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ellagic acid
FOOD CHEMISTRY · 2025 · IF 9.8

Tracking the gastrointestinal fate and prebiotic effect of ellagic acid-rich fruit byproducts: A comprehensive evaluation

Zhike Xie,Feng Chen,Pei Li,Yawen Xiao,Zheng Ruan

This study demonstrated the potential of ellagic acid-rich fruit byproducts, particularly pomegranate peel, as functional ingredients. During digestion, pomegranate peel exhibited superior antioxidant activity owing to its high phenolic content. Twenty-four phenolic compounds were released, with pomegranate peel maintaining higher bioactivity than chestnut and walnut peels. In vitro colonic fermentation with urolithin A-producing microbiota revealed that pomegranate peel stimulated butyrate synthesis (11.94 mM) and urolithin A production (6.31 μM), highlighting the prebiotic role of ellagic acid. Gut microbiota modulation by pomegranate peel increased Bacteroide s and Bifidobacterium (a potential key for ellagic acid conversion) while suppressing Alistipes . Functional analyses confirmed its effect on carbohydrate, lipid, and amino acid metabolism. In contrast, chestnut and walnut peels exhibited lower bioactivity and microbial selectivity. These findings positioned pomegranate peel as a superior ingredient for gut health and microbial metabolism optimization, offering targeted nutritional benefits over conventional byproducts.

CAS / MDL: 64-19-7
✓ 已验证 产品关联 DOI PubMed 高影响因子
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AAPS PHARMSCITECH · 2025 ·Vol. 26 ·期 4 ·1-17 · IF 4

Treatment of Bleomycin-induced Pulmonary Fibrosis by Intratracheal Instillation Administration of Ellagic Acid-Loaded Chitosan Nanoparticles

Luo Zhilin,Sun Yao,Cai Shihao,Liu Hongting,Zhao Conglu,Xu Xiang,Xu Aiguo,Zhou Honggang,Yang Cheng,Gu Xiaoting,Ai Xiaoyu

Idiopathic Pulmonary Fibrosis (IPF) is a rare and serious chronic interstitial lung disease that may endanger the lives of patients. The median survival time of patients with idiopathic pulmonary fibrosis is short, and the mortality rate is higher than that of many types of cancer. At present, pirfenidone (PFD) and nintedanib (NDNB) have been approved by FDA for IPF, but they can only delay the process of pulmonary fibrosis and cannot cure the disease. Therefore, it is urgent to develop other drugs with the effect of improving pulmonary fibrosis. Ellagic acid (EA) can inhibit the Wnt-signaling pathway and has an effect in treating pulmonary fibrosis induced by bleomycin (BLM) in mice. However, its solubility is poor, resulting in its low bioavailability and limited therapeutic benefits, so its clinical application has been limited. Herein, based on the characteristics of nano-drug lung delivery system, chitosan (CS) was selected as the carrier, and ellagic acid-loaded chitosan nanoparticles (EA-CS-NPs) were prepared by ionic gelation method. The EE% and DL% of prepared EA-CS-NPs was 73.73 ± 4.52% and 6.23 ± 1.09%, the particle size was 119.6 ± 5.51 nm (PDI = 0.234 ± 0.017), the zeta potential was 29.833 ± 0.503 mV. The morphology of the nanoparticles was observed by TEM microscope, which was round, uniform dispersion, indicating that the preparation process is stable and feasible. The toxicity experiment showed that EA-CS-NPs maintained 80% cell viability, significantly higher than that of the NDNB group, indicating lower toxicity and better inhibitory effects on TGF-β1-stimulated MLg and NIH-3T3 cells. Wound healing assay results showed that the inhibitory effect of EA-CS-NPs on cell migration was more pronounced than that of EA in the same amount of EA-containing drugs. Drug uptake experiments revealed that EA-CS-NPs significantly enhanced drug uptake in MLg and NIH-3T3 cells. In vivo , Cy7-CS-NPs exhibited higher fluorescence intensity in rat lungs compared to Cy7 solution, indicating better lung retention. The in vivo efficacy test showed that compared with the EA group, EA-CS-NPs could better reduce the area of pulmonary fibrosis and collagen deposition, improve lung function, and have a longer retention time in the lung. In summary, our results revealed that EA-CS-NPs may be a good choice for the treatment of pulmonary fibrosis. Graphical

CAS / MDL: 476-66-4
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Current Traditional Medicine · 2024 ·Vol. 11 ·期 6 ·E22150838296794 · IF 0.6

Exploring the Anti-melanogenic, Antioxidant, and Anti-inflammatory Activities of a Composition: Glabridin, Resveratrol and Ellagic Acid

Jie Huang,Chong Xie,Zhi Pan,Mengya Lin,Qingsheng Chen,Shengzhao Gong,Yadong Huang

BackgroundPlant extracts have wide applications in food, nutrition, and cosmetics, which results in a deeper investigation of natural ingredients. Numerous natural ingredients have been demonstrated to exhibit multiple activities, including antioxidation, anti-inflammation, and anti-melanogenesis. However, their combinations have not been well investigated, which could provide stronger performance with less toxicity and easier applications.MethodsWe used B16F10 cells treated with alpha-melanocyte stimulating hormone (αMSH) for melanogenesis-related studies, including cellular melanin content, tyrosinase activity, and gene or protein expression. MTT assay was used to evaluate cell viability. DPPH scavenging activity was measured for antioxidation. Nitric oxide (NO) content was evaluated in lipopolysaccharide (LPS) treated RAW264.7 cells to indicate the performance on anti-inflammation.ResultsIn this study, six different compounds and their combinations were tested for melanogenesis. The results showed that the combination of glabridin, resveratrol, and ellagic acid (GRE) exhibited the highest efficiency, which was mainly manifested as inhibition of melanin production and tyrosinase activity, higher DPPH scavenging rate, and inhibition of nitric oxide (NO) production. Meanwhile, our results showed that GRE could significantly downregulate the expression of microphthalmia-associated transcription factor (MITF) related genes and proteins and could also inhibit the phosphorylation of cyclic AMP response element-binding protein (CREB), which was the upstream signal of MITF.ConclusionThe results suggest GRE exhibits high efficiency in inhibiting anti-melanogenesis, antioxidation, and anti-inflammation. Furthermore, GRE could downregulate the phosphorylation of the CREB and MITF signal pathway, which provides a theoretical basis for its application in pigmentation disorder disease and cosmetics.

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IET Nanobiotechnology · 2023 ·Vol. 17 ·期 4 ·368-375 · IF 2.3

Xanthine oxidase inhibitory kinetics and mechanism of ellagic acid: In vitro, in silico and in vivo studies

Jianmin Chen,Zemin He,Sijin Yu,Xiaozhen Cai,Danhong Zhu,Yanhua Lin

Ellagic acid (EA), which is widely distributed in many foods, has been found to possess inhibitory activity against xanthine oxidase (XO). However, there is ongoing debate about the difference in XO inhibitory activity between EA and allopurinol. Additionally, the inhibitory kinetics and mechanism of EA on XO are still unclear. Herein, the authors systematically studied the inhibitory effects of EA on XO. The authors’ findings showed that EA is a reversible inhibitor with mixed-type inhibition, and its inhibitory activity is weaker than allopurinol. Fluorescence quenching experiments suggested that the generation of EA-XO complex was exothermic and spontaneous. In silico analysis further confirmed that EA entered the XO catalytic centre. Furthermore, the authors verified the anti-hyperuricemia effect of EA in vivo. This study elucidates the inhibition kinetics and mechanism of EA on XO, and lays a theoretical foundation for the further development of drugs and functional foods containing EA for the treatment of hyperuricemia.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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Analytical Methods · 2013 ·Vol. 5 ·期 13 ·3228-3234 · IF 1.855

Determination of ellagic acid by fluorescence quenching method with glutathione capped CdTe quantum dots as the probe

Yizhong Shen,Shaopu Liu,Jian Wang,Dan Li,Youqiu He

A sensitive and simple method for the determination of ellagic acid (EA) was developed based on the fluorescence quenching effect of EA for glutathione (GSH)-capped CdTe quantum dots (QDs). Under optimum conditions, a good linear relationship was obtained from 0.3118 to 55.0 μg mL−1 with a correlation coefficient of 0.9983, and the detection limit (3σ/K) was 0.0936 μg mL−1. The fluorescence quenching mechanism has been proposed on the basis of electron transfer supported by ultraviolet-visible (UV-vis) absorption, fluorescence (FL) spectroscopy and the measurement of fluorescence lifetime. The method has been applied to the determination of EA in synthetic samples and fresh urine samples of healthy humans with satisfactory results. The proposed method manifested several advantages such as high sensitivity, short analysis time, low cost and ease of operation.

CAS / MDL: 476-66-4 70-18-8
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APPLIED MICROBIOLOGY AND BIOTECHNOLOGY · 2024 ·Vol. 108 ·期 1 ·1-14 · IF 3.9

In vitro conversion of ellagic acid to urolithin A by different gut microbiota of urolithin metabotype A

He Fuxiang,Bian Yingying,Zhao Yaling,Xia Mengjie,Liu Shu,Gui Jiajin,Hou Xiaoyue,Fang Yaowei

Abstract The metabolite urolithin A, a metabolite of the dietary polyphenol ellagic acid (EA), has significant health benefits for humans. However, studies on the gut microbiota involved in ellagic acid metabolism are limited. In this study, we conducted in vitro fermentation of EA using human intestinal microbiome combined with antibiotics (vancomycin, polymyxin B sulfate, and amphotericin B). Liquid chromatography-mass spectrometry (LC–MS/MS) analysis demonstrated that the production capacity of urolithin A by gut microbiota co-treated with polymyxin B sulfate and amphotericin B (22.39 µM) was similar to that of untreated gut microbiota (24.26 µM). Macrogenomics (high-throughput sequencing) was used to analyze the composition and structure of the gut microbiota. The results showed that the abundance of Bifidobacterium longum , Bifidobacterium adolescentis , and Bifidobacterium bifidum in the gut microbiota without antibiotic treatment or co-treated with polymyxin B sulfate and amphotericin B during EA fermentation was higher than that in other antibiotic treatment gut microbiota. Therefore, B. longum , B. adolescentis , and B. bifidum may be new genera involved in the conversion of EA to urolithin A. In conclusion, the study revealed unique interactions between polyphenols and gut microbiota, deepening our understanding of the relationship between phenolic compounds like EA and the gut microbiota. These findings may contribute to the development of gut bacteria as potential probiotics for further development. Key points • Intestinal microbiome involved in ellagic acid metabolism. • Gram-positive bacteria in the intestinal microbiome are crucial for ellagic acid metabolism. • Bifidobacterium longum, Bifidobacterium adolescentis, and Bifidobacterium bifidum participate in ellagic acid metabolism.

CAS / MDL: 75-05-8 64-18-6
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Sustainable Chemistry and Pharmacy · 2024 · IF 5.5

Optimization of the preparation of high-purity ellagic acid from blueberry pomace through an antisolvent precipitation method

Jiao Xie,Huiqun Wang,Tingyuan Ren,Qijian Zheng,Mengxue Chen

Due to the low purity of natural ellagic acid, its clinical application has been less reported. Currently, blueberry pomace is discarded as processing waste. However, it is rich in ellagic acid and a good raw material for producing high-purity ellagic acid. Therefore, this study aimed to investigate an optimal horizontal combination scheme for producing of high-purity ellagic acid by antisolvent precipitation using crude ellagic acid extracted from blueberry pomace. Solvent screening results indicated that n-methylpyrrolidone had the highest ellagic acid solubility. Single-factor analysis showed that the oscillation speed, reaction time, crystallization temperature and antisolvent-to-solvent ratio had significantly affected ellagic acid purity, but solid-liquid ratio had little effect. A Box-Behnken-Centre combined design was used to determine the optimal combined scheme. The results showed that at a solvent concentration of 20 mg/mL, the optimal parameters were crystallization temperature 21.1 °C, reaction time 11.2 min, volume ratio of 15.6:1 antisolvent to solvent and oscillation speed of 144 r/min. Under these conditions, ellagic acid purity was 96.63%, relative standard deviation (RSD) was 1.20%, and recovery rate was 69.60%. Fourier transform infrared analysis showed that the spectral peak of purified ellagic acid matched that of the standard. In summary, the antisolvent precipitation method greatly improved the purity of ellagic acid extracted from blueberry pomace, which is not only conducive to the resource recycling, but also provides a theoretical basis for the production of high-purity ellagic acid and the possibility of expanding the application scope of ellagic acid in pharmaceuticals and nutraceuticals.

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Journal of Functional Foods · 2026 · IF 3.9

Anti-colitis benefits of ellagic acid-Fucus vesiculosus polysaccharide solid dispersions by regulating intestinal microbiota dysfunction in mice

Weipei Li,Zhao-Rong Li,Guanghuo Liu,Fenghua Liang,Chunxia Zhou,Pengzhi Hong,Mouming Zhao,Jinsong Wang,Donghui Luo,Rui-Bo Jia

The current study was aimed to investigate the anti-inflammatory effects and potential mechanisms of ellagic acid- Fucus vesiculosus polysaccharide solid dispersion (EA/FVP SD) based on lipopolysaccharide (LPS)-induced inflammatory cell and dextran sulfate sodium (DSS)-induced colitis mice models. The cell experiment showed that EA/FVP SD possessed a better in vitro anti-inflammatory activity than EA or FVP alone. Further colitis mice experiments showed that EA/FVP SD administration significantly ameliorated symptoms in colitis mice by reversing the weight loss, reducing the disease activity index (DAI) scores, maintaining the colon length and decreasing the levels of pro-inflammatory factors (such as TNF- α , IL-6, and IL-1 β ). Immunofluorescent staining suggested that the anti-inflammatory activity was related to the down-regulation of CD11b and F4/80 protein expression levels. Notedly, high dose EA/FVP SD exhibited the best performance in reducing the fluorescence intensity. Moreover, microbiome analysis indicated that EA/FVP SD administration could reverse the abnormal bacteria composition changes and enhance the intestinal barrier function. Metabolomic profiling suggested the alterations of EA/FVP SD in key metabolic pathways, including linoleic acid metabolism, sphingolipid metabolism, necroptosis/apoptosis-related processes, and FoxO signaling pathway, which may be associated with changes in gut microbiota. These findings support EA/FVP SD as a candidate adjuvant strategy for colitis management, while further pharmacokinetic and pathway-validation studies are still needed.

CAS / MDL: 599-79-1
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Journal of Functional Biomaterials · 2023 ·Vol. 14 ·期 5 ·278 · IF 4.8

Ellagic Acid Inclusion Complex-Loaded Hydrogels as an Efficient Controlled Release System: Design, Fabrication and In Vitro Evaluation

Chengqun Yu,Abid Naeem,Yali Liu,Yongmei Guan

Oxidants play a crucial role in the development of oxidative stress, which is linked to disease progression. Ellagic acid is an effective antioxidant with applications in the treatment and prevention of several diseases, since it neutralizes free radicals and reduces oxidative stress. However, it has limited application due to its poor solubility and oral bioavailability. Since ellagic acid is hydrophobic, it is difficult to load it directly into hydrogels for controlled release applications. Therefore, the purpose of this study was to first prepare inclusion complexes of ellagic acid (EA) with hydroxypropyl-β-cyclodextrin and then load them into carbopol-934-grafted-2-acrylamido-2-methyl-1-propane sulfonic acid (CP-g-AMPS) hydrogels for orally controlled drug delivery. Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), scanning electron microscopy (SEM), thermogravimetric analysis (TGA), and differential scanning calorimetry (DSC) were used to validate ellagic acid inclusion complexes and hydrogels. There was slightly higher swelling and drug release at pH 1.2 (42.20% and 92.13%) than at pH 7.4 (31.61% and 77.28%), respectively. Hydrogels had high porosity (88.90%) and biodegradation (9.2% per week in phosphate-buffered saline). Hydrogels were tested for their antioxidant properties in vitro against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS). Additionally, the antibacterial activity of hydrogels was demonstrated against Gram-positive bacterial strains (Staphylococcus aureusandEscherichia coli) and Gram-negative bacterial strains (Pseudomonas aeruginosa).Keywords:hydrogels;polyphenol;phytoconstituents;inclusion complexation;anti-oxidants;bioavailability

CAS / MDL: 7631-90-5
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Foods · 2022 ·Vol. 11 ·期 17 ·2621 · IF 5.561

Lactococcus garvieae FUA009, a Novel Intestinal Bacterium Capable of Producing the Bioactive Metabolite Urolithin A from Ellagic Acid

Haoyu Mi,Shu Liu,Yang Hai,Guang Yang,Jing Lu,Fuxiang He,Yaling Zhao,Mengjie Xia,Xiaoyue Hou,Yaowei Fang

Dietary polyphenol ellagic acid has anti-cancer and anti-inflammatory activities, and these biological activities require the conversion of ellagic acid to urolithins by intestinal microbes. However, few gut microbes are capable of metabolizing ellagic acid to produce urolithins, limiting the beneficial effects of ellagic acid on health. Here, we describe an intestinal bacteriumLactococcus garvieaeFUA009 isolated from the feces of a healthy volunteer. It was demonstrated via HPLC and UPLC-MS analysis that the end product of ellagic acid metabolism of FUA009 was urolithin A. In addition, we also examined the whole genome sequence of FUA009 and then assessed the safety and probiotic properties of FUA009 based on a complete genome and phenotype analysis. We indicated that FUA009 was safe, which was confirmed by FUA009 being sensitive to multiple antibiotics, having no hemolytic activity, and being free of aggressive putative virulence factors. Moreover, 19 stress-responsive protein genes and 8 adhesion-related genes were predicted in the FUA009 genome. Furthermore, we demonstrated that FUA009 was tolerant to acid and bile salt by determining the cell viability in a stress environment. In summary,LactococcusgarvieaeFUA009, as a novel UA-producing bacterium, not only contributes to the study of the metabolic pathway of ellagic acid but is also expected to be a novel probiotic candidate.Keywords:plant-derived activities;Lactococcusgarvieae;ellagic acid;urolithin A;complete genome;safety and probiotic characteristics

CAS / MDL: 75-05-8 64-19-7 67-56-1
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ANALYTICA CHIMICA ACTA · 2017 · IF 4.95

Seed-mediated growth of Au@Ag core-shell nanorods for the detection of ellagic acid in whitening cosmetics

Yi Wang,Yang Zeng,Wensheng Fu,Pu Zhang,Ling Li,Cuiying Ye,Lan Yu,Xiaochun Zhu,Song Zhao

Seed-mediated growth has been employed as a simple and powerful means to the shape-controlled synthesis of metal nanocrystals . In this work, we apply the principle of seed-mediated growth in analytical chemistry , and achieve improved sensitivity due to the low energy barrier in the target-induced formation of bimetallic nanoparticles with core-shell structure. As a result, a simple, reliable, highly sensitive and selective method for the detection of ellagic acid (EA), a naturally occurring polyphenolic antioxidant , has been developed. With the aid of EA in alkaline solution, Ag + ions can be transformed to Ag atoms and deposit on the surfaces of Au nanorods (AuNRs, act as seeds here) to generate Au@Ag core-shell nanorods, accompanied by blue shift of the longitudinal localized surface plasmon resonance (LSPR) band of AuNRs from near-infrared region to shorter wavelengths. Based on the linear relationship between the wavelength change of longitudinal LSPR band and the concentration of EA, our method achieves a detectable range of 0.2–20 μM and a limit of detection as low as 40 nM toward EA. This approach is highlighted by its high sensitivity for EA assay, which benefits from the viewpoint of thermodynamics in the nucleation/growth mode of metal nanoparticles. Moreover, this method shows high selectivity for EA detection when potential species coexist, and thus has been successfully applied in the detection of EA in skin-whitening cosmetics. The proposed strategy of seed-mediated growth herein can also be extended to other systems for sensing.

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Journal of Biomaterials and Tissue Engineering · 2019 ·Vol. 9 ·期 8 ·1108-1113 · IF 0.824

Effect of Ellagic Acid on Wound Healing of Chronic Skin Ulceration in Diabetic Mice and Macrophage Phenotype Transformation

Fan Gaofu,Xu Zhenguo,Tang Jie,Liu Longyun,Dai Ruomeng

Objection: To study the effect of modified formulae for ellagic acid (EA) on wound healing and macrophage phenotype transformation in diabetic mice. Materials and Methods: 10 db/m mice regarded as normal group, Dividing 20 db/db mice as the model group and EA group, 10 in every group. Surgical operation on the back was made to prepare experimental wound models. External medicines were applied and changed dressings every other day and measurement. Wound tissues were gained when animals were sacrificed by anesthesia 7 days later. Pathological changes were observed by HE and Masson staining methods, while using RT-PCR and IHC to measure mRNA and protein levels of MI/M2 type cytokines of the wound tissues. Results: Compared with the normal group, the wound area of db/db was greater (P < 0.001), while EA group less (P < 0.001). IL-12 and TNF-α mRNA and proteins levels in model group were higher (P < 0.001, respectively), while VEGF and TGF-βmRNA and proteins were lower. mRNA and protein levels of inflammato cytokines of EA group was all lower (P < 0.001), while the growth factor were significantly higher (P < 0.001). Conclusion: Wound healing of db/db mice was delayed and modified formulae for EA had effects on wound healing. The way by decreasing the Ml type inf1ammatory factors and improving the M2 type growth factors might be one of the mechanisms for wound healing.

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