LWT-FOOD SCIENCE AND TECHNOLOGY
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2021
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IF 4.952
Haihua Jiang,Xing Hu,Junhui Pan,Deming Gong,Guowen Zhang
This research aimed to investigate the changes in the structure and functional properties of glutenin (Glu) induced by hesperetin (Ht) or hesperidin (Hd). Both Ht and Hd quenched the fluorescence of Glu through a static process and formed a Ht/Hd–Glu complex in one binding site. The binding constants between Glu and Ht and Hd were 4.20 × 10 4 L mol −1 and 3.59 × 10 4 L mol −1 at 25 °C, respectively. The computer simulations showed their bindings were dominated by hydrogen bonds and hydrophobic forces, and also provided the changes in particle motion and macroscopic properties of Glu induced by Ht/Hd. The presence of Ht/Hd promoted the exchange of sulfhydryl and disulfide bonds, resulting in the structural changes of Glu and the free sulfhydryl groups more exposed. Meanwhile, the increase in β-sheet content of Glu might cause the contraction of the carbon chain, thereby increasing the surface hydrophobicity. Due to the increase in rigid clusters and the decrease in flexibility, thermal stability of Glu was enhanced. Moreover, the emulsifying activity of Glu was significantly improved. This research lays the foundation for the application of Ht/Hd and Glu in healthy food or the optimization of Glu-based products.
研究领域:
食品科学
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生物化学
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DOI
高影响因子
FOOD CHEMISTRY
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2026
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IF 10.4
Tao Chen,Yangjing Li,Xuesong Chi,Xinru Tang,Lihang Chen,Di Wu,Jiangning Hu
Films derived from polysaccharides, such as bacterial cellulose (BC), present promising alternatives to conventional petroleum-based plastics but suffer from brittleness and a lack of bioactivity. To address these limitations, hesperetin nanoparticles (HST-NPs) were synthesized through a Mannich reaction and incorporated into BC films. The HST-NPs served dual roles by improving ductility as nanofillers and providing functionality as bioactive components. Compared with the pure BC film, the composite films showed a 34.75% increase in elongation at break, and its contact angle reached 72.55°, reflecting improved flexibility and hydrophobicity. The incorporation of HST-NPs provided UV-blocking, antioxidant, and antimicrobial properties, thereby extending strawberry shelf life. Soil degradation tests confirmed that the composite films degraded within 15 days, similar to pure BC films. This study presents an approach to improve the mechanical, bioactive, and environmental performance of BC-based films, demonstrating significant potential for sustainable food packaging.
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PubMed
高影响因子
Journal of Orthopaedic Translation
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2026
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IF 9.8
Yimin Pi,Haodong Zhu,Jian Xie,Furui Tang,Zhuoya Wang,Li Liu,Yuchun Zhong,Zhidong He,Tian Liu,Jiacheng Zheng,Yuwen Tang,Jun Luo,Cihua Zheng
Inflammatory bowel disease (IBD) is a chronic inflammatory disorder frequently accompanied by extraintestinal complications such as bone loss, yet effective treatment options remain elusive. In this study, we investigated whether hesperetin mitigates colitis-associated bone loss by modulating the “gut–bone axis.” Using a DSS-induced mouse model of chronic colitis, we found that hesperetin significantly reduced intestinal inflammation, restored mucosal barrier integrity, and suppressed serum inflammatory cytokines. Furthermore, hesperetin effectively alleviated DSS-induced bone microstructure damage, promoted the expression of ALP, Runx2, OCN, and inhibited NFATc1 and CTSK. Fecal microbiota transplantation experiments further confirmed that the intestinal microbiota from hesperetin-treated group attenuated intestinal inflammation and bone loss. 16S rRNA sequencing and metabolomics revealed that hesperetin enriched Akkermansia muciniphila ( A. muciniphila ) and increased the tryptophan metabolite 3-indoleacrylic acid (IDA). Supplementation with A. muciniphila or IDA alone simulated the therapeutic benefits of hesperetin. Furthermore, RNA-seq revealed that hesperetin regulated bone metabolism-related gene expression by ECM-receptor interaction and PI3K-AKT signaling, while inhibiting the NOD-like receptor pathway. In conclusion, hesperetin mitigates intestinal inflammation and bone homeostasis imbalance by reshaping the gut microbiota, enriching A. muciniphila, and promoting IDA production, thus providing new insights into potential therapies for IBD-related bone loss. Download: Download high-res image (369KB) Download: Download full-size image
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PubMed
高影响因子
Materials Today Bio
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2026
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IF 11
Liang Feng,Huan Wang,Zuodi Liang,Ying Tian,Yang Guo,Zhuo Li
This study focused on developing a novel nanodelivery system, BP-PEG-S2P@H, with hesperetin-loaded black phosphorus nanosheets to target tumor-associated macrophages (TAMs) in triple-negative breast cancer (TNBC). Through RNA sequencing and proteomic analyses, CEBPG upregulation was observed in TAMs, potentially controlling the SLC7A11-mediated ferroptosis pathway. In vitro and in vivo experiments, including FerroOrange and malondialdehyde assays, demonstrated the induction of ferroptosis by BP-PEG-S2P@H. The nanoplatform facilitated the transition of TAMs from the M2 to the M1 subtype, enhancing IL-12 secretion while reducing IL-10 levels. Functional analyses confirmed the reversal of the pro-migratory TAM phenotype and inhibition of tumor cell invasion. In vivo imaging validated efficient tumor targeting, with immunohistochemical staining revealing decreased CEBPG/SLC7A11 expression in tumors, reduced macrophage infiltration, and enhanced CD8 + T cell activation, promoting the efficacy of PD-L1 immunotherapy. Biosafety assessments indicated no apparent toxicity, supporting the potential of the BP-PEG-S2P@H nanoplatform for TAM-targeted nano-immunotherapy in TNBC.
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PubMed
高影响因子
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
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2022
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IF 4.831
Xi Peng,Kai Liu,Xing Hu,Deming Gong,Guowen Zhang
Inhibition of α-amylase and α-glucosidase activity is an effective way for controlling postprandial blood glucose-related diabetes. The study found that hesperetin-Cu(II) complex (Hsp-Cu(II)) exhibited a stronger inhibitory ability on α-amylase and α-glucosidase compared to hesperetin (Hsp), with smaller IC 50 values of Hsp-Cu(II) (60.3 ± 0.9 µM for α-amylase; 1.25 ± 0.03 µM for α-glucosidase) than Hsp (115.6 ± 1.1 µM for α-amylase; 55.2 ± 0.1 µM for α-glucosidase). Interestingly, Hsp-Cu(II) and acarbose exerted a synergistic effect on inhibition of α-glucosidase. The binding affinities of Hsp-Cu(II) to α-amylase and α-glucosidase were strong with the K a values (binding constant) in the magnitude order of 10 5 , which was 9 times larger than Hsp. After interacting, Hsp-Cu(II) reduced α-helix contents of α-amylase and α-glucosidase, resulting in a looser conformation of these two enzymes. Molecular simulations manifested that Hsp-Cu(II) bound to the active center of enzymes driven by hydrogen bonds and interacted with the key catalytic amino acids (α-amylase: Gln63, Asp300 and His305; α-glucosidase: Tyr158, Asp215, Glu277 and Glu411), altering the conformation of enzymes, blocking the entrance of substrates, ultimately reducing the activities of α-glucosidase and α-amylase. This study has demonstrated that Hsp-Cu(II) may be a promising candidate of functional nutritional additive and medicine for the prevention of diabetes.
研究领域:
生物化学
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药理学
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糖尿病研究
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产品关联
DOI
PubMed
高影响因子
CHEMICO-BIOLOGICAL INTERACTIONS
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2020
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IF 3.723
Mingfei Wu,Xingxing Zhu,Yilong Zhang,Min Wang,Tongtong Liu,Jianfei Han,Jun Li,Zeng Li
A series of 7- O -amide hesperetin derivatives were subjected to multi-target biological evaluation of anti-Alzheimer's disease. Most of the compounds showed good in vitro inhibitory activity against cholinesterase , of which compound 7c (7- O -(4-(morpholinoethyl)-acetamide) hesperetin) was the most effective anti-eqBuChE derivative (IC 50 = 0.28 ± 0.05 μM) and exerted neuroprotective effects. Further biological evaluation found that compounds 4d , 4e and 7c showed strong antioxidant, anti-Aβ self-aggregation and anti-neuroinflammatory activities. Compound 7c could inhibit the expression of iNOS and COX-2 proteins and prevent LPS-induced inflammatory response in BV2 cells. In addition, compound 7c could chelate biometal ions such as Cu 2+ and Zn 2+ . In the vivo study, the MWM test confirmed that compound 7c could improve the cognitive impairment caused by scopolamine . In summary, the above studies have shown that the optimized compound 7c has great development potential as MTDL for the treatment of AD.
研究领域:
药理学
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神经科学
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药物化学
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DOI
PubMed
高影响因子
Discover Nano
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2026
·Vol. 21
·期 1
·415
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IF 6.7
Long Lin,Zhang Yexi,Xiao Jun,Zang Jianhua
Purpose To fabricate hesperetin-loaded fucoidan-selenium (Hes/Fu-Se) nanoparticles (NPs) for alleviating cisplatin-induced acute kidney injury (AKI), overcoming hesperetin’s low solubility and bioavailability and boosting antioxidant and anti-inflammatory efficacy. Methods Hes/Fu-Se NPs were prepared by encapsulating hesperetin within fucoidan, and then functionalized selenium (Se) NPs. Nanoparticle physicochemical properties and antioxidant activity (FRAP, ABTS) were characterized. Cisplatin-stimulated HK-2 cells were used for in vitro detection of cell viability, apoptosis, ROS accumulation, mitochondrial function and cGAS-STING signaling. A cisplatin-induced AKI mouse model was adopted to test renal biochemical indexes, renal histopathology and renal injury-related protein expression. Results Synthesized Hes/Fu-Se NPs exhibited uniform particle size, superior aqueous solubility and potent antioxidant activity. In vitro, the NPs restored HK-2 cell viability, mitigated apoptosis and ROS overproduction, and inhibited DNA damage and cGAS-STING cascade activation. In vivo, Hes/Fu-Se markedly reduced serum BUN and CRE, alleviated renal histological lesions and inflammatory infiltration, and downregulated the expression of cGAS, STING, γH2AX and TNF-α in kidney tissues. Conclusions Hes/Fu-Se NPs relieve cisplatin-triggered AKI via amplified antioxidation, DNA damage restoration and cGAS-STING pathway suppression. This nanoformulation provides a promising nephroprotective strategy against chemotherapy-related renal toxicity for clinical translation. Graphical abstract
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高影响因子
BIOCHEMICAL PHARMACOLOGY
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2026
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IF 6.5
Chunyu Pan,Min Li
Ovarian cancer is the most fatal gynecological malignancy, characterized by difficult early diagnosis, high invasiveness and metastasis, and frequent chemoresistance, highlighting an urgent need for targeted therapeutic agents with high efficacy and low toxicity. Hesperetin is a natural flavonoid with antitumor potential but limited activity and druggability. In this study, a novel hesperetin derivative DU12 was synthesized, and its anti-ovarian cancer effects in vitro and in vivo as well as the underlying molecular mechanisms were systematically investigated. In vitro experiments demonstrated that DU12 concentration-dependently inhibited the proliferation, colony formation, migration, and invasion of SKOV3 and A2780 ovarian cancer cells. Kinase profiling, surface plasmon resonance (SPR), isothermal titration calorimetry (ITC), and molecular docking assays confirmed that cyclin-dependent kinase 17 (CDK17) is the direct target of DU12, and DU12 markedly suppressed CDK17 kinase activity. RNA sequencing (RNA-seq) and functional assays revealed that DU12 downregulated the semaphorin 6C (SEMA6C)‑plexin A2 (PLXNA2) signaling pathway by targeting CDK17. Mechanistic studies suggested that CDK17 directly bound to SEMA6C and may maintain its protein stability by inhibiting K63-linked ubiquitination and degradation of SEMA6C, thereby promoting malignant progression of ovarian cancer, The cytoplasmic domain of SEMA6C is the key core region responsible for its specific binding to CDK17. rescue experiments verified that the CDK17-SEMA6C-Plexin A2 axis is the key mediator of the anti-ovarian cancer effects of DU12. In vivo nude mouse xenograft assays revealed that DU12 significantly suppressed tumor growth and downregulated the expression of CDK17, SEMA6C, and PLXNA2 in tumor tissues. Meanwhile, absorption, distribution, metabolism, excretion, and toxicity (ADMET) prediction and in vivo safety evaluation indicated that DU12 exhibited favorable water solubility, oral bioavailability, and plasma protein binding rate, with no obvious hepatorenal or hematologic toxicity at effective doses. Collectively, this study confirms that the hesperetin derivative DU12 inhibits ovarian cancer proliferation and metastasis by targeting the CDK17-SEMA6C −Plexin A2 axis, with favorable bioactivity and safety, providing a novel candidate small-molecule drug and a new therapeutic target for ovarian cancer
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PubMed
高影响因子
Aquaculture Reports
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2025
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IF 3.7
Yu Wang,Jie Hua Xu,Fei Yu,Cheng Chen,Kai Hao,Zhe Zhao
Channel catfish virus (CCV) is an acute and highly contagious pathogen that easily causes large-scale infections and substantial economic losses to the catfish industry. Currently, there are no commercially available licensed prophylactic vaccines or therapeutic agents specifically developed for the treatment and control of CCV infection. In recent years, the use of natural products with antimicrobial properties has attracted increasing attention in aquaculture. Hesperetin is a plant-derived flavonoid monomer and has a wide range of pharmacology effects. Nevertheless, the antiviral effect of hesperetin against CCV needs to be further elucidated. In this study, we evaluated the antiviral efficacy and potential mechanisms of hesperetin against CCV infection in CCO cells. The results demonstrated that hesperetin possessed remarkable anti-CCV properties, effectively inhibiting viral replication and protecting CCO cells from virus-induced cytopathic effects at non-cytotoxic concentration of 500 μg/ml. Further results revealed that hesperetin significantly suppressed viral gene expression and protein synthesis, reduced progeny virus production, and preserved normal cellular morphology in a dose-dependent manner, based on assessments including quantitative real-time PCR (RT-qPCR), western blot, viral cytopathic effects, viral titer, and plaque formation. Notably, the hesperetin exhibited a 10-fold safety window, with effective antiviral activity at 50 μg/ml well below its tolerated cytotoxicity level. Mechanistically, time-of-addition assays indicated that hesperetin probably acted at the viral entry process and early replication stage. Furthermore, hesperetin exerted its antiviral activity by specifically interfering with the internalization phase of viral entry, which was evidenced by suppression of viral protein expression, viral titer and plaque formation in adsorption and penetration assays. Together, these results identify hesperetin as a promising candidate antiviral agent against CCV infection, which shed light on the development of a novel and potent treatment for herpesvirus infection in aquaculture.
研究领域:
病毒学
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水产养殖
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抗病毒研究
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天然产物
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药理学
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DOI
高影响因子
TALANTA
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2018
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IF 4.244
Dan-Dan Wang,Die Gao,Wan-Jun Xu,Fan Li,Man-Ni Yin,Qi-Feng Fu,Zhi-Ning Xia
In present study, novel magnetic molecularly imprinted polymers for hesperetin were successfully prepared by surface molecular imprinting method using functionalized Fe 3 O 4 particles as the magnetic cores. Hesperetin as the template, N-Isopropylacrylamide as the functional monomer , ethylene glycol dimethyl acrylate as the crosslinker, 2,2-azobisisobutyonnitrile as initiator and acetonitrile-methanol (3:1, v/v) as the porogen were applied in the preparation process. Fourier transform infrared spectroscopy, scanning electron microscopy, transmission electron microscope, x-ray diffraction and vibrating sample magnetometry were applied to characterize the magnetic molecularly imprinted polymers. The adsorption experiments indicated that the magnetic molecularly imprinted polymers performed high selective recognition property to hesperetin. The selectivity experiment indicated that the adsorption capacity and selectivity of polymers to hesperetin was higher than that of luteolin , baicalein and ombuin. Furthermore, the magnetic molecularly imprinted polymers were employed as adsorbents for extraction and enrichment of hesperetin from the dried pericarp of Citrus reticulata Blanco . The recoveries of hesperetin in the dried pericarp of Citrus reticulata Blanco ranged from 90.5% to 96.9%. The linear range of 0.15–110.72 µg/mL was obtained with correlation coefficient of greater than 0.9991. The limit of detection and quantification of the proposed method was 0.06 µg/mL and 0.15 µg/mL, respectively. Based on three replicate measurements, intra-day RSD was 0.71% and inter-day RSD was 2.31%. These results demonstrated that the prepared magnetic molecularly imprinted polymers were proven to be an effective material for the selective adsorption and enrichment of hesperetin from natural medicines, fruits and et al.
研究领域:
分析化学
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药学
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天然产物研究
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DOI
PubMed
高影响因子
CHEMICO-BIOLOGICAL INTERACTIONS
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2021
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IF 5.194
Min Wang,Longji Fang,Tongtong Liu,Xuejie Chen,Yan Zheng,Yilong Zhang,Shiming Chen,Zeng Li
The development of multi-target-directed ligands (MTDLs) may improve complex central nervous system diseases such as Alzheimer's disease (AD). Here, a series of 7-O-1, 2, 3-triazole hesperetin derivatives was evaluated for their inhibition of cholinesterase , anti-neuroinflammatory, and neuroprotective activity. Among the hesperetin derivatives, compound a8 (7-O-((1-(3-chlorobenzyl)-1H-1,2,3-triazol-4-yl)methyl)hesperetin) possessed excellent anti-butyrylcholinesterase activity (IC 50 = 3.08 ± 0.29 μM) and exhibited good anti-neuroinflammatory activity (IC 50 = 2.91 ± 0.47 μM) against NO production through remarkably blocking the NF-κB signaling pathway and inhibiting the phosphorylation of P65. In addition, a8 showed a remarkable neuroprotective effect and lacked neurotoxicity up to 50 μM concentration. Furthermore, possessing significant self-mediated Aβ 1-42 aggregation inhibitory activity, chelated biometals and reduced ROS production were found in compound a8 . In the bi-directional transport assay, a8 exhibited a blood–brain barrier penetrating ability. In this study, the Morris water maze task showed that compound a8 significantly improved the learning and memory impairment of the scopolamine-induced AD mice model. Results highlighted the potential of compound a8 to be a potential MTDL for the development of anti-AD agents.
研究领域:
神经科学
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药理学
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药物发现
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产品关联
DOI
PubMed
高影响因子
FOOD HYDROCOLLOIDS
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2025
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IF 12.4
Xi Peng,Yushi Wei,Deming Gong,Guowen Zhang
Starch intake is the main cause of postprandial hyperglycemia. This study aimed to investigate the effect of hesperetin-copper (II) complex [Hsp-Cu(II)] on the physico-chemical properties and digestibility of gelatinized corn starch (GCS). It was found that with the addition of 1.44 mg/mL Hsp-Cu(II), the digestion rate of GCS decreased from 87.0% to 52.2%, the rapidly digestible starch content reduced from 22.7% to 14.4%, and the resistant starch content increased from 18.1% to 55.0%, suggesting that Hsp-Cu(II) decreased the digestion rate of GCS by increasing the content of resistant starch. The analysis of X-ray diffraction, rheology and differential scanning calorimetry showed that Hsp-Cu(II) increased the crystallinity, viscosity, storage modulus (G′), loss modulus (G′′) and thermal stability of GCS. Fourier transform infrared spectroscopy found that Hsp-Cu(II) bound with GCS through hydrogen bonds. In addition, scanning electron microscopy showed that Hsp-Cu(II)‒GCS complex possessed a denser structure, thicker crystalline flakes and thinner amorphous flakes in comparison with GCS. Therefore, Hsp-Cu(II) may inhibit the digestion of GCS by changing the physicochemical properties and increasing the content of resistant starch of GCS, and inhibiting the activities of α-amylase and α-glucosidase at the same time by hindering the binding of GCS to the enzymes. These findings have demonstrated the potential ability of Hsp-Cu(II) to lower the level of postprandial blood glucose. This study may provide new insights into the development of Hsp-Cu(II) as a novel anti-diabetic nutritional supplement.
研究领域:
食品科学
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营养学
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糖尿病研究
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产品关联
DOI
高影响因子
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