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INDUSTRIAL CROPS AND PRODUCTS · 2022 · IF 6.449

Integration of morphological, physiological, cytological, metabolome and transcriptome analyses reveal age inhibited accumulation of flavonoid biosynthesis in Ginkgo biloba leaves

Qingjie Wang,Yang Jiang,Xinyu Mao,Wanwen Yu,Jinkai Lu,Li Wang

Age affects the content of flavonoids in ginkgo ( Ginkgo biloba L.) leaves, such that only 1-to-5-year-old ginkgo leaves are suitable for the extraction of medicinal compounds. Nevertheless, the relationship between age and flavonoids in ginkgo leaves is unclear. In this study, we compared 1-to-7-year-old ginkgo trees, and found that the flavonoid content decreased with age. The total flavonol aglycones content of 1-year old ginkgo was 9.88 ± 0.27 mg/g, significantly higher than those of 4- and 7-year-old gingko, and there was a marked difference in quercetin content. Next, we extensively compared the transcriptome and metabolome in leaves of 1-, 4-, and 7-year-old ginkgo. Metabolome profiles showed that flavonoid metabolites were the most abundant in different metabolities, and 82 % of the flavonoids exhibited a decreasing trend with increasing age. Downregulation of key structural genes (chalcone synthase, CHS ; flavanone 3-hydroxylase, F3H ; flavonol synthase , FLS ) in the flavonoid biosynthesis pathway may explain the decreased flavonoid content with age. Furthermore, GO and KEGG analysis revealed photosynthesis- and hormone-related genes were downregulated with increasing age, implying that photosynthesis, salicylic acid, and jasmonic acid influence the flavonoid content. These results provide a theoretical basis for leaves ginkgo seedlings and new clues for understanding how age regulates flavonoids.

研究领域: 植物学 · 药理学 · 分子生物学 · 植物生理学
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JOURNAL OF FOOD SCIENCE · 2026 ·Vol. 91 ·期 8 ·e71394 · IF 4.1

Phenolic, Flavonoid, Short-Chain Fatty Acid, and Probiotic Biomass Changes During In Vitro Digestion and Fermentation of Litchi Seed Vinegar

Yizhuo Zhang,Jun Huang,Rongqing Zhou,Suyi Zhang,Yong Li,Rui Huang,Rui Liu,Chongde Wu

Litchi processing generates large quantities of seed by-products that are rich in starch and polyphenols but remain underutilized. In this study, the bioactivity and prebiotic potential of litchi seed vinegar (EHA-B-S1), a sustainable product derived from litchi seed by-products, were systematically evaluated. EHA-B-S1 displayed measurable in vitro antioxidant activity: total antioxidant capacity (4 mmol Trolox equivalents per mL), DPPH radical-scavenging of 50 µmol Vc equivalents per mL, and ABTS radical-scavenging activity of 1.0 mmol Vc equivalents per mL. EHA-B-S1 displayed moderate inhibitory capacity against α-amylase, α-glucosidase, and pancrelipase, and its performance was close to that of acarbose and orlistat. During probiotic-mediated fermentation, EHA-B-S1 rapidly acidified the fermentation environment, treatment resulted in higher measured biomass of Lactobacillus acidophilus , Lactobacillus rhamnosus , Lactiplantibacillus plantarum , and partially sustained Bifidobacterium longum compared with the control. The increase in metabolic activity showed higher short-chain fatty acid production, especially acetic acid, and expanded flavonoid diversity from 36 to 47 detected compounds; total flavonoid content increased to approximately 176% of the initial level. Network pharmacology analysis further predicted that these flavonoids may be associated with multiple metabolic and inflammatory pathways, providing hypotheses for future mechanistic studies. Collectively, the experimentally observed in vitro activities and fermentation-associated metabolite changes support further investigation of litchi seed vinegar as an upcycled bioactive fermented-food candidate, whereas its molecular targets, physiological effects, and health relevance require targeted cellular and in vivo validation.

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

H₂O₂-induced green synthesis of EGCG-flavonoid carrier-free nanoparticles:The role of hydroxyl group number governing formation and function

Qian Zhou,Ran Feng,Chen-Chen Wang,Si-Jie Wu,Qiu-Ya Ji,Ran Meng,Bao Zhang

Nanoparticles are successfully constructed by a green H₂O₂ oxidation strategy. • Formation entails EGCG oxidation, Mannich cross-linking and H-bonding/π-π stacking. • Nanoparticles show excellent antioxidant activity and enhanced stability. • The greater the number of hydroxyl groups, the stronger the interaction force. This study developed a green, carrier-free EGCG-flavonoid nanoparticle assembly strategy driven by H₂O₂. This approach overcomes the drawbacks of traditional formaldehyde-induced methods, including solvent toxicity and poor biocompatibility. It further investigated how the number of flavonoid hydroxyl groups regulates the assembly process and properties of EGCG-flavonoid nanoparticles. The formation involves H₂O₂-mediated oxidation of EGCG hydroxyl groups to generate aldehyde and carboxyl groups, which then undergo covalent bonding with the amino group of glycine. Flavonoids are embedded into the EGCG–glycine network through noncovalent interactions, resulting in spherical nanoparticles (200–260 nm, PDI ≈ 0.3). Increasing hydroxyl groups on flavonoids enhanced their loading capacity and interaction with EGCG. Nanoparticles with polyhydroxylated flavonoids exhibited strong antioxidant activity (>85% DPPH•/ABTS• + scavenging), high storage stability (>70% retention after 60 days), and improved thermal stability. This work provides a theoretical foundation for green synthesis of polyphenol-flavonoid nanosystems in functional foods and targeted delivery. Download: Download high-res image (114KB) Download: Download full-size image

✓ 已验证 DOI PubMed 高影响因子
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Nanoscale · 2026 · IF 5.2

AI-guided design of self-assembled flavonoid-cisplatin nanoparticles enhances triple-negative breast cancer therapy via three cell-death pathways

MarMar Tuohan,Geng Hu,Di Zhu,Bo Hu,Mengyue Ni,Liujia Chan,Yu Lu,Yuji Wang

Triple-negative breast cancer (TNBC) remains challenging to treat because of its aggressiveness and poor response to chemotherapy. Although cisplatin is clinically used for TNBC, its therapeutic window is narrow due to severe systemic toxicity and rapid development of drug resistance, underscoring the need for new strategies. To address this, we developed LMCDPS, a molecular language-model platform that learns the structural grammar of natural compounds, predicts their compatibility for co-assembly with cisplatin, and uniquely traces active small molecules back to their botanical origins. Using LMCDPS, we identified persimmon leaf-derived flavonoids as optimal cisplatin partners and confirmed their ability to spontaneously form stable, excipient-free nanoparticles (PLF-Cis NPs) via π–π interaction and hydrogen bonding. These nanoparticles eliminate synthetic carriers, reduce impurities in crude extracts, and substantially enhance tumor delivery, achieving an 11.3-fold increase in intracellular platinum accumulation. PLF-Cis NPs exert potent anti-TNBC activity by coordinating cisplatin-induced apoptosis, flavonoid-mediated ferroptosis, and immunogenic cell death, thereby promoting dendritic-cell maturation and robust CD8+ T-cell infiltration. In an orthotopic 4T1 model, they achieved a 71.5% reduction in tumor growth. This study establishes a language-model-driven framework for designing natural product-based, excipient-free nanomedicines, offering a scalable path to enhance chemotherapy while mitigating systemic toxicity.

✓ 已验证 DOI PubMed 高影响因子
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Journal of Herbal Medicine · 2024 · IF 2.2

Optimisation and Evaluation of the Correlation of Extraction Conditions for Total Flavonoid Content and Antixanthine Oxidase Activity in Psidium guajava

T.M. Le,C.D.P. Nguyen,A.C. Ha

ABSTRACT Introduction Psidium guajava L. ( P guajava ) and its leaf, one of the most popular plants in traditional medicine and cuisine, were demonstrated to have high flavonoid content with many bioactivities, including antigout activity. However, the correlation between total flavonoid content ( TFC ) and antigout activities and the optimal conditions for extracting P guajava have not been reported. Methods This study established the optimisation of ethanol extracts of P guajava leaves for TFC and antigout activities using the single-factor method and response surface methodology. The antigout activities were determined through the xanthine oxidase inhibition ( XOI ) method. Results The four independent variables (ethanol concentration, plant-solvent ratio, extraction time, and temperature) significantly impacted two response variables (TFC and XOI activity). The optimal extracts for XOI activity reach the maximum TFC of 323.86 ± 2.26 mg quercetin/g and XOI activity of 26.37 ± 0.5 μg/ml. The changes in the chemical structure of extracts were analysed by Fourier transform infrared, which indicated that several flavonoids in P guajava do not have XOI activity. The correlation of TFC and XOI is robust with the Pearson correlation of −0.882 and Spearman Rho test of −0.884. Additionally, the biological activities, such as antioxidant and anti-inflammatory, of optimal extracts for XOI and TFC were determined to extend the application capacity to support the treatment of gout diseases. Conclusions The optimised extraction conditions are critical to isolating flavonoids, which can serve as functional food or medicine for managing gout and its complications.

研究领域: 药用植物学 · 天然产物化学 · 生物活性研究
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JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY · 2025 · IF 6.2

Tricetin, a Dietary Flavonoid, Alleviates Neuroinflammation and Promotes Autophagy in Alzheimer’s Disease by Regulating the PI3K/Akt/mTOR Signaling Pathway

Xinyuan Wu,Dan Su,Jiaxin Xu,Ge Ge,Yongzhen Zhang,Bingjian Wu,Kun Hu,Jie Ren,Hao Yang

Alzheimer’s disease (AD), the most prevalent neurodegenerative disorder among older adults, significantly impairs behavioral and cognitive functions, posing a severe threat to patients’ health and quality of life. The Tricetin (TRN), a natural flavonoid found in wheat, pomegranate, and eucalyptus honey, has demonstrated anti-inflammatory, antitumor, and neuroprotective properties. However, its role in the context of AD has not been previously explored. This study investigated the antineuroinflammatory and autophagic protective effects of TRN in lipopolysaccharide (LPS)-induced BV2 cells and D-galactose/sodium nitrite/aluminum chloride (D-gal/NaNO2/AlCl3)-induced AD mice. The RNA sequencing examined the underlying mechanisms by which TRN ameliorates AD-related pathologies. Our research findings revealed that TRN significantly improved memory and mobility in AD mice, reduced Aβ deposition, and inhibited Tau protein phosphorylation. Furthermore, TRN regulated enzyme activities and reduced pathological markers associated with AD. Moreover, it modulated inflammatory mediators, inhibited the nuclear translocation of NF-κB in LPS-induced BV2 cells, and exerted anti-inflammatory and autophagic protective effects via the PI3K/Akt/mTOR signaling pathway. In conclusion, TRN demonstrated robust neuroprotective effects in vitro and in vivo AD models by regulating the PI3K/Akt/mTOR signaling pathway. These findings highlight its potential as a promising therapeutic agent for treating AD.

研究领域: 神经科学 · 药理学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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MOLECULES · 2018 ·Vol. 23 ·期 5 ·1110 · IF 3.098

Quantitative and Discriminative Evaluation of Contents of Phenolic and Flavonoid and Antioxidant Competence for Chinese Honeys from Different Botanical Origins

Shi Shen,Jingbo Wang,Qin Zhuo,Xi Chen,Tingting Liu,Shuang-Qing Zhang

Phenolics and flavonoids in honey are considered as the main phytonutrients which not only act as natural antioxidants, but can also be used as floral markers for honey identification. In this study, the chemical profiles of phenolics and flavonoids, antioxidant competences including total phenolic content, DPPH and ABTS assays and discrimination using chemometric analysis of various Chinese monofloral honeys from six botanical origins (acacia,Vitex, linden, rapeseed,AstragalusandCodonopsis) were examined. A reproducible and sensitive ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was optimized and validated for the simultaneous determination of 38 phenolics, flavonoids and abscisic acid in honey. Formononetin, ononin, calycosin and calycosin-7-O-β-d-glucoside were identified and quantified in honeys for the first time. Principal component analysis (PCA) showed obvious differences among the honey samples in three-dimensional space accounting for 72.63% of the total variance. Hierarchical cluster analysis (HCA) also revealed that the botanical origins of honey samples correlated with their phenolic and flavonoid contents. Partial least squares-discriminant analysis (PLS-DA) classification was performed to derive a model with high prediction ability. Orthogonal partial least squares-discriminant analysis (OPLS-DA) model was employed to identify markers specific to a particular honey type. The results indicated that Chinese honeys contained various and discriminative phenolics and flavonoids, as well as antioxidant competence from different botanical origins, which was an alternative approach to honey identification and nutritional evaluation.Keywords:UPLC-MS/MS;antioxidant competence;phenolic;flavonoid;chemometrics;monofloral honey

研究领域: 植物学 · 食品科学 · 分析化学
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS · 2024 · IF 3.1

Rapid determination of total flavonoid content, xanthine oxidase inhibitory activities, and antioxidant activity in Prunus mume by near-infrared spectroscopy

Jing-Wen Hao,Nai-Dong Chen,Xuan-Xuan Fan,Wei-Ting Wang,Huan-Huan Jiang,Zi-Yi Zhang,Rui-Ze Gong,Xiao-Li Ruan,Xue Chen

Evaluating the quality of herbal medicine based on the content and activity of its main components is highly beneficial. Developing an eco-friendly determination method has significant application potential. In this study, we propose a new method to simultaneously predict the total flavonoid content (TFC), xanthine oxidase inhibitory (XO) activity, and antioxidant activity (AA) of Prunus mume using near-infrared spectroscopy (NIR). Using the sodium nitrite-aluminum nitrate-sodium hydroxide colorimetric method , uric acid colorimetric method , and 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) free radical scavenging activity as reference methods, we analyzed TFC, XO, and AA in 90  P. mume samples collected from different locations in China. The solid samples were subjected to NIR. By employing spectral preprocessing and optimizing spectral bands , we established a rapid prediction model for TFC, XO, and AA using partial least squares regression (PLS). To improve the model's performance and eliminate irrelevant variables, competitive adaptive reweighted sampling (CARS) was used to calculate the pretreated full spectrum. Evaluation model indicators included the root mean square error of cross-validation (RMSECV) and determination coefficient ( R 2 ) values. The TFC, XO, and AA model, combining optimal spectral preprocessing and spectral bands, had RMSECV values of 0.139, 0.117, and 0.121, with R CV 2 values exceeding 0.92. The root mean square error of prediction (RMSEP) for the TFC, XO, and AA model on the prediction set was 0.301, 0.213, and 0.149, with determination coefficient ( R P 2 ) values of 0.915, 0.933, and 0.926. The results showed a strong correlation between NIR with TFC, XO, and AA in P. mume . Therefore, the established model was effective, suitable for the rapid quantification of TFC, XO, and AA. The prediction method is simple and rapid, and can be extended to the study of medicinal plant content and activity.

CAS / MDL: 64-18-6
研究领域: 药用植物学 · 分析化学
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SCIENTIA HORTICULTURAE · 2025 · IF 4.2

Integrated transcriptomics and metabolomics revealed the role of the flavonoid pathway in the resistance of Zanthoxylum bungeanum against leaf rust

Xia Yang,Yun Wang,Yan Sun,Jiali Guo,Zhaojun Geng,Bingyao Wei,Peiqin Li,Guanghui Tang

Leaf rust caused by Coleosporium zanthoxyli is a destructive disease that threatens Zanthoxylum bungeanum plantations. To address this, screening for resistant cultivars and exploring their resistance mechanisms are crucial for effective disease management. However, the mechanisms underlying Z. bungeanum 's resistance remain unclear. In this study, we conducted in vivo and in vitro experiments to screen for the resistant cultivar Qiujiao (QJ) and the susceptible cultivar Fengxian Dahongpao (FD). Subsequently, the resistance mechanisms of Z. bungeanum were analyzed by integrating transcriptome and metabolome, the result showed the flavonoid pathway served as the primary metabolic pathway for QJ to confer resistance against C. zanthoxyli . Upon infection with C. zanthoxyli , the key genes ( PAL, CHI , and HCT ) and enzymes (PAL, C4H, and 4CL) involved in the flavonoid pathway were upregulated in QJ, and the total flavonoid content was increased in QJ. Additionally, eight flavonoids from this pathway demonstrated inhibitory effects on C. zanthoxyli spore germination, with naringenin and phloretin exhibiting the stronger activity. Collectively, the flavonoid pathway plays a dominant role in the resistance of Z. bungeanum leaves against C. zanthoxyli .

研究领域: 植物病理学 · 分子生物学 · 转录组学 · 代谢组学
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JOURNAL OF PHYSICAL CHEMISTRY B · 2026 · IF 3.2

Turning on the Fluorescence of Flavonoid Anions: Synergistic Roles of Spatial Constraints and Microbasicity in Poly(vinyl alcohol)/DMSO Films

Zheng Li,Mengrong Hu,Siyu Hou,Shufang Gao,Ziyi Wang,Jian Luo

Deprotonated flavonoids typically undergo efficient nonradiative relaxation in solution, rendering them nonemissive. In this study, we successfully activate the fluorescence of such anions by embedding five representative flavonoids─galangin, apigenin, luteolin, kaempferol, and quercetin─into DMSO-doped poly(vinyl alcohol) (PVA/DMSO) films. The unique microenvironment of the composite film provides dual functionalities: intrinsic microbasicity facilitates flavonoid deprotonation, while spatial constraints effectively suppress the nonradiative decay pathways. Consequently, strong visible-light emission is observed for all flavonoids except galangin upon excitation at 440 nm. Time-dependent density functional theory calculations were employed to model the emission energies of various anionic species. By correlating the calculated trends with experimental spectra, we identify the emissive species as anions deprotonated specifically at the C4′–OH position, rationalizing the absence of emission from galangin, which lacks this moiety. This work not only demonstrates a general strategy to unlock the fluorescence of nonemissive anionic chromophores through synergistic matrix control but also establishes PVA/DMSO films as a versatile platform for modulating the photophysics of charged organic molecules.

✓ 已验证 产品关联 DOI PubMed 高影响因子
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MOLECULES · 2017 ·Vol. 22 ·期 7 ·1165 · IF 2.861

Role of the p-Coumaroyl Moiety in the Antioxidant and Cytoprotective Effects of Flavonoid Glycosides: Comparison of Astragalin and Tiliroside

Xican Li,Yage Tian,Tingting Wang,Qiaoqi Lin,Xiaoyi Feng,Qian Jiang,Yamei Liu,Dongfeng Chen

The aim of this study was to explore the role ofp-coumaroyl in the antioxidant and cytoprotective effects of flavonoid glycosides. The antioxidant effects of astragalin and tiliroside were compared using ferric ion reducing antioxidant power, DPPH• scavenging, ABTS•+scavenging, •O2–scavenging, and Fe2+-chelating assays. The results of these assays revealed that astragalin and tiliroside both exhibited dose-dependent activities; however, tiliroside exhibited lower IC50values than astragalin. In the Fe2+-chelating assay, tiliroside gave a larger shoulder-peak at 510 nm than astragalin, and was also found to be darker in color. Both of these compounds were subsequently evaluated in a Fenton-induced mesenchymal stem cell (MSC) damaged assay, where tiliroside performed more effectively as a cytoprotective agent than astragalin. Tiliroside bearing a 6′′-O-p-coumaroyl moiety exhibits higher antioxidant and cytoprotective effects than astragalin. The 6′′-O-p-coumaroyl moiety of tiliroside not only enhances the possibility of electron-transfer and hydrogen-atom-transfer-based multi-pathways, but also enhances the likelihood of Fe-chelating. Thep-coumaroylation of the 6"-OH position could therefore be regarded as a potential approach for improving the antioxidant and cytoprotective effects of flavonoid glycosides in MSC implantation therapy.Keywords:tiliroside;astragalin;p-coumaroyl;flavonoid glycoside;mesenchymal stem cells

研究领域: 药理学 · 生物化学 · 细胞生物学
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ECOTOXICOLOGY AND ENVIRONMENTAL SAFETY · 2023 · IF 6.8

Exogenous tannic acid relieves imidacloprid-induced oxidative stress in tea tree by activating antioxidant responses and the flavonoid biosynthetic pathway

Yue Wang,Guojun Pan,Tingjie Huang,Tao Zhang,Jin Lin,Lubin Song,Guangshuo Zhou,Xiaoping Ma,Yanqing Ge,Yongyu Xu,Chunhao Yuan,Nan Zou

Pesticide stress on plants is receiving increased scrutiny due to its effect on plant secondary metabolism and nutritional quality. Tannic acid (TA) is a natural polyphenolic compound showing excellent antioxidant properties and is involved in alleviating stress. The present study thoroughly investigated the effects and mechanism of exogenous TA on relieving imidacloprid (IMI) stress in tea plants. Our research found that TA(10 mg/L) activated the antioxidant defense system, enhanced the antioxidant ability, reduced the accumulation of ROS and membrane peroxidation, and notably promoted tea plant tolerance to imidacloprid stress. Additionally, TA boosted photosynthetic capacity, strengthened the accumulation of nutrients. regulated detoxification metabolism, and accelerated the digestion and metabolism of imidacloprid in tea plants. Furthermore, TA induced significant changes in 90 important metabolites in tea, targeting 17 metabolic pathways through extensively targeted metabolomics. Specifically, TA activated the flavonoid biosynthetic pathway, resulting in a 1.3- to 3.1-fold increase in the levels of 17 compounds and a 1.5- to 63.8-fold increase in the transcript level of related genes, such as ANR , LAR and CHS in this pathway. As a potential tea health activator, TA alleviates the oxidative damage caused by imidacloprid and improves the yield and quality of tea under pesticide stress.

CAS / MDL: 87-69-4 81167-16-0
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