT whole and skim milk when inoculated with ∼4 log10 cfu/mL of each bacteria was also determined over 21 d of storage at 7°C. Glycolipid addition at 50 mg/L was bactericidal against P. odorifer and B. weihenstephanensis in inoculated UHT skim milk through 21 d of storage, whereas 100 mg/L was needed for similar control of V. arenosi. Concentrations of 100 and 200 mg/L inhibited the growth of vegetative cells of B. weihenstephanensis and P. odorifer, respectively, in inoculated UHT whole milk, whereas 200 mg/L was also bactericidal to B. weihenstephanensis. Additional studies are necessary to identify effective concentrations for the inhibition of Viridibacillus spp. growth in whole milk beyond 7 d. Findings from this study demonstrate that natural glycolipids have the potential to inhibit the growth of dairy-spoilage bacteria and extend the shelf life of milk.


Asunto(s)
Antiinfecciosos , Leche , Animales , Antiinfecciosos/farmacología , Glucolípidos/farmacología , Paenibacillus , Planococcaceae , Esporas , Esporas Bacterianas
5.
Carbohydr Polym ; 254: 117433, 2021 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-33357906

RESUMEN

Driven by the need to find alternatives to control Staphylococcus aureus infections, this work describes the development of chitosan-based particulate systems as carriers for antimicrobial glycolipids. By using a simple ionic gelation method stable nanoparticles were obtained showing an encapsulation efficiency of 41.1 ± 8.8 % and 74.2 ± 1.3 % and an average size of 210.0 ± 15.7 nm and 329.6 ± 8.0 nm for sophorolipids and rhamnolipids chitosan-nanoparticles, respectively. Glycolipids incorporation and particle size was correspondingly corroborated by FTIR-ATR and TEM analysis. Rhamnolipids chitosan nanoparticles (RLs-CSp) presented the highest antimicrobial effect towards S. aureus (ATCC 25923) exhibiting a minimal inhibitory concentration of 130 µg/mL and a biofilm inhibition ability of 99 %. Additionally, RLs-CSp did not interfere with human dermal fibroblasts (AG22719) viability and proliferation under the tested conditions. The results revealed that the RLs-CSp were able to inhibit bacterial growth showing adequate cytocompatibility and might become, after additional studies, a valuable approach to prevent S. aureus related infections.


Asunto(s)
Antibacterianos/química , Quitosano/química , Portadores de Fármacos , Glucolípidos/química , Ácidos Oléicos/química , Staphylococcus aureus/efectos de los fármacos , Tensoactivos/química , Antibacterianos/aislamiento & purificación , Antibacterianos/farmacología , Biopelículas/efectos de los fármacos , Biopelículas/crecimiento & desarrollo , Ciclo Celular/efectos de los fármacos , Línea Celular , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Fibroblastos/citología , Fibroblastos/efectos de los fármacos , Glucolípidos/aislamiento & purificación , Glucolípidos/farmacología , Humanos , Pruebas de Sensibilidad Microbiana , Nanopartículas/química , Nanopartículas/ultraestructura , Ácidos Oléicos/aislamiento & purificación , Ácidos Oléicos/farmacología , Tamaño de la Partícula , Staphylococcus aureus/crecimiento & desarrollo , Tensoactivos/aislamiento & purificación , Tensoactivos/farmacología
6.
Molecules ; 26(1)2020 Dec 23.
Artículo en Inglés | MEDLINE | ID: mdl-33374771

RESUMEN

The hemibiotrophic fungus Zymoseptoria tritici, responsible for Septoria tritici blotch, is currently the most devastating foliar disease on wheat crops worldwide. Here, we explored, for the first time, the ability of rhamnolipids (RLs) to control this pathogen, using a total of 19 RLs, including a natural RL mixture produced by Pseudomonas aeruginosa and 18 bioinspired RLs synthesized using green chemistry, as well as two related compounds (lauric acid and dodecanol). These compounds were assessed for in vitro antifungal effect, in planta defence elicitation (peroxidase and catalase enzyme activities), and protection efficacy on the wheat-Z. tritici pathosystem. Interestingly, a structure-activity relationship analysis revealed that synthetic RLs with a 12 carbon fatty acid tail were the most effective for all examined biological activities. This highlights the importance of the C12 chain in the bioactivity of RLs, likely by acting on the plasma membranes of both wheat and Z. tritici cells. The efficacy of the most active compound Rh-Est-C12 was 20-fold lower in planta than in vitro; an optimization of the formulation is thus required to increase its effectiveness. No Z. tritici strain-dependent activity was scored for Rh-Est-C12 that exhibited similar antifungal activity levels towards strains differing in their resistance patterns to demethylation inhibitor fungicides, including multi-drug resistance strains. This study reports new insights into the use of bio-inspired RLs to control Z. tritici.


Asunto(s)
Ascomicetos/efectos de los fármacos , Glucolípidos/química , Glucolípidos/farmacología , Plaguicidas/farmacología , Enfermedades de las Plantas/prevención & control , Hojas de la Planta/efectos de los fármacos , Triticum/efectos de los fármacos , Ascomicetos/patogenicidad , Enfermedades de las Plantas/microbiología , Hojas de la Planta/microbiología , Triticum/microbiología
7.
J Agric Food Chem ; 68(52): 15478-15489, 2020 Dec 30.
Artículo en Inglés | MEDLINE | ID: mdl-33319980

RESUMEN

Rhamnolipid is the main group of biosurfactants predominantly produced by Pseudomonas aeruginosa, a ubiquitous and opportunistic pathogen, which limits its large-scale exploitation. Thus, cost-effective rhamnolipid production from a newly isolated nonpathogenic Enterobacter sp. UJS-RC was investigated. The highest rhamnolipid production (4.4 ± 0.2 g/L) was achieved in a medium constituting agroindustrial wastes (sugarcane molasses and corn steep liquor) as substrates. Rhamnolipid exhibited reduced surface tension to 72-28 mN/m with an emulsification index of 75%. The structural analyses demonstrated the presence of methoxyl, carboxyl, and hydroxyl groups in rhamnolipid. Mass spectra indicated eight rhamnolipid congeners, where dirhamnolipid (m/z 650.01) was the dominant congener. Rhamnolipid inhibited biofilm formation of Staphylococcus aureus in a dose-dependent manner, supported by scanning electron microscopy disclosing the disruption of the microcolony/exopolysaccharide matrix. Rhamnolipid's ability to generate reactive oxygen species has thrown light on the mechanism through which the killing of test bacteria may occur.


Asunto(s)
Biopelículas/efectos de los fármacos , Enterobacter/metabolismo , Glucolípidos/metabolismo , Glucolípidos/farmacología , Staphylococcus aureus/efectos de los fármacos , Tensoactivos/metabolismo , Agricultura , Biotransformación , Enterobacter/química , Glucolípidos/química , Melaza/análisis , Saccharum/metabolismo , Saccharum/microbiología , Staphylococcus aureus/fisiología , Tensoactivos/química , Residuos/análisis , Microbiología del Agua , Zea mays/metabolismo , Zea mays/microbiología
8.
Anim Sci J ; 91(1): e13464, 2020 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-33021004

RESUMEN

Methyl-mannosylerythritol lipid (MEL), a new sugar esterified lipid synthesized by Pseudozyma aphidis, was assessed for its functionality in modulating rumen fermentation and microbiota toward more propionate and less methane production. A pure culture study using rumen representatives showed that MEL selectively inhibited the growth of most Gram-positive bacteria including Streptococcus bovis, ruminococci, and Fibrobacter succinogenes, but not Gram-negative bacteria such as Megasphaera elsdenii, Succinivibrio dextrinosolvens, and Selenomonas ruminantium. A batch culture study revealed that MEL significantly decreased methane production in a dose-dependent manner with accumulation of hydrogen, while propionate production was enhanced. A continuous culture (Rusitec) study confirmed all of these changes. A feeding study revealed that sheep fed a MEL diet showed an increased proportion of propionate, while proportions of acetate and butyrate were decreased without affecting total VFA level. These changes disappeared after cessation of MEL feeding. Based on these results, dietary application of MEL can favorably modify rumen fermentation in terms of the efficiency of dietary energy utilization.


Asunto(s)
Alimentación Animal , Antibacterianos , Dieta/veterinaria , Suplementos Dietéticos , Fermentación/efectos de los fármacos , Glucolípidos/administración & dosificación , Glucolípidos/farmacología , Bacterias Grampositivas/crecimiento & desarrollo , Rumen/metabolismo , Rumen/microbiología , Tensoactivos/farmacología , Animales , Relación Dosis-Respuesta a Droga , Metabolismo Energético , Masculino , Metano/metabolismo , Propionatos/metabolismo , Ovinos
9.
Arch Biochem Biophys ; 691: 108486, 2020 09 30.
Artículo en Inglés | MEDLINE | ID: mdl-32710880

RESUMEN

Nonalcoholic fatty liver disease (NAFLD) is emerging as the most common liver disease in industrialized countries. Because hepatic steatosis is an early pathogenesis of NAFLD, the discovery of food components that could ameliorate hepatic steatosis is of interest. Susabinori (Pyropia yezoensis) is recognized as one of the most delicious edible brown algae, and we prepared lipid component of susabinori (SNL), which is rich in eicosapentaenoic acid (EPA)-containing polar lipids. In this study, we tested whether feeding SNL to db/db mice protects them from developing obesity-induced hepatic steatosis. After four weeks of feeding, hepatomegaly, hepatic steatosis, and hepatic injury were markedly alleviated in SNL-fed db/db mice. These effects were partly attributable to the suppression of activities and mRNA expressions of lipogenic enzymes and enhanced levels of adiponectin due to the SNL diet. Additionally, mRNA expression of monocyte chemoattractant protein-1, an inflammatory chemokine, was markedly suppressed, and the mRNA levels of PPARδ, the anti-inflammatory transcription factor, were strongly enhanced in the livers of db/db mice by the SNL diet. We speculate that the development and progression of obesity-induced hepatic steatosis was prevented by the suppression of chronic inflammation due to the combination of bioactivities of EPA, phospholipids, and glycolipids in the SNL diet.


Asunto(s)
Ácido Eicosapentaenoico/análogos & derivados , Ácido Eicosapentaenoico/farmacología , Enfermedad del Hígado Graso no Alcohólico/prevención & control , Extractos Vegetales/farmacología , Algas Marinas/química , Animales , Quimiocina CCL2/metabolismo , Glucolípidos/farmacología , Hepatomegalia/metabolismo , Hepatomegalia/prevención & control , Lipogénesis/efectos de los fármacos , Hígado/metabolismo , Masculino , Ratones Endogámicos C57BL , Ratones Obesos , Enfermedad del Hígado Graso no Alcohólico/metabolismo , PPAR delta/metabolismo , Fosfolípidos/farmacología , ARN Mensajero/metabolismo , Rhodophyta/química
10.
J Biotechnol ; 313: 1-10, 2020 Apr 10.
Artículo en Inglés | MEDLINE | ID: mdl-32151643

RESUMEN

The endophyte Burkholderia sp. WYAT7 isolated from the medicinal plant Artemisia nilagirica (Clarke) Pamp. was analyzed for its ability to produce biosurfactant. The evaluation of biosurfactant production was conducted using different screening methods which confirmed the presence of biosurfactant in the culture supernatant. CTAB- methylene blue agar plate method was used for the screening of glycolipid biosurfactant production. The biosurfactant produced by the bacteria effectively metabolized hydrocarbons present in the bacterial culture media. Fourier transform infrared spectroscopic (FTIR) analysis of biosurfactant provided the details regarding OH stretching, stretching vibrations of acyl chain, CO stretching, stretching vibrations of ether and vibrations of glycosidic linkages in the biosurfactant. The stretching vibrations of glycosidic linkage in the fingerprint regions of FTIR spectrum (1200 cm-1 to 800 cm-1 regions) confirms that the biosurfactant produced was a glycolipid. The GC-MS analysis confirmed the methyl and ethyl esters of fatty acids. The biosurfactant from the bacteria exhibited antibacterial activity against bacterial pathogens such as Pseudomonas aeruginosa (MTCC 2453), Escherichia coli (MTCC 1610), Salmonella paratyphi and Bacillus subtilis. The glycolipid biosurfactant had antibiofilm activity as evidenced in Staphylococcus aureus (MTCC 1430). All these results indicated the beneficial effect of the biosurfactant in plant-endophyte interactions. The properties exhibited by the biosurfactant suggest that it can be exploited commercially for the production of novel antibiotics.


Asunto(s)
Antibacterianos/química , Artemisia/microbiología , Biopelículas/efectos de los fármacos , Burkholderia/química , Glucolípidos/química , Tensoactivos/química , Antibacterianos/farmacología , Bacillus subtilis/efectos de los fármacos , Endófitos , Escherichia coli/efectos de los fármacos , Glucolípidos/farmacología , Hidrocarburos/metabolismo , Pseudomonas aeruginosa/efectos de los fármacos , Espectroscopía Infrarroja por Transformada de Fourier , Staphylococcus aureus/efectos de los fármacos , Tensoactivos/farmacología
11.
J Vasc Surg Venous Lymphat Disord ; 8(2): 268-278, 2020 03.
Artículo en Inglés | MEDLINE | ID: mdl-32067728

RESUMEN

OBJECTIVE: There is an inter-relationship between thrombosis and inflammation. Previously, we have shown the importance of P-selectin in thrombogenesis and thrombus resolution in many preclinical animal models. The role of E-selectin has been explored in rodent models and in a small pilot study of clinical calf vein deep venous thrombosis. The purpose of this study was to determine the role of E-selectin in thrombosis in a primate model of proximal iliac vein thrombosis, a model close to the human condition. METHODS: Iliac vein thrombosis was induced with a well-characterized primate model. Through a transplant incision, the hypogastric vein and iliac vein branches were ligated. Thrombus was induced by balloon occlusion of the proximal and distal iliac vein for 6 hours. The balloons were then deflated, and the primates recovered. Starting on postocclusion day 2, animals were treated with the E-selectin inhibitor GMI-1271, 25 mg/kg subcutaneously, once daily until day 21 (n = 4). Nontreated control animals received no treatment (n = 5). All animals were evaluated by magnetic resonance venography (MRV); evaluation of vessel area by ultrasound, protein analysis, hematology (complete blood count), and coagulation tests (bleeding time, prothrombin time, activated partial thromboplastin time, fibrinogen, and thromboelastography) were performed at baseline, day 2, day 7, day 14, and day 21 with euthanasia. In addition, platelet function and CD44 expression on leukocytes were determined. RESULTS: E-selectin inhibition by GMI-1271 significantly increased vein recanalization by MRV vs control animals on day 14 (P < .05) and day 21 (P < .0001). GMI-1271 significantly decreased vein wall inflammation by MRV with gadolinium vein wall enhancement vs control also on day 14 (P < .0001) and day 21 (P < .0001). The thromboelastographic measure of clot strength (maximum amplitude) showed significant decreases in animals treated with GMI-1271 vs controls at day 2 (P < .05) and day 7 (P < .05). Animals treated with GMI-1271 had significant vessel area increase by day 21 vs controls (P < .05) by ultrasound. Vein wall intimal thickening (P < .001) and intimal fibrosis (P < .05) scores were significantly decreased in GMI-1271-treated animals vs controls. Importantly, no significant differences in hematology or coagulation test results were noted between all groups, suggesting that E-selectin inhibition carries no bleeding potential. GMI-1271 did not affect platelet function or aggregation or CD44 expression on leukocytes. In addition, no episodes of bleeding were noted in either group. CONCLUSIONS: This study suggests that E-selectin modulates venous thrombus progression and that its inhibition will increase thrombus recanalization and decrease vein wall inflammation, without affecting coagulation. The use of an E-selectin inhibitor such as GMI-1271 could potentially change how we treat deep venous thrombosis.


Asunto(s)
Antiinflamatorios/farmacología , Selectina E/antagonistas & inhibidores , Fibrinolíticos/farmacología , Glucolípidos/farmacología , Vena Ilíaca/efectos de los fármacos , Trombosis de la Vena/tratamiento farmacológico , Animales , Modelos Animales de Enfermedad , Selectina E/metabolismo , Vena Ilíaca/diagnóstico por imagen , Vena Ilíaca/metabolismo , Papio , Transducción de Señal , Trombosis de la Vena/diagnóstico por imagen , Trombosis de la Vena/metabolismo
12.
ACS Appl Mater Interfaces ; 12(5): 5488-5499, 2020 Feb 05.
Artículo en Inglés | MEDLINE | ID: mdl-31927982

RESUMEN

Nanomaterials have emerged as antimicrobial agents due to their unique physical and chemical properties. The development of nanoparticles (NPs) composed of natural biopolymers and biosurfactants have sparked interest, as they can be obtained without the use of complex chemical synthesis and toxic materials. In this study, we develop antimicrobial nanoparticles combining the biopolymer chitosan with the biosurfactant rhamnolipid. Addition of rhamnolipid reduced the size and polydispersity index of chitosan nanoparticles showing a more positive surface charge with improved stability, suggesting that chitosan-free amino groups are predominantly present on the surface of nanoparticles. Antimicrobial activity of chitosan/rhamnolipid nanoparticles (C/RL-NPs) against Staphylococcus strains surpassed that of either single rhamnolipid or chitosan, both in planktonic bacteria and biofilms. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of C/RL-NPs were determined considering the concentration of each individual molecule in NPs. MIC values of 14/19 µg mL-1 and MBC of 29/37 µg mL-1 were observed for S. aureus DSM 1104 and MIC and MBC of 29/37 and 58/75 µg mL-1 were observed against S. aureus ATCC 29213, respectively. For S. epidermidis, MIC and MBC of 7/9 and 14/19 µg mL-1 were noticed. Chitosan and chitosan nanoparticles eliminate the bacteria present in the upper parts of biofilms, while C/RL-NPs were more effective, eradicating most sessile bacteria and reducing the number of viable cells below the detection limit, when NPs concentration of 58/75 µg mL-1 was applied for both S. aureus DSM 1104 and S. epidermidis biofilms. The improved antibacterial efficacy of C/RL-NPs was linked to the increased local delivery of chitosan and rhamnolipid at the cell surface and, consequently, to their targets in Gram-positive bacteria. The combination of chitosan and rhamnolipid offers a promising strategy to the design of novel nanoparticles with low cytotoxicity, which can be exploited in pharmaceutical and food industries.


Asunto(s)
Antiinfecciosos , Bacterias/efectos de los fármacos , Quitosano , Glucolípidos , Nanopartículas/química , Antiinfecciosos/química , Antiinfecciosos/farmacología , Biopelículas/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Quitosano/química , Quitosano/farmacología , Glucolípidos/química , Glucolípidos/farmacología , Células Endoteliales de la Vena Umbilical Humana , Humanos , Pruebas de Sensibilidad Microbiana
13.
Appl Microbiol Biotechnol ; 104(6): 2297-2318, 2020 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-31980917

RESUMEN

Mannosylerythritol lipids (MELs) have attracted particular interest of medical, pharmaceutical, and cosmetic fields, due to their specific characteristics, including non-toxicity, easy biodegradability, and environmental compatibility. Therefore, this review aims to highlight recent findings on MEL biological properties, focusing on issues related to therapeutic applications. Among the main findings is that MELs can play a fundamental role due to their antimicrobial properties against several nosocomial pathogen microorganisms. Other remarkable biological properties of MELs are related to skincare, as antiaging (active agent), and in particular on recover of skin cells that were damaged by UV radiation. MEL is also related to the increased efficiency of DNA transfection in liposome systems. Regarding the health field, these glycolipids seem to be associated with disturbance in the membrane composition of cancerous cells, increasing expression of genes responsible for cytoplasmic stress and apoptosis. Moreover, MELs can be associated with nanoparticles, as a capping agent, also acting to increase the solubility and cytotoxicity of them. Furthermore, the differences in the chemical structure of MEL could improve and expand their biochemical diversity and applications. Such modifications could change their interfacial properties and, thus, reduce the surface tension value, enhance the solubility, lower critical micelle concentrations, and form unique self-assembly structures. The latest is closely related to molecular recognition and protein stabilization properties of MEL, that is, essential parameters for their effective cosmetical and pharmaceutical effects. Thus, this current research indicates the huge potential of MEL for use in biomedical formulations, either alone or in combination with other molecules.


Asunto(s)
Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Glucolípidos/química , Glucolípidos/farmacología , Antibacterianos/química , Bacterias/patogenicidad , Cosméticos , Humanos , Micelas , Tensoactivos
14.
Braz. arch. biol. technol ; 63: e20180568, 2020. tab, graf
Artículo en Inglés | LILACS | ID: biblio-1132273

RESUMEN

Abstract Sophorolipids are glycolipids that have natural antimicrobial properties and present great potential in the pharmaceutical field. The present study aimed to produce sophorolipids from Candida bombicola using a chicken fat-based medium and evaluate the antimicrobial activity against Gram-negative (Proteus mirabilis, Escherichia coli, Salmonella enterica subsp. enterica) and Gram-positive bacteria (Enterococcus faecium, Staphylococcus aureus and Streptococcus mutans). The production of sophorolipids reached 27.86 g L-1. Based on the structural characterization, 73.55% of the sophorolipids present a mixture of acidic monoacetylated C18:2 and lactonic diacetylated C16:0, and 26.45% were present in the diacetylated C18:1 lactonic form. Bacteria submitted to sophorolipid exposure showed a reduction in viability at doses of 500 μg mL-1 and 2,000 μg mL-1 against Gram-positive and Gram-negative bacteria, respectively. These results suggest that sophorolipids produced in chicken fat medium may be used as antimicrobial agents to prevent or eliminate contamination by different pathogens.


Asunto(s)
Candida/metabolismo , Glucolípidos/farmacología , Enterococcus faecium/efectos de los fármacos , Bacterias Gramnegativas/efectos de los fármacos , Antibacterianos/farmacología , Proteus mirabilis/efectos de los fármacos , Glucolípidos/aislamiento & purificación , Salmonella enterica/efectos de los fármacos , Escherichia coli/efectos de los fármacos , Antibacterianos/aislamiento & purificación
15.
Cells ; 9(1)2019 Dec 20.
Artículo en Inglés | MEDLINE | ID: mdl-31877673

RESUMEN

Metastatic castration resistant prostate cancer (mCRPC) relapses due to acquired resistance to docetaxel-based chemotherapy and remains a major threat to patient survival. In this report, we tested the effectiveness of a dual CXCR4/E-selectin antagonist, GM-I1359, in vitro and in vivo, as a single agent or in combination with docetaxel (DTX). This agent was compared to the single CXCR4 antagonist, CTCE-9908, and E-selectin antagonist, GMI-1271. Here we demonstrate that CXCR4 antagonism reduced growth and enhanced DTX treatment in PCa cell lines as well as restored DTX effectiveness in DTX-resistant cell models. The efficacy of dual antagonist was higher respect to those observed for single CXCR4 antagonism. GM1359 impacted bone marrow colonization and growth in intraventricular and intratibial cell injection models. The anti-proliferative effects of GMI-1359 and DTX correlated with decreased size, osteolysis and serum levels of both mTRAP and type I collagen fragment (CTX) in intra-osseous tumours suggesting that the dual CXCR4/E-selectin antagonist was a docetaxel-sensitizing agent for bone metastatic growth. Single agent CXCR4 (CTCE-9908) and E-selectin (GMI-1271) antagonists resulted in lower sensitizing effects compared to GMI-1359. These data provide a biologic rationale for the use of a dual E-selectin/CXCR4 inhibitor as an adjuvant to taxane-based chemotherapy in men with mCRPC to prevent and reduce bone metastases.


Asunto(s)
Neoplasias Óseas/tratamiento farmacológico , Neoplasias Óseas/secundario , Docetaxel/administración & dosificación , Neoplasias de la Próstata Resistentes a la Castración/tratamiento farmacológico , Bibliotecas de Moléculas Pequeñas/administración & dosificación , Animales , Neoplasias Óseas/metabolismo , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Docetaxel/farmacología , Sinergismo Farmacológico , Selectina E/antagonistas & inhibidores , Glucolípidos/administración & dosificación , Glucolípidos/farmacología , Humanos , Masculino , Ratones , Células PC-3 , Péptidos/administración & dosificación , Péptidos/farmacología , Neoplasias de la Próstata Resistentes a la Castración/metabolismo , Receptores CXCR4/antagonistas & inhibidores , Bibliotecas de Moléculas Pequeñas/química , Bibliotecas de Moléculas Pequeñas/farmacología , Ensayos Antitumor por Modelo de Xenoinjerto
16.
Sci Rep ; 9(1): 16362, 2019 11 08.
Artículo en Inglés | MEDLINE | ID: mdl-31704965

RESUMEN

The contribution of natural killer (NK) cells to the clearance of hepatic viral infections is well recognized. The recently discovered heterogeneity of NK cell populations renders them interesting targets for immune interventions. Invariant natural killer T (iNKT) cells represent a key interaction partner for hepatic NK cells. The present study addressed whether characteristics of NK cells in the liver can be shaped by targeting iNKT cells. For this, the CD1d-binding pegylated glycolipid αGalCerMPEG was assessed for its ability to modulate the features of NK cells permanently or transiently residing in the liver. In vivo administration resulted in enhanced functionality of educated and highly differentiated CD27+ Mac-1+ NK cells accompanied by an increased proliferation. Improved liver homing was supported by serum-derived and cellular factors. Reduced viral loads in a mCMV infection model confirmed the beneficial effect of NK cells located in the liver upon stimulation with αGalCerMPEG. Thus, targeting iNKT cell-mediated NK cell activation in the liver represents a promising approach for the establishment of liver-directed immune interventions.


Asunto(s)
Infecciones por Citomegalovirus/inmunología , Citomegalovirus/inmunología , Células Asesinas Naturales/inmunología , Hígado/inmunología , Activación de Linfocitos/inmunología , Células T Asesinas Naturales/inmunología , Animales , Antígenos CD1d/metabolismo , Movimiento Celular , Proliferación Celular , Citomegalovirus/efectos de los fármacos , Infecciones por Citomegalovirus/tratamiento farmacológico , Infecciones por Citomegalovirus/virología , Galactosilceramidas/farmacología , Glucolípidos/farmacología , Células Asesinas Naturales/efectos de los fármacos , Células Asesinas Naturales/metabolismo , Hígado/efectos de los fármacos , Hígado/metabolismo , Ratones , Ratones Endogámicos C57BL , Células T Asesinas Naturales/efectos de los fármacos , Células T Asesinas Naturales/metabolismo , Polietilenglicoles/química
17.
J Pediatr ; 215: 24-31.e8, 2019 12.
Artículo en Inglés | MEDLINE | ID: mdl-31668885

RESUMEN

OBJECTIVE: To evaluate neurodevelopment, growth, and health outcomes in infants receiving bovine milk fat globule membrane (MFGM) and lactoferrin in infant formula. STUDY DESIGN: Healthy term infants were randomized to a cow's milk-based infant formula or MFGM + LF (a similar infant formula, with an added source of bovine milk fat globule membrane [bMFGM; whey protein-lipid concentrate, 5 g/L] and bovine lactoferrin [0.6 g/L]) through 365 days of age. The Bayley Scales of Infant Development, 3rd edition cognitive composite score at day 365 was the primary outcome. Secondary outcomes included tolerance measures through day 365, additional neurodevelopmental and language outcomes, growth, and medically confirmed adverse events through day 545. RESULTS: Of 451 infants enrolled (control, 228; MFGM + LF, 223), 291 completed study feeding and Bayley-III testing at day 365 (control, 148; MFGM + LF, 143). The mean cognitive (+8.7), language (+12.3), and motor (+12.6) scores were higher (P < .001) for the MFGM + LF group; no differences were observed at day 545. Global development scores from day 120 to day 275 and attention at day 365 were significantly improved. Few group differences in day 545 neurodevelopmental outcomes were detected, however scores of some subcategories of the MacArthur-Bates Communicative Development Inventories were higher (P < .05) in the MFGM + LF group. The overall incidence of respiratory-associated adverse events and diarrhea were significantly lower for the MFGM + LF group through day 545. CONCLUSIONS: Infants receiving formula with added bovine MFGM and bovine lactoferrin had an accelerated neurodevelopmental profile at day 365 and improved language subcategories at day 545. Formulas were associated with age-appropriate growth and significantly fewer diarrhea and respiratory-associated adverse events through 545 days of age. TRIAL REGISTRATION CLINICALTRIALS.GOV:: NCT02274883.


Asunto(s)
Desarrollo Infantil/fisiología , Cognición/fisiología , Glucolípidos/farmacología , Glicoproteínas/farmacología , Fórmulas Infantiles/química , Lactoferrina/farmacología , Leche , Trastornos del Neurodesarrollo/prevención & control , Animales , Preescolar , Método Doble Ciego , Femenino , Estudios de Seguimiento , Humanos , Lactante , Recién Nacido , Gotas Lipídicas , Masculino , Trastornos del Neurodesarrollo/fisiopatología , Trastornos del Neurodesarrollo/psicología , Pronóstico , Valores de Referencia , Estudios Retrospectivos
18.
J Nutr Sci Vitaminol (Tokyo) ; 65(5): 405-413, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-31666477

RESUMEN

Since the decline of physical performance gradually progresses with aging, continuous exercise with nutritional supplementation from a young age is a feasible and effective way to maintain a comfortable life until late old age. We examined the effects of continuous milk fat globule membrane (MFGM) supplementation combined with voluntary running exercise (VR) for prevention of aging-associated declines in physical performance in naturally aging mice. The MFGM with VR group showed a significantly attenuated age-related decline in motor coordination and suppression of the loss of muscle mass and strength. Compared with the control group, the MFGM with VR group showed significantly higher mRNA and protein expression for docking protein 7, which maintains neuromuscular junction (NMJ) integrity, in the quadriceps muscles. These results suggest that dietary MFGM and VR attenuate natural aging-related decline in motor coordination and muscle function by regulating NMJ integrity.


Asunto(s)
Envejecimiento/efectos de los fármacos , Suplementos Dietéticos , Glucolípidos/farmacología , Glicoproteínas/farmacología , Músculo Esquelético/efectos de los fármacos , Desempeño Psicomotor/efectos de los fármacos , Animales , Gotas Lipídicas , Ratones , Condicionamiento Físico Animal , Rendimiento Físico Funcional , Carrera/fisiología , Fenómenos Fisiológicos en la Nutrición Deportiva/efectos de los fármacos
19.
Int J Biol Macromol ; 140: 156-167, 2019 Nov 01.
Artículo en Inglés | MEDLINE | ID: mdl-31398404

RESUMEN

Presently, through the preliminary screening assays, the Salmonella bongori BH11 was found to be an effective biosurfactants (BSFs) producer. The secreted BSFs were extracted using methanol: chloroform and characterized through FTIR, TLC, HPLC and GCMS analyses. Further, the extracellular protein was extracted (TCA/acetone method), estimated (Lowry's method) and separated (standard and modified SDS-PAGE). Through the obtained characteristic FTIR peaks (1107.09cm-1), its content was presumed to be glycolipids and as rhamnose/rhamnolipids through the TLC-Rf value. GCMS revealed 6 compounds, in which Toluene (32%) and 5-(2-Thienyl) pentanoic acid (23%) are the major ones. The crude BSFs exhibited preponderant antibacterial effects on Staphylococcus aureus and Serratia marcescens. Also, it inhibited the biofilm formation of S. aureus, Pseudomonas aeruginosa, P. fluorescens and S. marcescens. Considerably, 76% mortality of IV instar larvae of Culex quinquefasciatus was recorded from BSFs, when compared to SDS. The presently followed protein separation technique using two petridishes might attract the attention of the researchers, as it would emerge as a standard procedure in future. This is the first report on the screening of BSFs from Salmonella bongori that showed antagonistic property, larvicidal potentials and the presently followed modified SDS-PAGE protein separation technique is a simple, reliable and cost effective one.


Asunto(s)
Antibacterianos , Proteínas Bacterianas , Culex/crecimiento & desarrollo , Glucolípidos , Insecticidas , Salmonella/química , Tensoactivos , Animales , Antibacterianos/química , Antibacterianos/farmacología , Proteínas Bacterianas/química , Proteínas Bacterianas/farmacología , Peces/microbiología , Glucolípidos/química , Glucolípidos/farmacología , Insecticidas/química , Insecticidas/farmacología , Larva/crecimiento & desarrollo , Tensoactivos/química , Tensoactivos/farmacología
20.
Molecules ; 24(16)2019 Aug 08.
Artículo en Inglés | MEDLINE | ID: mdl-31398901

RESUMEN

The unique stereoelectronic properties of sp2-iminosugars enable their participation in glycosylation reactions, thereby behaving as true carbohydrate chemical mimics. Among sp2-iminosugar conjugates, the sp2-iminosugar glycolipids (sp2-IGLs) have shown a variety of interesting pharmacological properties ranging from glycosidase inhibition to antiproliferative, antiparasitic, and anti-inflammatory activities. Developing strategies compatible with molecular diversity-oriented strategies for structure-activity relationship studies was therefore highly wanted. Here we show that a reaction sequence consisting in stereoselective C-allylation followed by thiol-ene "click" coupling provides a very convenient access to α-C-glycoside sp2-IGLs. Both the glycone moiety and the aglycone tail can be modified by using sp2-iminosugar precursors with different configurational profiles (d-gluco or d-galacto in this work) and varied thiols, as well as by oxidation of the sulfide adducts (to the corresponding sulfones in this work). A series of derivatives was prepared in this manner and their glycosidase inhibitory, antiproliferative and antileishmanial activities were evaluated in different settings. The results confirm that the inhibition of glycosidases, particularly α-glucosidase, and the antitumor/leishmanicidal activities are unrelated. The data are also consistent with the two later activities arising from the ability of the sp2-IGLs to interfere in the immune system response in a cell line and cell context dependent manner.


Asunto(s)
Química Clic , Glucolípidos/síntesis química , Glucolípidos/farmacología , Glicósidos/química , Iminoazúcares/química , Compuestos de Sulfhidrilo/química , Antiprotozoarios/síntesis química , Antiprotozoarios/farmacología , Activación Enzimática/efectos de los fármacos , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/farmacología , Glucolípidos/química , Glicósido Hidrolasas/antagonistas & inhibidores , Glicósido Hidrolasas/química , Humanos , Pruebas de Sensibilidad Parasitaria
SELECCIÓN DE REFERENCIAS
DETALLE DE LA BÚSQUEDA
...