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1.
Biomacromolecules ; 25(6): 3432-3448, 2024 Jun 10.
Artículo en Inglés | MEDLINE | ID: mdl-38771294

RESUMEN

Preventing bacterial infections is a crucial aspect of wound healing. There is an urgent need for multifunctional biomaterials without antibiotics to promote wound healing. In this study, we fabricated a guar gum (GG)-based nanocomposite hydrogel, termed GBTF, which exhibited photothermal antibacterial therapy for infected wound healing. The GBTF hydrogel formed a cross-linked network through dynamic borate/diol interactions between GG and borax, thereby exhibiting simultaneously self-healing, adaptable, and injectable properties. Additionally, tannic acid (TA)/Fe3+ nanocomplexes (NCs) were incorporated into the hydrogel to confer photothermal antibacterial properties. Under the irradiation of an 808 nm near-infrared laser, the TA/Fe3+ NCs in the hydrogel could rapidly generate heat, leading to the disruption of bacterial cell membranes and subsequent bacterial eradication. Furthermore, the hydrogels exhibited good cytocompatibility and hemocompatibility, making them a precandidate for preclinical and clinical applications. Finally, they could significantly promote bacteria-infected wound healing by reducing bacterial viability, accelerating collagen deposition, and promoting epithelial remodeling. Therefore, the multifunctional GBTF hydrogel, which was composed entirely of natural substances including guar gum, borax, and polyphenol/ferric ion NCs, showed great potential for regenerating infected skin wounds in clinical applications.


Asunto(s)
Antibacterianos , Galactanos , Hidrogeles , Mananos , Nanocompuestos , Terapia Fototérmica , Gomas de Plantas , Cicatrización de Heridas , Mananos/química , Mananos/farmacología , Gomas de Plantas/química , Gomas de Plantas/farmacología , Galactanos/química , Galactanos/farmacología , Cicatrización de Heridas/efectos de los fármacos , Antibacterianos/farmacología , Antibacterianos/química , Nanocompuestos/química , Hidrogeles/química , Hidrogeles/farmacología , Animales , Terapia Fototérmica/métodos , Ratones , Taninos/química , Taninos/farmacología , Staphylococcus aureus/efectos de los fármacos , Humanos , Escherichia coli/efectos de los fármacos , Boratos
2.
Fish Shellfish Immunol ; 151: 109753, 2024 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-38977111

RESUMEN

Bimetallic (Au/Ag) nanoparticles (BNPs) have shown enhanced antibacterial activity compared to their monometallic counterparts. Sulfated galactans (SG) are a naturally occurring polymer commonly found in red seaweed Gracilaria fisheri. They are biocompatible and biodegradable and environmentally friendly. In this study, we utilized SG in combination with BNPs to develop composite materials that potentially enhance antibacterial activity against shrimp pathogens Vibrio parahaemolyticus and Vibrio harveyi, compared to BNPs or SG alone. BNPs were coated with sulfated galactan (SGBNPs) and characterized using UV-vis spectroscopy, Fourier transform infrared (FTIR) spectroscopy, zeta potential, and transmission electron microscopy (TEM). UV-vis spectroscopy analysis revealed that the surface plasmon peaks of BNPs and SGBNPs appeared at 530 nm and 532 nm, respectively. Zeta potential measurements showed that SGBNPs had a negative charge of -32.4 mV, while the BNPs solution had a positive charge of 38.7 mV. TEM images demonstrated the spherical morphology of both BNPs and SGBNPs with narrow size distributions (3-10 nm). Analysis of the FTIR spectra indicated that SG maintained its backbone structure in SGBNPs, but some functional groups were altered. Notably, SGBNPs showed superior antimicrobial and antibiofilm activities against V. parahaemolyticus and V. harveyi compared to SG and BNPs. Furthermore, treatment with SGBNPs significantly down-regulated the expression of virulence-related genes (toxR, cpsQ, and mfpA) for V. parahaemolyticus 3HP compared to the respective control, bacteria treated with BNPs or SG. Diets supplemented with SGBNPs, BNPs, or SG showed no detrimental impact on the growth of shrimp Penaeus vannamei. Shrimp fed with SGBNPs-supplemented feed showed significantly higher survival rates than those fed with BNPs-supplemented feed when infected with 3HP after being on the supplemented feed for seven days and a subsequent number of fifteen days. These findings collectively demonstrate the benefit of using SG capped Au-Ag BNPs as an antibacterial agent for the prevention and control of Vibrio sp. Infection in shrimp while reducing the risk of environmental contamination.


Asunto(s)
Galactanos , Nanopartículas del Metal , Penaeidae , Vibrio parahaemolyticus , Vibrio , Animales , Vibrio parahaemolyticus/efectos de los fármacos , Vibrio parahaemolyticus/fisiología , Penaeidae/inmunología , Nanopartículas del Metal/química , Galactanos/química , Galactanos/farmacología , Vibrio/efectos de los fármacos , Vibrio/fisiología , Antibacterianos/farmacología , Antibacterianos/química , Plata/farmacología , Plata/química , Oro/química , Oro/farmacología
3.
An Acad Bras Cienc ; 96(3): e20230073, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38896737

RESUMEN

In this study, the Box-Behnken experimental planning was used to optimize the extraction of polysaccharides from the cell wall of Rhizopus microspore var. oligosporus, with analysis of the quantitative effects of parameters pH, temperature and extraction time for polysaccharide yield. The optimal conditions for extraction were determined by the regression equation and evaluation of the response surface graphs, which indicated: pH 13, temperature of 120ºC and time of 60 min, with maximum yield around 18.5%. Fourier transform infrared spectroscopy analysis indicated typical polysaccharide signals. Nuclear magnetic resonance spectroscopy and monosaccharide analysis indicated a ß(1,3) ß(1,6) glucogalactan. The polysaccharide exhibited an average molecular weight of 120 kDa and a polymerization degree of 741. Antioxidant assays in vitro revealed the potential of polysaccharide in elimination of ABTS+ radical and hydroxyl radicals. EC50 values for free radical elimination were 7.69 and 17.8 mg/mL, for ABTS+ and hydroxyls, respectively. The polysaccharides showed potential for α-amylase inhibition with an EC50 of 1.66 mg/mL. The results suggest that ß(1,3) ß(1,6) glucogalactan from Rhizopus microsporus var. oligosporus can be used in biotechnological applications.


Asunto(s)
Antioxidantes , Rhizopus , alfa-Amilasas , Antioxidantes/farmacología , Antioxidantes/aislamiento & purificación , alfa-Amilasas/antagonistas & inhibidores , Espectroscopía Infrarroja por Transformada de Fourier , Galactanos/aislamiento & purificación , Galactanos/farmacología , Galactanos/química , Espectroscopía de Resonancia Magnética , Inhibidores Enzimáticos/farmacología , Inhibidores Enzimáticos/aislamiento & purificación , Concentración de Iones de Hidrógeno
4.
Int J Food Sci Nutr ; 75(5): 518-526, 2024 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-38910266

RESUMEN

Functionally distinct dietary fibre sources may be combined in reformulated foods to restore a natural spectrum of health attributes. Effects of wheat bran (WB), psyllium husk, guar gum and Raftilose™ combinations on hydrated faecal mass (HFM), were determined. A valid rat model was fed diets supplemented with 10% WB, 10% WB with 1-6% psyllium in 1% steps, and 10% WB/5% psyllium with 1-7% guar gum or 1-6% Raftilose in 1% steps. Fully hydrated faecal pellets gave HFM values in the human range, increasing by 2.4 ± 0.29 g per gram of WB ingested, and by 15.6 ± 1.52 g per g of psyllium. Equations for incremental changes in HFM predicted intakes of fibre combinations required for adequate daily HFM, and it is shown how expressing relative effects of foods on HFM as functional equivalents would allow quantitative personalised management of HFM for reduced constipation and colorectal cancer in humans.


Asunto(s)
Fibras de la Dieta , Heces , Galactanos , Mananos , Gomas de Plantas , Psyllium , Fibras de la Dieta/farmacología , Animales , Heces/química , Humanos , Mananos/farmacología , Gomas de Plantas/farmacología , Galactanos/farmacología , Ratas , Psyllium/farmacología , Masculino , Ratas Sprague-Dawley , Estreñimiento/dietoterapia , Modelos Animales
5.
Bull Exp Biol Med ; 177(5): 621-625, 2024 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-39347869

RESUMEN

The hemocompatibility of arabinogalactan, betulin and its derivatives was evaluated in vitro and samples suitable for creation of nanostructures or materials in contact with blood were selected. The prospects of arabinogalactan as a component of the construct (nanostructure) for drug delivery are due to the fact that it did not affect blood/plasma coagulation (at concentrations of 0.0033-3.333 mg/ml and 0.00465-4.65 mg/ml, respectively), platelet aggregation (0.00182-0.182 mg/ml), and demonstrated the degree of erythrocyte hemolysis less than 3%. Sodium salt of betulin monosulfate, diarginine salt of betulin disulfate (up to 0.465 mg/ml), and especially betulin and allobetulin formate with procoagulant properties (degree of hemolysis less than 2%) can be used to create a material, for example, sponge, gel, active against blood coagulation.


Asunto(s)
Coagulación Sanguínea , Galactanos , Hemólisis , Agregación Plaquetaria , Triterpenos , Triterpenos/química , Triterpenos/farmacología , Hemólisis/efectos de los fármacos , Galactanos/química , Galactanos/farmacología , Coagulación Sanguínea/efectos de los fármacos , Agregación Plaquetaria/efectos de los fármacos , Ensayo de Materiales , Humanos , Materiales Biocompatibles/química , Materiales Biocompatibles/farmacología , Eritrocitos/efectos de los fármacos , Animales , Ácido Betulínico
6.
J Biol Chem ; 298(5): 101856, 2022 05.
Artículo en Inglés | MEDLINE | ID: mdl-35337800

RESUMEN

Sulfation pattern and molecular weight (MW) play a key role in the biological actions of sulfated glycans. Besides anticoagulant effects, certain sulfated glycans can also exhibit anti-SARS-CoV-2 properties. To develop a more selective antiviral carbohydrate, an efficient strategy to separate these two actions is required. In this work, low MW fractions derived from the red alga Botryocladia occidentalis sulfated galactan (BoSG) were generated, structurally characterized, and tested for activity against SARS-CoV-2 and blood coagulation. The lowest MW fraction was found to be primarily composed of octasaccharides of monosulfated monosaccharides. Unlike heparin or native BoSG, we found that hydrolyzed BoSG products had weak anticoagulant activities as seen by aPTT and inhibitory assays using purified cofactors. In contrast, lower MW BoSG-derivatives retained anti-SARS-CoV-2 activity using SARS-CoV-2 spike (S)-protein pseudotyped lentivirus vector in HEK-293T-hACE2 cells monitored by GFP. Surface plasmon resonance confirmed that longer chains are necessary for BoSG to interact with coagulation cofactors but is not required for interactions with certain S-protein variants. We observed distinct affinities of BoSG derivatives for the S-proteins of different SARS-CoV-2 strains, including WT, N501Y (Alpha), K417T/E484K/N501Y (Gamma), and L542R (Delta) mutants, and stronger affinity for the N501Y-containing variants. Docking of the four possible monosulfated BoSG disaccharides in interactions with the N501Y mutant S-protein predicted potential binding poses of the BoSG constructs and favorable binding in close proximity to the 501Y residue. Our results demonstrate that depolymerization and fractionation of BoSG are an effective strategy to segregate its anticoagulant property from its anti-SARS-CoV-2 action.


Asunto(s)
Anticoagulantes , Antivirales , Galactanos , Rhodophyta , SARS-CoV-2 , Anticoagulantes/química , Anticoagulantes/farmacología , Antivirales/química , Antivirales/farmacología , COVID-19 , Galactanos/química , Galactanos/farmacología , Células HEK293 , Humanos , Rhodophyta/química , SARS-CoV-2/efectos de los fármacos , Glicoproteína de la Espiga del Coronavirus/química , Sulfatos/química
7.
Br J Nutr ; 129(10): 1703-1713, 2023 05 28.
Artículo en Inglés | MEDLINE | ID: mdl-35837742

RESUMEN

Recent meta-analytic work indicated that guar gum supplementation might improve lipid profile markers in different populations. However, critical methodological limitations such as the use of some unreliable data and the lack of inclusion of several relevant studies, and the scarcity in assessments of regression and dose-specific effects make it difficult to draw meaningful conclusions from the meta-analysis. Therefore, current evidence regarding the effects of guar gum supplementation on lipid profile remains unclear. The present systematic review, meta-regression and dose-response meta-analysis aimed to examine the effects of guar gum supplementation on lipid profile (total cholesterol (TC), LDL, TAG and HDL) in adults. Relevant studies were obtained by searching the PubMed, SCOPUS, Embase and Web of Science databases (from inception to September 2021). Weighted mean differences (WMD) and 95 % CI were estimated via a random-effects model. Heterogeneity, sensitivity analysis and publication bias were reported using standard methods. Pooled analysis of nineteen randomised controlled trials (RCT) revealed that guar gum supplementation led to significant reductions in TC (WMD: -19·34 mg/dl, 95 % CI -26·18, -12·49, P < 0·001) and LDL (WMD: -16·19 mg/dl, 95 % CI -25·54, -6·83, P = 0·001). However, there was no effect on TAG and HDL among adults in comparison with control group. Our outcomes suggest that guar gum supplementation lowers TC and LDL in adults. Future large RCT on various populations are needed to show further beneficial effects of guar gum supplementation on lipid profile and establish guidelines for clinical practice.


Asunto(s)
Suplementos Dietéticos , Lípidos , Galactanos/farmacología , Mananos/farmacología , Ensayos Clínicos Controlados Aleatorios como Asunto
8.
J Sci Food Agric ; 103(10): 5165-5170, 2023 Aug 15.
Artículo en Inglés | MEDLINE | ID: mdl-36914415

RESUMEN

BACKGROUND: The intestinal epithelium acts as a barrier against harmful luminal materials, thus preventing intestinal diseases and maintaining intestinal health. Heat shock protein 27 (HSP27) promotes intestinal epithelial integrity under both physiological and stressed conditions. The effects of partially hydrolyzed guar gum (PHGG) on HSP27 expression in intestinal Caco-2 cells and mouse intestines were investigated. RESULTS: The present study showed that PHGG upregulated HSP27 expression in Caco-2 cells without upregulating Hspb1, the gene encoding HSP27. Feeding PHGG increased HSP25 expression in epithelial cells of the small intestine of mice. Inhibition of protein translation using cycloheximide suppressed PHGG-mediated HSP27 expression, indicating that PHGG upregulated HSP27 via translational modulation. Signaling inhibition of the mechanistic target of rapamycin (mTOR) and phosphatidyl 3-inositol kinase reduced PHGG-mediated HSP27 expression, whereas mitogen-activated protein kinase kinase inhibition by U0126 increased HSP27 expression, irrespective of PHGG administration. PHGG increases mTOR phosphorylation and reduces extracellular signal-regulated protein kinase (ERK) phosphorylation. CONCLUSION: PHGG-mediated translation of HSP27 in intestinal Caco-2 cells and mouse intestine via the mTOR and ERK signaling pathways may promote intestinal epithelial integrity. These findings help us better understand how dietary fibers regulate the physiological function of the intestines. © 2023 Society of Chemical Industry.


Asunto(s)
Proteínas de Choque Térmico HSP27 , Intestinos , Humanos , Ratones , Animales , Células CACO-2 , Proteínas de Choque Térmico HSP27/genética , Galactanos/farmacología , Mananos/farmacología , Gomas de Plantas/farmacología , Serina-Treonina Quinasas TOR/genética
9.
Mar Drugs ; 20(8)2022 Jul 23.
Artículo en Inglés | MEDLINE | ID: mdl-35892937

RESUMEN

Various seaweed sulfated polysaccharides have been explored for antimicrobial application. This study aimed to evaluate the antibacterial activity of the native Gracilaria fisheri sulfated galactans (NSG) and depolymerized fractions against the marine pathogenic bacteria Vibrio parahaemolyticus and Vibrio harveyi. NSG was hydrolyzed in different concentrations of H2O2 to generate sulfated galactans degraded fractions (SGF). The molecular weight, structural characteristics, and physicochemical parameters of both NSG and SGF were determined. The results revealed that the high molecular weight NSG (228.33 kDa) was significantly degraded to SGFs of 115.76, 3.79, and 3.19 kDa by hydrolysis with 0.4, 2, and 10% H2O2, respectively. The Fourier transformed spectroscopy (FTIR) and 1H- and 13C-Nuclear magnetic resonance (NMR) analyses demonstrated that the polysaccharide chain structure of SGFs was not affected by H2O2 degradation, but alterations were detected at the peak positions of some functional groups. In vitro study showed that SGFs significantly exerted a stronger antibacterial activity against V. parahaemolyticus and V. harveyi than NSG, which might be due to the low molecular weight and higher sulfation properties of SGF. SGF disrupted the bacterial cell membrane, resulting in leakage of intracellular biological components, and subsequently, cell death. Taken together, this study provides a basis for the exploitation and utilization of low-molecular-weight sulfated galactans from G. fisheri to prevent and control the shrimp pathogens.


Asunto(s)
Gracilaria , Rhodophyta , Vibrio parahaemolyticus , Antibacterianos/farmacología , Galactanos/química , Galactanos/farmacología , Gracilaria/química , Peróxido de Hidrógeno/farmacología , Polisacáridos/farmacología , Sulfatos , Vibrio
10.
Mol Reprod Dev ; 88(7): 516-524, 2021 07.
Artículo en Inglés | MEDLINE | ID: mdl-34096128

RESUMEN

Xanthan gum (XG) and locust bean gum (LBG) are nontoxic polysaccharides that produce culture substrates. The present study examined the effect of XG-LBG gel on in vitro bovine oocyte growth and gene expression in granulosa cells. Oocytes and granulosa cell complexes (OGCs) were cultured in vitro on plastic culture plate (Plate) or XG-LBG gel for 16 days. OGCs formed a dome-like cavity surrounding the oocytes on plate but formed a spherical follicle structure on XG-LBG gel. The total granulosa cell numbers of the OGCs and their survival rate was greater for OGCs cultured on XG-LBG gel than for those cultured on plate. Oocytes grown on XG-LBG gels had higher lipid and mitochondrial content, as well as a larger diameter, than their plate counterparts. When oocytes grown in vitro were subjected to in vitro maturation and fertilization, the normal fertilization rate was significantly higher for oocytes developed on XG-LBG gel than that of oocytes cultured on the plate counterpart. RNAseq of the granulosa cells revealed that genes associated with focal adhesion, phosphatidylinositol 3'-kinase-Akt and Hippo signaling, and regulation of actin cytoskeleton were upregulated in granulosa cells of OGCs cultured on XG-LBG gel compared with those cultured on plate.


Asunto(s)
Galactanos/farmacología , Células de la Granulosa/efectos de los fármacos , Técnicas de Maduración In Vitro de los Oocitos/métodos , Mananos/farmacología , Oogénesis/efectos de los fármacos , Gomas de Plantas/farmacología , Polisacáridos Bacterianos/farmacología , Animales , Bovinos , Células Cultivadas , Femenino , Galactanos/química , Geles/química , Geles/farmacología , Expresión Génica/efectos de los fármacos , Células de la Granulosa/metabolismo , Técnicas de Maduración In Vitro de los Oocitos/veterinaria , Mananos/química , Oocitos/efectos de los fármacos , Oocitos/fisiología , Oogénesis/genética , Gomas de Plantas/química , Polisacáridos/química , Polisacáridos/farmacología , Polisacáridos Bacterianos/química , Técnicas de Cultivo de Tejidos/métodos , Técnicas de Cultivo de Tejidos/veterinaria , Andamios del Tejido/química
11.
Mar Drugs ; 19(5)2021 Apr 30.
Artículo en Inglés | MEDLINE | ID: mdl-33946151

RESUMEN

Sulfated galactans (SG) isolated from red alga Gracilaria fisheri have been reported to inhibit the growth of cholangiocarcinoma (CCA) cells, which was similar to the epidermal growth factor receptor (EGFR)-targeted drug, cetuximab. Herein, we studied the anti-cancer potency of SG compared to cetuximab. Biological studies demonstrated SG and cetuximab had similar inhibition mechanisms in CCA cells by down-regulating EGFR/ERK pathway, and the combined treatment induced a greater inhibition effect. The molecular docking study revealed that SG binds to the dimerization domain of EGFR, and this was confirmed by dimerization assay, which showed that SG inhibited ligand-induced EGFR dimer formation. Synchrotron FTIR microspectroscopy was employed to examine alterations in cellular macromolecules after drug treatment. The SR-FTIR-MS elicited similar spectral signatures of SG and cetuximab, pointing towards the bands of RNA/DNA, lipids, and amide I vibrations, which were inconsistent with the changes of signaling proteins in CCA cells after drug treatment. Thus, this study demonstrates the underlined anti-cancer mechanism of SG by interfering with EGFR dimerization. In addition, we reveal that FTIR signature spectra offer a useful tool for screening anti-cancer drugs' effect.


Asunto(s)
Antineoplásicos/farmacología , Neoplasias de los Conductos Biliares/tratamiento farmacológico , Colangiocarcinoma/tratamiento farmacológico , Galactanos/farmacología , Simulación del Acoplamiento Molecular , Espectroscopía Infrarroja por Transformada de Fourier , Compuestos de Azufre/farmacología , Antineoplásicos/metabolismo , Neoplasias de los Conductos Biliares/metabolismo , Neoplasias de los Conductos Biliares/patología , Línea Celular Tumoral , Movimiento Celular/efectos de los fármacos , Cetuximab/farmacología , Colangiocarcinoma/metabolismo , Colangiocarcinoma/patología , Receptores ErbB/antagonistas & inhibidores , Receptores ErbB/metabolismo , Galactanos/metabolismo , Humanos , Microespectrofotometría , Unión Proteica , Multimerización de Proteína , Transducción de Señal , Compuestos de Azufre/metabolismo , Sincrotrones
12.
Molecules ; 26(13)2021 Jun 30.
Artículo en Inglés | MEDLINE | ID: mdl-34209325

RESUMEN

Polysaccharides can form interfacial complexes with proteins to form emulsions with enhanced stability. We assessed the effect of adding gum guar or gum arabic to egg yolk/fish oil emulsions. The emulsions were produced using simple or high-pressure homogenization, stored for up to 10 days at 45 °C, and characterized for their particle size and distribution, viscosity, encapsulation efficiency, oxidative stability, and cytotoxicity. Emulsions containing gum guar and/or triglycerides had the highest viscosity. There was no significant difference in the encapsulation efficiency of emulsions regardless of the polysaccharide used. However, emulsions containing gum arabic displayed a bridging flocculation effect, resulting in less stability over time compared to those using gum guar. Emulsions produced using high-pressure homogenization displayed a narrower size distribution and higher stability. The formation of peroxides and propanal was lower in emulsions containing gum guar and was attributed to the surface oil. No significant toxicity toward Caco-2 cells was found from the emulsions over time. On the other hand, after 10 days of storage, nonencapsulated fish oil reduced the cell viability to about 80%. The results showed that gum guar can increase the particle stability of egg yolk/fish oil emulsions and decrease the oxidation rate of omega-3 fatty acids.


Asunto(s)
Yema de Huevo/química , Aceites de Pescado/química , Galactanos/química , Goma Arábiga/química , Mananos/química , Gomas de Plantas/química , Polisacáridos/química , Células CACO-2 , Emulsiones , Aceites de Pescado/farmacología , Galactanos/farmacología , Goma Arábiga/farmacología , Humanos , Mananos/farmacología , Oxidación-Reducción , Gomas de Plantas/farmacología , Polisacáridos/farmacología
13.
Molecules ; 26(6)2021 Mar 10.
Artículo en Inglés | MEDLINE | ID: mdl-33802031

RESUMEN

Nimesulide (NIM, N-(4-nitro-2-phenoxyphenyl)methanesulfonamide) is a relatively new nonsteroidal anti-inflammatory analgesic drug. It is practically insoluble in water (<0.02 mg/mL). This very poor aqueous solubility of the drug may lead to low bioavailability. The objective of the present study was to investigate the possibility of improving the solubility and the bioavailability of NIM via complexation with polysaccharide arabinogalactan (AG), disodium salt of glycyrrhizic acid (Na2GA), hydroxypropyl-ß-cyclodextrin (HP-ß-CD) and MgCO3. Solid dispersions (SD) have been prepared using a mechanochemical technique. The physical properties of nimesulide SD in solid state were characterized by differential scanning calorimetry and X-ray diffraction studies. The characteristics of the water solutions which form from the obtained solid dispersions were analyzed by reverse phase and gel permeation HPLC. It was shown that solubility increases for all complexes under investigation. These phenomena are obliged by complexation with auxiliary substances, which was shown by 1H-NMR relaxation methods. The parallel artificial membrane permeability assay (PAMPA) was used for predicting passive intestinal absorption. Results showed that mechanochemically obtained complexes with polysaccharide AG, Na2GA, and HP-ß-CD enhanced permeation of NIM across an artificial membrane compared to that of the pure NIM. The complexes were examined for anti-inflammatory activity on a model of histamine edema. The substances were administered per os to CD-1 mice. As a result, it was found that all investigated complexes dose-dependently reduce the degree of inflammation. The best results were obtained for the complexes of NIM with Na2GA and HP-ß-CD. In noted case the inflammation can be diminished up to 2-fold at equal doses of NIM.


Asunto(s)
Galactanos/farmacología , Sulfonamidas/química , Sulfonamidas/farmacología , 2-Hidroxipropil-beta-Ciclodextrina/química , Animales , Antiinflamatorios no Esteroideos/química , Disponibilidad Biológica , Rastreo Diferencial de Calorimetría/métodos , Química Farmacéutica/métodos , Galactanos/química , Ácido Glicirrínico/química , Magnesio/química , Masculino , Ratones , Permeabilidad , Preparaciones Farmacéuticas , Solubilidad , Difracción de Rayos X/métodos , beta-Ciclodextrinas/química
14.
Molecules ; 26(23)2021 Nov 29.
Artículo en Inglés | MEDLINE | ID: mdl-34885828

RESUMEN

The properties of mixtures of two polysaccharides, arabinogalactan (AG) and hyaluronic acid (HA), were investigated in solution by the measurement of diffusion coefficients D of water protons by DOSY (Diffusion Ordered SpectroscopY), by the determination of viscosity and by the investigation of the affinity of a small molecule molecular probe versus AG/HA mixtures in the presence of bovine submaxillary mucin (BSM) by 1HNMR spectroscopy. Enhanced mucoadhesive properties, decreased mobility of water and decreased viscosity were observed at the increase of AG/HA ratio and of total concentration of AG. This unusual combination of properties can lead to more effective and long-lasting hydration of certain tissues (inflamed skin, dry eye corneal surface, etc.) and can be useful in the preparation of new formulations of cosmetics and of drug release systems, with the advantage of reducing the viscosity of the solutions.


Asunto(s)
Galactanos/farmacología , Ácido Hialurónico/farmacología , Sales (Química)/química , Sodio/química , Animales , Bovinos , Óxido de Deuterio/química , Diclofenaco/química , Diclofenaco/farmacología , Difusión , Galactanos/química , Ácido Hialurónico/química , Mucinas/química , Espectroscopía de Protones por Resonancia Magnética , Soluciones , Viscosidad , Agua/química
15.
J Membr Biol ; 253(4): 343-356, 2020 08.
Artículo en Inglés | MEDLINE | ID: mdl-32725429

RESUMEN

The effect of the natural saponin glycyrrhizic acid (GA) and polysaccharide arabinogalactan (AG) on the transmembrane potential of rat thymocytes was investigated using the potential-sensitive fluorescent probe 4-(p-dimethylaminostyryl)-1-methylpyridinium (DSM). Incubation of cells with GA in micellar form resulted in a decrease of the amplitude of observed fluorescence kinetics that points out to a decrease of the transmembrane potential. The proposed mechanism is an increase of membrane ion permeability (passive ion transport) of the plasma cell membrane due to GA incorporation. The incorporation of GA molecules into the cell membrane is extremely sensitive to the degree of GA dissociation. The neutral form of glycyrrhizic acid enters the lipid bilayer in contrast to the deprotonated anionic form. The incubation of rat thymocytes with anionic form of GA, namely with its disodium salt, has no effect on the fluorescence kinetics. The possible reasons of this phenomenon are discussed in the light of the nuclear magnetic resonance (NMR) and molecular dynamics (MD) data. The treatment of thymocytes with AG affects only the initial rate of the probe incorporation. The proposed mechanism is that AG covers the surface of the cell membrane and forms a barrier for the probe. Additionally, our experiments demonstrated that both polysaccharide AG and GA in the neutral form (but not Na2GA) effectively capture the cationic probe in an aqueous solution and then deliver it to the cell membrane.


Asunto(s)
Galactanos/farmacología , Ácido Glicirrínico/farmacología , Potenciales de la Membrana/efectos de los fármacos , Timocitos/efectos de los fármacos , Timocitos/fisiología , Animales , Permeabilidad de la Membrana Celular/efectos de los fármacos , Colorantes Fluorescentes , Galactanos/química , Ácido Glicirrínico/química , Concentración de Iones de Hidrógeno , Cinética , Espectroscopía de Resonancia Magnética , Masculino , Conformación Molecular , Simulación de Dinámica Molecular , Ratas
16.
Exp Eye Res ; 196: 108058, 2020 07.
Artículo en Inglés | MEDLINE | ID: mdl-32380019

RESUMEN

Dry eye syndrome is a common disease associated to eyes inflammation, irritation and tear film instability. The enzymatic complex of xanthine oxidoreductase (XOR) is involved in the generation of reactive oxygen species (ROS) and uric acid that, in the end, can cause reperfusion injuries, irritation and pathological conditions. Furthermore, in the eye, it has been proposed that oxygen free radicals might play a significant role in retinal ischemic damage. A new artificial drop formulation based on arabinogalactan and hyaluronic acid has been proposed in this article. The uric acid and the ROS formation have been monitored. The effect of the arabinogalactan, the hyaluronic acid and their mixture has been studied. The arabinogalactan entails a uric acid and ROS reduction of 27% and 38% respectively; no significant reduction of uric acid or ROS has been observed after the addition of hyaluronic acid alone. Notably the combination of arabinogalactan and hyaluronic acid involves the reduction of uric acid and ROS equal to 38% and 62%, namely. This study demonstrates that this artificial drop formulation can markedly reduce the uric acid and ROS formation in vitro; thus, the use of this formulation may contribute in the resolution of the dry eye syndrome.


Asunto(s)
Galactanos/farmacología , Ácido Hialurónico/farmacología , Inflamación/tratamiento farmacológico , Viscosuplementos/farmacología , Xantina Deshidrogenasa/metabolismo , Sinergismo Farmacológico , Inflamación/metabolismo , Soluciones Oftálmicas/farmacología , Especies Reactivas de Oxígeno/metabolismo , Ácido Úrico/metabolismo
17.
Fish Shellfish Immunol ; 99: 35-43, 2020 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-32032761

RESUMEN

Carob leaves, the main residues of the carob tree, were investigated as a renewable and abundant source of bioactive compounds for fish aquaculture. Aqueous and ethanolic extracts obtained from carob leaves were characterized in terms of biochemical composition, antiradical and cytotoxic effects and immunostimulant and antibacterial activities. The ethanolic extract showed higher levels of total phenolics, flavonoids and condensed tannins and higher antioxidant activity than the aqueous extract. No significant immunostimulant effects were observed on gilthead seabream (Sparus aurata) head kidney leucocytes (viability, phagocytosis and respiratory burst activities and peroxidase content) after incubation for 24 h with different extracts. Furthermore, the ethanolic extracts used at 0.5, 0.75 and 1 mg mL-1 and aqueous extracts at 1 g mL-1 had a cytotoxic effect on PLHC-1 cells. When the bactericidal activity was tested against three fish pathogenic bacteria (Vibrio harveyi, Vibrio anguillarum and Photobacterium damselae) notable activity of the different extracts was detected against P. damselae at all three concentrations. A similar effect was demonstrated against V. haryeri when ethanolic extracts were used in the same range of concentrations. This work demonstrates interesting in vitro effects of carob leaf extracts and suggests it could be used as an alternative to chemical compounds with farmed fish. The concentration and nature of the extracts were very important in terms of any positive results.


Asunto(s)
Antibacterianos/farmacología , Antioxidantes/farmacología , Citotoxinas/farmacología , Galactanos/farmacología , Leucocitos/efectos de los fármacos , Mananos/farmacología , Extractos Vegetales/farmacología , Gomas de Plantas/farmacología , Animales , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Riñón Cefálico/citología , Riñón Cefálico/inmunología , Leucocitos/microbiología , Peroxidasa/análisis , Fagocitosis/efectos de los fármacos , Hojas de la Planta/química , Estallido Respiratorio/efectos de los fármacos
18.
Mar Drugs ; 18(5)2020 Apr 29.
Artículo en Inglés | MEDLINE | ID: mdl-32365741

RESUMEN

Sulfated polysaccharides (SPs) obtained from green seaweeds are structurally heterogeneous molecules with multifunctional bioactivities. In this work, two sulfated and pyruvated galactans were purified from Caulerpa cupressoides var. flabellata (named SP1 and SP2), and their immunostimulatory effect was evaluated using cultured murine macrophage cells. Both SPs equally increased the production of nitric oxide, reactive oxygen species, and the proinflammatory cytokines TNF-α and IL-6. NMR spectroscopy revealed that both galactans were composed primarily of 3)-ß-d-Galp-(1→3) units. Pyruvate groups were also found, forming five-membered cyclic ketals as 4,6-O-(1'carboxy)-ethylidene-ß-d-Galp residues. Some galactoses are sulfated at C-2. In addition, only SP2 showed some galactose units sulfated at C-4, indicating that sulfation at this position is not essential for the immunomodulatory activity of these galactans. Overall, the data showed that the galactans of C. cupressoides exhibited immunostimulating activity with potential therapeutic applications, which can be used in the development of new biomedical products.


Asunto(s)
Adyuvantes Inmunológicos/metabolismo , Caulerpa/metabolismo , Galactanos/metabolismo , Macrófagos/efectos de los fármacos , Algas Marinas , Adyuvantes Inmunológicos/farmacología , Animales , Supervivencia Celular/efectos de los fármacos , Citocinas/metabolismo , Galactanos/farmacología , Macrófagos/metabolismo
19.
Mar Drugs ; 18(8)2020 Jul 29.
Artículo en Inglés | MEDLINE | ID: mdl-32751049

RESUMEN

Seaweed sulfated polysaccharides have attracted significant attention due to their antibacterial activity. This work investigated the antibacterial activity and mechanism of depolymerized sulfated galactans from Eucheuma serra (E. serra) and Gracilaria verrucosa (G. verrucosa) against enterotoxigenic Escherichia coli (ETEC) K88. The results show that removing the metal ions improves the anti-ETEC K88 activity of the galactans. The fluorescence labeling study confirmed that the sulfated galactans penetrated the cell walls and eventually reached the interior of the ETEC K88. Nucleic acid staining and intracellular protein leakage were also observed, indicating the destruction of permeability and integrity of the cell membrane. Interestingly, the two polysaccharides exhibited no effect on the proliferation of the selected Gram-positive bacteria and yeast. This indicates that the cell wall structure of the microorganisms could influence the bacteriostatic activity of the sulfated polysaccharides, as well. These results suggest that the sulfated seaweed polysaccharides might have potential application value in antibacterial diarrhea.


Asunto(s)
Antibacterianos/farmacología , Membrana Celular/efectos de los fármacos , Pared Celular/efectos de los fármacos , Escherichia coli Enterotoxigénica/efectos de los fármacos , Galactanos/farmacología , Gracilaria/química , Algas Marinas/química , Sulfatos/farmacología , Antibacterianos/química , Antibacterianos/aislamiento & purificación , Membrana Celular/patología , Pared Celular/patología , Escherichia coli Enterotoxigénica/crecimiento & desarrollo , Galactanos/química , Galactanos/aislamiento & purificación , Bacterias Grampositivas/efectos de los fármacos , Bacterias Grampositivas/crecimiento & desarrollo , Estructura Molecular , Permeabilidad , Saccharomyces cerevisiae/efectos de los fármacos , Saccharomyces cerevisiae/crecimiento & desarrollo , Sulfatos/química , Sulfatos/aislamiento & purificación
20.
Reprod Domest Anim ; 55(9): 1124-1131, 2020 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-32562321

RESUMEN

One of the major difference between the in vivo and in vitro embryonic environments is the stiffness of the culture substrate. Xanthan gum (XG) and locust bean gum (LBG) are natural materials that are safe, inexpensive and easy to handle. In this study, we investigated the effects of using a polysaccharide culture substrate made from 1% XG and 1% LBG (XG-LBG gel) on bovine embryonic development. Oocytes collected from bovine ovaries were subjected to maturation, and fertilization to generate embryos at an early developmental stage (>4 cell stage). Cleaved embryos were further cultured in a well of 96-well cell culture plate coated with or without XG-LBG gel for 5 days. While the developmental rate up to the blastocyst stage did not differ between the two culture systems (control, 38.0 vs. gel, 38.6%), blastocysts developed on the XG-LBG gel produced significantly high cell numbers and ATP content. Embryos cultured on XG-LBG gels for 24 hr had high expression levels of F-actin and a highly even distribution of E-cadherin. In addition, embryos developed on XG-LBG gel demonstrated increased translocation of YAP to the nucleus and increased connective tissue growth factor (CTGF) protein levels (downstream of Hippo signalling). These findings suggest that soft culture substrates improve embryonic development by enhancing mechanotransduction, including YAP-CTGF signalling.


Asunto(s)
Medios de Cultivo , Desarrollo Embrionario/efectos de los fármacos , Galactanos/farmacología , Mananos/farmacología , Gomas de Plantas/farmacología , Polisacáridos Bacterianos/farmacología , Adenosina Trifosfato/análisis , Animales , Bovinos , Proteínas de Ciclo Celular/metabolismo , Femenino , Fertilización In Vitro/veterinaria , Geles/farmacología , Técnicas de Maduración In Vitro de los Oocitos/veterinaria , Masculino , Oocitos/fisiología , Transducción de Señal
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