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INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES · 2025 ·Vol. 26 ·期 20 ·9887 · IF 4.9

Transcriptomic Insights into the Dual-Modulatory Role of EGCG in Alleviating Glyphosate-Induced Oxidative Stress in Cucumis melo

Qiuying Lu,Dongmiao Zhai,Yaxian Wu,Yihu Mao,Golam Jalal Ahammed,Xinzhong Zhang,Jingbo Yu,Xin Li

Glyphosate is one of the most widely used herbicides in agricultural, horticultural, and urban environments. However, its residue accumulation and oxidative damage pose serious threats to crop health and food safety. In this study, we evaluated the potential of epigallocatechin gallate, a natural polyphenol derived from tea, to alleviate glyphosate-induced stress in melon (Cucumis meloL.). LC-MS/MS analysis revealed that EGCG significantly reduced glyphosate residues in plant tissues. Transcriptome analysis indicated that glyphosate induced extensive transcriptional reprogramming, activating genes involved in detoxification and antioxidant defense. Co-treatment with glyphosate and EGCG partially mitigated this stress response and redirected gene expression toward secondary metabolic pathways, particularly flavonoid and phenylalanine biosynthesis. Under herbicide stress, EGCG restored the transcription of key flavonoid biosynthetic genes, includingPAL,C4H,CHI, andOMT. Meanwhile, EGCG also modulated the expression ofAPX,SOD, andGST, suggesting a selective effect on antioxidant systems. Co-expression network analysis identified key hub genes associated with oxidative stress and flavonoid metabolism. These findings demonstrate the dual regulatory role of EGCG in suppressing acute oxidative stress while enhancing metabolic adaptability, highlighting its potential as a natural additive for reducing herbicide residues in fruit crops.

CAS / MDL: 9005-65-6
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Research · 2025 · IF 10.7

A Multifunctional Fe-EGCG@RSL3 Nanomedicine Synergizes Ferroptosis Induction and Tumor Microenvironment Remodeling for Enhanced Bladder Cancer Immunotherapy

Chengjunyu Zhang,Sen Liu,Jianhui Zhang,Junlin Lu,Zehua Chen,Bolin Pan,Chu Liu,Ming Huang,Hengji Zhan,Hongjin Wang,Siting Chen,Kaiwen Jie,Baoqing He,Jingdie Wu,Ye Li,Haifeng Wang,Jing Zhao,Qiang Zhang,Xu Chen

Ferroptosis has promising potential for augmenting antitumor effects, but monotherapy with ferroptosis inducers in vivo has been reported to have limited efficacy in tumor management. The development of synergistic strategies with targeted capabilities is crucial for enhancing the antitumor efficacy of ferroptosis inducers. In this study, we designed and characterized a novel self-assembled nanomedicine by mixing ferrous ions (Fe 2+ ) and epigallocatechin gallate (EGCG) in a controllable manner and encapsulating the ferroptosis inducer RSL3, named Fe-EGCG@RSL3. This multifunctional nanomedicine effectively induces ferroptosis and growth inhibition in bladder cancer cells and patient-derived organoids. In vivo, Fe-EGCG@RSL3 was enriched in the subcutaneous tumors of allogenic and xenograft mouse models, thereby substantially overcoming RSL3 resistance. Intravesical instillation of Fe-EGCG@RSL3 controls orthotopic bladder tumor progression. Furthermore, nanomedicine potentiates the therapeutic effect of anti-programmed cell death protein 1 (PD1) immunotherapy by increasing the cytotoxicity of CD8 + T cells to cancer cells and modulating the proportions of both T-cell and myeloid cell subpopulations within the tumor immune microenvironment. Overall, Fe-EGCG@RSL3 has dual functions as a multifaceted nanomedicine that integrates ferroptosis induction with immunomodulation, offering a novel and clinically translatable strategy for bladder cancer therapy.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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FOOD CHEMISTRY · 2026 · IF 10.4

Modulation of protein self-assembly via hydrolysis and metal ion coordination: Effects on EGCG encapsulation and controlled release

Qian-Da Xu,Qiang He,Wei-Cai Zeng

To enhance the stability of EGCG-encapsulated protein carriers under processing and preservation, a zinc-mediated self-assembly strategy was developed. Limited protein hydrolysis combined with cyclodextrin pre-encapsulation was employed to regulate the encapsulation and release of EGCG. Cyclodextrin pre-encapsulation effectively reduced EGCG degradation and loss during particle fabrication. Increasing the protein hydrolysis degree promoted Zn 2+ -induced coordination and self-assembly, resulting in smaller, more uniform, and compact particles. Cyclodextrin pre-encapsulation improved the encapsulation efficiency of EGCG from average 68.69% to 81.23% and reduced surface-associated EGCG. Compared with free EGCG and samples without Zn 2+ (lower than 10%), the strengthened particle structure induced by metal ion showed better stability (maximum 75.1% of EGCG retention rate) after 24 h of alkaline incubation. During simulated digestion, the release of EGCG was delayed until the late intestinal phase and reached maximum 46.53% of EGCG bioaccessibility. Moderate protein hydrolysis and metal-induced self-assembly is a potential strategy to optimize EGCG encapsulation and release in protein-based delivery systems.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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FOOD CHEMISTRY · 2026 · IF 10.4

Binding mechanisms of quinone-modified EGCG (QEGCG) with plant proteins: Enhanced foaming-emulsifying properties and improved hypoglycemic activity

Yufan Dong,Xu Chen,Yiyi Lv,Shuaida Wang,Ling Jia,Xixi Cai,Shaoyun Wang

Plant protein has attracted wide attention due to its sustainability, but its poor foaming and emulsifying properties limit its application. EGCG can cross-link proteins to improve functional properties, but it is easily oxidized to quinone form (QEGCG), which may have different protein interaction mechanisms from natural EGCG. This study investigated the interaction mechanism between QEGCG and plant proteins. Multi-spectral and molecular docking showed that QEGCG formed a more broken and porous stable complex through covalent/non-covalent interactions, with a stronger binding. These structural changes resulted in significantly enhanced foaming and emulsifying properties (pea protein 2.84 × and chickpea protein 3.2 ×) compared to EGCG. The QEGCG-conjugate had stronger inhibition on α-amylase (70.02%) and α-glucosidase (77.27%). Quinoa protein could delay the intestinal release of QEGCG by 33.39% in simulated digestion, achieving synergistic functional complementation. These findings provide strategies for broadening the application of QEGCG, improving the function of plant proteins, and developing hypoglycemic foods.

CAS / MDL: 989-51-5
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FOOD CHEMISTRY · 2020 · IF 6.306

Role of green tea nanoparticles in process of tea cream formation – A new perspective

Cheng Guo,Yijie Chen,Jing Li,Fuchao Zhan,Xianling Wei,Bin Li

Green tea nanoparticles (gTNPs) are considered as the precursors of tea cream, while the role of gTNPs in the process of tea cream formation remains obscure. This study indicated that gTNPs could be coated with epigallocatechin gallate (EGCG)-caffeine (CAF) complexes to form a ternary aggregate participating in tea cream formation. First, the ζ-potentials of gTNPs and EGCG-CAF complexes were adjusted by charge screening. Then, gTNPs were introduced into EGCG + CAF mixture solutions under different ζ-potential conditions to examine their effect on turbidity, particle size and components of mixture solutions. Finally, isothermal titration calorimetry (ITC) was applied to investigate the influence of gTNPs on the thermal effects of the interaction between EGCG and CAF. Our results reveal that hydrophobic interaction exceeded electrostatic repulsion to dominate the interaction between gTNPs and EGCG-CAF complexes at the low ζ-potential condition, thus forming the gTNPs/EGCG/CAF ternary aggregate.

CAS / MDL: 7789-75-5 989-51-5
研究领域: 食品科学 · 纳米生物学 · 物理化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Journal of Functional Foods · 2022 · IF 5.223

Positive effects of Epigallocatechin-3-gallate (EGCG) intervention on insulin resistance and gut microbial dysbiosis induced by bisphenol A

Xiang Li,Yunhui Zhang,Congying Zhao,Bowei Zhang,Bo Peng,Yan Zhang,Jin Wang,Shuo Wang

Bisphenol A (BPA), a plasticizer, is widely believed to cause metabolic disorders. However, an effective intervention is still absent. This study investigated the beneficial effects of Epigallocatechin-3-gallate (EGCG) on insulin resistance and microbial disturbance induced by BPA. The serum glucose, insulin, total triglyceride, and total cholesterol were decreased in BPA-treated mice after the intervention of EGCG. The sensitivity of insulin signals in peripheral tissue was improved by modulating the phosphorylation of IRS-1, Akt, and GSK-3β. In addition, 16S rRNA analysis for fecal microbiota showed the relative abundance of Ruminiclostridium , Blautia , unidentified_Ruminococcaceae , and Candidatus_Saccharimonas were restored by the high dose of EGCG. Furthermore, EGCG increased the concentrations of fecal short-chain fatty acids and protected the gut barrier impaired by BPA. Overall, our results demonstrated the positive effects of EGCG on BPA-induced insulin resistance and gut microbial dysbiosis. The current study provides a potential treatment for the chronic metabolic toxicity of BPA.

研究领域: 药理学 · 代谢学 · 微生物学 · 毒理学
✓ 已验证 DOI 高影响因子
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FOOD CHEMISTRY · 2021 · IF 7.514

High internal phase pickering emulsions stabilized by pea protein isolate-high methoxyl pectin-EGCG complex: Interfacial properties and microstructure

Tingting Feng,Xuejiao Wang,Xingwei Wang,Xiaoming Zhang,Yao Gu,Shuqin Xia,Qingrong Huang

The pea protein isolate-high methoxyl pectin-epigallocatechin gallate (PPI-HMP-EGCG) complex was used to stabilize Pickering emulsions (PEs) and high internal phase PEs (HIPPEs), and the effect of interfacial rheology on the microstructure, bulk rheology and stability of these emulsions was investigated. The PPI-HMP-EGCG complex with PPI to EGCG 30:1 exhibited partial wettability (81.6 ± 0.4°) and optimal viscoelasticity for the formation of stable interfacial layer. The microstructure demonstrated that the PPI-HMP-EGCG complex acted as an interfacial layer and surrounded the oil droplets, and continuous phases were mainly filled with excessive HMP, which enhanced emulsion stability. The formation of a firm gel-like network structure required a dense interfacial layer to provide the PEs (complex concentration of 0.1%) and HIPPEs (oil-phase up to 0.83) with ideal viscoelasticity and stability. The results provide the guidelines for the rational design of EGCG-loaded HIPPEs stabilized by water-soluble protein/polysaccharide complexes.

CAS / MDL: 7385-67-3
研究领域: 食品科学 · 胶体科学 · 材料科学
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JOURNAL OF NANOBIOTECHNOLOGY · 2023 ·Vol. 21 ·期 1 ·1-12 · IF 10.2

Synergetic regulation of cancer cells and exhausted T cells to fight cold tumors with a fluorinated EGCG-based nanocomplex

Zhang Jinlin,Wang Mingyue,He Doudou,Zhang Liang,Liu Tianqing,Wang Kaikai

Immune therapy that targets PD-L1 (programmed cell death-ligand 1) is attractive to augment immune response by breaking the programmed cell death-1 (PD-1)/PD-L1 axis. However, T cell exhaustion associated with insufficient T cells infiltration may diminish the efficacy of cancer therapy. Here, we report a novel delivery system of FEGCG/FPEI@siTOX composed of fluorinated EGCG (FEGCG) and fluorinated polyethyleneimine (FPEI) for delivery of small interfering RNA anti-TOX (thymus high mobility group box protein, TOX) to treat tumor and metastasis. In this way, the reduction in PD-L1 expression by FEGCG can promote T-cell function, while inhibition of TOX expression with siTOX can alleviate T-cell exhaustion. FPEI are designed to deliver siRNA with high efficiency and low toxicity compared to classical PEI. Integrating FEGCG, FPEI and siTOX into such a novel system resulted in excellent anti-tumor and antimetastatic effects. It is a promising delivery system and potential strategy for the treatment of “cold” tumors.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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CHEMICO-BIOLOGICAL INTERACTIONS · 2023 · IF 5.1

Hormetic effects of EGC and EGCG on CES1 activity and its rescue from oxidative stress in rat liver S9

Xiaoting Luo,Feifei Lu,Zhiyue Yin,Zhiyun Zhou,Zhongmin Wang,Hongjian Zhang

Carboxylesterase 1 (CES1) is a hydrolytic enzyme that plays an important role in the activation or deactivation of many therapeutic agents, thus affecting their pharmacokinetic and pharmacodynamic outcomes. Using rat liver S9 as an enzyme source and enalapril as a CES1 substrate, the present study examined effects of a number of flavonoids on the formation of enalaprilat (the active form of enalapril) produced by CES1-mediated hydrolysis. While a majority of flavonoids tested showed inhibition on CES1, an unexpected hormetic effect was observed for epigallocatechin (EGC) and epigallocatechin gallate (EGCG), i.e., stimulatory effect at low concentrations and enzyme inhibition at high concentrations. Further experiments revealed that oxidative stress caused by hydrogen peroxide, arachidonic acid plus iron, and oxidized low density lipoproteins (oxLOL) reduced CES1 activity in rat liver S9 and the loss of CES1 enzyme activity could be rescued largely by EGC or EGCG. In contrast, such effects were minimal in human liver S9, probably due to the presence of a higher ratio of reduced vs oxidized forms of glutathione . The above findings suggest that the polyphenolic nature of EGC or EGCG might be responsible for rescuing CES1 activity under oxidative stress. Because of the importance of CES1 in drug activation or deactivation and rat liver S9 as a versatile in vitro system used for drug metabolism studies and drug safety assessment , caution should be exercised to avoid potential biases for data interpretation and decision making when CES1 activity in rat liver S9 is evaluated with dependency on experimental conditions.

CAS / MDL: 506-32-1 7705-08-0
研究领域: 药理学 · 毒理学 · 生物化学 · 药物代谢 · 酶学
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INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES · 2023 ·Vol. 24 ·期 7 ·6013 · IF 5.6

Inhibitory Activities of Samples on Tyrosinases Were Affected by Enzyme Species and Sample Addition Methods

Wei Wang,Lijuan Yang,Weiwei Wang,Jianyong Zhang,Ulrich H. Engelhardt,Heyuan Jiang

The inhibition of tyrosinase (TYR) activity is an effective measure to inhibit melanin synthesis. At present, there are many methods with discrepant details that study the TYR inhibitory activity of samples. Under the same experimental conditions, this paper systematically studies whether enzyme species and sample addition methods are the key factors that determine the TYR inhibitory activity of samples. TYRs extracted from B16F10 cells, apple and mushroom, called BTYR, ATYR and MTYR, respectively, were selected to implement this study. Results showed that TYR inhibitory activities of samples were obviously affected by the above two factors. It was necessary to select the appropriate enzyme according to the problems to be explained. It was speculated that indirectly inhibitory activity reflected the comprehensive effects of samples on TYR catalytic activity and intracellular TYR synthesis pathway, while directly inhibitory activity reflected the effects of samples on TYR catalytic activity. Additionally, kojic acid could be used as a positive control for both B16F10 cells and MTYR models. The TYR inhibitory activity of β-arbutin was complicated and fickle, while that of epigallocatechin gallate (EGCG) was universal and stable, which is to say, EGCG always inhibited TYR activity in a dose-dependent manner. In conclusion, the TYR inhibitory activities of samples were affected by enzyme species and sample addition methods. Compared with the unstable β-arbutin, EGCG was more valuable for clinical research.Keywords:tyrosinase;species;sample addition methods;EGCG;kojic acid;β-arbutin

CAS / MDL: 497-76-7 9003-39-8
研究领域: 生物化学 · 药理学 · 皮肤病学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Acta Biomaterialia · 2023 · IF 9.7

Small-size Ti3C2Tx MXene nanosheets coated with metal-polyphenol nanodots for enhanced cancer photothermal therapy and anti-inflammation

Tao Liao,Zhongyin Chen,Ying Kuang,Zhe Ren,Wenqian Yu,Wen Rao,Linwei Li,Yun Liu,Ziqiang Xu,Bingbing Jiang,Cao Li

As a controllable, simple method with few side effects, near-infrared (NIR) light-based photothermal therapy (PTT) has been proven an effective cancer therapeutic approach. However, PTT-induced inflammation is a potential negative factor. And the overexpressed heat shock proteins (HSPs) by cancer cells can protect them from hyperthermia during PTT. In this work, small-size Ti 3 C 2 T x MXene nanosheets with high photothermal conversion efficiency in the region of NIR, high cargo loading capability and good free radical scavenging capability were chosen for cancer PTT and anti-inflammation. And (-)-epigallocatechin gallate (EGCG) was applied to form EGCG/Fe metal-polyphenol nanodots on the nanosheets. EGCG being released in acid cancer cells could reduce the expression of HSPs and could be used for anti-inflammation. As a result, the complex nanosheets named MXene@EGCG could achieve enhanced cancer PTT and be anti-inflammatory. Both in vitro and in vivo studies proved the good photothermal ability of MXene@EGCG and demonstrated that it could inhibit the expression of HSPs in tumor cells and relieve PTT-induced inflammation. Therefore, the nanosheets show good results in tumor ablation with a low level of inflammation, which provides another possibility for cancer therapy. Statement of significance Photothermal therapy (PTT)-induced inflammation plays an essential role in some important stages of tumor development and is unfavorable for cancer treatment. And hyperthermia leads to the overexpression of heat shock proteins (HSPs) in cancer cells, which limits the therapeutic effect of PTT. Therefore, we coated small-size Ti 3 C 2 T x MXene nanosheets with (-)-epigallocatechin gallate (EGCG)/Fe metal-polyphenol nanodots and named them as MXene@EGCG. This system shows a good photothermal conversion efficiency at 808 nm. And it can release EGCG in cancer cells to inhibit the expression of HSPs, thus achieving an enhanced cancer PTT. Both MXene and EGCG can also diminish the PTT-trigged inflammation. Both in vitro and in vivo studies prove the good anti-cancer PTT effect and anti-inflammation capability of MXene@EGCG.

CAS / MDL: 989-51-5
研究领域: 生物医学工程 · 纳米技术 · 癌症治疗 · 药学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Journal of Functional Foods · 2021 · IF 4.451

(-)-Epigallocatechin-3-gallate (EGCG) modulates polarized macrophages to suppress M1 phenotype and promote M2 polarization in vitro and in vivo

Yaozhong Hu,Jiaxin Gu,Jing Lin,Yi Wang,Feier Yang,Jia Yin,Zhenting Yu,Sihao Wu,Huan Lv,Xuemeng Ji,Shuo Wang

The intervention of EGCG on M1/M2 macrophage polarization was still unclear and should be studied comprehensively. In this context, the intervention of EGCG on macrophage polarization has been investigated to reveal that EGCG promoted M2 polarization of RAW264.7 upon treating with EGCG. A significant inhibitory effect of EGCG on M1 polarization was observed upon stimulating with LPS and IFN-γ. The expression of macrophage phenotype related marker genes (iNOS, COX-2, IL-1β for M1; Arg-1, Ym-1, IL-10 for M2) demonstrated the suppression of M1 polarization and the promotion of M2 polarization in liver, colon, spleen, and brain. Further analysis against peritoneal macrophages verified the increased M2 phenotypes and decreased M1 macrophages, and the similar variation in liver were confirmed by immunohistochemistry (IHC). No significant variation of spleen macrophages was observed with the general macrophages in declined tendency. Bio-distribution of EGCG and its metabolites (EGC, GA) in different organs has been further determined.

研究领域: 免疫学 · 药理学 · 细胞生物学
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