FOOD CHEMISTRY
·
2024
·
IF 8.5
Peng Zhou,Xiangzhou Li,Zhi Jiang,Jun Zhou,Liqun Shen
Constructing carrier materials with polysaccharides to enhance the solubility of insoluble active ingredients is a crucial strategy for improving bioavailability. This research constructed pectin-based hesperidin microcapsules (PHM) through self-assembly processes in the deep eutectic solvent , improving the solubility, storage stability, and bioavailability of hesperidin (HES). PHM exhibited high encapsulation efficiency (91.7%) and loading capacity (11.5%), with a small particle size (1.73 μm). The interaction mechanism was clarified through physical characterization and density functional theory (DFT) calculations. The vitro release demonstrated that the release ratio of PHM was only 6.4% in simulated gastric fluid (SGF), but reached 80.9% in simulated intestinal fluid (SIF). The release mechanism of PHM in SGF followed Fickian diffusion, while in SIF followed skeleton dissolution diffusion with a stable rate. Furthermore, the cell cytotoxicity experiments confirmed the remarkable biocompatibility of PHM toward human colon cells, which suggested its potential application in food and pharmaceutical fields.
研究领域:
食品科学
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药学
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材料科学
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PubMed
高影响因子
Foods
·
2026
·Vol. 15
·期 10
·1636
·
IF 6
Xiaohong Ge,Yuxiang Wang,Guoyang Liu,Benguo Liu,Sheng Geng
The development of novel multifunctional emulsifiers using protein–polyphenol interactions is a common strategy. Previously, we investigated the emulsifying properties of the four citrus flavonoids alone. This study investigated how complexing lysozyme (LY) with four citrus-derived flavonoids affects emulsifying properties. Results demonstrated that the emulsification performance was enhanced when flavonoids were complexed with LY, following the order: hesperidin (Hpd) > neohesperidin dihydrochalcone (Neohpddic) > neohesperidin (Neohpd) > hesperetin (Hpt). This enhancement was positively correlated with the intrinsic emulsification abilities of the flavonoids, suggesting that the synergistic effect should not overlook the emulsifying capacity of the flavonoids themselves. The Hpd-LY mixture increased the three-phase contact angle (to near 90°) compared to Hpd alone (51.16° ± 0.58), which helped form high internal phase emulsion (HIPE) gels. Stable HIPEs were achieved at an oil phase fraction φ = 80%, mixture concentration w ≥ 0.8%, and Hpd-to-LY ratio k ≥ 1:1. Droplet size decreased as w increased from 0.6% to 1.2%, but increased with higher φ and k, while gel strength improved. In addition, these HIPEs protected encapsulated lutein and suppressed lipid oxidation. The findings show that flavonoid–protein complexes, especially Hpd-LY, can build stable and functional HIPEs for protecting bioactive compounds.
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Journal of Functional Foods
·
2026
·
IF 3.9
Lu Wang,Kejian Wei,Jiahua Yan,Kun Wang,Siqi Liu,Fei Fang,Yu Jiang
As a major citrus flavonoid, hesperidin (HP) shows bone-protective potential, yet its role in calcium–phosphorus homeostasis and antioxidant mechanisms remains unclear. This study investigated the anti-osteoporotic effects of HP in retinoic acid (RA)-induced osteoporotic mice and primary bone marrow mesenchymal stem cells (BMSCs). HP promoted BMSC proliferation, migration, and osteogenic differentiation, with increased alkaline phosphatase (ALP) activity and mineralization. Network pharmacology identified antioxidant PI3K/AKT/FOXO1 pathways as key targets, with fibroblast growth factor 23 (FGF23) as a pivotal effector. In osteoporotic mice, HP normalized serum calcium, phosphorus, and 25-hydroxyvitamin D, increased bone formation and decreased resorption markers, alleviating bone loss and preserving trabecular microarchitecture and enhancing biomechanical properties. Mechanistically, PI3K/AKT/FOXO1-mediated FGF23 suppression was essential for osteoprotection, as confirmed using a PI3K inhibitor. Collectively, these findings suggest that HP ameliorates RA-induced osteoporosis by restoring calcium–phosphorus homeostasis via PI3K/AKT/FOXO1-dependent FGF23 inhibition, underscoring its potential as a functional food ingredient.
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NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
·
2026
·
IF 4
Liu Man,Wu Songze
Myocardial infarction (MI) is recognized by its rapid onset and higher mortality rate. The intricate nature of its pathological process has rendered targeted therapy for MI a persistent issue. Hesperidin (HES) has been identified that may protect cardiac cells and promote myocardial tissue regeneration. Nonetheless, its effectiveness in addressing MI-related ischemia situations is hindered by its insufficient angiogenesis and poor bioavailability. This present investigation demonstrates that the effective therapy of HES is augmented by mesoporous copper carbonate (MCC) microspheres, owing to their superior drug-delivery capacity and consistent release of angiogenic degradation (Cu). The cellular examinations demonstrated that HES and Cu could produce synergic effects on endothelial cell angiogenesis and anti-cardiomyocyte apoptosis. Additionally, an in vivo MI model showed that the HES-loaded MCC (MCC@HES) significantly reduced cardiomyocyte apoptosis, decreased infarct size, and enhanced vascularization in myocardial tissue. Overall, the present study is groundbreaking for indicating the benefits of integrating HES with MCC nanocarriers for myocardial remodeling and for presenting an innovative, meticulously designed MCC@HES system as a prospective treatment approach for MI.
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PubMed
高影响因子
Food Bioscience
·
2026
·
IF 6.2
Jiaxiong Wu,Laiming Zhang,Chengxiao Yu,Yi Wang,Huan Cheng,Haibo Pan,Xingqian Ye,Shiguo Chen,Jianle Chen
Emerging evidence highlights the pivotal role of gut microbiota in mediating the health effects of dietary flavonoids. In this study, we uncover a novel mechanism through which hesperidin, a citrus-derived flavonoid glycoside, ameliorates high-fat diet-induced metabolic dysregulation by modulating the gut-adipose axis and activating UCP1 independent thermogenesis. The twelve-week hesperidin intervention significantly reduced weight gain, hepatic steatosis, adipose hypertrophy, dyslipidemia, and systemic inflammation in high-fat diet-fed mice. Multi-omics analyses revealed that hesperidin selectively enriched beneficial bacteria ( Lactobacillus , Bifidobacterium , Akkermansia ) and elevated microbial metabolites (e.g., cinnamic acid, hippuric acid). Transcriptomic profiling of inguinal white adipose tissue indicated upregulation of calcium cycling-associated thermogenic genes (ATP2A1, RYR1, RYR3, ITPR3) without affecting UCP1, suggesting an alternative thermogenic route. Notably, antibiotic-induced microbiota depletion abolished the metabolic benefits and impaired hesperidin bioactivation. These findings propose a previously underexplored microbiota–metabolite–calcium signaling axis, supporting hesperidin's potential as a microbiota-responsive dietary agent for obesity management.
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ACTA PHARMACOLOGICA SINICA
·
2016
·Vol. 37
·期 8
·1091-1100
·
IF 3.166
Xiong Yong-jian,Chu Hong-wei,Lin Yuan,Han Fang,Li Ya-chan,Wang Ai-guo,Wang Fu-jin,Chen Da-peng,Wang Jing-yu
Aim: Postoperative ileus (POI) is a postoperative dysmotility disorder of gastrointestinal tract, which remains one of the most perplexing problems in medicine. In the present study we investigated the effects of hesperidin, a major flavonoid in sweet oranges and lemons, on POI in rats. Methods: SD rats were administered hesperidin (5, 20, and 80 mg·kg −1 ·d −1 , ig) for 3 consecutive days. POI operation (gently manipulating the cecum for 1 min) was performed on d 2. The gastrointestinal motility and isolated intestinal contraction were examined 1 d after the operation. Then the myosin phosphorylation and inflammatory responses in cecum tissue were assessed. Smooth muscle cells were isolated from rat small intestine for in vitro experiments. Results: The gastric emptying and intestinal transit were significantly decreased in POI rats, which were reversed by administration of hesperidin. In ileum and cecum preparations of POI rats in vitro , hesperidin (2.5–160 μmol/L) dose-dependently increased the spontaneous contraction amplitudes without affecting the contractile frequency, which was blocked by the myosin light chain kinase (MLCK) inhibitor ML-7 or verapamil, but not by TTX. Furthermore, administration of hesperidin increased the phosphorylation of MLC 20 in the cecum tissue of POI rats. Moreover, administration of hesperidin reversed the increased levels of inflammatory cytokines, iNOS and COX-2 in cecum tissue of POI rats. In freshly isolated intestinal smooth muscle cells, hesperidin (5–80 μmol/L) dose-dependently increased the intracellular Ca 2+ concentration as well as the phosphorylation of MLC 20 , which was abrogated by ML-7 or siRNA that knocked down MLCK. Conclusion: Oral administration of hesperidin effectively alleviates rat POI through inhibition of inflammatory responses and stimulation of Ca 2+ -dependent MLC phosphorylation.
研究领域:
药理学
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胃肠病学
·
外科
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PubMed
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Frontiers in Nutrition
·
2023
·
IF 5
Wang Yin,Guo Yangkai,Zhang Longtao,Yuan Meilan,Zhao Li,Bai Chunqing,McClements David Julian
The objective of this work was to explore the possibility of improving the antioxidant capacity and application of whey protein (WP) through non-covalent interactions with hesperidin (HES), a citrus polyphenol with nutraceutical activity. The interaction mechanism was elucidated using several spectroscopic methods and molecular docking analysis. The antioxidant capacity of the WP-HES complexes was analyzed and compared to that of the proteins alone. Moreover, the resistance of oil-in-water emulsions formulated using the WP-HES complexes as antioxidant emulsifiers to changes in environmental conditions (pH, ion strength, and oxidant) was evaluated. Our results showed that HES was incorporated into a single hydrophobic cavity in the WP molecule, where it was mainly held by hydrophobic attractive forces. As a result, the microenvironments of the non-polar tyrosine and tryptophan residues in the protein molecules were altered after complexation. Moreover, the α-helix and β-sheet regions in the protein decreased after complexation, while the β-turn and random regions increased. The antioxidant capacity of the WP-HES complexes was greater than that of the proteins alone. Non-radiative energy transfer from WP to HES was detected during complex formation. Compared to WP alone, the WP-HES complexes produced emulsions with smaller mean droplet diameters, exhibited higher pH and salt stability, and had better oxidative stability. The magnitude of these effects increased as the HES concentration was increased. This research would supply valuable information on the nature of the interactions between WP and HES. Moreover, it may lead to the creation of dual-function antioxidant emulsifiers for application in emulsified food products.
研究领域:
食品科学
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化学
·
营养学
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PubMed
高影响因子
MOLECULES
·
2023
·Vol. 28
·期 14
·5316
·
IF 4.6
Hong-Qi Xia,Wanbing Chen,Diyang Qiu,Jiwu Zeng
Portable and low-cost analytical devices are essential for rapid detection of bioactive substrates in agricultural products. This study presents the first highly integrated microelectrochemical sensor based on pencil graphite for rapid and sensitive detection of hesperidin inCitrus reticulate‘Chachi’ peel. The surface morphology and characterization as well as the electrochemical property of pencil graphite was investigated and discussed. A high electrocatalytic efficiency of hesperidin has been found at used pencil graphite-based microelectrodes. Kinetic analysis was carried out to further understand the electrochemical process of hesperidin at a pencil graphite microelectrode. Consequently, a portable and highly-integrated microelectrochemical sensor exhibits a sensitivity of 0.7251 μA cm−2μM−1and a detection limit as low as 25 nM (S/N = 3), and high selectivity was fabricated. Proposed microelectrochemical sensors were applied to electrochemically determinate the hesperidin content in the extract ofCitrus reticulata“chachi” peel. As a result, the concentration of hesperidin in the actual real sample detected electrochemically with the proposed portable and low-cost microelectrochemical sensors is highly consistent to that obtained with a common chromatographic method, thus indicating the good reliability and that it can be used in practical applications.Keywords:microelectrochemical sensor;hesperidin;Citrus reticulata“chachi”
研究领域:
分析化学
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食品科学
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PubMed
高影响因子
ACS Biomaterials Science & Engineering
·
2026
·
IF 6
Minglan Wang,Menglei Wang,Changhao Dong,Yanyi Chen,Heyang Liu,Hao Yao,Yang Qiming,Haitao Ran,Danning Liu,Xiyuan Zhou
Retinal neovascularization is closely linked to retinal inflammation. Microglia, the resident immune cells of the retina and the primary responders to inflammatory stimuli, play a central role in pathological retinal vascular remodeling, including aberrant neovascularization and increased vascular tortuosity. High-mobility group box 1 (HMGB1), a ubiquitously expressed DNA-binding protein, functions as a damage-associated molecular pattern and has been shown to drive microglial polarization toward the pro-inflammatory M1 phenotype. Whereas M1 microglia exacerbate inflammatory responses, M2 microglia exhibit anti-inflammatory and tissue-repair functions. Accordingly, inhibition of HMGB1 to induce metabolic reprogramming of microglia may promote the transition from the M1 to the M2 phenotype. In this study, we adopted a targeted therapeutic strategy aimed at modulating the M1/M2 polarization balance of microglia to attenuate retinal inflammation and suppress pathological angiogenesis, thereby offering a potential treatment for retinal neovascularization. To achieve this, we engineered a self-assembled nanoparticle delivery system (H–H@MG1) designed to selectively target M1 microglia. These nanoparticles encapsulate the anti-inflammatory flavonoid hesperidin and are functionalized with an M1 microglia-targeting peptide (MG1). In vitro experiments demonstrated that H–H@MG1 efficiently targets M1 microglia, inhibits HMGB1-induced activation of resting microglia, and promotes their polarization toward the M2 phenotype. Furthermore, in vivo studies using an oxygen-induced retinopathy mouse model revealed that H–H@MG1 rebalances M1/M2 microglial polarization within the retina, remodels the retinal immune microenvironment, and significantly reduces the expression of pro-inflammatory cytokines, including IL-6 and TNF-α. Collectively, these effects suppress abnormal retinal vascular remodeling and pathological angiogenesis. Overall, this nanodelivery system effectively reshapes the retinal immune microenvironment and represents a promising therapeutic strategy for the treatment of retinal neovascularization.
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2026
·
IF 6.7
Yexuan Yao,Mingfeng Fang,Jihang Hou,Qiang Yu,Chengwei Yu,Zeyuan Deng,Ting Luo
Abstract Hesperidin (HES) exhibits limited oral delivery potential because of poor aqueous solubility and low bioaccessibility. Here, HES-loaded liposomes were incorporated into a sodium alginate/gelatin (SA/G) composite hydrogel to construct a liposome-in-hydrogel delivery system. The SA/G ratio was systematically optimized to establish a balanced polymer network through the complementary functions of SA and gelatin. The optimized formulation (H5) exhibited a compact three-dimensional network with cooperative intermolecular interactions, favorable thermal behavior and improved colloidal stability. During simulated gastrointestinal digestion, H5 suppressed premature HES release under oral and gastric conditions while promoting sustained intestinal release. H5 achieved a bioaccessibility of 26.80%, compared with 21.26% for liposomes and 14.26% for free HES, and showed approximately 23-fold and 5-fold higher intestinal tissue-associated accumulation, respectively. These findings indicate that rational optimization of the SA/G network balances matrix integrity, hydration, and liposome stabilization, providing a promising food-grade strategy for controlled gastrointestinal delivery of poorly soluble bioactive compounds.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Yijin Wu,Shaofeng Wang,Hui Huang,Jingling Yu,Jieren Liang,Hai Huang,Jianying Guo,Zhaoxin Tang,Jianzhao Liao
Background With the increasing application of copper nanoparticles (CuNPs) across various fields, its toxicity and hazards are gradually being confirmed. Hesperidin (Hes), a flavonoid compound with extensive antioxidant and anti-inflammatory effects, has recently attracted public attention. Methods Molecular docking was employed to investigate the potential binding sites between Hes and SIRT3. The activation of the SIRT3-FOXO3A signaling pathway by Hes was further validated through a series of experiments in vitro and vivo. Results The results indicate that exposure to CuNPs can cause pathological damage to liver. Compared with the control group, exposure to CuNPs induced the accumulation of reactive oxygen species and mitochondrial UPR mt in broiler liver, specifically manifested as an increase in reactive oxygen species and the gene and protein levels of UPR mt related proteins. The molecular docking results indicate that Hes and SIRT3 have potential binding sites. However, after treatment with Hes, pathological damage in liver was alleviated. At the same time, we found that the SIRT3-FOXO3A signaling pathway was activated, leading to a significant decrease in the expression levels of proteins and genes related to UPR mt . Conclusion Hes can ameliorate hepatic oxidative damage and UPR mt induced by exposure to CuNPs by activating the SIRT3-FOXO3A pathway.
研究领域:
毒理学
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药理学
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分子生物学
·
纳米技术
·
生物化学
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JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
·
2025
·
IF 2.8
Qiurui Zhao,Xinyao Yu,Mengyuan Liu,Chuansen Qin,Yahui He,Suilou Wang,Haixiang Wang
Orange peels are a common by-product in the global food processing industry, leading to resource wastage and environmental pollution. They are rich in hesperidin, a flavonoid with multiple pharmacological and biological activities, possessing significant economic value. Based on this, in this study, a one-pot method was developed to create hesperidin MIPs for selective separation and purification of hesperidin from waste orange peels. To obtain the optimal MIPs, the best functional monomer was first determined through computer simulations and spectroscopic scanning, and the synthesis process was optimized. The characterization results demonstrated that the obtained MIPs, due to the presence of the functional monomer 2-vinylpyridine (2-VP), effectively adsorbs hesperidin through hydrophobic interactions and π-π stacking between the benzene ring and pyridine ring, achieving an adsorption capacity of 74.18 mg/g. MIPs exhibited excellent selectivity in the presence of two structural analogs, naringin and neohesperidin, and the imprinting factor reached 2.01. Furthermore, the MIPs exhibited excellent selectivity in the presence of structurally similar compounds within a complex matrix. In practical applications using MIPs as the adsorbent, the maximum extraction efficiency of hesperidin can reach 73.88 %, with the purity of extracted hesperidin reaching 81.24 %. After seven consecutive adsorption-desorption cycles, the adsorption capacity of MIPs for hesperidin decreased by only 1.55 mg/g. This research provides a simple and efficient integrated strategy for the separation and purification of hesperidin from orange peel waste, with great potential for commercial application.
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