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Ellagic acid
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY · 2026 · IF 4.8

Inhibition of lipoxygenase by ellagic acid: Insights from multi-spectroscopic techniques and molecular docking

Xiaoqin Diao,Mei Tian,Shulei Li,Gaojie Zhao,Nike Tian,Qiao Guan,Dengyong Liu,Haining Guan

Lipoxygenase (LOX)-induced endogenous lipid peroxidation significantly contributes to food nutrient loss and flavor deterioration. This study aimed to investigate the inhibitory mechanism of ellagic acid (EA) on LOX by integrating enzyme kinetics, multi-spectroscopic techniques, and molecular docking. The results showed that EA inhibited LOX in a dose-dependent manner, achieving an inhibition rate of 87.73% at 600 μg/mL and an IC 50 of 20.84 μg/mL. The inhibition was identified as mixed-type competitive inhibition. EA effectively quenched the endogenous fluorescence of LOX through static quenching, and the association constant increased with rising temperature. Thermodynamic parameters suggested that the formation of the EA-LOX complex was spontaneous and endothermic, primarily driven by hydrophobic interactions. EA preferentially interacted with tryptophan residues, inducing changes in the microenvironment and secondary structure of LOX. Additionally, an increase in the average particle size confirmed complex formation. The molecular docking results were consistent with the spectroscopic experiments, providing a possible microscopic mechanism for the maintenance of the three-dimensional conformation of the complex through hydrophobic interactions and hydrogen bonding. This study provides a theoretical foundation for the use of EA to regulate LOX activity and highlights its promising application in food quality preservation.

✓ 已验证 DOI PubMed 高影响因子
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CARBOHYDRATE POLYMERS · 2025 · IF 12.5

Ellagic acid-grafted carboxymethyl chitosan/graphene oxide-coated nanofibrous membrane for immunomodulatory periosteal regeneration

Xue Zhang,Chunyi Luo,Na Liu,Siyu Liu,Zhouquan Jiang,Jinjun Zhou,Lishu Shao,Weihua Luo

To enhance the clinical value of carboxymethyl chitosan (CMCS) as an osteogenic material, improving its bioactivity and mechanical strength is crucial. Meanwhile, ellagic acid (EA) has strong bioactivities but low bioavailability due to its hydrophobicity. In this study, by introducing EA units into CMCS molecules, a near-infrared (NIR) light-mediated nanofiber membrane based on polycaprolactone (PCL)/EA-CMCS blended nanofibers coated with an EA-CMCS/graphene oxide (GO) layer (PCL/EA-CMCS@EA-CMCS/GO) was designed. The bioactivity of CMCS and bioavailability of EA could be significantly improved by covalent coupling of EA with CMCS. Blending EA-CMCS with PCL significantly enhanced the mechanical properties of nanofiber membranes. The coated nanofibrous membrane featured a multi-level structure of coating and blending. By leveraging the photothermal conversion effect of GO, it enabled the programmed and sustained release of EA-CMCS from both the coating and the nanofibers. Moreover, the membrane exhibited excellent biomineralization and antioxidant capabilities. It effectively regulated macrophage polarization and promoted the adhesion, proliferation, and osteogenic differentiation of MC3T3-E1 osteoblasts. These properties enabled the membrane to regulate the harsh osteogenic immune microenvironment and promote bone regeneration. This biomimetic periosteum holds great potential as a substitute for periosteal grafts and offers a novel strategy for developing artificial periosteum.

CAS / MDL: 476-66-4 6066-82-6
研究领域: 生物材料学 · 组织工程学 · 医学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF FOOD BIOCHEMISTRY · 2019 ·Vol. 43 ·期 11 ·e12996 · IF 1.358

Antityrosinase mechanism of ellagic acid in vitro and its effect on mouse melanoma cells

Qian Huang,Wei-Ming Chai,Zuo-Yuan Ma,Wei-Liang Deng,Qi-Ming Wei,Shuang Song,Zheng-Rong Zou,Yi-Yuan Peng

The activities of ellagic acid in inhibiting mushroom tyrosinase and cell proliferation were evaluated in this research. The results of enzyme kinetics indicated that ellagic acid could effectively inhibit tyrosinase activity. The value of the semi-inhibitory rate (IC 50 ) was 0.2 ± 0.05 mM. Ellagic acid inhibited tyrosinase activity in a reversible manner and was a mixed tyrosinase inhibitor. Furthermore, ellagic acid had a good inhibitory effect on the proliferation of mouse melanoma B 16 cells and could induce apoptosis. The results acquired from fluorescence spectroscopy revealed that the interaction of ellagic acid with tyrosinase depended on hydrogen bond and electrostatic force. In addition, computational docking showed that ellagic acid interacted with amino acid residues of tyrosinase (Asn19 and Lys372) by hydrogen bond and produced electrostatic interaction with amino residue Lys18. Practical applications In the present research, the antityrosinase mechanism of ellagic acid and its effect on mouse melanoma cells were investigated. This study suggested that ellagic acid had a strong inhibitory activity against tyrosinase and cell proliferation,which laid an experimental foundation for the development of new drugs and whitening products. The combined multispectral methods used in this research can be applied to the screening of other antityrosinase inhibitors, further promoting the development and utilization of tyrosinase inhibitors.

研究领域: 生物化学 · 药理学 · 肿瘤学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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FOOD CHEMISTRY · 2023 · IF 8.8

Oral supplementation of Gordonibacter urolithinfaciens promotes ellagic acid metabolism and urolithin bioavailability in mice

Yang Yang,Pui-Kei Lee,Ho-Ching Wong,Danyue Zhao

Ellagic acid (EA) is an abundant dietary polyphenol with multifarious health benefits but low bioavailability. To increase its bio-efficacy, converting EA to urolithins by supplementing urolithin-producing bacteria, e.g., Gordonibacter urolithinfaciens ( G.uro ), could be a solution. This work first tested three methods for oral delivery of live G.uro . Intestinal colonization of G.uro and its impact on local gut microbiota, EA-to-urolithin conversion and bioavailability were then investigated in C57BL/6J mice administered to EA only or a synbiotic ( G. uro  + EA). In vitro results suggested that G.uro largely survived simulated gastrointestinal digestion and could be administered without protection. In vivo results showed that G.uro had little impact on local gut microbiota but could not colonize the gut. Moreover, synbiotic remarkably promoted Akkermansia , Lactobacillus and Bifidobacterium growth, and significantly enhanced the bioavailability of urolithins compared with the EA-only group. This study demonstrated the potential of oral supplementation of G.uro for enhancing EA-to-urolithin bioconversion and bioavailability.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2021 · IF 5.279

Maillard Browning Inhibition by Ellagic Acid via Its Adduct Formation with the Amadori Rearrangement Product

Heping Cui,Ziyan Wang,Mengyu Ma,Khizar Hayat,Qiang Zhang,Yan Xu,Xiaoming Zhang,Chi-Tang Ho

The Maillard reaction performed under a stepwise increase of temperature was applied for researching the inhibition of Maillard browning caused by ellagic acid. Ellagic acid was found effective for the inhibition of melanoidin formation in the xylose–glycine Maillard reaction but depended on its dosage and the point of time it was added in the reaction system. The lightest color of the Maillard reaction products was observed when ellagic acid was added at the 90th min, which was the point of time when the Amadori rearrangement product (ARP) developed the most. LC-ESI-MS/MS analysis results showed a significant tendency of the ellagic acid hydrolysis product to react with the predominant intermediate ARP to yield an adduct. The adduct stabilized the ARP and delayed its decomposition and inhibited the downstream reactions toward browning. After the ARP was depleted, ellagic acid also showed an effect on scavenging some short-chain dicarbonyls which contributed to the inhibition of Maillard browning.

研究领域: 食品科学 · 生物化学
✓ 已验证 DOI 高影响因子
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Frontiers of Chemical Science and Engineering · 2023 ·Vol. 17 ·期 6 ·784-794 · IF 4.5

Enzyme@bismuth-ellagic acid: a versatile platform for enzyme immobilization with enhanced acid-base stability

Xu Junyang,Liu Guanhua,He Ying,Zhou Liya,Ma Li,Liu Yunting,Zheng Xiaobing,Gao Jing,Jiang Yanjun

In situ encapsulation is an effective way to synthesize enzyme@metal-organic framework biocatalysts; however, it is limited by the conditions of metal-organic framework synthesis and its acid-base stability. Herein, a biocatalytic platform with improved acid-base stability was constructed via a one-pot method using bismuth-ellagic acid as the carrier. Bismuth-ellagic acid is a green phenol-based metal-organic framework whose organic precursor is extracted from natural plants. After encapsulation, the stability, especially the acid-base stability, of amyloglucosidases@bismuth-ellagic acid was enhanced, which remained stable over a wide pH range (2–12) and achieved multiple recycling. By selecting a suitable buffer, bismuth-ellagic acid can encapsulate different types of enzymes and enable interactions between the encapsulated enzymes and cofactors, as well as between multiple enzymes. The green precursor, simple and convenient preparation process provided a versatile strategy for enzymes encapsulation.

研究领域: 生物技术 · 催化 · 材料科学 · 酶学
✓ 已验证 DOI 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2025 · IF 8.5

Zinc ions coordinated carboxymethyl chitosan hydrogel doped with ellagic acid for accelerative diabetic wound healing

Junbo Zhao,Jiyuan Du,Yilu Zheng,Yifei Fang,Jianlin Huang,Jun Wu,Yiqun Wu,Tianqi Nie

Diabetic wound healing remains a critical clinical challenge due to persistent inflammation derived from long-term hyperglycemia. To address this challenge, we reported a zinc ion coordinated CMCS hydrogel for pH responsive delivery of ellagic acid to fulfill diabetic wound management. The incorporation of zinc ions and EA reinforce the hydrogel network via coordination and hydrogen bonding, and confer a pH-responsive release of EA under simulative wound microenvironment. CMCS-Zn@EA hydrogel exhibited substantial scavenge capacity against multiple oxidative species (·OH and ABTS), which may protect fibroblasts from oxidative damage, and thereby promoting cellular migration and angiogenesis. Further investigation on diabetic wound models revealed that the topical administration of CMCS-Zn@EA effectively accelerated the wound healing ratio through promoting angiogenesis, re-epithelialization, and collagen deposition. Moreover, the incorporation of Zn 2+ into the hydrogel framework through coordination bonding dynamically aligned with the whole wound healing phases to modulate macrophage polarization and thus providing a more favorable environment for the wound healing. Together with the great biocompatibility, CMCS-Zn@EA hydrogel may hold great potency to be applied in the clinical diabetic wound management.

CAS / MDL: 872-50-4 9012-76-4
研究领域: 生物材料学 · 伤口修复与再生医学 · 纳米医学 · 药剂学 · 免疫调节 · 糖尿病并发症
✓ 已验证 产品关联 DOI PubMed 高影响因子
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PHYTOMEDICINE · 2025 · IF 8.3

Pomegranate peel and ellagic acid attenuate ulcerative colitis by targeting AKR1B1/B3 to inhibit NLRP3

Huimin Li,Jingya Ruan,Jiayan Huang,Yijin Wu,Jiaming Cheng,Ongher Kouye,Yi Zhang,Tao Wang

Background Ulcerative colitis (UC) therapy remains challenging due to limited options. Pomegranate peel, rich in bioactive compounds, shows potential, but its key components and mechanisms underlying its action against UC are unclear. Purpose The present investigation was undertaken to assess the therapeutic efficacy of 70 % ethanolic (PPEE) and aqueous extracts (PPWE) derived from pomegranate peel, determine the primary active component, and clarify the underlying molecular mechanism. Study design and methods The anti-UC effects of PPEE and PPWE extracts were first assessed in DSS-induced mice. Differential constituents underlying their efficacy disparities were identified using LC-MS/UHPLC and chemometric analyses. Key bioactive compounds were screened via a model of Caco-2/THP-1 co-culture evaluating intestinal barrier function. The action mechanisms were further elucidated through molecular docking, surface plasmon resonance (SPR), co-immunoprecipitation (Co-IP), and other assays, validated across inflammatory cell models, DSS-induced mice, and human UC colon tissues. Results PPEE showed superior efficacy over PPWE, as evidenced by enhanced intestinal barrier function and suppressed inflammation and NLRP3 inflammasome activation. Ellagic acid (EA) was identified as the core active constituent, which directly targeted AKR1B1/AKR1B3, thereby inhibiting NLRP3-ASC oligomerization and subsequent cleavage of caspase-1 and IL-1 β . Conclusion This study unveils a novel pathogenic mechanism in UC, namely the AKR1B1/AKR1B3-NLRP3 axis, and identifies EA as its effective inhibitor. These results demonstrate the potential of pomegranate peel extracts and offer a novel therapeutic approach for UC.

研究领域: 药理学 · 胃肠病学 · 分子生物学 · 天然产物研究
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2021 · IF 5.279

Ellagic Acid Exerts Beneficial Effects on Hyperuricemia by Inhibiting Xanthine Oxidase and NLRP3 Inflammasome Activation

Ze-Rui Sun,Hua-Rong Liu,Di Hu,Mao-Si Fan,Ming-Yue Wang,Meng-Fei An,Yun-Li Zhao,Ze-Min Xiang,Jun Sheng

Hyperuricemia is a metabolic disease caused by impaired uric acid (UA) metabolism. Ellagic acid (EA) is a natural small-molecule polyphenolic compound with known antioxidative and anti-inflammatory properties. Here, we evaluated the regulatory effects of EA on hyperuricemia and explored the underlying mechanisms. We found that EA is an effective xanthine oxidase (XOD) inhibitor (IC50 = 165.6 μmol/L) and superoxide anion scavenger (IC50 = 27.66 μmol/L). EA (5 and 10 μmol/L) treatment significantly and dose-dependently reduced UA levels in L-O2 cells; meanwhile, intraperitoneal EA administration (50 and 100 mg/kg) also significantly reduced serum XOD activity and UA levels in hyperuricemic mice and markedly improved their liver and kidney histopathology. EA treatment significantly reduced the degree of foot edema and inhibited the expression of NLPR3 pathway-related proteins in foot tissue of monosodium urate (MSU)-treated mice. The anti-inflammatory effect was also observed in lipopolysaccharide-stimulated RAW-264.7 cells. Furthermore, EA significantly inhibited the expressions of XOD and NLRP3 pathway-related proteins (TLR4, p-p65, caspase-1, TNF-α, and IL-18) in vitro and in vivo. Our results indicated that EA exerts ameliorative effects in experimental hyperuricemia and foot edema via regulating the NLRP3 signaling pathway and represents a promising therapeutic option for the management of hyperuricemia.

CAS / MDL: 3562-84-3 68-94-0
研究领域: 药理学 · 代谢疾病 · 炎症 · 生物化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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FOOD CHEMISTRY · 2022 · IF 9.231

Quantitative conversion of free, acid-hydrolyzable, and bound ellagic acid in walnut kernels during baking

Xin Guo,Fengying Gu,Tingting Yang,Zhixiao Shao,Qiaozhen Zhang,Jinjin Zhu,Feng Wang

Ellagitannins, the main components of walnut kernel polyphenols, are easily degraded by heating to produce ellagic acid, precursor in the production of urolithins that show multiple physiological functions. To analyze the conversion of ellagitannins to free ellagic acid in walnut kernels during baking, a quantitative method was developed to investigate the ellagic acid content (EAC) in free phenolic acid (FPA), acid-hydrolyzable phenolic acid (AHPA), and bound phenolic acid (BPA) fractions. The results showed that the EAC in FPA reached its maximum (5.17 ± 0.30 mg/g DW) after baking at 165 °C for 30 min, which increased by 99.52% compared with the control. Meanwhile, the content of ellagitannins (ETC) in AHPA and BPA dropped by 89.14% and 26.08%, respectively. It suggested that baking promoted the conversion of ellagitannins in AHPA and BPA to ellagic acid in FPA. Eight ellagitannins were regarded as the main precursors of ellagic acid in walnut kernels.

研究领域: 食品科学 · 植物化学
✓ 已验证 DOI PubMed 高影响因子
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Foods · 2026 ·Vol. 15 ·期 15 ·2587 · IF 6

Fucus vesiculosus Polysaccharide-Based Solid Dispersions Enhance Aqueous Dispersion and Gut Microbial Biotransformation of Ellagic Acid

Rui-Bo Jia,Dapei Ou,Fenghua Liang,Zhao-Rong Li,Jinsong Wang,Chunxia Zhou,Pengzhi Hong

Ellagic acid (EA) is a food-derived polyphenol with multiple biological activities, but its poor water solubility and aggregation in aqueous systems limit its accessibility to gut microorganisms. In this study,Fucus vesiculosuspolysaccharide (FVP) was used as a natural carrier to prepare EA/FVP solid dispersions (SDs) with different mass ratios by solvent-assisted evaporation. Compared with pure EA, the SDs markedly improved the apparent solubility and aqueous dispersion stability of EA. The highest apparent solubility was observed for the EA/FVP 3/1 formulation (0.75 ± 0.03 mg/mL), which was approximately 6.25-fold higher than that of pure EA (0.12 ± 0.01 mg/mL). The improved dispersion behavior was associated with increased apparent viscosity, reduced aggregation, decreased crystallinity and possible non-covalent interactions between EA and the polysaccharide matrix.In vitrofecal fermentation showed that SDs enhanced the production of urolithins, including urolithin M5, urolithin M6, urolithin C, iso-urolithin A and urolithin B, without generating new metabolite types. The EA/FVP 1/3 formulation showed the strongest promotion of urolithin production, with iso-urolithin A reaching 2.36 ± 0.28 μM. 16S rRNA sequencing showed that the enhanced urolithin production was accompanied by shifts in the fecal microbial community. Several bacterial genera positively correlated with urolithin biosynthesis, includingBacteroides_H,Negativicoccus,Parabacteroides_B,Unclassified_EggerthellaceaeandLactococcus_A, were significantly enriched in the SDs groups. These findings suggest that FVP-based SDs may serve as a potential strategy for improving the apparent solubility, aqueous dispersion and microbial biotransformation of EA.

CAS / MDL: 64-18-6
✓ 已验证 产品关联 DOI PubMed 高影响因子
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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
研究领域: 食品科学 · 营养学 · 微生物学 · 肠胃健康
✓ 已验证 产品关联 DOI PubMed 高影响因子
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