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NEW JOURNAL OF CHEMISTRY · 2025 · IF 2.5

γ-Cyclodextrin metal-organic framework enhanced the bioavailability of vitexin in rats by increasing solubility and inhibiting re-crystallization

Qinghua Ni,Qiao Chen,Haixia Xu,Wenjun Wang,Zhongping Yin,Qing-Feng Zhang

γ-Cyclodextrin metal-organic frameworks (γ-CD-MOFs) were prepared by using γ-CD and KOH as the raw materials. The γ-CD-MOFs showed a cubic shape with particle size in the range of 400~700 nm and Langmuir surface area of 406.88 m2/g. The γ-CD-MOFs were used as the carrier of vitexin through adsorption in methanol, and the loading capacity was 34.9 mg/g. XRD showed that vitexin lost its crystal structure and FTIR showed vitexin had secondary interaction with the carrier. The structure of γ-CD-MOFs collapsed quickly in water, thereby rapidly releasing the loaded vitexin. Through the carrier, the water solubility of vitexin was increased from 31.79 μg/mL to 581.78 μg/mL in simulated gastric fluid at 37 oC, which was increased by about 18.3 times. Meanwhile, the presence of γ-CD inhibited the re-crystallization of vitexin and maintained its supersaturated status through formation of complexes. A pharmacokinetic study showed that the oral bioavailability of vitexin was enhanced by 1.99 times in rats through γ-CD-MOFs carrier.

CAS / MDL: 3681-93-4
研究领域: 药剂学 · 材料科学 · 药理学 · 纳米技术
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Food & Function · 2024 · IF 5.1

Protective effect of vitexin against high fat-induced vascular endothelial inflammation through inhibiting trimethylamine N-oxide-mediated RNA m6A modification

wenwen Li,Zeyuan Deng,Shuang Xiao,qian Du,Mengru Zhang,Hailing Song,Caidong Zhao,Liufeng Zheng

The high-fat diet (HFD) is a major risk factor for cardiovascular disease. However, the specific effects of HFD on vascular inflammation and the protective role of vitexin, a bioactive small-molecule compound derived from food, require further research. This study investigated the protective effects of vitexin intervention against HFD-induced vascular inflammation and its underlying mechanism. The results demonstrated that vitexin intervention significantly reduced body weight, serum total cholesterol, and low-density lipoprotein cholesterol levels in HFD-fed mice. Vitexin also improved vascular pathological changes and inflammatory status in the mice. Furthermore, vitexin intervention reduced serum TMAO levels in HFD-fed mice and achieved this effect by altering gut microbiota composition. HFD significantly increased N6-methyladenosine (m6A) levels in aorta tissues, while vitexin intervention reversed this abnormal m6A level. Vitexin could directly bind to fat mass and obesity-associated protein (FTO), potentially promoting m6A demethylation. The dose-response relationship between TMAO and inflammation/m6A was further validated in HUVEC cell and in vivo mouse experiments. Specifically, TMAO increased m6A levels and inflammation, while vitexin inhibited TMAO-mediated m6A modification, exhibiting anti-inflammatory effects. In conclusion, this study demonstrates the protective role of vitexin against HFD-induced vascular inflammation by inhibiting TMAO-mediated RNA m6A modification and laying the foundation for the development of functional foods.

CAS / MDL: 3681-93-4 1184-78-7
研究领域: 药理学 · 心脏病学 · 分子生物学 · 营养学
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Advances in Bamboo Science · 2025 · IF 3.7

Synthesis and characterization of magnetic molecularly imprinted polymers and application to the direct extraction of flavonoids from bamboo leaves

Danyang Liu,Hao Zhou,Changwei Zhang,Zhiwen Qi,Xianghui Kong,Chengzhang Wang

Molecularly imprinted polymers were employed for the purification and enrichment of flavonol glycosides and other flavonoid compounds to address the challenges of low content and structural similarity of polyphenolic flavonoids in plants, which render their separation very difficult. A magnetic molecularly imprinted polymer (MMIP) was synthesized via surface imprinting technology on Fe₃O₄@SiO₂ using vitexin as the template. Computational simulations identified methyl methacrylate (MMA) as the optimal functional monomer, with a template-to-monomer binding ratio of 1:6 and methanol as the most suitable porogen. Characterizations by TEM, XRD, VSM and FT-IR confirmed the successful synthesis of the MMIP under optimized conditions, which exhibited high adsorption capacity, rapid mass transfer and good regenerability. Binding experiments demonstrated that the MMIP had a maximum adsorption capacity of 16.1 mg/g. When directly applied to bamboo Leaves, the MMIP enabled the isolation of high-purity flavonoids, with HPLC successfully detecting six flavonoid compounds.

研究领域: 材料科学 · 高分子化学 · 分析化学 · 植物化学 · 纳米技术
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JOURNAL OF CELLULAR AND MOLECULAR MEDICINE · 2024 ·Vol. 28 ·期 7 ·e18157 · IF 4.3

Calycosin alleviates titanium particle-induced osteolysis by modulating macrophage polarization and subsequent osteogenic differentiation

Hui Jiang,Yang Wang,Zhao Tang,Xianjiang Peng,Chan Li,Yangjie Dang,Rui Ma

Periprosthetic osteolysis (PPO) caused by wear particles is one of the leading causes of implant failure after arthroplasty. Macrophage polarization imbalance and subsequent osteogenic inhibition play a crucial role in PPO. Calycosin (CA) is a compound with anti-inflammatory and osteoprotective properties. This study aimed to evaluate the effects of CA on titanium (Ti) particle-induced osteolysis, Ti particle-induced macrophage polarization and subsequent osteogenic deficits, and explore the associated signalling pathways in a Ti particle-stimulated calvarial osteolysis mouse model using micro-CT, ELISA, qRT-PCR, immunofluorescence and western blot techniques. The results showed that CA alleviated inflammation, osteogenic inhibition and osteolysis in the Ti particle-induced calvarial osteolysis mouse model in vivo. In vitro experiments showed that CA suppressed Ti-induced M1 macrophage polarization, promoted M2 macrophage polarization and ultimately enhanced osteogenic differentiation of MC3T3-E1 cells. In addition, CA alleviated osteogenic deficits by regulating macrophage polarization homeostasis via the NF-κB signalling pathway both in vivo and in vitro. All these findings suggest that CA may prove to be an effective therapeutic agent for wear particle-induced osteolysis.

CAS / MDL: 7440-70-2
研究领域: 骨科 · 药理学 · 免疫学 · 细胞生物学
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AAPS PHARMSCITECH · 2023 ·Vol. 24 ·期 4 ·1-18 · IF 3.3

Microfluidic Generation of Near-Infrared Photothermal Vitexin/ICG Liposome with Amplified Photodynamic Therapy

Cao Xia,Liu Qi,Adu-Frimpong Michael,Shi Wenwan,liu Kai,Deng Tianwen,Yuan Hui,Weng Xuedi,Gao Yihong,Yu Qingtong,Deng Wenwen,Yu Jiangnan,Wang Qilong,Xiao Gao,Xu Ximing

Glioma, in which a malignant tumor cell occurs in neural mesenchymal cells, has a rapid progression and poor prognosis, which is still far from desirable in clinical treatments. We developed a lab-on-a-chip (LOC) device for the rapid and efficient preparation of vitexin/indocyanine green (ICG) liposomes. Vitexin could be released from liposome to kill cancer cell, which can potentially improve the glioma therapeutic effect and reduce the treatment time through synergistic photodynamic/photothermal therapies (PDT/PTT). The vitexin/ICG liposome was fabricated via LOC and its physicochemical property and release in vitro were evaluated. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method and live/dead staining were used to examine the enhanced antitumor effect of vitexin/ICG liposome in cooperation with PDT/PTT, while the related mechanism was explored by flow cytometry and western blot. The results were as follows: (1) The prepared vitexin/ICG liposome was smaller in size, homogenous in particle size distribution with significant low polydispersity index (PDI), and enhanced cumulative release in vitro . (2) We found that the formulated liposome presented strong cancer cell inhibition and suppression of its migration in a dose-dependent manner. (3) Further mechanistic studies showed that liposome combined with near-infrared irradiation could significantly upregulate levels of B cell lymphoma 2-associated X (Bax) protein and decrease B cell lymphoma 2 (Bcl-2) at protein levels. The vitexin/ICG liposomes prepared based on a simple LOC platform can effectively enhance the solubility of insoluble drugs, and the combined effect of PTT/PDT can effectively increase their antitumor effect, which provides a simple and valid method for the clinical translation of liposomes. Graphical Abstract

研究领域: 肿瘤学 · 药学 · 生物医学工程 · 纳米技术
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JOURNAL OF SEPARATION SCIENCE · 2021 ·Vol. 45 ·期 2 ·638-649 · IF 3.645

Screening for potential quality markers of Callerya nitida var. hirsutissima. Z.Wei based on components profile, pharmacokinetics, and anti-inflammatory study

Jingbin Chen,Yonggui Song,Mingyue Zhou,Ming Yang,Ling Zhang,Abid Naeem,Zexie Li,Yaqiong Deng,Yali Liu,Zhifu Ai,Dan Su

Callerya nitida var. hirsutissima. Z.Wei is a classical, traditional Chinese herbal medicine mostly used to treat rheumatoid arthritis. Recent reports suggest that inconsistent and poor-quality control levels have primarily affected the therapeutic efficacy. Therefore, the aim of the current study was to investigate the active chemical ingredients, stability of components in blood, pharmacokinetics, and pharmacodynamics to specify the potential markers for quality control and quality evaluation of Callerya nitida . The active components in vitro and in vivo were obtained by ultra-high-performance liquid chromatography-mass spectrometry. Moreover, the changes of the bioactive components in the blood were monitored over time (0–24 h) in order to identify stable active components. On this basis, the pharmacokinetic characteristics of these ingredients combined with the anti-inflammatory activity were determined to screen out the potential markers for ensuring the quality control of Callerya nitida . The identified four components, such as calycosin, daidzein, formononetin, and 5-hydroxymethylfurfural, have the characteristics of intrinsic components, clearly defined structures, high exposure values, and in vivo stability, which are important for the therapeutic activity of pharmacologically active materials. Therefore, they can be used as potential markers to control the quality levels of Callerya nitida .

CAS / MDL: 64-18-6
研究领域: 药理学 · 中药学 · 分析化学 · 药代动力学 · 药效学
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INFLAMMATION · 2025 · IF 5

Vitexin Alleviates Kainic Acid-Induced Seizure Through Inhibiting P2X7R/NLRP3 Signaling Pathway

Chen Ru,Cheng Si-Min,Wang Hao-Chuan,Kun-Dong,Sun Hui-Li,Sun Meng-Mei,Gao Bo,Wu Wen-Ning

Epilepsy, a prevalent chronic brain disorder, remains inadequately controlled by current antiepileptic drugs. Neuroinflammation is considered a crucial component in the process of epileptogenesis. Vitexin (VT), primarily derived from medicinal plants, is a flavonoid monomer with significant biological activity that has demonstrated benefits in various neurological disorders by suppressing neuroinflammation. However, the role and underlying mechanism of VT in epileptic seizures are incompletely understood. We herein investigate VT’s antiseizure potential and the related mechanism utilizing a mouse model of status epilepticus induced by kainic acid (KA). Our findings indicate that VT pre-treatment exerts an antiseizure effect in a dose-dependent manner and attenuates KA-induced hippocampal neuronal damage in mice. Moreover, VT post-treatment (administration after the appearance of generalized seizures) can also alleviate KA-induced seizure and neuronal damage. Furthermore, VT suppresses the activity of hippocampal P2X7R and NLRP3 inflammasome in KA-treated mice. A438079, a specific P2X7R antagonist, inhibits NLRP3 inflammasome activation and reduces seizure severity and hippocampal neuronal damage. Conversely, the P2X7R activator BzATP negates the antiseizure and neuroprotective effects of VT. These findings demonstrate that VT can alleviate KA-induced seizure and neuronal damage by inhibiting P2X7R-NLRP3 inflammasome signaling in mice, potentially providing a novel strategy for prevention and treatment of acute seizures.

CAS / MDL: 3681-93-4
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FOOD CHEMISTRY · 2018 · IF 4.946

Plasma protein binding of dietary polyphenols to human serum albumin: A high performance affinity chromatography approach

Hui Cao,Xiaojuan Liu,Nataša Poklar Ulrih,Pradeep K. Sengupta,Jianbo Xiao

Herein, the protein binding rates of structurally different flavonoids to human serum albumin (HSA) were elucidated by applying the high performance affinity chromatography (HPAC). The flavonoids with hydroxyl groups on ring A showed a higher protein binding rate compared with those that there was no hydroxyl on ring A. However, the hydroxylation of ring B lowered the protein binding rate. It was also found that an additional methoxy group in flavone ring A would decrease the protein binding rate. Nevertheless, the methoxy group in flavanone ring A (position 6) and isoflavone ring B (position 4′) increased the protein binding rate. Methoxy group at other positions of flavonoids slightly enhanced or no significantly affected the binding rates on human serum albumin. Hydrogenation of C2 C3 double bond of flavonoids decreased the protein binding rate and had the same effect as glycosylation which decrease the protein binding rate by 5%–25%.

研究领域: 药理学 · 生物化学
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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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POSTHARVEST BIOLOGY AND TECHNOLOGY · 2024 · IF 6.4

Vitexin is a potential postharvest treatment for ameliorating litchi fruit pericarp browning by regulating autophagy

Qiuxiao Yang,Dingding Shi,Yanling Ren,Chao Yang,Hongxia Qu,Yueming Jiang,Taotao Li

Pericarp browning is a vital factor limiting postharvest life of litchi fruit. The influence of vitexin on pericarp browning as well as the related mechanisms in litchi fruit were investigated. Results demonstrated that 1 mM vitexin ameliorated pericarp browning when litchi fruit were stored at 25 °C. Meanwhile, vitexin blocked reactive oxygen species (ROS) production but increased the glutathione peroxidase activity, thereby playing a protective role in oxidative injury. Additionally, vitexin attenuated ATP content decline in relation to regulation of LcSnRK1 as well as LcbZIP1/3 expressions. Furthermore, vitexin regulated expression levels of autophagy-related genes. Finally, LcbZIP3 activated the expressions of LcATG2 and Lcbeclin-1-like protein based on dual-luciferase report (DLR) assay. This is the first report that confers vitexin-meditated protective role in delaying litchi pericarp browning that could be linked to its effects on autophagy particularly regulated via LcSnRK1a–LcbZIP1/3 signaling pathway. Vitexin treatment might be an effective approach to control postharvest senescence of fruit during storage.

CAS / MDL: 3681-93-4
研究领域: 植物科学 · 采后生理学 · 分子生物学
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JOURNAL OF ETHNOPHARMACOLOGY · 2024 · IF 4.8

Vitexin alleviates MNNG-induced chronic atrophic gastritis via inhibiting NLRP3 inflammasome

Jiaying Liu,Yuanfan Chen,Jing Zhang,Yun Zheng,Yun An,Chenglai Xia,Yonger Chen,Song Huang,Shaozhen Hou,Dong Deng

Ethnopharmacological relevance The dried fruit of Crataegus pinnatifida Bunge (Hawthorn in Chinese) is a traditional medicine used in China, Japan and Korea for thousands of years. Hawthorn is documented in the Chinese Pharmacopoeia , as a folk medicine that is used to eliminate food, strengthen the stomach, move qi and dissipate blood stasis, treat stagnation of meat and food, gastric distention and fullness, and has anti-inflammatory effects. Vitexin, a flavonoid glycoside, is an important biologically active compound derived from Hawthorn, with significant antioxidant and anti-inflammatory properties. The pharmacological effects of Hawthorn are highly correlated with the antioxidant and anti-inflammatory effects of vitexin. Aim of the study The aim of the present study was to investigate the effect of vitexin on the alleviation of chronic atrophic gastritis (CAG) induced by 1-methyl-3-nitro-1-nitrosoguanidine (MNNG) in a rat model, as well as to elucidate the underlying mechanisms involved. Materials and methods CAG was administered at a concentration of 170 μg/mL MNNG in the drinking water of rats, and the effects of vitexin (30 mg/kg, once daily for 6 weeks) on gastric tissues were subsequently analyzed. Pathological damage was assessed using H&E and AB-PAS staining. Gastrointestinal hormone levels, specifically motilin (MTL) and gastrin (GAS), were quantified using biochemical index determination kits. To evaluate the levels of cytokines, specifically IL-1β and IL-18, in gastric tissue, an enzyme-linked immunosorbent assay (ELISA) was performed. Additionally, to investigate the effects of vitexin on the NLRP3 inflammasome, GES-1 cells were subjected to treatment with lipopolysaccharide (LPS) and adenosine triphosphate (ATP). The targeting of NLRP3 by vitexin was assessed in vitro using CESTA, DARTS, and a synthesized biotin-labeled vitexin probe (biotin-vitexin) in conjunction with dual immunofluorescence. RT-PCR, Western blotting and immunofluorescence were used to evaluate the ameliorative effect of oysterin on LPS + ATP-induced GES-1 cells in vitro. Results Administration of vitexin significantly alleviated the symptoms of chronic atrophic gastritis (CAG) by reducing weight loss and minimizing gastric tissue damage. Treatment with vitexin in CAG rats effectively reduces the production of pro-inflammatory cytokines. Furthermore, vitexin attenuated the activation of the NLRP3 inflammasome in CAG induced by MNNG. Mechanistic experiments showed that NLRP3 is a direct cellular target of vitexin, while vitexin inhibited rat NLRP3 inflammasome. Conclusion Vitexin mitigates MNNG-induced CAG, and its protective effect is linked to the inhibition of NLRP3 inflammasome activation.

CAS / MDL: 3681-93-4
研究领域: 药理学 · 民族药理学 · 胃肠病学
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ADVANCED FUNCTIONAL MATERIALS · 2025 · IF 19

Ferritin-Nanocaged Aggregation-Induced Emission Drug Vitexin Inhibits Ferroptosis to Treat Asthenozoospermia

Xinghua Yu,Yujun Zhang,Lingan Zeng,Haiyan Chen,Xuemei Dong,Tianfu Zhang,Ben Zhong Tang,Fei Sun

Asthenozoospermia, a major cause of male infertility characterized by impaired sperm motility, is critically driven by oxidative stress and dysregulated iron metabolism, which directly induce ferroptosis in sperm cells. To address this, a novel nanotheranostic platform utilizing ferritin nanocages to encapsulate vitexin, a natural flavonoid with potent antioxidant properties and unique aggregation-induced emission (AIE) characteristics, is introduced. This ferritin nanocage-loaded vitexin (HFn@VI) system combines the iron-chelating capability of ferritin with vitexin's ability to mitigate oxidative stress, enabling precise dual-targeting of the ferroptotic pathways in spermatogenic cells. In the asthenozoospermia model mice, HFn@VI significantly improves sperm count and kinematic parameters (motility, velocity) without observable systemic toxicity, demonstrating superior therapeutic efficacy. Mechanistic studies reveal that the ferritin component elevates ferritin heavy chain 1(FTH1) levels, sequestering free iron ions and reducing cellular iron overload. Concurrently, vitexin activates the nuclear factor erythroid 2-related factor 2 (Nrf2)/heme oxygenase-1 (HO-1) pathway, enhancing glutathione peroxidase 4 (GPX4) expression to inhibit lipid peroxidation and ferroptosis. This study pioneers the application of vitexin, a natural product exhibiting AIE characteristics, as a therapeutic agent in reproductive medicine and underscores the potential of dual-target nanomedicines for precise ferroptosis intervention, establishing a new paradigm for treating male infertility through advances in material science.

研究领域: 纳米医学 · 生殖医学 · 泌尿科学 · 分子生物学 · 材料科学
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