FOOD HYDROCOLLOIDS
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2022
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IF 11.504
Fuqiang Liang,Yumeng Shi,Jiayi Shi,WeiWei Cao
Apigenin is a vital flavonoid that has attracted considerable attention in recent years due to its potent health benefits. Pumpkin seed protein (PSP) is a valuable by-product after pumpkin seed processing. However, the non-covalent interaction mechanism between apigenin and PSP remains to be explored. Here, the structural and conformational changes and molecular mechanisms underlying their interaction were investigated using multi-spectroscopic analysis integrated with molecular simulation approaches. The experimental results indicated that apigenin statically quenched the intrinsic fluorescence of PSP, indicating that the interaction between them did occur. Thermodynamic analysis and computational simulation results showed that the driving forces between apigenin and PSP were the hydrophobic interactions that predominated. The binding of apigenin resulted in changes in the conformation, microenvironment, and surface hydrophobicity of PSP. Furthermore, it was revealed by molecular docking and molecular dynamic (MD) simulations that apigenin maintained binding stability in the hydrophobic pockets of the protein through its interaction with several key residues. Additionally, it was found that the movement strength and directions of individual resides were altered after apigenin binding, which is the molecular basis of protein structural and conformational changes induced by apigenin. This study may provide theoretical evidence for the potential application of PSP and apigenin complex products in the food industry.
研究领域:
食品科学
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分子生物学
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生物物理学
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光谱学
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计算化学
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高影响因子
JOURNAL OF LIPOSOME RESEARCH
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2025
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IF 4.3
Amna Naz,Sadia Haider,Malik Ihsan Ullah Khan,Rabia Khokhar,Mavra Rubab,Muhammad Farooq,Attia Afzal,Muhammad Sarfraz
This study addresses the limitations of traditional cancer therapies—such as high toxicity and non-selectivity—by developing a novel nanoparticulate system co-loaded with plant-derived compounds, apigenin (APG) and oleanolic acid (OA). These naturally occurring phytochemicals are known for their anticancer properties but face clinical challenges due to poor solubility and limited efficacy. The Apigenin and Oleanolic Acid Nanoparticulate System (AONS) was refined and optimized using the Box-Behnken statistical design approach, resulting in nanoparticles with a mean diameter of 169 nm and size homogeneity. A validated HPLC technique was employed to simultaneously quantify both apigenin and oleanolic acid in the developed formulation as well as in various biological matrices. In vitro drug release was enhanced at acidic pH (5.5), mimicking the tumor microenvironment. AONS showed strong physicochemical stability under refrigerated storage. Cytotoxicity tests on HepG2, MDA-MB-231, and U87 glioma cells demonstrated significantly improved anticancer activity compared to control, free drugs, or individual nanoformulations. Cellular uptake studies confirmed efficient internalization in U87 cells, and ELISA results indicated apoptosis via activation of the p53 pathway. Biodistribution analysis revealed prolonged systemic drug retention with AONS (up to 72 hours), surpassing the short circulation time of free drugs. Notably, LC-MS data confirmed that the nanoparticle system could cross the blood-brain barrier, highlighting its therapeutic potential for treating brain cancers.
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高影响因子
EUROPEAN POLYMER JOURNAL
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2022
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IF 5.546
Qiao Zhang,Wei Shi,Wenmei Tan,Zhengfeng Xie
The construction of polymer/phosphazene organic-inorganic hybrids using biomass can improve the sustainability of their preparation. In addition, introducing diverse functional units to these hybrids is a potential way to broaden their downstream applications. Herein, a benzoxazine derivative (AP-f), prepared from biomasses (apigenin and furfurylamine), is used as starting materials to construct a polymer/phosphazene hybrid. Through efficient benzoxazine-isocyanide-mechanochemistry (BIC-MC), a bio-polyamide derivative (PA-af) containing diverse molecular fragments (amide, phenolic hydroxyl, and tertiary amine) is prepared by solid-state ball-milling. Using PA-af as a phenolic source, a novel polyamide (PA)/phosphazene organic-inorganic hybrid (PACP-af) is successfully constructed by condensation with hexachlorocyclotriphosphazene (HCCP). PACP-af shows selective adsorption for cationic dye methylene blue (MB). Experimental results show that the maximum adsorption capacity of MB by PACP-af reaches 598.4 mg/g, and the adsorption process followed the pseudo-second-order kinetic and Langmuir adsorption model. PACP-af is also used as an enrichment-type Pb (II) electrochemical probe with an acceptable detection range (1–100 μM) and detection limit (0.085 μM).
研究领域:
材料科学
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环境科学
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电化学
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DOI
高影响因子
Frontiers in Molecular Biosciences
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2026
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IF 4.4
Guozhen Ni,Ning Ma,Jian Xu
IntroductionApigenin (API) has been utilized in the treatment of atherosclerosis. Senescent macrophages exhibit a senescence-associated secretory phenotype (SASP), which plays a critical role in the progression of atherosclerosis. IL1A expression is thought to be involved in the transition of macrophages to the SASP phenotype. This study explored the effect of API on the atherosclerosis-related SASP in macrophages and the underlying mechanism.MethodsMacrophages were treated with different concentrations of API. The expression of DOT1-like histone lysine methyltransferase (DOT1L) was manipulated in macrophages. Stimulation with lipopolysaccharide (LPS) was conducted to induce the SASP. Macrophage senescence was detected by senescence-associated-β-galactosidase staining. The expressions of interleukin 1 α (IL1A), DOT1L, and markers related to senescence, the SASP, and inflammation in macrophages were assessed. Chromatin immunoprecipitation was performed to check DOT1L-mediated H3K79me2 enrichment at the promoter of IL1A.ResultsAPI treatment effectively reduced cellular senescence in LPS-exposed macrophages. Furthermore, it downregulated markers associated with senescence, SASP, and inflammation, while upregulating the anti-inflammatory cytokine IL-10. Moreover, LPS-induced DOT1L and H3K79me2 enrichment at the IL1A promoter, as well as DOT1L and IL1A upregulation in macrophages, were hindered by API. DOT1L overexpression counteracted API’s effects, including its ability to inhibit senescence, downregulate senescence/SASP/inflammation markers, upregulate IL-10, and prevent H3K79me2 and DOT1L binding at the IL1A promoter. DOT1L silencing reduced LPS-induced senescence, SASPs, and H3K79me2 enrichment in macrophages.ConclusionAPI inhibits DOT1L-mediated H3K79me2 enrichment to downregulate IL1A, thus reducing the SASP of macrophages.
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高影响因子
PHYTOMEDICINE
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2026
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IF 11.3
Fen Xiong,Yingruo Xu,Xinran Wang,Yiwen Peng,Tian Tang,Kaiyuan Jiang,Ruguang Wang,Yutong Wu,Huarui Wang,Chen Li,Hongchang Gao
Apigenin alleviates methionine-choline deficient (MCD) diet-induced metabolic-associated fatty liver disease (MAFLD), with improved liver function and reduced oxidative stress. • Lipidomic evidence of apigenin-driven hepatic remodeling: decreased SFAs/PUFAs and increased MUFAs. • Lactobacillus and Akkermansia reshaping as mediators of apigenin’s protective effects in MAFLD. • Homocysteine identified as a microbiota-associated metabolite driving oxidative stress and lipid dysregulation. • Translational potential of apigenin as a phytochemical therapy targeting the gut–liver axis in MAFLD. Introduction Apigenin, a naturally occurring flavone widely present in the plant kingdom, possesses antioxidant, anti-inflammatory, and metabolic regulatory activities. Metabolic-associated fatty liver disease (MAFLD), a chronic liver disorder driven by metabolic stress, currently lacks effective pharmacological therapies. Given these pharmacological properties, apigenin may represent a promising candidate for MAFLD intervention. Objective This study aimed to evaluate the therapeutic potential of apigenin in MAFLD and to elucidate the underlying mechanisms linking the gut microbiota and host lipid metabolism. Methods A methionine-choline deficient (MCD) diet-induced mouse model of MAFLD, combined with lipidomic profiling, microbiota analysis, and metabolite assessment, was used to determine the beneficial effects of apigenin. Results Apigenin markedly ameliorated hepatic steatosis in MCD-fed mice, as demonstrated by reduced hepatic triglyceride accumulation, improved liver function markers, and alleviated hepatic inflammation and oxidative stress. Lipidomic profiling showed decreased hepatic saturated and polyunsaturated fatty acids accompanied by an increase in monounsaturated fatty acids and their related lipid species. Apigenin remodeled the gut microbiota, characterized by increased Lactobacillus abundance and decreased Akkermansia abundance. Further analyses identified homocysteine (HCY) as a key microbiota-associated metabolite that induced oxidative stress and reproduced the lipid dysregulation observed in MAFLD, thereby linking microbial alterations to hepatic lipid metabolism. Conclusion These findings demonstrate that apigenin alleviates MAFLD by remodeling the gut microbiota-metabolite network, lowering HCY levels, and subsequently improving hepatic function, lipid metabolism, and oxidative stress, highlighting its potential as a phytochemical-based therapeutic strategy. Download: Download high-res image (198KB) Download: Download full-size image
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高影响因子
FOOD HYDROCOLLOIDS
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2024
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IF 11
Yingrui Wang,Tianqi Zhou,Lin Li,Yuqiao Wang,Jianan Yan,Ce Wang,Bin Lai,Haitao Wu
The novel food composite hydrogel with delivery function consisting of shrimp powder (SP) and κ-carrageenan (κ-C) was constructed and used for loading apigenin (API). Binary mixtures of liquid SP and κ-C could form gels with solid behavior. Furthermore, the addition of API increased the initial modulus of elasticity of SP/κ-C by approximately 47.3%, as well as a 14.9% reduction in the relaxation time T 23 . Moreover, the O-H stretching band and the amide I band of SP/κ-C binary gel loaded with API were blue shifted, and the XRD characteristic peak of API disappeared in SP/κ-C/API. In addition, broken macropores and dispersed patch microstructures were presented in SP and κ-C, whereas the SP/κ-C and SP/κ-C/API hydrogels were homogeneously distributed with dense mesh and solid mesh walls. Hydrophobic interactions were the main forces in the SP/κ-C/API composite hydrogels, which were improved 1.3-fold. Furthermore, SP/κ-C/API was extended and released to more than 55% extent during simulated intestinal colonic digestion. These results suggested that a stable and dense binary gel was formed by SP and κ-C, which could seal and extended release effect of API to the colon.
研究领域:
食品科学
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生物材料学
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DOI
高影响因子
PHYTOMEDICINE
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2021
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IF 5.34
Yongmei Li,Zean Zhao,Jian Luo,Yanqing Jiang,Lu Li,Yanyu Chen,Leqi Zhang,Qinghua Huang,Ying Cao,Pingzheng Zhou,Ting Wu,Jianxin Pang
Background Hyperuricemia (HUA) is characterized by abnormal serum uric acid (UA) levels and demonstrated to be involved in renal injury leading to hyperuricemic nephropathy (HN). Apigenin (API), a flavonoid naturally present in tea, berries, fruits, and vegetables, exhibits various biological functions, such as antioxidant and anti-inflammatory activity. Purpose To investigate the effect of API treatment in HN and to reveal its underlying mechanisms. Methods The mice with HN were induced by potassium oxonate intraperitoneally and orally administered for two weeks. The effects of API on renal function, inflammation, fibrosis, and uric acid (UA) metabolism in mice with HN were evaluated. The effects of API on urate transporters were further examined in vitro . Results The mice with HN exhibited abnormal renal urate excretion and renal dysfunction accompanied by increased renal inflammation and fibrosis. In contrast, API reduced the levels of serum UA, serum creatinine (CRE), blood urea nitrogen (BUN) and renal inflammatory factors in mice with HN. Besides, API ameliorated the renal fibrosis via Wnt/β-catenin pathway suppression. Furthermore, API potently promoted urinary UA excretion and inhibited renal urate transporter 1 (URAT1) and glucose transporter 9 (GLUT9) in mice with HN. In vitro , API competitively inhibited URAT1 and GLUT9 in a dose-dependent manner, with IC 50 values of 0.64 ± 0.14 μM and 2.63 ± 0.69 μM, respectively. Conclusions API could effectively attenuate HN through co-inhibiting UA reabsorption and Wnt/β-catenin pathway, and thus it might be a potential therapy to HN.
研究领域:
药理学
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肾病学
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分子生物学
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PubMed
高影响因子
INFLAMMATION
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2020
·Vol. 43
·期 5
·1634-1648
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IF 3.212
Yue Shuwen,Xue Ning,Li Honglei,Huang Baosheng,Chen Zhen,Wang Xing
Apigenin, a flavonoid found in many plants, has various biological properties. We aimed to investigate the anti-inflammatory and anti-oxidative activity of apigenin against carbon tetrachloride (CCl 4 )-induced acute liver injury in mice and hydrogen peroxide (H 2 O 2 )-induced oxidative stress in HepG2 cells and possible mechanism. In vivo , apigenin significantly reduced alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activity in serum of mice challenged by CCl 4 and markedly alleviated the lipid peroxidation as indicated by the increased level of superoxide dismutase (SOD), reduced glutathione (GSH), glutathione peroxidases (GSH-Px) and catalase (CAT), and the decreased malondialdehyde (MDA) in liver tissue. Apigenin also ameliorated inflammation by downregulating tumor necrosis factor-alpha (TNF-α), interleukin-6 (IL-6), and upregulating IL-10. Consistently, the elevated ALT and AST level; the impaired balance between SOD, GSH activity, and excessive ROS; and the increased gene expression of TNF-α and IL-6 resulting from H 2 O 2 -induced oxidative stress were restored by apigenin. Moreover, the results from Western blot, real-time qPCR, and immunofluorescence assay indicated that apigenin enhanced the activity of TNF receptor-associated factor (TRAF) 2/3 and cellular inhibitor of apoptosis protein (c-IAP) 1, ameliorated NF-κB-inducing kinase (NIK), and mediated the nuclear translocation of NF-κB2, therefore had an inhibitory effect on the non-canonical NF-κB pathway which was activated in both models. siNIK canceled the protective effect of apigenin on H 2 O 2 -induced HepG2 cells. Altogether, our results demonstrated that apigenin mitigated liver injury by ameliorating inflammation and oxidative stress through suppression of the non-canonical NF-κB pathway, indicating the potential of apigenin for treatment of the liver injury.
研究领域:
药理学
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分子生物学
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毒理学
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免疫学
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PubMed
高影响因子
FOOD AND CHEMICAL TOXICOLOGY
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2022
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IF 5.572
Dongxu Han,Yujie Yao,Lu Chen,Zhiying Miao,Shiwen Xu
Di(2-ethylhexyl) phthalate (DEHP) is a widely artificial persistent organic pollutant, the contamination of which infiltrates daily human life from many aspects, imperceptibly causing damage to multiple organs in the body, including the liver. Apigenin (APG) is widely distributed in vegetables and fruits and can relieve or prevent the injuries caused by exogenous chemicals through various pharmacological effects, such as antioxidant effects. To investigate the mechanism of DEHP-induced liver injury and the antagonistic effects of APG, we treated AML12 cells with 1 mM DEHP and/or APG. Ultrastructural morphology analysis indicated that DEHP induced typical ferroptosis-like damage. In addition, we found that DEHP exposure induced ferroptosis by enhancing reactive oxygen species (ROS) levels, disrupting iron homeostasis and lipid peroxidation, and regulating the expression of ferroptosis-related genes. Notably, supplementation with APG significantly inhibited these abnormal changes, and molecular docking further showed evidence of the activating effects of APG ligand on glutathione peroxidase 4 (GPX4). These results demonstrated that the protective effects of APG on DEHP-induced ferroptosis were achieved by activating GPX4 and suppressing intracellular iron accumulation. This information not only adds to DEHP toxicological data but also provides a basis for the practical application of APG.
研究领域:
毒理学
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药理学
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细胞生物学
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环境健康
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PubMed
高影响因子
Food Packaging and Shelf Life
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2023
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IF 8
Lihan Wang,Shasha Cheng,Kaiwen Qin,Xinyan Yang,Hao Wang,Chaoxin Man,Qianyu Zhao,Yujun Jiang
Packaging films containing antibacterial substances play a crucial role in controlling contamination caused by food-borne pathogens. Herein, apigenin (APG) was encapsulated in zeolitic imidazolate frameworks 8 (ZIF-8) to achieve a synergistic antibacterial effect and prolonged drug release, aiming to extend the shelf life of food products. Under acidic condition, the release rate of APG reached 73.70 % after 12 h. Subsequently, propolis-gelatin (PG) films were prepared for food packaging. The addition of APG@ZIF-8 enhanced the hydrophobicity of PG films, making them more suitable for food packaging. However, the composite film exhibited reduced damage resistance and flexibility. The composite films demonstrated 100 % inhibition against Staphylococcus aureus and Escherichia coli under appropriate amount of APG@ZIF-8. The composite film coating significantly reduced the bacteria count on apple surfaces by 99.95% during storage, while maintaining their appearance. This study provides an effective way to develop novel antibacterial composite films.
研究领域:
食品科学
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材料科学
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微生物学
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高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2024
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IF 7.7
Fuqiang Liang,Keyu Meng,Xinran Pu,Yubo Cao,Yumeng Shi,Jiayi Shi
This study investigated the molecular mechanism underlying the binding interaction between apigenin (API) and α-glucosidase (α-glu) by a combination of experimental techniques and computational simulation strategies. The spontaneously formation of stable API-α-glu complex was mainly driven by hydrogen bonds and hydrophobic forces, leading to a static fluorescence quenching of α-glu. The binding of API induced secondary structure and conformation changes of α-glu, decreasing the surface hydrophobicity of protein. Computational simulation results demonstrated that API could bind into the active cavity of α-glu via its interaction with active residues at the binding site. The important roles of key residues responsible for the binding stability and affinity between API and α-glu were further revealed by MM/PBSA results. In addition, it can be found that the entrance of active site tended to close after API binding as a result of its interaction with gate keeping residues. Furthermore, the structural basis for the binding interaction behavior of API was revealed and visualized by weak interaction analysis. The findings of our study revealed atomic-level mechanism of the interaction between API, which might shed light on the development of better inhibitors.
研究领域:
药理学
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生物化学
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分子生物学
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计算化学
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PubMed
高影响因子
Foods
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2023
·Vol. 12
·期 11
·2120
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IF 5.2
Jie Li,Bingyong Mao,Xin Tang,Qiuxiang Zhang,Jianxin Zhao,Hao Zhang,Shumao Cui
Naringenin and apigenin are common flavonoids derived from edible plants with the potential to alleviate inflammation and improve skin antioxidation. This study aimed to evaluate the effects of naringenin and apigenin on oleic acid-induced skin damage in mice and compare their underlying mechanisms of action. Triglycerides and non-esterified fatty acids were significantly decreased by naringenin and apigenin, while apigenin intervention resulted in a better recovery of skin lesions. Naringenin and apigenin improved the antioxidative abilities of the skin by increasing catalase and total antioxidant capacity levels and decreasing malondialdehyde and lipid peroxide levels. The release of skin proinflammatory cytokines, such as interleukin (IL)-6, IL-1β, and tumor necrosis factor α, was inhibited after naringenin and apigenin pretreatments, but naringenin only promoted the excretion of IL-10. Additionally, naringenin and apigenin regulated antioxidant defense and inflammatory response by activating nuclear factor erythroid-2 related factor 2-dependent mechanisms and suppressing the expression of nuclear factor-kappa B. In summary, naringenin and apigenin are prospective ingredients that contribute to the amelioration of skin damage by activating anti-inflammatory and antioxidative responses.Keywords:naringenin;apigenin;antioxidative system;inflammation;signaling pathway
研究领域:
药理学
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皮肤病学
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分子生物学
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PubMed
高影响因子
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