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The onset and progression of ulcerative colitis (UC) are intricately linked to the worsening of intestinal inflammation, an imbalance in oxidative stress, and impairment of the intestinal mucosal barrier. Although chlorogenic acid (CA) shows potential in effectively alleviating the symptoms of UC, its clinical application is hindered by its poor bioavailability, stability, rapid metabolism, and quick excretion. This study utilized a one-step enzyme-catalyzed polymerization technique to create chlorogenic acid nanoparticles (CA NPs), aiming to improve the bioavailability and stability of CA. The CA NPs exhibited an optimal nanosize (106.65 ± 4.12 nm) and showed increased cellular uptake over time. Importantly, CA NPs significantly prolonged retention time in inflamed colonic tissues, enhancing accumulation and providing a targeted therapy for UC. Animal studies confirmed the substantial benefits of CA NPs, including reduced weight loss, lessened reduction in colon length, and a lowered disease activity index (DAI) score in DSS-induced UC mice. Moreover, CA NPs effectively reduced oxidative stress and levels of inflammatory factors in the colonic tissues of UC mice, thus mitigating tissue damage and restoring the integrity of the intestinal mucosal barrier. In conclusion, our research proposes a novel approach to increase the bioavailability and stability of CA, offering a promising avenue for its effective application in preventing UC.
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Incorporating polysaccharide-based composite films with nanobiotechnology offers a new strategy for food preservation. This study initially focuses on the preparation of tea polyphenol nanoparticles (TPNP), novel and derived from natural antibacterial agents, which serve to improve stability. Afterwards chitosan-based composite films loaded with TPNP (CTN film) were developed using solution casting method. The incorporation of TPNP significantly improved the UV/water/oxygen barrier properties, mechanical properties and thermal stability, alongside notable physical properties including water contact angle (93.65 ± 0.04°), low water vapor permeability (33.72 ± 3.32 g/m2h) and oxygen permeability (0.11 ± 0.02 g/m2h), tensile strength (61.83 ± 0.70 %), and elongation at break (31.60 ± 6.12 %). The CTN film not only exhibited exceptional biodegradability and nontoxicity, but also demonstrated remarkable antimicrobial efficacy against Escherichia coli and Bacillus subtilis. Additionally, it showcased potent antioxidant activity, boasting DPPH and ABTS radical scavenging rates up to 89.25 ± 0.18 % and 93.84 ± 0.42 %. The CTN film was successfully formed on the surface of strawberries through dip-coating process and their shelf life was extended from 4 to 6 days at 20 °C without side-effect on the weight loss, harness, pH and total soluble solids, illustrating its potential for enhancing food preservation.
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Antioxidantes , Quitosana , Conservação de Alimentos , Fragaria , Nanopartículas , Polifenóis , Chá , Quitosana/química , Quitosana/farmacologia , Polifenóis/química , Polifenóis/farmacologia , Nanopartículas/química , Fragaria/química , Conservação de Alimentos/métodos , Chá/química , Antioxidantes/farmacologia , Antioxidantes/química , Antibacterianos/farmacologia , Antibacterianos/química , Escherichia coli/efeitos dos fármacos , Embalagem de Alimentos/métodos , Permeabilidade , Bacillus subtilis/efeitos dos fármacos , Resistência à TraçãoRESUMO
Metal-organic frameworks (MOFs) offer diverse applications in the food industry, facilitating loading, protection, and controlled release of functional ingredients despite encountering loading capacity and functional activity limitations. This study focuses on curcuminzinc MOFs, harnessing curcumin's renowned health benefits and zinc to enhance pharmacological properties. We evaluated their synthesis efficiency, stability under varying conditions (pH, salt concentration, temperature), loading and antioxidant capacity. The results showed that microwave synthesis yielded MOFs with a 23.2 ± 4.5% yield, stable within pH 4-10, gradually decomposing in PBS. DPPH, ABTS, and H2O2 assays revealed varying free radical scavenging abilities. MOFs disintegrate in either acidic environments or contain H2O2 (at a concentration threshold of 10 µM). Post-disintegration, these MOFs significantly inhibiting the secretion of TNF-α by RAW264.7 cells induced by LPS. These findings highlight the potential of novel curcuminzinc MOF materials for nutrient delivery, addressing challenges in effectively delivering functional ingredients.
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Spirulina protein (SP) is recognized as a nutritious edible microbial protein and holds potential as a natural emulsifier. Due to the inherent challenges SP faces in stabilizing high internal phase emulsions (HIPEs), ultrasonic techniques were utilized for modification. Noticeable alterations in the structural and functional properties of SP were observed following ultrasonic treatment at various power levels (0, 100, 300, and 500 W). Ultrasound treatment disrupted non-covalent interactions within the protein polymer structure, leading to the unfolding of molecular structures and the exposure of hydrophobic groups. Importantly, the particle size of SP was reduced the most at an ultrasonic power of 300 W, and the three-phase contact angle reached its peak at 84.3°. The HIPEs stabilized by SP modified with 300 W ultrasonication have high apparent viscosity and modulus values and strong storage stability under different environmental conditions. Additionally, the encapsulation of curcumin in HIPEs led to improved retention of curcumin across various settings. The bioavailability increased to 35.36, which is 2.8 times higher than the pure oil. These findings suggest that ultrasound-modified SP is a promising emulsifier for HIPEs, and is expected to encapsulate hydrophobic nutrients such as curcumin more effectively.
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Cyclodextrin-based metal-organic framework (CD-MOF) has been widely used in various delivery systems due to its excellent edibility and high drug loading capacity. However, its typically bulky size and high brittleness in aqueous solutions pose significant challenges for practical applications. Here, we proposed an ultrasonic-assisted method for rapid synthesis of uniformly-sized nanoscale CD-MOF, followed by its hydrophobic modification through ester bond cross-linking (Nano-CMOF). Proper ultrasound treatment effectively reduced particle size to nanoscale (393.14 nm). Notably, carbonate ester cross-linking method significantly improved water stability without altering its cubic shape and high porosity (1.3 cm3/g), resulting in a retention rate exceeding 90% in various media. Furthermore, the loading of quercetin did not disrupt cubic structure and showcased remarkable storage stability. Nano-CMOF achieved controlled release of quercetin in both aqueous environments and digestion. Additionally, Nano-CMOF demonstrated exceptional antioxidant (free radical scavenging 82.27%) and biocompatibility, indicating its significant potential as novel nutritional delivery systems in food and biomedical fields.
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Ciclodextrinas , Preparações de Ação Retardada , Portadores de Fármacos , Interações Hidrofóbicas e Hidrofílicas , Estruturas Metalorgânicas , Quercetina , Quercetina/química , Estruturas Metalorgânicas/química , Ciclodextrinas/química , Portadores de Fármacos/química , Preparações de Ação Retardada/química , Nanopartículas/química , Materiais Biocompatíveis/química , Tamanho da Partícula , Humanos , Estabilidade de MedicamentosRESUMO
Oral targeted anti-inflammatory drugs have garnered significant interest in treating ulcerative colitis (UC) due to their potential in reducing medical costs and enhancing treatment efficacy. Magnolol (Mag), a natural anti-inflammatory compound, has demonstrated protective effects against UC. However, its application as an alternative therapeutic agent for UC is limited by poor gastrointestinal stability and inadequate accumulation at inflamed colonic lesions. This study introduces a novel nanoparticle (NPs) formulation based on Mag, functionalized with hyaluronic acid (HA) for targeted UC therapy. Bovine serum albumin (BSA) was modified with 2-thiamine hydrochloride to synthesize BSA·SH. Thiol-ene click reaction with Mag led to the formation of BSA·SH-Mag NPs, which were further modified with HA through dehydration condensation, regular spherical inflammation-targeting HA-BSA·SH-Mag nanoparticles with a charge of -23.6 mV and a particle size of 403 ± 4 nm were formed. In vitro studies revealed significant macrophage targeting and enhanced uptake by colon epithelial cells. Oral administration of HA-BSA·SH-Mag facilitated colon mucosal barrier repair by modulating pro-inflammatory cytokines (TNF-α, IL-6, IL-1ß), anti-inflammatory cytokines (IL-10), and tight junction proteins (ZO-1, Claudin, Occludin). Crucially, HA-BSA·SH-Mag was found to inhibit the JAK2/STAT3/NF-κB signaling pathway, reducing DSS-induced colon tissue inflammation. This research provides valuable insights into the oral use of natural compounds in UC therapy, highlighting the therapeutic potential of HA-BSA·SH-Mag NPs.
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Compostos de Bifenilo , Colite Ulcerativa , Ácido Hialurônico , Lignanas , Nanopartículas , Colite Ulcerativa/tratamento farmacológico , Nanopartículas/química , Ácido Hialurônico/química , Ácido Hialurônico/farmacologia , Lignanas/química , Lignanas/farmacologia , Animais , Compostos de Bifenilo/química , Camundongos , Soroalbumina Bovina/química , Humanos , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Citocinas/metabolismo , Masculino , Colo/patologia , Colo/efeitos dos fármacos , Colo/metabolismoRESUMO
In the contemporary era, heightened emphasis on health and safety has emerged as a paramount concern among individuals with food. The concepts of "natural" and "green" have progressively asserted dominance in the food consumption market. Consequently, through continuous exploration and development, an escalating array of natural bioactive ingredients is finding application in both nutrition delivery and the broader food industry. Chlorogenic acid (CGA), a polyphenolic compound widely distributed in various plants in nature, has garnered significant attention. Abundant research underscores CGA's robust biological activity, showcasing notable preventive and therapeutic efficacy across diverse diseases. This article commences with a comprehensive overview, summarizing the dietary sources and primary biological activities of CGA. These encompass antioxidant, anti-inflammatory, antibacterial, anti-cancer, and neuroprotective activities. Next, a comprehensive overview of the current research on nutrient delivery systems incorporating CGA is provided. This exploration encompasses nanoparticle, liposome, hydrogel, and emulsion delivery systems. Additionally, the article explores the latest applications of CGA in the food industry. Serving as a cutting-edge theoretical foundation, this paper contributes to the design and development of CGA in the realms of nutrition delivery and the food industry. Finally, the article presents informed speculations and considerations for the future development of CGA.
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Ácido Clorogênico , Indústria Alimentícia , Ácido Clorogênico/química , Ácido Clorogênico/farmacologia , Humanos , Animais , Antioxidantes/farmacologia , Antioxidantes/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/química , Sistemas de Liberação de Medicamentos/métodosRESUMO
Gastric ulcer, a significant health issue characterized by the degradation of the gastric mucosa, often arises from excessive gastric acid secretion and poses a challenge in current medical treatments due to the limited efficacy and side effects of first-line drugs. Addressing this, our study develops a novel therapeutic strategy leveraging gas therapy, specifically targeting the release of hydrogen sulfide (H2S) in the treatment of gastric ulcers. We successfully developed a composite nanoparticle, named BSA·SH-DATS, through a two-step process. Initially, bovine serum albumin (BSA) was sulfhydrated to generate BSA·SH nanoparticles via a mercaptosylation method. Subsequently, these nanoparticles were further functionalized by incorporating diallyltrisulfide (DATS) through a precise Michael addition reaction. This sequential modification resulted in the creation of BSA·SH-DATS nanoparticles. Our comprehensive in vitro and in vivo investigations demonstrate that these nanoparticles possess an exceptional ability for site-specific action on gastric mucosal cells under the controlled release of H2S in response to endogenous glutathione (GSH), markedly diminishing the production of pro-inflammatory cytokines, thereby alleviating inflammation and apoptosis. Moreover, the BSA·SH-DATS nanoparticles effectively regulate critical inflammatory proteins, including NF-κB and Caspase-3. Our study underscores their potential as a transformative approach for gastric ulcer treatment.
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Compostos Alílicos , Etanol , Mucosa Gástrica , Sulfeto de Hidrogênio , Nanopartículas , Soroalbumina Bovina , Úlcera Gástrica , Sulfetos , Animais , Sulfetos/química , Sulfetos/administração & dosagem , Sulfetos/farmacologia , Nanopartículas/química , Etanol/química , Compostos Alílicos/química , Compostos Alílicos/farmacologia , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/tratamento farmacológico , Mucosa Gástrica/metabolismo , Mucosa Gástrica/efeitos dos fármacos , Sulfeto de Hidrogênio/química , Soroalbumina Bovina/química , Masculino , Apoptose/efeitos dos fármacos , Glutationa/metabolismo , Camundongos , Citocinas/metabolismo , Humanos , NF-kappa B/metabolismoRESUMO
Morin, a naturally occurring bioactive compound shows great potential as an antioxidant, anti-inflammatory agent, and regulator of blood glucose levels. However, its low water solubility, poor lipid solubility, limited bioavailability, and rapid clearance in vivo hinder its application in blood glucose regulation. To address these limitations, we report an enzymatically synthesized nanosized morin particle (MNs) encapsulated in sodium alginate microgels (M@SA). This approach significantly enhances morin's delivery efficiency and therapeutic efficacy in blood glucose regulation. Utilizing horseradish peroxidase, we synthesized MNs averaging 305.7 ± 88.7 nm in size. These MNs were then encapsulated via electrohydrodynamic microdroplet spraying to form M@SA microgels. In vivo studies revealed that M@SA microgels demonstrated prolonged intestinal retention and superior efficacy compared with unmodified morin and MNs alone. Moreover, MNs notably improved glucose uptake in HepG2 cells. Furthermore, M@SA microgels effectively regulated blood glucose, lipid profiles, and oxidative stress in diabetic mice while mitigating liver, kidney, and pancreatic damage and enhancing anti-inflammatory responses. Our findings propose a promising strategy for the oral administration of natural compounds for blood glucose regulation, with implications for broader therapeutic applications.
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Glicemia , Diabetes Mellitus Experimental , Flavonas , Flavonoides , Nanopartículas , Animais , Humanos , Glicemia/efeitos dos fármacos , Glicemia/metabolismo , Camundongos , Flavonoides/química , Flavonoides/farmacologia , Células Hep G2 , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/sangue , Nanopartículas/química , Nanopartículas/uso terapêutico , Alginatos/química , Estresse Oxidativo/efeitos dos fármacos , Antioxidantes/química , Antioxidantes/farmacologia , Masculino , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Hipoglicemiantes/administração & dosagem , Hipoglicemiantes/farmacocinética , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologiaRESUMO
Ethanol (EtOH) has been identified as a potential pathogenic factor in gastric ulcer development primarily due to its association with gastric injury and excessive production of reactive oxygen species. Magnolol (Mag), the principal active compound in Magnolia officinalis extract, is well studied for its notable anti-inflammatory and antioxidant properties. However, its limited solubility, propensity for agglomeration, and low absorption and utilization rates significantly restrict its therapeutic use. This study aims to overcome these challenges by developing a Mag nanoparticle system targeting the treatment and prevention of EtOH-induced gastric ulcers in mice. Utilizing a click chemistry approach, we successfully synthesized this system by reacting thiolated bovine serum albumin (BSA·SH) with Mag. The in vitro analysis revealed effective uptake of the BSA·SH-Mag nanoparticle system by human gastric epithelial cells (GES-1), showcasing its antioxidant and anti-inflammatory capabilities. Additionally, BSA·SH-Mag exhibited gradual disintegration and release in simulated gastric fluid, resulting in a notable reduction of oxidative stress in gastric tissues and mucosal tissue repair and effectively reducing inflammatory expression. Furthermore, BSA·SH-Mag attenuated EtOH-induced gastric inflammation by decreasing the level of NOX4 protein expression and augmenting the level of Nrf2 protein expression. In conclusion, our findings indicate that BSA·SH-Mag represents a promising candidate as an oral therapeutic for gastric ulcer treatment.
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Compostos de Bifenilo , Lignanas , Nanopartículas , Úlcera Gástrica , Camundongos , Humanos , Animais , Etanol/efeitos adversos , Etanol/metabolismo , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/tratamento farmacológico , Antioxidantes/metabolismo , Anti-Inflamatórios/farmacologia , Mucosa Gástrica/metabolismoRESUMO
As a global public health issue, the treatment of acute liver injury (ALI) is severely limited due to the lack of specific drugs. In order to address the challenges, innovative strategies for selenium nanoparticles (Se NPs) with excellent antioxidant properties have been actively developed to effectively prevent ALI. However, the functional activity of Se NPs is severely affected by poor stability and bioavailability. The aim of this work is to develop a stabilization system (ASP-Se NPs) for Angelica sinensis polysaccharides modified Se NPs. The results showed that ASP-Se NPs with smaller size (62.38 ± 2.96 nm) showed good stability, specific accumulation in liver and enhanced cell uptake, thus exerting strong antioxidant and anti-inflammatory functions. The results of in vivo experiments further confirmed that ASP-Se NPs effectively prevented CCl4-induced ALI by improving liver function, inhibiting oxidative stress and inflammatory response, and liver pathological damage. This work provides a new alternative method for effectively preventing ALI and improving liver function.
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Angelica sinensis , Nanopartículas , Selênio , Selênio/farmacologia , Antioxidantes/farmacologia , Polissacarídeos/farmacologia , Polissacarídeos/uso terapêutico , Fígado , Nanopartículas/uso terapêuticoRESUMO
In our study, ammoniated hollow mesoporous silica nanoparticles (NH2-HMSN) with uniform diameter and stable structure were successively prepared via SiO2 core hard template method. Fourier transformed infrared spectroscopy revealed that amino group was effectively modified. Adsorption experiments showed that adsorption capacity of NH2-HMSN towards free fatty acids (FFAs) was superior to aminated mesopores or silica microspheres. Following through optimization of extraction conditions, FFAs from edible oil samples were successfully gathered by NH2-HMSN and showed favorable linearities (0.2-90 µg g-1), remarkably low limit of detections (0.03-0.15 nmol g-1), acceptable recoveries (85.08-96.82 %) and relatively accurate precisions (1.64-4.99 %). In comparison to existing adsorbent, NH2-HMSN could be successfully prepared via the chemical reaction of common raw materials under normal pressure and temperature. Furthermore, NH2-HMSN with hollow and mesoporous structure was more effective than the current adsorbents aimed at FFAs analysis in aspect of surface area and adsorption capacity.
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Neuropatia Hereditária Motora e Sensorial , Nanopartículas , Humanos , Ácidos Graxos não Esterificados , Dióxido de Silício/química , Nanopartículas/química , Espectroscopia de Infravermelho com Transformada de Fourier , AdsorçãoRESUMO
Over the past decade, a remarkable surge in the development of functional nano-delivery systems loaded with bioactive compounds for healthcare has been witnessed. Notably, the demanding requirements of high solubility, prolonged circulation, high tissue penetration capability, and strong targeting ability of nanocarriers have posed interdisciplinary research challenges to the community. While extensive experimental studies have been conducted to understand the construction of nano-delivery systems and their metabolic behavior in vivo, less is known about these molecular mechanisms and kinetic pathways during their metabolic process in vivo, and lacking effective means for high-throughput screening. Molecular dynamics (MD) simulation techniques provide a reliable tool for investigating the design of nano-delivery carriers encapsulating these functional ingredients, elucidating the synthesis, translocation, and delivery of nanocarriers. This review introduces the basic MD principles, discusses how to apply MD simulation to design nanocarriers, evaluates the ability of nanocarriers to adhere to or cross gastrointestinal mucosa, and regulates plasma proteins in vivo. Moreover, we presented the critical role of MD simulation in developing delivery systems for precise nutrition and prospects for the future. This review aims to provide insights into the implications of MD simulation techniques for designing and optimizing nano-delivery systems in the healthcare food industry.