RESUMEN
The goal of this research was to analyse the synergistic effect between selected plant extracts with zinc oxide particles, and zinc stearate. The influence of ZnO on the antimicrobial effectiveness of the selected extracts was confirmed in previous research carried out by the authors. However, the impact of zinc stearate on extract activity has yet to be analysed. The aim was to cover PLA films with active coatings based on hydroxy-propyl-methyl-cellulose (HPMC), or/and ethyl cellulose (EC) containing plant extracts and ZnO which has a synergistic effect. An additional aim was to use a CO2 extract of raspberry seed (RSE) with zinc stearate as active additives within the coatings. An examination of the antimicrobial properties (against Staphylococcus aureus, Escherichia coli, Bacillus subtilis, Pseudomonas syringae and Φ6 bacteriophage) of the covered films, as well as an investigation of layer presence with regards to PLA morphology (SEM, ATR-FTIR analysis) was carried out. The research work that was performed indicated that black chokeberry extract (ChE) and zinc oxide particles were effective against S. aureus, P. syringae and B. subtilis strains. In addition, the ChE with zinc stearate (ZnSt) was active against all analysed strains. The HPMC with ChE and ZnO as additives had antimicrobial properties against S. aureus, P. syringae and E. coli strains. The ChE was found to inhibit the growth of all of the analysed bacterial strains. When considering the coatings based on EC with the CO2 extract of raspberry seed (RSE) and ZnO, it was noted that they were only active against Gram-negative bacteria. The results of the experiments confirmed that AC1 (EC with RSE with ZnO) and AC2 (EC with RSE with ZnSt) coatings were not active against a phi6 bacteriophage. The HPMC coating containing the AC3 layer (ChE and ZnO) eliminated Φ6 particles, confirming its antiviral properties. In addition, the presence of the active (AC1, AC2 and AC3) coatings was confirmed by SEM and FTIR analysis.
Asunto(s)
Extractos Vegetales , Rubus , Óxido de Zinc , Óxido de Zinc/química , Óxido de Zinc/farmacología , Extractos Vegetales/farmacología , Extractos Vegetales/química , Rubus/química , Pruebas de Sensibilidad Microbiana , Ácidos Esteáricos/química , Ácidos Esteáricos/farmacología , Antiinfecciosos/farmacología , Antiinfecciosos/química , Antibacterianos/farmacología , Antibacterianos/química , Escherichia coli/efectos de los fármacos , Escherichia coli/crecimiento & desarrollo , Bacillus subtilis/efectos de los fármacos , Staphylococcus aureus/efectos de los fármacosRESUMEN
Herein, the surface-enhanced Raman scattering (SERS) platform was combined with an azo coupling reaction and an aluminum alloy covered with a hydrophobic layer of praseodymium oxide and stearic acid complexes for the detection of histamine. The praseodymium oxide on aluminum alloy was successfully synthesized by the rare-earth-salt-solution boiling bath method and modified by stearic acid. Its surface exhibits a water contact angle (WCA) of 125.0°. Through the azo derivatization reaction with 3-amino-5-mercapto-1,2,4-triazole (AMTA) diazonium salts, histamine can be converted into the derivatization product with higher Raman activity. The mixture of the derivatization product and ß-cyclodextrin-modified Ag nanoparticles (ß-CD-AgNPs) were dropped onto the surface of an aluminum alloy covered with a hydrophobic layer of praseodymium oxide and stearic acid complexes, and dried for SERS measurement. The intensity ratio between the SERS peaks at 1246 cm-1 and 1104 cm-1 (I1246/I1104) of the derivatization product was used for the quantification of histamine. Under the selected conditions, the limit of detection (LOD) and the limit of quantification (LOQ) for this method were 7.2 nM (S/N = 3) and 24 nM (S/N = 10), respectively. The relative standard deviation (RSD) of this method for the determination of 1 µM histamine was 6.1 % (n = 20). The method was also successfully used for the determination of histamine in fish samples with recoveries ranging from 92 % to 111 %. The present method is simple, sensitive, reliable, and may provide a new approach for preparing the composite hydrophobic layer that can enhance SERS signals through hydrophobic condensation effect. Meanwhile, it may have a promising future in the determination of small molecular compounds containing an imidazole ring.
Asunto(s)
Histamina , Interacciones Hidrofóbicas e Hidrofílicas , Nanopartículas del Metal , Plata , Espectrometría Raman , Espectrometría Raman/métodos , Histamina/análisis , Histamina/química , Plata/química , Nanopartículas del Metal/química , Límite de Detección , Compuestos Azo/química , Ácidos Esteáricos/química , Animales , Peces , Propiedades de SuperficieRESUMEN
Dietary lipids play an essential role in regulating the function of the gut microbiota and gastrointestinal tract, and these luminal interactions contribute to mediating host metabolism. Palmitic Acid Hydroxy Stearic Acids (PAHSAs) are a family of lipids with antidiabetic and anti-inflammatory properties, but whether the gut microbiota contributes to their beneficial effects on host metabolism is unknown. Here, we report that treating chow-fed female and male germ-free (GF) mice with PAHSAs improves glucose tolerance, but these effects are lost upon high fat diet (HFD) feeding. However, transfer of feces from PAHSA-treated, but not vehicle-treated, chow-fed conventional mice increases insulin sensitivity in HFD-fed GF mice. Thus, the gut microbiota is necessary for, and can transmit, the insulin-sensitizing effects of PAHSAs in HFD-fed GF male mice. Analyses of the cecal metagenome and lipidome of PAHSA-treated mice identified multiple lipid species that associate with the gut commensal Bacteroides thetaiotaomicron (Bt) and with insulin sensitivity resulting from PAHSA treatment. Supplementing live, and to some degree, heat-killed Bt to HFD-fed female mice prevented weight gain, reduced adiposity, improved glucose tolerance, fortified the colonic mucus barrier and reduced systemic inflammation compared to HFD-fed controls. These effects were not observed in HFD-fed male mice. Furthermore, ovariectomy partially reversed the beneficial Bt effects on host metabolism, indicating a role for sex hormones in mediating the Bt probiotic effects. Altogether, these studies highlight the fact that PAHSAs can modulate the gut microbiota and that the microbiota is necessary for the beneficial metabolic effects of PAHSAs in HFD-fed mice.
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Dieta Alta en Grasa , Microbioma Gastrointestinal , Resistencia a la Insulina , Obesidad , Animales , Masculino , Femenino , Ratones , Microbioma Gastrointestinal/efectos de los fármacos , Obesidad/metabolismo , Obesidad/microbiología , Obesidad/etiología , Dieta Alta en Grasa/efectos adversos , Ratones Endogámicos C57BL , Ácidos Esteáricos/metabolismo , Ácido Palmítico/metabolismo , Heces/microbiología , Ratones ObesosRESUMEN
Previous RS5 (type 5 resistant starch) research has significantly broadened starch use and benefited society, yet the effects of the molecular weight of amylose on RS5 remain underexplored. In this study, amyloses with different molecular weights were complexed with caproic acid (C6), lauric acid (C12), and stearic acid (C18) to observe the effects of the molecular weight of amylose on the structure and in vitro digestive properties of RS5. Gel permeation chromatography revealed that the peak average molecular weight (Mp) values of high-amylose cornstarch NF-CGK (CGK), high-amylose cornstarch obtained via cornstarch via autoclave (high temperature and high pressure)-cooling combined pullulanase enzymatic hydrolysis (CTE), and high-amylose cornstarch NF-G370 (HCK) were 21,282, 171,537, and 188,084 before fatty acid complexation, respectively. Additionally, their weight average molecular weight (Mw) values of 32,429, 327,344, and 410,610 and hydrolysis rates of 58.12 %, 86.77 %, and 64.58 %, respectively. The hydrolysis rate of low-Mw amylose (GCK) complexes with fatty acids was lower than that of HCK and CTE starch-lipid complexes. However, HCK and CTE having similar molecular weights, there was no significant difference in the hydrolysis rate of starch-lipid complexes. X-ray diffraction, Fourier transform infrared spectroscopy, scanning electron microscopy and complexing index analyses confirmed the formation of these complexes. This study proposed the mechanism of RS5 formation and provided guidance for its future development.
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Amilosa , Ácidos Láuricos , Peso Molecular , Amilosa/química , Ácidos Láuricos/química , Hidrólisis , Almidón/química , Almidón/metabolismo , Digestión , Ácidos Esteáricos/química , Lípidos/química , CaprilatosRESUMEN
This study aimed to explore the effects of various lipids on the structure, cooking quality, and in vitro starch digestibility of extruded buckwheat noodles (EBNs) with and without 20% high-amylose corn starch (HACS). Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction revealed that lauric acid bound more strongly to starch than did stearic acid and oleic acid, and the binding capacity of fatty acids with starch was stronger than that of glycerides. The presence of HACS during extrusion facilitated increased formation of starch-lipid complexes. Evaluations of cooking quality and digestion characteristics showed that EBNs containing 20% HACS and 0.5% glycerol monooleate demonstrated the lowest cooking loss (7.28%), and that with 20% HACS and 0.5% oleic acid displayed the lowest predicted glycemic index (pGI) (63.54) and highest resistant starch (RS) content (51.64%). However, excessive starch-lipid complexes were detrimental to EBNs cooking quality and the resistance of starch to digestive enzymes because of the damage to the continuity of the starch gel network. This study establishes a fundamental basis for the development of EBNs with superior cooking quality and a relatively lower GI.
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Culinaria , Digestión , Fagopyrum , Ácidos Grasos , Almidón , Fagopyrum/química , Ácidos Grasos/química , Almidón/química , Glicéridos/química , Índice Glucémico , Espectroscopía Infrarroja por Transformada de Fourier , Amilosa/química , Difracción de Rayos X , Rastreo Diferencial de Calorimetría , Ácidos Esteáricos/química , Ácido Oléico/química , Ácidos Láuricos/químicaRESUMEN
In order to introduce a cost-effective strategy method for commercial scale dry granulation at the early clinical stage of drug product development, we developed dry granulation process using formulation without API, fitted and optimized the process parameters adopted Design of Experiment (DOE). Then, the process parameters were confirmed using one formulation containing active pharmaceutical ingredient (API). The results showed that the roller pressure had significant effect on particle ratio (retained up to #60 mesh screen), bulk density and tapped density. The roller gap had significant influence on particle ratio and specific energy. The particle ratio was significantly affected by the mill speed (second level). The tabletability of the powder decreased after dry granulation. The effect of magnesium stearate on the tabletability was significant. In the process validation study, the properties of the prepared granules met the requirements for each response studied in the DOE. The prepared tablets showed higher tensile strength, good content uniformity of filled capsules, and the dissolution profiles of which were consistent with that of clinical products. This drug product process development and research strategies could be used as a preliminary experiment for the dry granulation process in the early clinical stage.
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Comprimidos , Comprimidos/química , Tamaño de la Partícula , Composición de Medicamentos , Polvos/química , Ácidos Esteáricos/química , Resistencia a la Tracción , Excipientes/química , SolubilidadRESUMEN
The compendial USPã701ã disintegration test method offers a crucial pass/fail assessment for immediate release tablet disintegration. However, its single end-point approach provides limited insight into underlying mechanisms. This study introduces a novel calorimetric approach, aimed at providing comprehensive process profiles beyond binary outcomes. We developed a novel disintegration reaction calorimeter to monitor the heat release throughout the disintegration process and successfully obtained enthalpy change profiles of placebo tablets with various porosities. The formulation comprised microcrystalline cellulose (MCC), anhydrous lactose, croscarmellose sodium (CCS), and magnesium stearate (MgSt). An abrupt temperature rise was observed after introducing the disintegration medium to tablets, and the relationship between the heat rise time and the tablet's porosity was investigated. The calorimeter's sensitivity was sufficient to discern distinct heat changes among individual tablets, and the analysis revealed a direct correlation between the two. Higher porosity corresponded to shorter heat rise time, indicating faster disintegration rates. Additionally, the analysis identified a concurrent endothermic process alongside the anticipated exothermic phenomenon, potentially associated with the dissolution of anhydrous lactose. Since lactose is the only soluble excipient within the blend composition, the endothermic process can be attributed to the absorption of heat as lactose molecules dissolve in water. The findings from this study underscore the potential of utilising calorimetric methods to quantify the wettability of complex compounds and, ultimately, optimise tablet formulations.
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Calorimetría , Celulosa , Excipientes , Calor , Lactosa , Ácidos Esteáricos , Comprimidos , Lactosa/química , Celulosa/química , Excipientes/química , Porosidad , Ácidos Esteáricos/química , Calorimetría/métodos , Solubilidad , Carboximetilcelulosa de Sodio/química , Química Farmacéutica/métodos , Liberación de Fármacos , Composición de Medicamentos/métodosRESUMEN
Limited attempts have been made previously to develop high-loading CBD inhalable powders, which are essential for high dose delivery. Therefore, this study aimed to develop and characterise inhalable powders with ≥ 95 % w/w CBD by wet ball milling. The effects of magnesium stearate (2 % and 5 %) and inhaler resistance (low-resistance and high-resistance RS01 inhalers) on aerosol performance were also compared. Wet ball milling produced CBD powders with > 50 % production yield. The milled particles showed irregular shapes. The powders were crystalline with minimal amorphous content, low residual solvent level (<1%), and low moisture sorption (<4%). Magnesium stearate improved both the emitted and fine particle fractions. The aerodynamic particle size distribution of the formulations differed between the low-resistance and high-resistance RS01 inhalers. The latter decreased throat deposition but increased inhaler retention. The dissolution profiles showed that all three formulations released CBD steadily and plateaued at 30 min. The best scenario was CBD with 5 % magnesium stearate dispersed from the high resistance RS01 inhaler, showing the highest FPF with the lowest throat deposition. This combination may be tested in vivo in the future to investigate its pharmacokinetic profile.
Asunto(s)
Cannabidiol , Tamaño de la Partícula , Polvos , Ácidos Esteáricos , Administración por Inhalación , Ácidos Esteáricos/química , Cannabidiol/administración & dosificación , Cannabidiol/química , Cannabidiol/farmacocinética , Aerosoles , Inhaladores de Polvo Seco , Excipientes/química , Química Farmacéutica/métodos , Liberación de Fármacos , Nebulizadores y Vaporizadores , Composición de Medicamentos/métodos , SolubilidadRESUMEN
Extensive evidence supports the connection between obesity-induced inflammation and the heightened expression of IL-6 adipose tissues. However, the mechanism underlying the IL-6 exacerbation in the adipose tissue remains unclear. There is general agreement that TNF-α and stearate concentrations are mildly elevated in adipose tissue in the state of obesity. We hypothesize that TNF-α and stearate co-treatment induce the increased expression of IL-6 in mouse adipocytes. We therefore aimed to determine IL-6 gene expression and protein production by TNF-α/stearate treated adipocytes and investigated the mechanism involved. To test our hypothesis, 3T3-L1 mouse preadipocytes were treated with TNF-α, stearate, or TNF-α/stearate. IL-6 gene expression was assessed by quantitative real-time qPCR. IL-6 protein production secreted in the cell culture media was determined by ELISA. Acetylation of histone was analyzed by Western blotting. Il6 region-associated histone H3 lysine 9/18 acetylation (H3K9/18Ac) was determined by ChIP-qPCR. 3T3-L1 mouse preadipocytes were co-challenged with TNF-α and stearate for 24 h, which led to significantly increased IL-6 gene expression (81 ± 2.1 Fold) compared to controls stimulated with either TNF-α (38 ± 0.5 Fold; p = 0.002) or stearate (56 ± 2.0 Fold; p = 0.013). As expected, co-treatment of adipocytes with TNF-α and stearate significantly increased protein production (338 ± 11 pg/mL) compared to controls stimulated with either TNF-α (28 ± 0.60 pg/mL; p = 0.001) or stearate (53 ± 0.20 pg/mL, p = 0.0015). Inhibition of histone acetyltransferases (HATs) with anacardic acid or curcumin significantly reduced the IL-6 gene expression and protein production by adipocytes. Conversely, TSA-induced acetylation substituted the stimulatory effect of TNF-α or stearate in their synergistic interaction for driving IL-6 gene expression and protein production. Mechanistically, TNF-α/stearate co-stimulation increased the promoter-associated histone H3 lysine 9/18 acetylation (H3K9/18Ac), rendering a transcriptionally permissive state that favored IL-6 expression at the transcriptional and translational levels. Our data represent a TNF-α/stearate cooperativity model driving IL-6 expression in 3T3-L1 cells via the H3K9/18Ac-dependent mechanism, with implications for adipose IL-6 exacerbations in obesity.
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Células 3T3-L1 , Adipocitos , Histonas , Interleucina-6 , Factor de Necrosis Tumoral alfa , Animales , Ratones , Acetilación , Adipocitos/metabolismo , Adipocitos/efectos de los fármacos , Regulación de la Expresión Génica/efectos de los fármacos , Histonas/metabolismo , Interleucina-6/metabolismo , Interleucina-6/genética , Ácidos Esteáricos/farmacología , Ácidos Esteáricos/metabolismo , Factor de Necrosis Tumoral alfa/metabolismo , Factor de Necrosis Tumoral alfa/farmacologíaRESUMEN
AIM: Fatty acid esters of hydroxy fatty acids (FAHFA) are a class of bioactive lipids with anti-inflammatory, antidiabetic and cardioprotective properties. FAHFA hydrolysis into its fatty acid (FA) and hydroxy fatty acid (HFA) constituents can affect the bioavailability of FAHFA and its subsequent biological effects. We aimed to investigate FAHFA levels and FAHFA hydrolysis activity in children with or without obesity, and in adults with or without coronary artery disease (CAD). MATERIALS AND METHODS: Our study cohort included 20 children without obesity, 40 children with obesity, 10 adults without CAD and 28 adults with CAD. We quantitated plasma levels of four families of FAHFA [palmitic acid hydroxy stearic acid (PAHSA), palmitoleic acid hydroxy stearic acid (POHSA), oleic acid hydroxy stearic acid (OAHSA), stearic acid hydroxy stearic acid] and their corresponding FA and HFA constituents using liquid chromatography-tandem mass spectrometry analysis. Surrogate FAHFA hydrolysis activity was estimated as the FA/FAHFA or HFA/FAHFA ratio. RESULTS: Children with obesity had lower plasma PAHSA (p = .001), OAHSA (p = .006) and total FAHFA (p = .011) levels, and higher surrogate FAHFA hydrolysis activity represented by PA/PAHSA (p = .040) and HSA/OAHSA (p = .025) compared with children without obesity. Adults with CAD and a history of myocardial infarction (MI) had lower POHSA levels (p = .026) and higher PA/PAHSA (p = .041), POA/POHSA (p = .003) and HSA/POHSA (p = .038) compared with those without MI. CONCLUSION: Altered FAHFA metabolism is associated with obesity and MI, and inhibition of FAHFA hydrolysis should be studied further as a possible therapeutic strategy in obesity and MI.
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Enfermedad de la Arteria Coronaria , Ácidos Grasos , Humanos , Masculino , Femenino , Niño , Enfermedad de la Arteria Coronaria/sangre , Adulto , Hidrólisis , Ácidos Grasos/sangre , Ácidos Grasos/metabolismo , Persona de Mediana Edad , Adolescente , Ácidos Esteáricos/sangre , Ácidos Esteáricos/metabolismo , Obesidad Infantil/sangre , Obesidad Infantil/complicaciones , Obesidad Infantil/metabolismo , Ésteres/sangre , Ácidos Grasos Monoinsaturados/sangre , Obesidad/sangre , Obesidad/complicaciones , Obesidad/metabolismo , Estudios de CohortesRESUMEN
Transport of oral nanocarriers across the GI epithelium necessitates transport across hydrophilic mucus layer and the hydrophobic epithelium. Based on hydrophobic-hydrophilic balance, Curcumin-Lipomer (lipid-polymer hybrid nanoparticles) comprising hydrophobic stearic acid and hydrophilic Gantrez™ AN 119 (Gantrez) were developed, by a radical in-situ approach, to successfully traverse both barriers. A monophasic preconcentrate (Cur-Pre) comprising Cur (Curcumin), stearic acid, Gantrez and stabilizers, prepared by simple solution, was added to an aqueous phase to instantaneously generate Curcumin-Lipomer (Cur-Lipo) of nanosize and high entrapment efficiency (EE). Cur-Lipo size and EE was optimized by Box-Behnken Design. Cur-Lipomers of varying hydrophobic-hydrophilic property obtained by varying the stearic acid: Gantrez ratio exhibited size in the range 200-400 nm, EE > 95% and spherical morphology as seen in the TEM. A decrease in contact angle and in mucus interaction, evident with increase in Gantrez concentration, indicated an inverse corelation with hydrophilicity, while a linear corelation was observed for mucopenetration and hydrophilicity. Cur-SLN (solid lipid nanoparticles) which served as the hydrophobic reference revealed contact angle > 90°, maximum interaction with mucus and minimal mucopenetration. The ex-vivo permeation study through chicken ileum, revealed maximum permeation with Cur-Lipo1 and comparable and significantly lower permeation of Cur-Lipo1-D and Cur-SLN proposing the importance of balancing the hydrophobic-hydrophilic property of the nanoparticles. A 1.78-fold enhancement in flux of hydrophobic Cur-SLN, with no significant change in permeation of the hydrophilic Cur-Lipomers (p > 0.05) following stripping off the mucosal layer was observed. This reiterated the significance of hydrophobic-hydrophilic balance as a promising strategy to design nanoformulations with superior permeation across the GI barrier.
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Curcumina , Portadores de Fármacos , Interacciones Hidrofóbicas e Hidrofílicas , Mucosa Intestinal , Nanopartículas , Ácidos Esteáricos , Nanopartículas/química , Administración Oral , Animales , Ácidos Esteáricos/química , Curcumina/administración & dosificación , Curcumina/farmacocinética , Curcumina/química , Mucosa Intestinal/metabolismo , Portadores de Fármacos/química , Tamaño de la Partícula , Lípidos/química , Polímeros/química , Transporte Biológico/fisiología , Polivinilos/químicaRESUMEN
In this study, five C18 fatty acids (FA) with different numbers of double bonds and configurations including stearic acid (SA), oleic acid (OA), elaidic acid (EA), linoleic acid (LA), and α-linolenic acid (ALA), were selected to prepare highland barely starch (HBS)-FA complexes to modulate digestibility and elaborate the underlying mechanism. The results showed that HBS-SA had the highest complex index (34.18 %), relative crystallinity (17.62 %) and single helix content (25.78 %). Furthermore, the HBS-C18 FA complexes were formed by EA (C18 FA with monounsaturated bonds) that had the highest R1047/1022 (1.0509) and lowest full width at half-maximum (FWHM, 20.85), suggesting good short-range ordered structure. Moreover, all C18 FAs could form two kinds of V-type complexes with HBS, which can be confirmed by the results of CLSM and DSC measurements, and all of them showed significantly lower digestibility. HBS-EA possessed the highest resistant starch content (20.17 %), while HBS-SA had the highest slowly digestible starch content (26.61 %). In addition, the inhibition of HBS retrogradation by fatty acid addition was further proven, where HBS-SA gel firmness (37.80 g) and aging enthalpy value were the lowest, indicating the most effective. Overall, compounding with fatty acids, especially SA, could be used as a novel way to make functional foods based on HBS.
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Digestión , Ácidos Grasos , Hordeum , Ácido Oléico , Almidón , Almidón/química , Ácidos Grasos/análisis , Ácidos Grasos/química , Hordeum/química , Ácido Oléico/química , Ácidos Esteáricos/química , Ácido Linoleico/química , Ácido alfa-Linolénico/química , Ácidos OléicosRESUMEN
Lubricants are essential for most tablet formulations as they assist powder flow, prevent adhesion to tableting tools and facilitate tablet ejection. Magnesium stearate (MgSt) is an effective lubricant but may compromise tablet strength and disintegratability. In the design of orodispersible tablets, tablet strength and disintegratability are critical attributes of the dosage form. Hence, this study aimed to conduct an in-depth comparative study of MgSt with alternative lubricants, namely sodium lauryl sulphate (SLS), stearic acid (SA) and hydrogenated castor oil (HCO), for their effects on the tableting process as well as tablet properties. Powder blends were prepared with lactose, sodium starch glycolate or crospovidone as the disintegrant, and a lubricant at different concentrations. Angle of repose was determined for the mixtures. Comparative evaluation was carried out based on the ejection force, tensile strength, liquid penetration and disintegratability of the tablets produced. As the lubricant concentration increased, powder flow and tablet ejection improved. The lubrication efficiency generally decreased as follows: MgSt > HCO > SA > SLS. Despite its superior lubrication efficacy, MgSt is the only lubricant of four evaluated that reduced tablet tensile strength. Tablet disintegration time was strongly determined by tensile strength and liquid penetration, which were in turn affected by the lubricant type and concentration. All the above factors should be taken into consideration when deciding the type and concentration of lubricant for an orodispersible tablet formulation.
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Excipientes , Lubricantes , Ácidos Esteáricos , Comprimidos , Resistencia a la Tracción , Lubricantes/química , Ácidos Esteáricos/química , Excipientes/química , Composición de Medicamentos/métodos , Polvos/química , Dodecil Sulfato de Sodio/química , Aceite de Ricino/química , Povidona/química , Almidón/química , Almidón/análogos & derivados , Lactosa/química , Administración Oral , Solubilidad , Química Farmacéutica/métodosRESUMEN
Magnesium alloy is currently regarded as the most favourable biodegradable metal; however, obstacles remain to be overcome in terms of managing its corrosion and ensuring its biocompatibility. In this study, a metal-organic complex comprising Ca ions incorporated in tannic acid (TA) was prepared and used to coat magnesium alloy by chemical conversion and dipping processes, followed by modification with stearic acid (SA). This metal-organic complex coating was demonstrated to be homogeneous and compact, and it significantly improved the electrochemical corrosion resistance and long-term degradation behaviour of the coated samples. Consequently, the well-controlled release of Mg and Ca ions, as well as the osteo-compatible TA and SA molecules, promoted the proliferation of osteoblast cells. This metal-organic complex coating offers a promising modifying strategy for magnesium-based orthopaedic implants.
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Aleaciones , Materiales Biocompatibles Revestidos , Magnesio , Magnesio/química , Aleaciones/química , Aleaciones/farmacología , Corrosión , Materiales Biocompatibles Revestidos/química , Materiales Biocompatibles Revestidos/farmacología , Ensayo de Materiales , Taninos/química , Taninos/farmacología , Proliferación Celular/efectos de los fármacos , Propiedades de Superficie , Osteoblastos/efectos de los fármacos , Osteoblastos/citología , Implantes Absorbibles , Humanos , Ácidos Esteáricos/química , Animales , Calcio/química , Calcio/metabolismo , Línea CelularRESUMEN
Constipation is a major gastrointestinal (GI) symptom worldwide, with diverse causes of formation, and requires effective and safe therapeutic measures. In the present study, we used loperamide hydrochloride to establish a constipation model and assessed the effect of Bifidobacterium on constipation and its possible mechanism of relief. The results showed that B. longum S3 exerted a constipation-relieving effect primarily by improving the gut microbiota, enriching genera including Lactobacillus, Alistipes, and Ruminococcaceae UCG-007, and decreasing the bacteria Lachnospiraceae NK4B4 group. These changes may thereby increase acetic acid and stearic acid (C18:0) levels, which significantly increase the expression levels of ZO-1 and MUC-2, repair intestinal barrier damage and reduce inflammation (IL-6). Furthermore, it also inhibited oxidative stress levels (SOD and CAT), decreased the expression of water channel proteins (AQP4 and AQP8), significantly elevated the Gas, 5-HT, PGE2, and Ach levels, and reduced nNOS and VIP levels to improve the intestinal luminal transit time and fecal water content. Collectively, these changes resulted in the alleviation of constipation.
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Ácido Acético , Bifidobacterium longum , Estreñimiento , Microbioma Gastrointestinal , Loperamida , Probióticos , Ácidos Esteáricos , Loperamida/efectos adversos , Estreñimiento/inducido químicamente , Estreñimiento/tratamiento farmacológico , Estreñimiento/metabolismo , Animales , Ratones , Probióticos/farmacología , Ácidos Esteáricos/metabolismo , Masculino , Microbioma Gastrointestinal/efectos de los fármacos , Modelos Animales de Enfermedad , Intestinos/microbiologíaRESUMEN
The effects of common migration substances in milk packaging on digestive protease were studied. We choose the common migrants found in eight types of multi-layer composite milk packaging. Enzyme activity experiments revealed that pepsin activity decreased by approximately 18 % at 500 µg/mL of stearic acid and stearamide treatment, while trypsin activity decreased by approximately 18 % only by stearic acid treatment (500 µg/mL). Subsequently, fluorescence spectroscopy, circular dichroism spectroscopy, and molecular docking technology were employed to investigate the inhibition mechanism of protease activity by migrating substances in three systems: stearic acid-trypsin, stearic acid-pepsin, and stearamide-pepsin. Results showed that the inhibitory effect of stearic acid on trypsin is a reversible mixed inhibition, whereas the inhibitory effects of stearic acid and stearamide on pepsin are non-competitive. In all three systems, ΔH < 0, ΔS < 0, and ΔG < 0, indicating the binding process between the migrant and the protease is a spontaneous exothermic process primarily driven by hydrogen bonding and van der Waals forces. In addition, their binding constants are all around 104 L/moL, indicating that there are moderate binding affinities exist between migrants and proteases. The binding process results in the quenching of the protease's endogenous fluorescence and induces alterations in the enzyme's secondary structure. Synchronized fluorescence spectroscopy showed that stearic acid enhanced the hydrophobicity near the Tyr residue of trypsin. The molecular docking results indicated that the binding affinity of stearic acid-trypsin, stearic acid-pepsin, and stearamide-pepsin was -22.51 kJ/mol, -12.35 kJ/mol, -19.28 kJ/mol respectively, which consistent with the trend in the enzyme activity results. This study can provide references for the selection of milk packaging materials and the use of processing additives, ensuring food health and safety.
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Embalaje de Alimentos , Leche , Simulación del Acoplamiento Molecular , Espectrometría de Fluorescencia , Tripsina , Animales , Leche/química , Tripsina/metabolismo , Tripsina/química , Ácidos Esteáricos/química , Ácidos Esteáricos/metabolismo , Pepsina A/metabolismo , Pepsina A/química , Dicroismo Circular , Péptido Hidrolasas/metabolismo , Péptido Hidrolasas/química , TermodinámicaRESUMEN
Understanding the impact of minor components and the fatty acid profile of oil on oleogel properties is essential for optimizing their characteristics. Considering the scarcity of literature addressing this aspect, this study aimed to explore the correlation between these factors and the properties of beeswax and stearic acid-based oleogels derived from rice bran oil and sesame oil. Minor oil components were modified by stripping the oil, heating the oil with water, and adding ß-sitosterol. Oleogels were then prepared using a mixture of beeswax and stearic acid (3:1, w/w) at a concentration of 11.74 % (w/w). The properties of oils and oleogels were evaluated. The findings indicated that minor components and fatty acid composition of the oils substantially influence the oleogel properties. Removing minor components by stripping resulted in smaller and less uniformly distributed crystals and less oil binding capacity compared to the oleogels prepared from untreated oils. A moderate amount of minor components exhibited a significant influence on oleogel properties. The addition of ß-sitosterol did not show any influence on oleogel properties except for the oleogel made from untreated oil blend added with ß-sitosterol which had more uniform crystals in the microstructure and demonstrated better rheological stability when stored at 5 °C for two months. The oil composition did not show any influence on the thermal and molecular properties of oleogels. Consequently, the oleogel formulation derived from the untreated oil blend enriched with ß-sitosterol was identified as the optimal formula for subsequent development. The findings of this study suggest that the physical and mechanical properties as well as the oxidative stability of beeswax and stearic acid-based oleogels are significantly affected by the minor constituents and fatty acid composition of the oil. Moreover, it demonstrates that the properties of oleogels can be tailored by modifying oil composition by blending different oils.
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Ácidos Grasos , Ácidos Esteáricos , Ceras , Aceite de Salvado de Arroz , Compuestos OrgánicosRESUMEN
BACKGROUND: Prior observational studies have suggested correlations between saturated fatty acids (SFAs) and monounsaturated fatty acids (MUFAs) with cognitive function. However, causal relationships remains unclear. METHODS: We assessed the causal impact of two SFAs (palmitic acid [PA] and stearic acid [SA]) and two MUFAs (oleic acid [OA] and palmitoleic acid [POA]) on cognitive function-related traits, and dementia-related traits by univariable Mendelian randomization (UVMR) and multivariable Mendelian randomization (MVMR) analyses. RESULTS: UVMR indicated ß of 0.060 (P = 4.05E-06) for cognitive performance score and 0.066 (P = 4.21E-04) for fluid intelligence per standard deviation (SD) increase in OA level. MVMR indicated: (i) ß of -0.608 (P = 8.37E-05) for fluid intelligence score per SD increase in POA; (ii) ß of 0.074 (P = 0.018) for fluid intelligence score per SD increase in OA; (iii) ß of 0.029 (P = 0.033) for number of incorrect matches in round per SD increase in PA; and (iv) ß of 0.039 (P = 0.032) for number of incorrect matches in round per SD increase in SA. In addition, a secondary MVMR analysis after excluding the effect of polyunsaturated fatty acids suggested that: (i) ß of -0.043 (P = 1.97E-02) for cognitive performance score per SD increase in PA and (ii) ß of -0.079 (P = 1.79E-03) for cognitive performance score per SD increase in SA. CONCLUSIONS: Overall, UVMR and MVMR suggest that OA may be beneficial for cognitive function, while POA, PA, and SA may have detrimental effects on cognitive function.
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Disfunción Cognitiva , Ácidos Grasos Monoinsaturados , Ácidos Grasos , Análisis de la Aleatorización Mendeliana , Humanos , Ácidos Esteáricos , Cognición/efectos de los fármacos , Ácido Oléico , Inteligencia/efectos de los fármacos , Ácido Palmítico , Polimorfismo de Nucleótido Simple , Demencia , Ácido Graso DesaturasasRESUMEN
Nanoenabled strategies have recently attracted attention as a sustainable platform for agricultural applications. Here, we present a mechanistic understanding of nanobiointeraction through an orthogonal investigation. Pristine (nS) and stearic acid surface-modified (cS) sulfur nanoparticles (NPs) as a multifunctional nanofertilizer were applied to tomato (Solanum lycopersicumL.) through soil. Both nS and cS increased root mass by 73% and 81% and increased shoot weight by 35% and 50%, respectively, compared to the untreated controls. Bulk sulfur (bS) and ionic sulfate (iS) had no such stimulatory effect. Notably, surface modification of S NPs had a positive impact, as cS yielded 38% and 51% greater shoot weight compared to nS at 100 and 200 mg/L, respectively. Moreover, nS and cS significantly improved leaf photosynthesis by promoting the linear electron flow, quantum yield of photosystem II, and relative chlorophyll content. The time-dependent gene expression related to two S bioassimilation and signaling pathways showed a specific role of NP surface physicochemical properties. Additionally, a time-dependent Global Test and machine learning strategy applied to understand the NP surface modification domain metabolomic profiling showed that cS increased the contents of IA, tryptophan, tomatidine, and scopoletin in plant leaves compared to the other treatments. These findings provide critical mechanistic insights into the use of nanoscale sulfur as a multifunctional soil amendment to enhance plant performance as part of nanoenabled agriculture.
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Nanopartículas , Solanum lycopersicum , Azufre , Solanum lycopersicum/metabolismo , Solanum lycopersicum/efectos de los fármacos , Azufre/metabolismo , Azufre/química , Nanopartículas/química , Nanopartículas/metabolismo , Fotosíntesis , Propiedades de Superficie , Factores de Tiempo , Fertilizantes , Ácidos Esteáricos/metabolismo , Ácidos Esteáricos/química , Hojas de la Planta/metabolismoRESUMEN
BACKGROUND: Intracellular lipids are sensitive to freezing. Lipidome modification is an important tool for studying the role of intracellular lipids in cryotolerance of mammalian oocytes and preimplantation embryos. OBJECTIVE: To study the effects of in vitro exposure of murine embryos to saturated stearic acid (SA) on the lipid content, embryo development and cryotolerance. MATERIALS AND METHODS: In vivo derived mouse embryos were cultured with 100 uM SA for 48 h up to the morula/blastocyst stage. Some of the SA-treated embryos were chosen for the evaluation of their development competence and the change in the lipidome, and other embryos were either slowly frozen or rapidly vitrified. RESULTS: Nile red staining combined with confocal laser scanning microscopy revealed a decrease in the total amount of lipids in the SA-treated embryos. Raman measurements showed that the lipid unsaturation was lower in embryos after in vitro SA culture. The addition of SA did not affect the embryo development before cryopreservation, but negatively affected the results of slow freezing cryopreservation and vitrification. CONCLUSION: In vitro SA exposure lowered the total amount of intracellular lipids and unsaturation in mouse embryos. The changes were accompanied with a significantly lower efficacy of embryo cryopreservation. https://doi.org/10.54680/fr24110110512.