RESUMO
The exopolymer (ESPp) was obtained from Bacillus licheniformis IDN-EC, composed of a polyglutamic acid and polyglycerol phosphate chain O-substituted with αGal moieties (αGal/αGlcNH2 3:1 molar ratio) and with a 5000 Da molecular weight. The cytotoxicity activity of EPSp was determined by reducing the MTT (3-[4,5-dimethyl-thiazol-2-yl]-2,5-diphenyltetrazolium bromide) to formazan on HeLa cells. This EPS did not show cytotoxicity against the tested cell line. The ESPp presented great advantages as an antioxidant with free radical scavenging activities (1,1-diphenyl-2-picryl-hydrazyl radical (DPPH),hydroxyl radical (OH), and superoxide anion (O2-)) (65 ± 1.2%, 98.7 ± 1.9%, and 97 ± 1.7%), respectively. Moreover, EPSp increased the enzyme activity for catalase (CAT) and glutathione peroxidase (GSH-Px) in HeLa cells (CAT, 2.6 ± 0.24 U/mL; and GSH-Px, 0.75 ± 0.3 U/L). The presence of ESPp showed a significant protective effect against H2O2 in the cell line studied, showing great viability (91.8 ± 2.8, 89.9 ± 2.9, and 93.5 ± 3.6%). The EPSp presented good emulsifying activity, only for vegetable oils, olive oil (50 ± 2.1%) and sesame (72 ± 3%). Sesame was effective compared to commercials products, Triton X-100 (52.38 ± 1.6%), Tween 20 (14.29 ± 1.1%), and sodium dodecyl sulphate (SDS) (52.63 ± 1.6%). Furthermore, the EPS produced at 0.6 M has potential for environmental applications, such as the removal of hazardous materials by emulsification whilst resulting in positive health effects such as antioxidant activity and non-toxicity. EPSp is presented as a good exopolysaccharide for various applications.
Assuntos
Antioxidantes , Bacillus licheniformis , Humanos , Bacillus licheniformis/metabolismo , Células HeLa , Antioxidantes/farmacologia , Antioxidantes/química , Emulsificantes/química , Emulsificantes/farmacologia , Sequestradores de Radicais Livres/farmacologia , Sequestradores de Radicais Livres/química , Catalase/metabolismo , Glutationa Peroxidase/metabolismoRESUMO
BACKGROUND: Reducing production costs while producing high-quality livestock and poultry products is an ongoing concern in the livestock industry. The addition of oil to livestock and poultry diets can enhance feed palatability and improve growth performance. Emulsifiers can be used as potential feed supplements to improve dietary energy utilization and maintain the efficient productivity of broilers. Therefore, further investigation is warranted to evaluate whether dietary emulsifier supplementation can improve the efficiency of fat utilization in the diet of yellow-feathered broilers. In the present study, the effects of adding emulsifier to the diet on lipid metabolism and the performance of yellow-feathered broilers were tested. A total of 240 yellow-feasted broilers (21-day-old) were randomly divided into 4 groups (6 replicates per group, 10 broilers per replicate, half male and half female within each replicate). The groups were as follows: the control group (fed with basal diet), the group fed with basal diet supplemented with 500 mg/kg emulsifier, the group fed with a reduced oil diet (reduced by 1%) supplemented with 500 mg/kg emulsifier, and the group fed with a reduced oil diet supplemented with 500 mg/kg emulsifier. The trial lasted for 42 days, during which the average daily feed intake, average daily gain, and feed-to-gain ratio were measured. Additionally, the expression levels of lipid metabolism-related genes in the liver, abdominal fat and each intestinal segment were assessed. RESULTS: The results showed that compared with the basal diet group, (1) The average daily gain of the basal diet + 500 mg/kg emulsifier group significantly increased (P < 0.05), and the half-even-chamber rate was significantly increased (P < 0.05); (2) The mRNA expression levels of Cd36, Dgat2, Apob, Fatp4, Fabp2, and Mttp in the small intestine were significantly increased (P < 0.05). (3) Furthermore, liver TG content significantly decreased (P < 0.05), and the mRNA expression level of Fasn in liver was significantly decreased (P < 0.05), while the expression of Apob, Lpl, Cpt-1, and Pparα significantly increased (P < 0.05). (4) The mRNA expression levels of Lpl and Fatp4 in adipose tissue were significantly increased (P < 0.05), while the expression of Atgl was significantly decreased (P < 0.05). (5) Compared with the reduced oil diet group, the half-evading rate and abdominal fat rate of broilers in the reduced oil diet + 500 mg/kg emulsifier group were significantly increased (P < 0.05), and the serum level of LDL-C increased significantly (P < 0.05)0.6) The mRNA expression levels of Cd36, Fatp4, Dgat2, Apob, and Mttp in the small intestine were significantly increased (P < 0.05). 7) The mRNA expression levels of Fasn and Acc were significantly decreased in the liver (P < 0.05), while the mRNA expression levels of Lpin1, Dgat2, Apob, Lpl, Cpt-1, and Pparα were significantly increased (P < 0.05). CONCLUSIONS: These results suggest that dietary emulsifier can enhance the fat utilization efficiency of broilers by increasing the small intestinal fatty acid uptake capacity, inhibiting hepatic fatty acid synthesis and promoting hepatic TG synthesis and transport capacity. This study provides valuable insights for the potential use of emulsifier supplementation to improve the performance of broiler chickens.
Assuntos
Ração Animal , Galinhas , Dieta , Suplementos Nutricionais , Emulsificantes , Metabolismo dos Lipídeos , Animais , Galinhas/metabolismo , Metabolismo dos Lipídeos/efeitos dos fármacos , Emulsificantes/farmacologia , Ração Animal/análise , Masculino , Feminino , Dieta/veterinária , Fígado/metabolismo , Fígado/efeitos dos fármacosRESUMO
In this study, we developed a green and multifunctional bioactive nanoemulsion (BBG-NEs) of Blumea balsamifera oil using Bletilla striata polysaccharide (BSP) and glycyrrhizic acid (GA) as natural emulsifiers. The process parameters were optimized using particle size, PDI, and zeta potential as evaluation parameters. The physicochemical properties, stability, transdermal properties, and bioactivities of the BBG-NEs under optimal operating conditions were investigated. Finally, network pharmacology and molecular docking were used to elucidate the potential molecular mechanism underlying its wound-healing properties. After parameter optimization, BBG-NEs exhibited excellent stability and demonstrated favorable in vitro transdermal properties. Furthermore, it displayed enhanced antioxidant and wound-healing effects. SD rats wound-healing experiments demonstrated improved scab formation and accelerated healing in the BBG-NE treatment relative to BBO and emulsifier groups. Pharmacological network analyses showed that AKT1, CXCL8, and EGFR may be key targets of BBG-NEs in wound repair. The results of a scratch assay and Western blotting assay also demonstrated that BBG-NEs could effectively promote cell migration and inhibit inflammatory responses. These results indicate the potential of the developed BBG-NEs for antioxidant and skin wound applications, expanding the utility of natural emulsifiers. Meanwhile, this study provided a preliminary explanation of the potential mechanism of BBG-NEs to promote wound healing through network pharmacology and molecular docking, which provided a basis for the mechanistic study of green multifunctional nanoemulsions.
Assuntos
Antioxidantes , Emulsificantes , Emulsões , Ácido Glicirrízico , Simulação de Acoplamento Molecular , Cicatrização , Cicatrização/efeitos dos fármacos , Animais , Emulsões/química , Emulsificantes/química , Emulsificantes/farmacologia , Ratos , Antioxidantes/farmacologia , Antioxidantes/química , Antioxidantes/síntese química , Ácido Glicirrízico/farmacologia , Ácido Glicirrízico/química , Polissacarídeos/química , Polissacarídeos/farmacologia , Química Verde , Humanos , Ratos Sprague-Dawley , Nanopartículas/química , Óleos de Plantas/química , Óleos de Plantas/farmacologia , Fabaceae/química , Masculino , Tamanho da Partícula , Movimento Celular/efeitos dos fármacosRESUMO
This study investigated the dual potential of Azolla pinnata fern protein hydrolysates (AFPHs) as functional and nutraceutical ingredients in an oil/water emulsion system. The AFPH-stabilised emulsion (AFPH-E) displayed a small and uniform droplet distribution and was stable to aggregation and creaming over a wide range of pH (5-8), salt concentrations ≤ 100 mM, and heat treatment ≤ 70 °C. Besides, the AFPH-E possessed and maintained strong biological activities, including antihypertensive, antidiabetic, and antioxidant, under different food processing conditions (pH 5-8; NaCl: 50-150 mM, and heat treatment: 30-100 °C). Following in vitro gastrointestinal digestion, the antihypertensive and antioxidant activities were unchanged, while a notable increase of 8% was observed for DPPH. However, the antidiabetic activities were partially reduced in the range of 5-11%. Notably, AFPH-E modulated the gut microbiota and short-chain fatty acids (SCFAs), promoting the growth of beneficial bacteria, particularly Bifidobacteria and Lactobacilli, along with increased SCFA acetate, propionate, and butyrate. Also, AFPH-E up to 10 mg mL-1 did not affect the proliferation of the normal colon cells. In the current work, AFPH demonstrated dual functionality as a plant-based emulsifier with strong biological activities in an oil/water emulsion system and promoted healthy changes in the human gut microbiota.
Assuntos
Suplementos Nutricionais , Emulsificantes , Emulsões , Gleiquênias , Microbioma Gastrointestinal , Hidrolisados de Proteína , Humanos , Microbioma Gastrointestinal/efeitos dos fármacos , Emulsões/química , Emulsificantes/farmacologia , Emulsificantes/química , Hidrolisados de Proteína/farmacologia , Hidrolisados de Proteína/química , Gleiquênias/química , Antioxidantes/farmacologia , Hipoglicemiantes/farmacologia , Ácidos Graxos Voláteis/metabolismoRESUMO
In this study, responsive Janus nanospheres were prepared by grafting LMA and DMAEMA monomers on both sides of SiO2 nanospheres using the Pickering emulsion stencil method and RAFT polymerization. The successful synthesis was verified through infrared spectroscopy (FTIR) and thermogravimetric analysis (TGA), scanning electron microscopy (SEM) characterizations. Subsequently, Pickering emulsion was formulated using Janus nanospheres as emulsifiers. The particle size of the emulsion droplets was systematically investigated by manipulating factors such as pH, nanosphere dosage, water to oil ratio, and oil phase polarity. Notably, the Pickering emulsion exhibited responsive properties to pH, temperature, and CO2. Furthermore, Janus nanospheres exhibited excellent emulsification property for real oil phases, including canola oil, kerosene, gasoline, and diesel oil. Building upon this, a smart antibacterial Pickering emulsion was developed using Janus nanospheres, and its inhibition rate against E. coli could reach 100% within 4 h, which would be beneficial for its application in the food field.
Assuntos
Antibacterianos , Emulsões , Escherichia coli , Nanosferas , Tamanho da Partícula , Emulsões/química , Nanosferas/química , Antibacterianos/farmacologia , Antibacterianos/química , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Dióxido de Silício/química , Concentração de Íons de Hidrogênio , Emulsificantes/química , Emulsificantes/farmacologiaRESUMO
Gut microbial homeostasis is crucial for the health of cognition in elderly. Previous study revealed that polysorbate 80 (P80) as a widely used emulsifier in food industries and pharmaceutical formulations could directly alter the human gut microbiota compositions. However, whether long-term exposure to P80 could accelerate age-related cognitive decline via gut-brain axis is still unknown. Accordingly, in this study, we used the senescence accelerated mouse prone 8 (SAMP8) mouse model to investigate the effects of the emulsifier P80 intake (1 % P80 in drinking water for 12 weeks) on gut microbiota and cognitive function. Our results indicated that P80 intake significantly exacerbated cognitive decline in SAMP8 mice, along with increased brain pathological proteins deposition, disruption of the blood-brain barrier and activation of microglia and neurotoxic astrocytes. Besides, P80 intake could also induce gut microbiota dysbiosis, especially the increased abundance of secondary bile acids producing bacteria, such as Ruminococcaceae, Lachnospiraceae, and Clostridium scindens. Moreover, fecal microbiota transplantation from P80 mice into 16-week-old SAMP8 mice could also exacerbated cognitive decline, microglia activation and intestinal barrier impairment. Intriguingly, the alterations of gut microbial composition significantly affected bile acid metabolism profiles after P80 exposure, with markedly elevated levels of deoxycholic acid (DCA) in serum and brain tissue. Mechanically, DCA could activate microglial and promote senescence-associated secretory phenotype production through adenosine triphosphate-binding cassette transporter A1 (ABCA1) importing lysosomal cholesterol. Altogether, the emulsifier P80 accelerated cognitive decline of aging mice by inducing gut dysbiosis, bile acid metabolism alteration, intestinal barrier and blood brain barrier disruption as well as neuroinflammation. This study provides strong evidence that dietary-induced gut microbiota dysbiosis may be a risk factor for age-related cognitive decline.
Assuntos
Barreira Hematoencefálica , Disfunção Cognitiva , Disbiose , Emulsificantes , Microbioma Gastrointestinal , Polissorbatos , Animais , Camundongos , Microbioma Gastrointestinal/efeitos dos fármacos , Polissorbatos/farmacologia , Disfunção Cognitiva/metabolismo , Disfunção Cognitiva/induzido quimicamente , Emulsificantes/metabolismo , Emulsificantes/farmacologia , Disbiose/metabolismo , Barreira Hematoencefálica/metabolismo , Barreira Hematoencefálica/efeitos dos fármacos , Envelhecimento/metabolismo , Encéfalo/metabolismo , Encéfalo/efeitos dos fármacos , Masculino , Microglia/metabolismo , Microglia/efeitos dos fármacos , Eixo Encéfalo-Intestino/efeitos dos fármacos , Cognição/efeitos dos fármacos , Ácidos e Sais Biliares/metabolismoRESUMO
Polysaccharides are a prominent choice in the realm of food-grade oral delivery systems due to their resistance to degradation by digestive enzymes in the oral, gastric, and small intestinal environments, as well as their ease of production, cost-effectiveness, and potential health benefits as prebiotics. Furthermore, their ability to respond to pH-induced dissolution, along with their emulsifying properties, can be strategically employed to achieve precise targeting of lipophilic bioactives to the small intestine. In this study, citrus peel pectin and alginate served as stabilizers for emulgel particles without supplementary emulsifiers or gelling agents. Within this system, pectin functioned as an emulsifier, while alginate acted as a gelling agent, facilitated by Ca2+-induced ionic crosslinking. The synergistic interplay between pectin and alginate efficiently protected curcumin in gastric conditions and controlled dissolution in the small intestine, depending on the pectin/alginate ratio. These controlled phenomena facilitated lipolysis, curcumin release, and ultimately enhanced curcumin bioaccessibility. Furthermore, once the emulgel particle released all the entrapped curcumin in the small intestine, residual polysaccharides underwent facile degradation by pectinase and alginate lyase, yielding fermentable monosaccharides. This confirms the potential of the emulgel particles for use as a prebiotic in the colon. These findings offer significant promise for enhancing the systematic design of food-grade delivery systems that encapsulate lipophilic bioactives, achieving controlled release, enhanced stability, and improved bioaccessibility. Importantly, this system can comprise components that undergo complete digestion, absorption, and utilization in the human body, encompassing materials such as oil, nutraceuticals, and prebiotics, all without presenting health risks.
Assuntos
Citrus , Curcumina , Humanos , Alginatos , Pectinas , Polissacarídeos , Emulsificantes/farmacologia , Intestino DelgadoRESUMO
Emulsifiers are essential for achieving a homogenous distribution of lipophilic supplements in in vitro rumen fluid incubations. Since emulsifiers can alter rumen fermentation, it is crucial to select one that minimally impacts fermentation parameters to reduce potential biases. This study aimed to evaluate seven emulsifiers' impact on in vitro ruminal fermentation using the Hohenheim Gas Test in order to identify the most inert emulsifier. Rumen fluids were collected from three non-lactating Original Brown-Swiss cannulated cows before morning feeding and incubated for 24 h with a basal diet in triplicates. The emulsifiers tested were ethanol, ethyl acetate, propylene glycol, glycerol, ethylene glycol, soy lecithin, and Tween® 80, each in two dosages (0.5% or 1% v/v). The untreated basal diet served as control. Compared to control, in vitro organic matter digestibility was enhanced by ethyl acetate (by 36.9 and 48.2%), ethylene glycol (by 20.6 and 20.1%), glycerol (by 46.9 and 56.8%) and soy lecithin (by 19.7 and 26.8%) at 0.5 and 1% dosage, respectively. Additionally, the 24-h methane production increased for ethanol (by 41.9 and 46.2%), ethylene glycol (by 50.5 and 51.5%), and glycerol (by 63.1 and 65.4%) for the 0.5 and 1% dosage, respectively, and 0.5% dosage for ethyl acetate (by 31.6%). The acetate molar proportion was 17.2%pt higher for ethyl acetate, and 25.5%pt lower for glycerol at 1% dosage, compared to the control. The propionate concentration was 22.1%pt higher 1% glycerol, and 15.2%pt and 15.1%pt higher for 0.5 and 1% propylene glycol, respectively, compared to the control. In summary, Tween® 80 did not significantly affect in vitro rumen fermentation parameters, making it the most suitable choice for in vitro incubations involving lipophilic substances in rumen fluid. Ethanol may be considered as an alternative emulsifier if methane production is not the variable of interest.
Assuntos
Emulsificantes , Fermentação , Polissorbatos , Rúmen , Animais , Rúmen/metabolismo , Bovinos , Polissorbatos/farmacologia , Polissorbatos/química , Emulsificantes/química , Emulsificantes/farmacologia , Feminino , Ração Animal/análiseRESUMO
Supplementation of a combination of lysolecithin, a synthetic emulsifier, and monoglycerides (LEX) in liquid and dry form to broiler diets with different energy levels was investigated to determine their effect on performance, litter quality and subsequent occurrence of footpad lesions. One thousand two hundred and forty-eight-day-old Ross 308 broilers were assigned to 1 of 6 treatments for a 42-day study: a basal diet with a normal energy content (NE); NE + 300 g/t LEX in liquid form (LEL); NE + 500 g/t LEX in dry form (LED); a basal diet with low energy (LE, -90 kcal/kg starter, -100 kcal/kg grower, finisher), LE + 300 g/t LEL and a LE + 500 g/t LED. Each treatment consisted of 13 pens of 16 birds each. Diets were fed in 3 phases (starter d 0-10, grower d 11-21, finisher d 22-42). Feed intake and weight were measured on d 0, 10, 21, and 42. On d 42 a litter sample was collected from each pen and 2 birds per pen were assessed for footpad lesions and breast scald. Data were analyzed using JMP 16, with means separation achieved using Tukey's HSD; significance was assumed at P < 0.05. Results showed a higher (P < 0.05) cumulative bodyweight gain with LEX supplementation (NE CON = 2,718 g, NE+LED = 2,829, NE+LEL = 2,895, LE CON = 2,722, LE+LED = 2,787, LE+LEL = 2,893; P = 0.0027). An increased feed intake was observed for the LE diets, however cumulative FCR of LE+LED and LE+LEL remained equal to the NE control (1.657 NE CON, 1.657 LE+LED, 1.623 LE+LEL; P > 0.05), suggesting LEX enabled the birds to compensate for the energy gap. Litter dry matter was significantly improved with both LED and LEL supplementation compared to the control groups, and resulted in lower (P < 0.05) occurrence and severity of footpad lesions and breast scalds. Considering the income over feed cost (IOFC) of the NE treatment as the reference point for comparison, all other treatments improved profitability, with NE+LEL and LE+LEL achieving the greatest IOFC with 154.58 and 175.96 /1,000 birds respectively. In conclusion, feeding broilers a combination of lysophospholipids, a synthetic emulsifier and monoglycerides resulted in improved bird performance. The use of the LEX also improved litter quality and footpad health, therefore improving animal welfare indicators such as breast scald and footpad measurements.
Assuntos
Suplementos Nutricionais , Lisofosfatidilcolinas , Animais , Galinhas , Monoglicerídeos/farmacologia , Dieta/veterinária , Nutrientes , Emulsificantes/farmacologia , Ração Animal/análise , Fenômenos Fisiológicos da Nutrição AnimalRESUMO
High water activity oil-in-water emulsions can promote survival and growth of Salmonella Typhimurium. Nevertheless, the precise effect of emulsifier type and oil content on bacterial growth and inactivation is not fully understood. Here, emulsions were prepared using different emulsifiers (Tween 20, Tween 80, and Triton X-100) and different oil fractions (20%, 40%, and 60% (v/v)). TSB (control), emulsifier solutions, and emulsions were inoculated with S. Typhimurium. Bacterial growth rate was measured at 7, 22, and 37°C, whereas thermal inactivation was performed at 55°C. Growth and inactivation data was fitted into Logistic and Weibull models, respectively. At an incubation temperature of 37°C, the presence of high amount of oil (60%) in Tween 20 and Triton X stabilized emulsions extended the lag phase (5.83 ± 2.20 and 9.43 ± 1.07 h, respectively, compared to 2.28 ± 1.54 h for TSB, p < 0.05), whereas individual emulsifiers had no effect on growth behavior compared to TSB. This effect was also prevalent but attenuated at 22°C, whereas no growth was observed at 7°C. In thermal inactivation, we observed protective effect in Tween 80 and Triton X-100 solutions, where time required for five-log reduction was 1914.70 ± 706.35 min and 795.34 ± 420.09 min, respectively, compared to 203.89 ± 10.18 min for TSB (p < 0.05). Interestingly, the presence of high amount of oil did not offer protective effect during thermal inactivation. We hypothesize that oleic acid in Tween 80 and lower hydrophobicity value of Triton X-100 help maintain membrane integrity and improve the resistance of bacteria to heat inactivation.
Assuntos
Polissorbatos , Salmonella typhimurium , Emulsões , Polissorbatos/farmacologia , Octoxinol , Emulsificantes/farmacologia , ÁguaRESUMO
In the last few decades, there has been a growing interest in understanding the mechanisms involved in lipid digestion with the purpose of developing strategies to control this complex physiological process. Bile salts (BS) are natural bio-surfactants that play crucial functions in this process and may represent a key strategy to modulate the lipolysis. One of the main functions is the removal of lipolysis products present at the interface of lipid droplets by solubilizing them in BS micelles, thus avoiding the reaction inhibition. However, there are few studies that analyzed the effects that could have the emulsion components on the solubilization capacity of BS micelles. Thus, the main purpose of the present work was to evaluate the impact of a typical food emulsifier (Tween 80) on the fatty acid (FA) solubilization capacity of BS micelles by using a method recently developed, involving a combination of turbidity and dynamic light scattering (DLS) determinations. As FA solubilization into BS micelles may strongly affect the kinetics of lipolysis, the lipolysis of T80-stabilized oil-in-water (O/W) emulsions was also studied. The results showed that a higher concentration of the emulsifier in the duodenal medium causes the lipolysis rate to be maximum for a longer time. The mechanism involved could be the contribution of T80 to increase the solubilization of FA (and possibly other products of the lipolysis) in the duodenal medium, consequently affecting the potential bioavailability of fatty acids.
Assuntos
Lipólise , Micelas , Ácidos e Sais Biliares , Emulsificantes/farmacologia , Emulsões , Ácidos Graxos , Ácido Oleico , Polissorbatos , ÁguaRESUMO
Glycolipids are a group of sugar-containing lipids with versatile functions. In this study, a natural glycolipid product was obtained from soy lecithin, and its emulsifying, oil-gelling, antibacterial and antiviral properties were investigated. A silica-based extraction method on a preparative scale was used to recover the glycolipid product (GLP) from soy lecithin. The GLP consisted of three different glycolipid classes: acylated sterol glucoside (64.16%), sterol glucoside (25.57%) and cerebroside (6.71%). As an emulsifier, the GLP was able to form a stable water-in-oil emulsion. The GLP exhibited a good oil-gelling property, capable of gelling rapeseed oil at a concentration of 6%. For the investigated microorganisms (Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus), the GLP did not show any antibacterial effects. The GLP exerted antiviral activity against lentivirus, but not adenovirus. The results of this study help in enriching the knowledge on the properties of naturally occurring glycolipids, which may find potential applications in the food, pharmaceutical and related industries.
Assuntos
Anti-Infecciosos , Produtos Biológicos , Glicolipídeos , Tensoativos , Adenoviridae/efeitos dos fármacos , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Bactérias/efeitos dos fármacos , Produtos Biológicos/química , Produtos Biológicos/farmacologia , Emulsificantes/química , Emulsificantes/farmacologia , Glicolipídeos/química , Glicolipídeos/farmacologia , Lentivirus/efeitos dos fármacos , Óleo de Brassica napus/química , Tensoativos/química , Tensoativos/farmacologiaRESUMO
Non-ionic emulsifiers have been continuous research focus in skin analysis. With the aim of finding their role as penetration enhancers in dermal drug delivery systems, PEGylated emulsifiers of polyethylene glycol (PEG) ethers were targeted to be investigated ex-vivo. The effectiveness of them in the enhancement of skin penetration was examined by conventional tape stripping method and confocal Raman spectroscopy (CRS). Fluorescein sodium salt (Fluo-Na) and procaine HCl were respectively used as model drugs. The drug delivery performances were compared in the aspects of penetration amount and depth. Based on the results from both analyses, all investigated emulsifiers have the ability to enhance the amount of drug penetration. PEG-20 ethers showed higher ability than PEG-2 oleyl ether (O2) in promoting drug distribution by depth, especially PEG-20 cetyl ether (C20) showed a distinct effect. According to this study, their penetration enhancing performances seem to be linked to their interruption of intercellular lipids, which can be considered as the underlying mechanism for governing the ability of PEGylated emulsifiers as penetration enhancers. Further instrumental comparison highlighted the benefits of using CRS as an alternative in skin penetration analysis.
Assuntos
Emulsificantes/farmacologia , Óleos de Plantas/farmacologia , Polietilenoglicóis/farmacologia , Absorção Cutânea , Espectrometria de Fluorescência/métodos , Análise Espectral Raman/métodos , Animais , Sistemas de Liberação de Medicamentos/métodos , Metabolismo dos Lipídeos/efeitos dos fármacos , Pele/efeitos dos fármacos , Absorção Cutânea/efeitos dos fármacos , Absorção Cutânea/fisiologia , Tensoativos/farmacologia , SuínosRESUMO
Pectin is widely used in food and pharmaceutical industries. However, due to its polysaccharide nature it lacks antimicrobial activity. In the current work, new pectin derivatives with interesting optical and antimicrobial properties were prepared via supramolecular chemistry utilizing Fe- or Cu-terpyridine (Tpy-Fe and Tpy-Cu) motifs. To proof derivatization of pectin, ultraviolet-visible spectroscopy (UV-Vis) and Fourier Transform infrared (FTIR) were used. In addition, the prepared pectin derivatives retained the known emulsification activity of the non-modified sugar beet pectin as seen from the particle size analysis of oil-in-water emulsions. The prepared derivatives showed antibacterial activity toward selected Gram-positive and Gram-negative bacteria. In addition, cytotoxicity test showed that the Tpy-Fe-pectin derivative was non-toxic to cells of human hepatocarcinoma, breast adenocarcinoma MCF7, and colorectal carcinoma cells at concentrations up to 100 µg/ml, while Tpy-Cu-pectin had moderate toxicity toward the aforementioned cells at the same concentration levels. The prepared derivatives could have potential applications in emulsions with antibacterial activity.
Assuntos
Antibacterianos/farmacologia , Complexos de Coordenação/farmacologia , Emulsificantes/farmacologia , Pectinas/farmacologia , Piridinas/farmacologia , Antibacterianos/síntese química , Antibacterianos/toxicidade , Beta vulgaris/química , Linhagem Celular Tumoral , Complexos de Coordenação/síntese química , Complexos de Coordenação/toxicidade , Cobre/química , Cobre/toxicidade , Emulsificantes/síntese química , Emulsificantes/toxicidade , Escherichia coli/efeitos dos fármacos , Humanos , Ferro/química , Ferro/toxicidade , Ligantes , Testes de Sensibilidade Microbiana , Pectinas/síntese química , Pectinas/toxicidade , Piridinas/síntese química , Piridinas/toxicidade , Staphylococcus aureus/efeitos dos fármacosRESUMO
Pantoea alhagi exopolysaccharides (PAPS) have been shown to enhance crop resistance to abiotic stress. However, physicochemical properties and structure of PAPS have not yet been analyzed. In this study, two PAPSs, named PAPS1 and PAPS2, were isolated and purified from the P. alhagi NX-11. The results showed PAPS1 and PAPS2 were composed of glucose, galactose, glucuronic acid, glucosamine and mannose with average molecular weight of 1.326 × 106 Da and 1.959 × 106 Da, respectively. Moreover, the structure of PAPS1 and PAPS2 was investigated by FT-IR and NMR analysis. PAPS1 was identified to have the backbone structure of â4)-ß-D-GlcpA-(1â2)-α-D-Galp-(1â3)-ß-D-Galp-(1â3)-ß-D-GlcpN- (1â3)-α-D-Galp-(1â3)-ß-D-Galp-(1â. PAPS2 had the backbone structure of â4)-ß-D-GlcpA-(1â2)-α-D-Galp-(1â3)-ß-D-Glcp-(1â3)-ß-D-GlcpN-(1â3)-α-D-Galp-(1â3)-α-D-GlcpN-(1â. In addition, PAPS1 and PAPS2 had moderate antioxidant and emulsifying capacities. Overall, the structure analysis of PAPS may point out the direction for the subsequent study of PAPS-mediated microbial and plant interactions, and further exploration of the application of PAPS.
Assuntos
Antioxidantes , Emulsificantes , Pantoea/química , Polissacarídeos Bacterianos , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Emulsificantes/química , Emulsificantes/isolamento & purificação , Emulsificantes/metabolismo , Emulsificantes/farmacologia , Fermentação , Hidrólise , Estrutura Molecular , Pantoea/metabolismo , Polissacarídeos Bacterianos/química , Polissacarídeos Bacterianos/isolamento & purificação , Polissacarídeos Bacterianos/metabolismo , Polissacarídeos Bacterianos/farmacologiaRESUMO
Breastfed infants have higher intestinal lipid absorption and neurodevelopmental outcomes compared to formula-fed infants, which may relate to a different surface layer structure of fat globules in infant formula. This study investigated if dairy-derived emulsifiers increased lipid absorption and neurodevelopment relative to soy lecithin in newborn preterm piglets. Piglets received a formula diet containing soy lecithin (SL) or whey protein concentrate enriched in extracellular vesicles (WPC-A-EV) or phospholipids (WPC-PL) for 19 days. Both WPC-A-EV and WPC-PL emulsions, but not the intact diets, increased in vitro lipolysis compared to SL. The main differences of plasma lipidomics analysis were increased levels of some sphingolipids, and lipid molecules with odd-chain (17:1, 19:1, 19:3) as well as mono- and polyunsaturated fatty acyl chains (16:1, 20:1, 20:3) in the WPC-A-EV and WPC-PL groups and increased 18:2 fatty acyls in the SL group. Indirect monitoring of intestinal triacylglycerol absorption showed no differences between groups. Diffusor tensor imaging measurements of mean diffusivity in the hippocampus were lower for WPC-A-EV and WPC-PL groups compared to SL indicating improved hippocampal maturation. No differences in hippocampal lipid composition or short-term memory were observed between groups. In conclusion, emulsification of fat globules in infant formula with dairy-derived emulsifiers altered the plasma lipid profile and hippocampal tissue diffusivity but had limited effects on other absorptive and learning abilities relative to SL in preterm piglets.
Assuntos
Emulsificantes/farmacologia , Alimentos Formulados , Lecitinas/farmacologia , Fosfolipídeos/farmacologia , Proteínas do Soro do Leite/farmacologia , Fenômenos Fisiológicos da Nutrição Animal/efeitos dos fármacos , Animais , Animais Recém-Nascidos/crescimento & desenvolvimento , Encéfalo/crescimento & desenvolvimento , Hipocampo/crescimento & desenvolvimento , Lipidômica , Lipídeos/sangue , Lipólise/efeitos dos fármacos , Glycine max/química , SuínosRESUMO
Erythorbyl myristate (EM), a potential multi-functional food emulsifier, was newly synthesized by immobilized lipase-catalyzed esterification between antioxidative erythorbic acid and antibacterial myristic acid. The yield and productivity of EM were 56.13 ± 2.51 mg EM/g myristic acid and 1.76 ± 0.08 mM/h, respectively. The molecular structure of EM was identified as (R)-2-((R)-3,4-dihydroxy-5-oxo-2,5-dihydrofuran-2-yl)-2-hydroxyethyl tetradecanoate using HPLC-ESI/MS and 2D [1H-1H] NMR COSY. The hydrophilic-lipophilic balance of EM was 11.5, suggesting that EM could be proper to stabilize oil-in-water emulsions. Moreover, isothermal titration calorimetry demonstrated the micellar thermodynamic behavior of EM and determined its critical micelle concentration (0.36 mM). In terms of antioxidative property, EM exhibited the radical scavenging activity against DPPH (EC50: 35.47 ± 0.13 µM) and ABTS (EC50: 36.45 ± 1.98 µM) radicals. Finally, EM showed bacteriostatic and bactericidal activities against Gram-positive foodborne pathogens (minimum inhibitory concentration: 0.06-0.60 mM; minimum bactericidal concentration: 0.07-0.93 mM).
Assuntos
Ácido Ascórbico/química , Emulsificantes/química , Emulsificantes/farmacologia , Ácido Mirístico/química , Antibacterianos/química , Antibacterianos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Cromatografia Líquida de Alta Pressão , Emulsificantes/síntese química , Esterificação , Microbiologia de Alimentos , Alimento Funcional , Lipase/química , Lipase/metabolismo , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Estrutura Molecular , Espectrometria de Massas por Ionização por Electrospray , Estereoisomerismo , TermodinâmicaRESUMO
Three phenolic acids including p-hydroxybenzoic acid (PHBA), 3,4-dihydroxybenzoic acid, (DHBA), and gallic acid (GA) were grafted onto native pectin (Na-Pe) through enzymatic method. Ultraviolet-visible spectrometry, Fourier transform infrared spectroscopy, and 1H NMR analyses were used to explore the reaction mechanism. Results indicated that the p-hydroxyl of the phenolic acids reacted with the methoxycarbonyl of pectin through transesterification, and a covalent connection was formed. The phenolic acid contents of PHBA modified pectin (Ph-Pe), DHBA modified pectin (Dh-Pe), and GA modified pectin (Ga-Pe) were 20.18%, 18.87%, and 20.32%, respectively. After acylation with phenolic acids, the 1,1-diphenyl-2-picryl hydrazine clearance of pectin changed from 7.68% (Na-Pe) to 6.88% (Ph-Pe), 40.80% (Dh-Pe), and 90.30% (Ga-Pe), whereas its inhibition ratio of pectin increased from 3.11% (Na-Pe) to 35.02% (Ph-Pe), 66.36% (Dh-Pe), and 77.89% (Ga-Pe). Moreover, compared with Na-Pe, modified pectins exhibited better emulsification properties and stronger antibacterial activities against both Escherichia coli and Staphylococcus aureus.
Assuntos
Ácido Gálico/química , Hidroxibenzoatos/química , Parabenos/química , Pectinas/farmacologia , Acilação , Antibacterianos/química , Antibacterianos/farmacologia , Emulsificantes/química , Emulsificantes/farmacologia , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Esterificação , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Viabilidade Microbiana/efeitos dos fármacos , Pectinas/química , Sódio/química , Espectroscopia de Infravermelho com Transformada de Fourier , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/crescimento & desenvolvimentoRESUMO
BACKGROUND: Curcumin was found to accelerate gastric ulcer healing by the main mechanism, i.e., the suppression of iNOS mediated inflammation. Although Tetrahydrocurcumin (THC) is claimed to be an active antioxidant element of curcumin, its antiulcer activity has not been systematically examined. The utility of Self-Microemulsifying Drug Delivery Systems (SMEDDSs) for curcumin and THC formulations in the liquid form was also found to increase the rate and extent of release of curcumin- and THC-SMEDDS. Nevertheless, the beneficial antiulcer effect of these nanoproducts has not yet been evaluated. OBJECTIVE: This study aimed to evaluate and compare the antiulcer efficacy of curcumin- and THCSMEDDS through the inhibition of the iNOS/NO system in the rat model. METHODS: Antiulcer efficacy was compared in terms of the ability to accelerate healing of gastric ulcer including the efficient inhibitory action on inflammatory NO production in activated macrophages and iNOS mRNA expression at the ulcerated area. RESULTS: THC was found to have less ulcer healing capacity than curcumin with a lack of significant inhibitory effect on the iNOS/NO system. The SMEDDS used in the study significantly increased the inhibitory efficacy of THC on iNOS/NO production and iNOS mRNA expression compared to the inhibitory potency of curcumin. An oral administration of curcumin- or THC-SMEDDS once a day was appropriate for exerting a comparable curative efficacy to a twice-daily oral administration of curcumin or THC. CONCLUSION: The SMEDDS used in the study was observed to enhance the inhibitory efficacy of the antiulcer drug on the iNOS/NO system, leading to a reduction of daily dosing and dosing frequency.
Assuntos
Curcumina/análogos & derivados , Curcumina/uso terapêutico , Emulsificantes/uso terapêutico , Óxido Nítrico Sintase Tipo II/antagonistas & inibidores , Óxido Nítrico/antagonistas & inibidores , Úlcera Gástrica/tratamento farmacológico , Administração Oral , Animais , Curcumina/farmacologia , Composição de Medicamentos/métodos , Emulsificantes/farmacologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Masculino , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Ratos , Ratos Wistar , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/metabolismoRESUMO
This study presents a method for modifying pectin with phenolic acids catalyzed by lipase in a two-phase system of water/tetrahydrofuran. Salicylic acid (SA) and its isomers, including m-hydroxybenzoic acid (MHBA) and p-hydroxybenzoic acid (PHBA), were grafted onto pectin, and the products were characterized via UV-vis, Fourier transform infrared spectroscopy (FTIR), and 1H NMR analyses to explore the reaction process and mechanism between pectin and the three phenolic acids. Results indicated that lipase played a dual role in the reaction, namely, catalyzing the hydrolysis of the methyl group in the aqueous phase and esterifying the carboxyl group of pectin with the phenolic hydroxyl group of the phenolic acids in tetrahydrofuran. The grafting ratio of SA-modified pectin, MHBA-modified pectin, and PHBA-modified pectin was 1.89, 10.58, and 20.32%, respectively, and it was affected by the position of phenolic hydroxyl. Moreover, the effects of phenolic acids on the emulsifying properties, antioxidant activities, and antibacterial activities of the native and modified pectins were evaluated. In several aspects, the emulsifying properties of the modified pectins were better than those of native pectin. Moreover, the grafting of phenolic acids only slightly affected the 1,1-diphenyl-2-picryl hydrazine (DPPH) clearance of the modified pectins but substantially improved their inhibition ratio in a ß-carotene bleaching assay. Furthermore, the modified pectins exhibited better bacteriostatic activity against both Escherichia coli and Staphylococcus aureus than native pectin.