LWT-FOOD SCIENCE AND TECHNOLOGY
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2020
·
IF 4.006
Li Na Wei,Chang Zheng Shi,Cang Xue Luo,Ching Yuan Hu,Yong Hong Meng
Biofilm is a critical factor for L. monocytogenes to persist in food processing. Phloretin is a natural product that is potent to antibacterial. In order to investigate the effects of phloretin on L. monocytogenes biofilm, we used sub-MIC phloretin to treat L. monocytogenes at 37 °C and 4 °C. The results show that L. monocytogenes biofilm maximum inhibitory rate was up to 60% when 20 μg/mL phloretin was used. The capacity of biofilm adhesion and aggregation of L. monocytogenes were declined. Meanwhile, biofilm protective capacity was impaired. The biofilm thickness of the treated group was decreased by 2 μm approximately at 20 μg/mL phloretin treatment. We also studied the mechanisms of biofilm inhibition by phloretin. The quorum sensing related genes were inhibited by phloretin. The relative transcript level of the agr system genes in quorum sensing was reduced by 50% with 20 μg/mL phloretin treatment. These findings suggest that phloretin has the potential to be developed as a natural antibacterial or biofilm inhibitor to control contamination in the food industry.
研究领域:
微生物学
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食品科学
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生物技术
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产品关联
DOI
高影响因子
Foods
·
2024
·Vol. 13
·期 22
·3537
·
IF 4.7
Siyang Chen,Wenxiu Zhu,Yiqun Zhan,Xiaodong Xia
Although phloretin is widely utilized in the food industry as an additive, its effects on foodborne pathogens remain insufficiently investigated. This study aimed to evaluate the antimicrobial properties of phloretin (PHL) againstVibrio parahaemolyticus(V. parahaemolyticus) and to elucidate the potential mechanisms of action. After PHL treatment, alterations in the cell morphology, cell microstructure, and intracellular contents ofV. parahaemolyticuswere assessed. Scanning electron microscopy revealed substantial damage to cell integrity, subsequent to PHL treatment. A notable reduction in intracellular components, including proteins, ATP, and DNA, was observed in samples treated with PHL. PHL was shown to inhibit the activities ofATPase, β-galactosidase, and respiratory chain dehydrogenase inV. parahaemolyticus. Furthermore, it was demonstrated to elevate the intracellular levels of reactive oxygen species and promote cell death. After being applied to sea bass, shrimp, and oysters, PHL effectively inactivatedV. parahaemolyticusin these seafoods. These findings demonstrate that PHL has potential for application in seafood to controlV. parahaemolyticus.
研究领域:
食品科学
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微生物学
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食品安全
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产品关联
DOI
PubMed
高影响因子
Colloid and Interface Science Communications
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2025
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IF 4.7
Shouguang Wang,Xiaofei Zhang,Dunmin Zhuang,Lina Dong,Bo Li
Objective Breast cancer remains a global health challenge due to limitations of conventional therapies, such as drug resistance and systemic toxicity. This study aimed to develop a novel synergistic chemo-immunotherapy platform by constructing Mn 2+ -coordinated oxidized hyaluronic acid (OHA)-based nanoparticles co-loaded with phloretin (PHL) (OHA@Lys/PHL Mn 2+ ). Methods A nanosystem was engineered using oxidized hyaluronic acid (OHA) modified with lysine (Lys) to co-encapsulate PHL and Mn 2+ ions. The anti-tumor efficacy was evaluated in vitro (4 T-1 breast cancer cells) and in vivo (4 T-1 tumor-bearing mice), including assessments of proliferation inhibition, apoptosis induction, reactive oxygen species (ROS) accumulation, DNA damage, cGAS-STING pathway activation, and dendritic cell (DC) maturation. Combination therapy with cisplatin (CDDP) was also investigated. Results OHA@Lys/PHL Mn 2+ achieved 80.3 % cell viability inhibition on 4 T-1 cells. Combined with CDDP, it further suppressed proliferation, induced apoptosis, and enhanced ROS accumulation. Mechanistically, the nanosystem induced DNA double-strand damage and activated the cGAS-STING pathway. In vivo , OHA@Lys/PHL Mn 2+ monotherapy showed significant tumor inhibition (46.4 %, p < 0.001). Combination with CDDP achieved near-complete tumor suppression (86.7 % inhibition) and reduced lung metastasis. The in vivo mechanism results indicated that nanosystem triggered DNA damage, activated cGAS-STING signaling, and significantly promoted DC maturation (48.5 % vs. 28.2 % in controls). Conclusion This strategy offers a promising and clinically translatable approach for advanced breast cancer treatment.
研究领域:
纳米医学
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肿瘤学
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药学
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免疫治疗
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药物递送系统
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生物化学
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分子生物学
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产品关联
DOI
高影响因子
RSC Advances
·
2026
·Vol. 16
·期 9
·7717-7725
·
IF 6.1
Siyang Chen,Jinhui Jia,Jian Du,Ningbo Qin,Xiaodong Xia
Due to its capacity to form complexes with polyphenols and to self-assemble as nanoparticles, zein could be utilized as an excellent carrier for polyphenols. The objective of this study was to examine the interaction between zein and phloretin (PHL) through multispectral analysis and molecular docking, and to prepare and characterize PHL-loaded zein nanoparticles. Spectral analysis and docking data confirmed that the binding process of the zein-PHL complex is mainly influenced by hydrogen bonding and van der Waals forces, and hydrophobic interaction was auxiliary, with static quenching as the primary fluorescence quenching mechanism. Meanwhile, zein nanoparticles loaded with PHL were successfully prepared using the anti-solvent precipitation method, which was evidenced by the morphology and size characterization. The hydrogen bond and hydrophobic interaction in the nanoparticles were further confirmed by Fourier transform infrared spectroscopy. This study elucidates the noncovalent interaction mechanism between zein and PHL, providing a theoretical foundation for the design of zein-polyphenol nanocarriers. These carriers show promising applications as emulsion stabilizers or delivery systems for lipophilic bioactives, thereby facilitating the development of functional foods with improved stability and enhanced bioavailability.
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DOI
PubMed
高影响因子
Scientific Reports
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2016
·Vol. 6
·期 1
·1-15
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IF 5.228
Zhang Tingjing,Liang Jianqiang,Wang Panxue,Xu Ying,Wang Yutang,Wei Xinyuan,Fan Mingtao
Phloretin-2′- O -glycosyltransferase (P2′GT) catalyzes the last glycosylation step in the biosynthesis of phloridzin that contributes to the flavor, color and health benefits of apples and processed apple products. In this work, a novel P2′GT of Malus x domestica (Md P2′GT) with a specific activity of 46.82 μkat/Kg protein toward phloretin and uridine diphosphate glucose (UDPG) at an optimal temperature of 30 °C and pH 8.0 was purified from the engineered Pichia pastoris broth to homogeneity by anion exchange chromatography, His-Trap affinity chromatography and gel filtration. The purified Md P2′GT was low N -glycosylated and secreted as a stable dimer with a molecular mass of 70.7 kDa in its native form. Importantly, Md P2′GT also exhibited activity towards quercetin and adenosine diphosphate glucose (ADPG), kaempferol and UDPG, quercetin and UDP-galactose, isoliquiritigenin and UDPG, and luteolin and UDPG, producing only one isoquercitrin, astragalin, hyperoside, isoliquiritin, or cynaroside, respectively. This broad spectrum of activities make Md P2′GT a promising biocatalyst for the industrial preparation of the corresponding polyphenol glycosides, preferably for their subsequent isolation and purification. Besides, Md P2′GT displayed the lowest K m and the highest k cat /K m for phloretin and UDPG compared to all previously reported P2′GTs, making Md P2′GT favor phloridzin synthesis the most.
研究领域:
植物学
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生物化学
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食品科学
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DOI
PubMed
高影响因子
Food Science & Nutrition
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2020
·Vol. 8
·期 7
·3545-3558
·
IF 1.797
Yiling Wang,Dongli Li,Huiqiong Lin,Sen Jiang,Lei Han,Shuli Hou,Shuying Lin,Zhefeng Cheng,Wangqing Bian,Xinxin Zhang,Yan He,Kun Zhang
Phloretin (Ph) is a natural active ingredient with wide biological properties. However, its poor water-solubility and low oral bioavailability limit the application significantly in functional food and drug. This study was to explore the mixed polymer Pluronic® F127 and P123 modified the different triglycerides (LCT, MCT, SCT) in self-nanoemulsions (SNEs) for enhancing the oral bioavailability and bioefficacy of Ph. The SNEs were characterized in terms of physical property study, lipolysis study, pharmacokinetic study, and anti-inflammatory effect. The water-solubility of LCT-Ph-SNE increased 3000-fold compared with Ph solution. Pharmacokinetic study of SNEs and other carriers (HP-β-CD, PVP) results indicated that LCT-Ph-SNE was 7.9-fold more bioavailable compared with unformulated Ph. The anti-inflammatory activity of LCT-Ph-SNE in vivo represented a 6.8-fold enhancement compared with unformulated Ph. This novel SNE formulation may also be used for other poorly soluble ingredients with high loading capacity, which made a significant impact on functional food and drug.
研究领域:
药剂学
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食品科学
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药物递送系统
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生物活性增强
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DOI
PubMed
高影响因子
Frontiers in Endocrinology
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2018
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IF 3.519
Ying Yin,Jin Jiye,Ye Li,Sun Pingping,Wang Hui,Wang Xiaodong
Hyperglycemia induces chronic inflammation and oxidative stress in cardiomyocyte, which are the main pathological changes of diabetic cardiomyopathy (DCM). Treatment aimed at these processes may be beneficial in DCM. Phloretin (PHL), a promising natural product, has many pharmacological activities, such as anti-inflammatory, anticancer, and anti-oxidative function. The aim of this study was to investigate whether PHL could ameliorate the high glucose-mediated oxidation, hypertrophy, and fibrosis in H9c2 cells and attenuate the inflammation- and oxidation-mediated cardiac injury. In this study, PHL induced significantly inhibitory effect on the expression of pro-inflammatory, hypertrophy, pro-oxidant, and fibrosis cytokines in high glucose-stimulated cardiac H9c2 cells. Furthermore, PHL decreased the levels of serum lactate dehydrogenase, aspartate aminotransferase, and creatine kinase-MB, and attenuated the progress in the fibrosis, oxidative stress, and pathological parameters via Kelch-like ECH-associated protein 1 (Keap1)/nuclear factor E2-related factor 2 (Nrf2) pathway in diabetic mice. In additional, molecular modeling and immunoblotting results confirmed that PHL might obstruct the interaction between Nrf2 and Keap1 through direct binding Keap1, and promoting Nrf2 expression. These results provided evidence that PHL could suppress high glucose-induced cardiomyocyte oxidation and fibrosis injury, and that targeting Keap1/Nrf2 may provide a novel therapeutic strategy for human DCM in the future.
研究领域:
药理学
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心脏病学
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糖尿病
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细胞生物学
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分子生物学
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DOI
PubMed
高影响因子
Food Frontiers
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2025
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IF 6.9
Jie Li,Qihui Zhu,Yang Li,Haiyu Zhao,Yi Bi,Chuanying Pan,Min Wang,Lin Han,Xianyong Lan
Phloretin, a plant-derived dihydrochalcone bioactive compound, potentially modulates preadipocyte differentiation, although this remains controversial and requires further clarification. To clarify this point, herein, phloretin gavage inhibited mice obesity, reduced adipocyte size, and ameliorated serum lipid parameters, including triglycerides. In vitro, phloretin suppressed the differentiation of 3T3-L1 and bovine preadipocytes, decreasing lipid droplet content and reducing CEBPα and PPARγ levels. Moreover, during differentiation, glutathione peroxidase (GSH-Px) ultimately decreased with elevations in malondialdehyde (MDA) and Fe 2+ levels, along with acyl-CoA synthetase long-chain family member 4 ( ACSL4 ), P53 , and SLC7A11 expression, indicating differentiation occurring under mild oxidation and slight ferroptosis activation. Similar to (1 S ,3 R )-RSL3, phloretin further stimulated the ferroptosis pathway by inhibiting glutathione reductase (GR) and GSH-Px, increasing the content of MDA and Fe 2+ . Simultaneously, the suppression of Fth1 , Slc7a11 , and Sod2 transcription, significantly elevated HMGB1 protein, and markedly downregulated glutathione peroxidase 4 (GPX4) and TFR protein collectively confirmed that phloretin activated the ferroptosis signaling pathway to inhibit differentiation. Further phosphoproteomic analysis identified dm-phosphorylation sites (p-eEF2K[S365], p-AMPKα1[S491], and p-CaMKK2[S495]) enriched in AMPK/MAPK signaling pathways and transferrin receptor binding. Further molecular docking simulations revealed that phloretin binds to PPARγ or transferrin to activate ferroptosis pathway, revealing the potential crosstalk between ferroptosis signaling pathway and adipogenic differentiation processes.
研究领域:
分子生物学
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细胞生物学
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脂肪生成
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营养生物化学
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药理学
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氧化应激与细胞死亡
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产品关联
DOI
高影响因子
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
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2019
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IF 2.931
Jianmin Chen,Qinglian Li,Yaling Ye,Ziyao Huang,Zhipeng Ruan,Nan Jin
Tyrosinase is the rate-limiting enzyme for controlling the production of melanin in the human body, and overproduction of melanin can lead to a variety of skin disorders. In this paper, the inhibitory kinetics of phloretin on tyrosinase and their binding mechanism were determined using spectroscopy, molecular docking, antioxidant assays and chromatography. The spectroscopic results indicate that phloretin reversibly inhibits tyrosinase in a mix-type manner through a multiphase kinetic process with the IC 50 of 169.36 μmol/L. It is shown that phloretin has a strong ability to quench the intrinsic fluorescence of tyrosinase mainly through a static quenching procedure, suggesting that a stable phloretin-tyrosinase complex is generated. Molecular docking results suggest that the dominant conformation of phloretin binds to the gate of the active site of tyrosinase. Moreover, the antioxidant assays demonstrate that phloretin has powerful antioxidant capacity and has the ability to reduce o -dopaquinone to l -dopa just like ascorbic acid . Interestingly, the results of spectroscopy and chromatography indicate that phloretin is a substrate of tyrosinase but also an inhibitor. The possible inhibitory mechanism is proposed, which will be helpful to design and search for tyrosinase inhibitors.
研究领域:
生物化学
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药理学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF MEMBRANE SCIENCE
·
2025
·
IF 9
Zhixiao Liu,Yuhang Zhao,Mingli Yi,Lintao Liao,Yangyang Huang,Guangqiu Lei,Gao Hu,Mayu Lan,Huiping Li,Zhiming Mi
Antibiotics in water bodies pose a significant threat to the health of plants, animals, and humans, thereby contributing to severe ecological crises. Polyamide nanofiltration (NF) membranes are extensively employed for the separation and purification of antibiotics but are limited by relatively low permeation fluxes. In this study, three biobased phloretin derivatives—phloretin (Pt), phlorizin (Pz), and naringenin dihydrochalcone (Ng), were selected as water-phase monomers and reacted with trimesoyl chloride to fabricate three novel polyester NF membranes. The results demonstrated that the variations in the molecular structure gradients, including twisted conformation and molecular weight, of the three derivatives significantly influenced the structure and properties of polyester NF membranes. In-depth mechanistic analysis revealed that the diffusion rates (mainly related to molecular weight) of the three derivatives into the oil-phase solution, rather than their reactivity with TMC, governed the interfacial polymerization (IP) process. Consequently, Pt-based polyester NF membranes exhibited relatively dense layers compared to Pz- and Ng-based ones, achieving rejections of 92.4 % and 85.7 % for bacitracin and erythromycin, respectively, while maintaining a permeance of 35.2 L/m 2 h bar, which was significantly higher than that of conventional polyamide NF membranes. Meanwhile, the relatively loose structure of the Pz- and Ng-based polyester NF membranes made their permeance reach as high as 65.8 L/m 2 ·h·bar and 107.2 L/m 2 h bar, respectively, while maintaining intermediate separation level for five antibiotic molecules. Furthermore, the three polyester NF membranes demonstrated excellent chlorine resistance, antifouling properties, and good environmental adaptability. The three biobased polyester NF membranes in this study offer a novel approach for the development of high-flux NF membranes for antibiotic separation and other specialized scenarios. The correlation between the molecular structure of the derivatives and the membrane separation performance further deepens the understanding of polyester-based IP theory.
研究领域:
环境科学
·
材料科学
·
化学工程
·
膜技术
·
药学
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产品关联
DOI
高影响因子
PHYTOMEDICINE
·
2023
·
IF 7.9
Xiangyun Li,Taoli Sun,Jiaqin Liu,Shanshan Wei,Yuanying Yang,Jian Liu,Bikui Zhang,Wenqun Li
Background Doxorubicin (Dox), a chemotherapeutic agent known for its efficacy, has been associated with the development of severe cardiotoxicity, commonly referred to as doxorubicin-induced cardiotoxicity (DIC). The role and mechanism of action of phloretin (Phl) in cardiovascular diseases are well-established; however, its specific function and underlying mechanism in the context of DIC have yet to be fully elucidated. Objective This research aimed to uncover the protective effect of Phl against DIC in vivo and in vitro , while also providing a comprehensive understanding of the underlying mechanisms involved. Methods DIC cell and murine models were established. The action targets and mechanism of Phl against DIC were comprehensively examined by systematic network pharmacology, molecular docking, transcriptomics technologies, transcription factor (TF) prediction, and experimental validation. Results Phl relieved Dox-induced cell apoptosis in vitro and in vivo . Through network pharmacology analysis, a total of 554 co-targeted genes of Phl and Dox were identified. Enrichment analysis revealed several key pathways including the PI3K-Akt signaling pathway, Apoptosis, and the IL-17 signaling pathway. Protein-protein interaction (PPI) analysis identified 24 core co-targeted genes, such as Fos, Jun, Hif1a, which were predicted to bind well to Phl based on molecular docking. Transcriptomics analysis was performed to identify the top 20 differentially expressed genes (DEGs), and 202 transcription factors (TFs) were predicted for these DEGs. Among these TFs, 10 TFs (Fos, Jun, Hif1a, etc.) are also the co-targeted genes, and 3 TFs (Fos, Jun, Hif1a) are also the core co-targeted genes. Further experiments validated the finding that Phl reduced the elevated levels of Hif3a (one of the top 20 DEGs) and Fos (one of Hif3a's predicted TFs) induced by Dox. Moreover, the interaction between Fos protein and the Hif3a promoter was confirmed through luciferase reporter assays. Conclusion Phl actively targeted and down-regulated the Fos protein to inhibit its binding to the promoter region of Hif3a, thereby providing protection against DIC.
研究领域:
药理学
·
分子生物学
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心血管疾病
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肿瘤学
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产品关联
DOI
PubMed
高影响因子
Food Bioscience
·
2024
·
IF 4.8
Jiaqi Wen,Shuling Chen,Le Deng,Xinru Chen,Xiaoyu Jiang,Xing Hu,Deming Gong,Guowen Zhang
The development of natural xanthine oxidase (XO) inhibitors is an effective strategy for the treatment of hyperuricemia. In this study, the inhibition mechanism of phloretin on XO and its joint inhibition with clinical drugs (allopurinol and febuxostat) were investigated, using multispectroscopic and molecular simulation techniques. The results showed that phloretin reversibly inhibited XO in a mixed type with an IC 50 value of 31.83 ± 0.32 μM. Phloretin quenched the fluorescence of XO with a static mechanism and hydrophobic interactions were the key binding force of phloretin binding to XO. Furthermore, the interaction between phloretin and XO resulted in a more relaxed structure and less stable of the enzyme with a reduction in the α-helix content from 21.5% to 11.3%. The heatmap analysis showed that a combination of phloretin (15 μM) and allopurinol (10 μM) or phloretin (30 μM) and febuxostat (0.01 μM) exhibited the strongest synergistic effect on XO inhibition in a mixed manner. The combination of phloretin and allopurinol/febuxostat enhanced the binding affinity with XO compared to the inhibitors individually. Molecular docking indicated that phloretin, allopurinol and febuxostat bound to different sites of XO to produce a synergistic inhibition by preventing substrate access to the Mo activity center and affecting electron transfer. This study may provide theoretical references for the development of phloretin and its formulation with clinical drugs as uric acid-lowering food functional factor or drug.
研究领域:
药理学
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生物化学
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分子生物学
·
药物开发
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产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）