Journal of Oceanology and Limnology
·
2024
·Vol. 42
·期 1
·163-173
·
IF 1.3
Ma Dandan,Zhou Qingli,Sui Liying,Guo Qingbin,Liu Huanhuan,Liang Honghe,Li Zhenjing,Sang Zhongna
Deltamethrin (DEL), a commonly used pyrethroid pesticide, results in higher reactive oxygen species (ROS) levels in aquatic animals, which consequently unbalance the redox state. Phlorizin (PHL) is a flavonoid and a natural product promising to prevent or reduce pesticide-induced oxidative stress. Artemia is a micro-crustacean widely used in marine hatcheries and an experimental aquatic organism for environmental toxicology research. This research aimed to evaluate the toxicity of DEL on Artemia and the antioxidative effect of PHL against the toxicity. Results show that 0.08-mg/mL PHL exerted its antioxidative effects on hatching percentage of the cysts in 24-h incubation and on body length and survival rate of Artemia in 12-d culture. After 12-d culture, 12-, 24-, and 36-h DEL exposure showed significant drops in SOD, CAT, and GSH-Px enzyme activities, and significant increases in ROS and malondialdehyde (MDA) levels in Artemia ( P <0.05). On the contrary, 0.08-mg/mL PHL application improved the enzyme activities and decreased the ROS and MDA levels ( P <0.05). Moreover, 0.08-mg/mL PHL significantly increased mRNA expression levels of Cu/Zn SOD, CAT, GST, HO-1, NQO1 , and Nrf2 , and decreased mRNA expression level of Keap1 in the DEL-exposed Artemia ( P <0.05). Therefore, DEL is toxic to Artemia , while PHL alleviates DEL-induced oxidative damage by possibly regulating the Nrf2 signaling pathway. This study provided a theoretical basis for PHL to reduce pesticide-induced toxicity in aquatic animals.
研究领域:
环境毒理学
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水产动物健康
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抗氧化研究
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DOI
高影响因子
Food Bioscience
·
2024
·
IF 4.8
Yushi Wei,Jianmei Wu,Xi Peng,Xing Hu,Deming Gong,Guowen Zhang
The anti-glycation potential and mechanism of phloretin and phlorizin were investigated in the study. In the methylglyoxal (MGO)-human serum albumin (HSA) glycosylation system, the inhibition against fluorescent advanced glycosylation end products (AGEs) was more than 60% at 960 μM phloretin and phlorizin. They decreased carbonylation and oxidative damage of protein, protected thiol groups and secondary structure of protein and inhibited protein aggregates. Treated with 1.37 mM phloretin or phlorizin, O 2 − · scavenging was more than 80%, and 1 mM phloretin or phlorizin chelated 60.08% or 28.11% of Fe 2+ , respectively. Analysis of HPLC and LC-QqQ-MS shown phloretin captured MGO by forming adducts with MGO, with capture rates of 92.67% within 24 h. The capture rate of phlorizin to MGO was 56.40%. The anti-glycosylation mechanisms of them could include the structural protection of HSA, capture of MGO, O 2 − · and ·OH scavenging and chelation of Fe 2+ . These findings may provide a theoretical basis for the application of phloretin and phlorizin as novel anti-glycosylation agents.
研究领域:
生物化学
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药理学
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产品关联
DOI
高影响因子
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS
·
2025
·
IF 3.3
Xiaoyu Wu,Chuanbo Ding,Xinglong Liu,Qiteng Ding,Shuai Zhang,Yue Wang,Ting Zhao,Wencong Liu
Carotid atherosclerosis (CAS) is a complex cardiovascular disease linked to inflammatory response and oxidative stress. This study aimed to develop and assess the therapeutic efficacy of Phlorizin liposomes (Phlorizin-Lips) in repairing CAS in rats. Phlorizin-Lips were prepared using the film dispersion method and evaluated for controlled release, antioxidant properties, and biocompatibility. The methodology included preparing Phlorizin-Lips, conducting in vitro and in vivo experiments, observing histopathological changes in carotid arteries in a rat model, and detecting inflammatory markers and antioxidant gene expression in arterial endothelial cells using immunoblotting and ELISA. Results showed that Phlorizin-Lips significantly lowered inflammatory markers TNF-α and IL-1β in endothelial cells while upregulating Nrf2 and its downstream antioxidant genes, enhancing the cells' antioxidant capacity and reducing oxidative damage by activating the Nrf2 signaling pathway. Additionally, Phlorizin-Lips reduced carotid plaque formation, improved vascular endothelial function, and promoted CAS repair. This study underscores Phlorizin's potential as a therapeutic agent for CAS and highlights the Nrf2 pathway's role in regulating inflammation and oxidative stress. Future research will explore the clinical potential of Phlorizin-Lips.
研究领域:
药理学
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心血管病学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
Food Bioscience
·
2026
·
IF 6.2
Mengqi Teng,Yuqing Zhang,Guorui Yang,Jiayu Sun,Haifang Xiao
This study aimed to characterize, clarify the α-glucosidase inhibitory activity and mechanism of phlorizin-Zn (II) complex (Phl-Zn) and phlorizin-Cu (II) complex (Phl-Cu). Phl-Zn and Phl-Cu were synthesized and preliminarily characterized using ultraviolet-visible spectroscopy (UV-Vis), Fourier transform infrared spectroscopy (FTIR), elemental analysis (EA) and thermogravimetric analysis (TGA). The formation of stable coordination structures between phlorizin and metal ions (Cu 2+ /Zn 2+ ) through metal-oxygen bonds was confirmed. Furthermore, inhibition kinetics and multispectral techniques including ultraviolet spectrophotometry and fluorescence spectrophotometry were employed to investigate the inhibitory effects of phlorizin and its complexes on α-glucosidase. Phlorizin, Phl-Zn and Phl-Cu reversibly inhibited the enzyme activity with IC50 values of 0.766 ± 0.012, 0.470 ± 0.035 and 0.084 ± 0.019 mg/mL, respectively, demonstrating superior efficacy of the metal complexes. Both complexes exhibited mixed-type inhibition and stronger binding affinity to α-glucosidase than the enzyme-substrate interaction (K is > K i ). Furthermore, the binding constants (Ka) of phlorizin and its two metal complexes toward the enzyme decreased with rising temperature, suggesting that their stability was weakened at higher temperatures. Additionally, both complexes bound to the single active site of α-glucosidase via hydrogen bonds and van der Waals forces, which induced fluorescence quenching, increased tryptophan polarity and reduced hydrophobicity, and finally altered the enzyme's conformation and secondary structure. It was concluded from molecular docking and molecular dynamics analysis that Phl-Cu exerted more significant stabilizing effect on the protein structure than phlorizin and exhibited favorable dynamic adaptability in its binding mode. This study provides supporting information to develop novel phlorizin-based α-glucosidase inhibitors.
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DOI
高影响因子
Food Bioscience
·
2023
·
IF 5.2
Jing Zhang,Yali Song,Xia Hu,Zhen Zeng,Jie Hu,Tingting Zeng,Fang Geng,Di Wu
Phlorizin (PHL) has various biological activities, especially powerful antioxidant effects, but its water solubility limits its application. In this study, zein-encapsulated PHL nanoparticles (zein-PHL nanoparticles), as well as zein and gum arabic (GA) co-encapsulated PHL nanoparticles (zein/GA-PHL nanoparticles) were prepared by the antisolvent precipitation method. On this basis, encapsulated PHL nanoparticles were added to yogurt to make fortified yogurt. Fourier transform infrared (FT-IR) spectroscopy and X-ray diffraction (XRD) experiments showed that the main driving forces for nanoparticle formation were electrostatic interactions and hydrogen bonding between compounds. Zein-PHL nanoparticles were more sensitive to temperature and salt ions than zein/GA-PHL nanoparticles. The addition of GA can improve the stability of the nanoparticles. In addition, the nanoparticles encapsulated with PHL were applied to yogurt. It was found that the nanoparticles improved the antioxidant capacity and water-holding capacity of yogurt, which provides a reference for the development of functional yogurt containing flavonoid compounds.
研究领域:
食品科学
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纳米技术
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营养学
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产品关联
DOI
高影响因子
EXPERIMENTAL GERONTOLOGY
·
2022
·
IF 4.253
Yan-Ling Su,Dong Liu,Yao-Jie Liu,Yang-Lin Ji,Gui-Shan Liu,Ji-Li-Te Wang,Biao Wang,Hao Wang
We explored the effect of phlorizin against cholinergic memory impairment and dysbacteriosis in D-galactose induced ICR mice . The control (CON) group, D-galactose model (DGM) group, and three groups (DG-PL, DG-PM, DG-PH) treated with phlorizin at 0.01%, 0.02%, and 0.04% (w/w) in diets were raised for 12 weeks. Supplementing with phlorizin reversed the loss of organ coefficient and body weight caused by D-galactose. The functional abilities of phlorizin on hippocampal-dependent spatial learning and memory, anti-oxidation, anti-inflammation were also observed. Meanwhile, phlorizin intervention upregulated the gene expression of Nrf2, GSH-PX, SOD1, decreased the gene expression of NF-κB, TLR-4, TNF-α, and IL-1β in the hippocampus , while enhanced the gene expression of JAM-A, Mucin2, Occludin in the caecum. Furthermore, a neurotransmitter of acetylcholine (ACh) was enhanced, while acetylcholinesterase (AChE) activity was inhibited by phlorizin administration. Moreover, phlorizin administration increased short-chain fatty acids (SCFAs) content, and reduced lipopolysaccharides (LPS) levels, which may relate to the rebuilding of gut microbiota homeostasis . Treatment with phlorizin may be an effective intervention for alleviating cognitive decline and gut microbiota dysbiosis.
研究领域:
神经科学
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药理学
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微生物学
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分子生物学
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DOI
PubMed
高影响因子
Food Science and Human Wellness
·
2023
·
IF 7
Jing Zhang,Di Wu,Lan Tang,Xia Hu,Zhen Zeng,Wen Wu,Fang Geng,Hui Li
Phlorizin (PHL) is a natural compound with strong antioxidant properties mainly found in apples. In this paper, the interaction mechanism of PHL with pepsin and trypsin was comparatively evaluated by computer simulation, fluorescence spectra, circular dichroism (CD), and fourier transform infrared (FT-IR) spectra at a molecular level. Fluorescence spectra showed that PHL quenches the pepsin/trypsin by static quenching. Thermodynamic parameters indicated that PHL binds to pepsin mainly through hydrogen bonds and van der Waals forces, and that of trypsin was electrostatic forces. The ground state complexes PHL and protease have a moderate affinity of 10 5 L/mol PHL binds more strongly to trypsin than to pepsin. CD and FT-IR spectra results showed that pepsin/trypsin decreased the β -sheet content and slightly changed its secondary structure upon PHL. These experimental results are mutually verified with the predicted computer-aid simulation results. Upon PHL and trypsin binding, the antioxidant capacity of PHL was elevated. Nevertheless, the antioxidant capacity of PHL was decreased after binding to pepsin. This work elucidates the binding of PHL binding mechanisms to pepsin/trypsin and provides useful information for the digestion of PHL to improve the application of PHL in food processing.
研究领域:
生物化学
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分子生物学
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食品科学
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Xiaoyu Wu,Chuanbo Ding,Xinglong Liu,Qiteng Ding,Shuai Zhang,Yue Wang,Chenran Xin,Hewei Wei,Rui Mao,Guiping Zhang,Ting Zhao,Wencong Liu
Wound healing in diabetic patients is often complicated by issues like inflammation, infection, bleeding, and fluid retention. To tackle these challenges, it is essential to create hydrogel dressings with anti-inflammatory, antibacterial, and antioxidative properties. This study aimed to synthesize Phlorizin-Liposomes (PL) through the thin-film dispersion method and integrate them into an oxidized sodium alginate (OSA) and carboxymethyl chitosan (CMCS) hydrogel scaffold, resulting in an OSA/CMCS/PL (PLOCS) composite hydrogel via a Schiff base reaction. Characterization of the composite was performed using FTIR, TEM, and SEM techniques. The research assessed the swelling behavior, antibacterial effectiveness, and biocompatibility of the PLOCS composite hydrogel, while also investigating how PLOCS facilitates diabetic wound healing. The results demonstrated that PLOCS effectively controls drug release, possesses favorable swelling and degradation characteristics, and shows significant antioxidative properties along with in vitro biocompatibility. Histological analysis confirmed that PLOCS supports the proliferation of healthy epithelial tissue and collagen production. Western blotting indicated that PLOCS diminishes inflammation by inhibiting the TLR4/NF-κB/MyD88 pathway and activates Nrf2 to boost wound healing, increasing the levels of antioxidative enzymes such as HO-1, NQO1, and GCLC. In summary, PLOCS presents a promising new option for advanced wound dressings aimed at treating diabetic ulcers.
研究领域:
材料科学
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生物医学工程
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药剂学
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伤口愈合
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糖尿病
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产品关联
DOI
PubMed
高影响因子
Food & Function
·
2021
·Vol. 12
·期 5
·2148-2160
·
IF 5.396
Yaojie Liu,Ying Liu,Yatu Guo,Lin Xu,Hao Wang
Phlorizin is the main active ingredient of apple peel and has potential utilization value. Some recent studies have suggested that phlorizin may have antioxidant capacity and protect the liver. The injection of a low dose of D-galactose can cause some changes that resemble accelerated aging in mice. This study explored the protective effects of phlorizin on D-galactose-induced mice and PC12 cells. In this study, ICR mice were divided into a normal group (NOR), a D-galactose model group (D-gal) and phlorizin treatment groups (100 mg kg−1, 200 mg kg−1 and 400 mg kg−1). In addition to the NOR group, four other groups were injected with D-galactose (120 mg kg−1) for 12 weeks. The results showed that phlorizin reduced the decline of strength, coordination and spatial memory caused by aging, increased the activity of superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GSH-Px), increased total antioxidant capacity (T-AOC), and reduced the content of malondialdehyde (MDA). On the other hand, phlorizin increased the levels of interleukin-2 (IL-2) and acetylcholine (ACh), reduced the release of interleukin-6 (IL-6), aspartate aminotransferase (AST) and alanine aminotransferase (ALT), and decreased the activity of acetylcholinesterase (AChE) in the brain, improved the expression of antioxidant genes related to the nuclear factor E2-related factor 2 (Nrf2) pathway, and reduced the occurrence of morphological lesions in the hippocampus and liver. In addition, phlorizin improved cell viability and reduced the cytotoxicity of D-galactose-induced oxidative stress in PC12 cells. Meanwhile, the protective effect of phlorizin was abolished in Nrf2 gene knockdown PC12 cells. Furthermore, molecular docking showed that phlorizin could bind Keap1 protein, which can interact with Nrf2 protein. Therefore, these results suggest that phlorizin may delay senescence and enhance antioxidant capacity through the Nrf2 pathway.
研究领域:
老年学
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药理学
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分子生物学
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DOI
PubMed
高影响因子
SEPARATION AND PURIFICATION TECHNOLOGY
·
2024
·
IF 8.1
Weijie Yang,Runping Wang,Lingqi Wang,Zhijian Tan
Switchable deep eutectic solvents (SDESs) have recently been developed to improve the recovery and reuse of the extractants. In this work, temperature-induced SDESs were prepared and used for the extraction of flavonoids (representative phlorizin and trilobatin) from sweet tea ( Lithocarpus litseifolius (Hance) Chun). These SDESs solution can switch between solution and sediment depending on the temperature, and the phase diagram of SDESs solution had been drawn. Their temperature-responsive characteristics were studied by various characterizations, including variable-temperature FT-IR, variable-temperature 1 H NMR, and variable-temperature dynamic light scattering (DLS). SDES-1 (Benzamide: Malic acid = 2:1) was screened as the optimal extractant, and the major factors affecting the extraction process were studied by single-factor experiments and optimized by response surface methodology (RSM). The extraction yields for phlorizin and trilobatin were 114.72 and 12.56 mg/g, respectively. Moreover, the recoveries for phlorizin and trilobatin reached 98.46 % and 94.64 %, respectively. This study thus provides an environmentally sound strategy for extracting bioactive compounds from plant resources.
研究领域:
化学
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药学
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环境科学
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产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2026
·
IF 8.7
Haiyan Xue,Yalin Tan,Baoyuan He,Yan Zhou,Bowei Ding,Yawen Wu,Jun Ma,JiaYi Wang,Wenmin Dong
Phlorizin (PZ), a naturally occurring flavonoid glycoside in Malus exhibits dual therapeutic potential as an antioxidant and antidiabetic agent, however its clinical translation is constrained by poor aqueous solubility (<0.1 mg/mL) and suboptimal bioavailability. To address these limitations, this study examined supramolecular complexation with β-lactoglobulin (β-LG), a whey protein carrier capable of hydrophobic nutrient transport and known for its immunomodulatory properties. Furthermore, the molecular binding mechanism, gastrointestinal stability, and synergistic effects of the PZ–β-LG complex on intestinal mucosal secretion were systematically characterized by integrating computational simulations, spectroscopic validation, and in vitro functional assays. Molecular dynamics simulations revealed that the PZ preferential bound within the calyx domain of β-LG (ΔG = −8.3 kcal/mol) through hydrophobic interactions and hydrogen bonding, as evidenced by emerging UV–Visible absorption peaks between 300 and 350 nm and intrinsic fluorescence spectroscopy. Simulated gastrointestinal digestion coupled with Liquid Chromatography–Tandem Mass Spectrometry(LC-MS/MS) peptidomics demonstrated a significant reduction in β-LG antigenicity reduction(52.1% vs. free β-LG; P < 0.01), which might be attributed to the enhanced gastrointestinal hydrolysis efficiency and the masking of immunoreactive epitopes Notably, 2 digestion-resistant peptides (VAGTWY-42 and LDAQSAPLR-89) persisted across all groups, suggesting potential allergenicity hotspots that may require further investigation. Cellular assessments using intestinal epithelium LS174T cells revealed that β-LG complexation reduced PZ associated cytotoxicity by 62% ( P < 0.05) while synergistically upregulating the expression of mucin-2 (MUC2) at both transcriptional (2.5-fold increase) and secretory levels (2.1-fold elevation vs. control). Overall, these findings indicate that hydrophobic-driven complexation PZ with β-LG not only enhances the bioavailability of polyphenol but also decreases the antigenicity of protein carrier in intestine cells.
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DOI
PubMed
高影响因子
Food & Function
·
2024
·
IF 5.1
Zhengming Xu,Kseniya Hileuskaya,Aliaksandr Kraskouski,Yujiao Yang,Zhe Huang,Zhengang Zhao
A diet containing natural active compounds that can inhibit the hydrolytic activity of α-glucosidase on carbohydrates and intestinal glucose absorption is an effective means of controlling postprandial hyperglycemia. Phlorizin and polydatin as phenolic glycosides had a high affinity to the catalytic site of α-glucosidase, but exhibited unsatisfactory competitive inhibitory capacity, with IC50 of 0.97 and > 2 mM, respectively. However, dodecyl-acylated derivatives of phlorizin and polydatin exerted α-glucosidase inhibitory capacity, with IC50 of 55.10 and 70.95 µM, respectively, which were greatly enhanced and much stronger than that of acarbose with IC50 of 2.46 mM. Both dodecyl phlorizin and dodecyl polydatin reduced the catalytic ability of α-glucosidase by reversible noncompetitive and uncompetitive mixed inhibition, which bind noncovalently to the allosteric site 2 through hydrogen bonds and hydrophobic interactions, thereby inducing the secondary structure unfolding and intrinsic fluorescence quenching of α-glucosidase. Confocal microscopy detection visually showed the significant inhibitory effects on FITC-labeled glucose uptake in intestinal Caco-2 cells by phlorizin, polydatin, dodecyl phlorizin and dodecyl polydatin. In addition, based on the differentiated Caco-2 cell monolayer model, dodecyl phlorizin and dodecyl polydatin suppressed intestinal glucose transport more effectively than phlorizin and polydatin, suggesting that they were promising in vivo hypoglycemic active compounds.
研究领域:
药理学
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生物化学
·
分子生物学
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营养学
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）