Biomedical Materials
·
2023
·Vol. 18
·期 4
·045005
·
IF 4
Jian Zhang,Xiaoxiao Li,Xiaoli Xia,Michael Adu-Frimpong,Xinyi Shen,Qing He,Wanjing Rong,Feng Shi,Xia Cao,Hao Ji,Elmurat Toreniyazov,Qilong Wang,Jiangnan Yu,Ximing Xu
In this regard, we developed vitexin (Vi)-loaded D-ɑ-tocopherol polyethylene glycol succinate, polyvinylpyrrolidone K30 and sodium cholate mixed micelles (Vi-MMs) mainly for improving oral bioavailability and enhancing anti-osteoporotic effect of Vi. Thin layer dispersion method was employed to prepare Vi-MMs, and then the optimal prescription was optimized by the orthogonal design-response surface method, wherein encapsulation efficiency (EE) was used as optimizing index. The physical properties of Vi-MMs such as appearance morphology, particle size, and zeta potential were also characterized. We further analyzed the in-vitro release of Vi and Vi-MMs in three media and investigated the pharmacokinetics of Vi and Vi-MMs in rats. Anti-osteoporotic activity of Vi and Vi-MMs was assessed by establishing a zebrafish osteoporosis model with prednisone. Drug loading, EE, particle size and zeta potential of the optimized Vi-MMs were 8.58 ± 0.13%, 93.86 ± 1.79%, 20.41 ± 0.64 nm and −10 ± 0.56 mV, respectively. The optimized Vi-MMs were shaped spherically as exhibited by transmission electron microscopic technique, with evident core shell nano-structure, well dispersed. In all three media, the release rate of Vi-MMs was significantly higher than that of free Vi. The oral bioavailability of Vi-MMs was increased by 5.6-fold compared to free Vi. In addition, alleviation of prednisone induced osteoporosis in zebrafish by Vi-MMs further demonstrated good anti-osteoporotic effect. In summary, Vi-MMs exhibited enhanced bioavailability and anti-osteoporotic effect, which is expected to be potential nanocarrier for Vi applications in drug development.
研究领域:
药学
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纳米技术
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药理学
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PubMed
高影响因子
JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY
·
2026
·Vol. 40
·期 7
·e70979
·
IF 3.6
Meng Wang,Guangwei Jiang,Xiangjun Meng,Lina Wang
Diabetic retinopathy (DR) stands as a common microvascular issue associated with diabetes mellitus, a condition defined by progressive structural decline in the retina. Although studies have reported that vitexin exhibits positive pharmacological activity in inflammatory eye diseases and has been shown to protect against neuronal damage, its efficacy in treating DR and its underlying mechanism of action remain unreported. Cellular viability was determined via the Cell Counting Kit-8 (CCK-8) approach. Oxidative stress, apoptosis, and inflammatory response in cells were assessed via flow cytometry, the thiobarbituric acid (TBA) assay, commercial kits, and western blot analysis. Combined with bioinformatics analysis (online Swiss Target Prediction, Comparative Toxicogenomics Database (CTD), online Gene Cards, and molecular docking), it was confirmed that vitexin's cytoprotection in ARPE-19 cells against damage is mediated by caspase-3 (CASP3). In HG-challenged ARPE-19 cells, vitexin successfully mitigated oxidative stress. This was evidenced by downregulated levels of malondialdehyde (MDA) and reactive oxygen species (ROS), coupled with enhanced enzymatic performance of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px). It also attenuated the inflammatory response by suppressing tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) while promoting interleukin-10 (IL-10), ultimately leading to reduced apoptosis. Differential gene screening and molecular docking analysis revealed an interaction between CASP3 and vitexin. Moreover, in HG challenged ARPE-19 cells, overexpressing CASP3 significantly compromised the protective benefits conferred by vitexin. Vitexin alleviates damage to ARPE-19 cells induced by HG via CASP3, exerting a protective effect in early DR.
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高影响因子
AAPS PHARMSCITECH
·
2023
·Vol. 24
·期 4
·1-18
·
IF 3.3
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
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药学
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生物医学工程
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纳米技术
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DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2021
·
IF 5.279
Mengting Ni,Xin Song,Junhui Pan,Deming Gong,Guowen Zhang
In this study, the antiglycation potential and mechanisms of vitexin were explored in vitro by multispectroscopy, microscope imaging, high-resolution mass spectrometry, and computational simulations. Vitexin was found to show much stronger antiglycation effects than aminoguanidine. The inhibition against the fluorescent advanced glycation end products was more than 80% at 500 μM vitexin in both bovine serum albumin (BSA)–fructose and BSA–methylglyoxal (MGO) models. Treated with 100 and 200 μM vitexin for 24 h, the contents of MGO were reduced to 4.97 and 0.2%, respectively, and only one vitexin–mono-MGO adduct was formed. LC–Orbitrap-MS/MS analysis showed that vitexin altered the glycated sites and reduced the glycation degree of some sites. The mechanisms of vitexin against protein glycation were mainly through BSA structural protection, MGO trapping, and alteration of glycation sites induced by interaction with BSA. These findings provided valuable information about the functional development of vitexin as a potential antiglycation agent.
研究领域:
生物化学
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药理学
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分子生物学
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PubMed
高影响因子
POSTHARVEST BIOLOGY AND TECHNOLOGY
·
2024
·
IF 6.4
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.
研究领域:
植物科学
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采后生理学
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分子生物学
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高影响因子
ULTRASONICS SONOCHEMISTRY
·
2017
·
IF 4.218
Fengli Chen,Qiang Zhang,Junling Liu,Huiyan Gu,Lei Yang
Ultrasonic circulating extraction (UCE) approach was developed for effective extraction of orientin and vitexin from the flowers of Trollius chinensis successfully. In this study, some parameters potentially influencing the yields of orientin and vitexin were systematically investigated and optimized by Plackett–Burman and Box-Behnken design, and the optimum operational conditions obtained were 60% ethanol volume fraction, 1000 r/min stirring speed, 30 °C temperature, 28 min ultrasonic irradiation time, 10 mL/g liquid-solid ratio and 738 W ultrasonic irradiation power. Satisfactory yields of orientin (6.05 ± 0.19 mg/g) and vitexin (0.96 ± 0.03 mg/g) were obtained in a relatively shorter extraction time under the derived optimum conditions, compared to other ultrasonic extraction methods and heat extraction methods. The mechanism of UCE procedure was discussed in detail, to illustrate the advantage of UCE in the extraction process. In addition, no degradation of orientin and vitexin and high reproducibility of the developed UCE method were observed under the optimum conditions. The proposed UCE technique with high-capacity and circulation function is a rapid and efficient sample extraction technique, and performs promising in large-scale sample preparation.
研究领域:
药学
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分析化学
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植物科学
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DOI
PubMed
高影响因子
Scientific Reports
·
2026
·
IF 4.9
Liu Jiaying,Liu Nan,Ye Yiting,Ye Zhandong,Jiang Dongxu,Huang Song
Precancerous gastric lesions (PLGC) represent a critical transitional stage toward gastric cancer, yet effective interventions to halt progression remain limited. Vitexin, a naturally occurring flavonoid, exhibits anti-cancer potential; however, its molecular targets and mechanisms in PLGC have not been fully defined. This study aimed to elucidate the targets and mechanisms of vitexin against PLGC using an integrative strategy combining network pharmacology, molecular docking/molecular dynamics (MD), and cellular validation. Putative targets of vitexin and PLGC-associated genes were intersected to obtain 33 common targets, followed by protein–protein interaction network construction and pathway enrichment analyses. Molecular docking was performed against core targets, and MD simulations were conducted to assess the stability of the EGFR–vitexin complex. In vitro validation was carried out in MNNG-induced MC cells using cell viability, migration, and invasion assays, phase-contrast imaging, and immunofluorescence staining of EGFR and E-cadherin. Network analysis highlighted CCND1, EGFR, and ABL1 as central nodes and implicated oncogenic programs including cell-cycle regulation and PI3K–Akt signaling pathway. Docking suggested favorable binding of vitexin to the core targets. MD simulations further supported a stable binding mode of vitexin within the EGFR pocket over 100 ns with preserved global compactness; a late-stage conformational adaptation accompanied by hydrogen-bond network reorganization was observed without signs of global unfolding. Functionally, vitexin reduced MC cell viability in a dose-dependent manner, reaching ~ 50% inhibition at 20 μM, and significantly suppressed cell migration and invasion. Immunofluorescence demonstrated decreased EGFR expression and altered membrane localization, together with restored E-cadherin expression and membrane localization, suggesting a shift toward an epithelial phenotype. Vitexin inhibits PLGC-associated malignant phenotypes through multi-target modulation. Among the identified candidates, EGFR may serve as a putative and functionally relevant target, while modulation of EGFR-associated signaling together with restoration of E-cadherin may contribute to the reversal of EMT-related phenotypes. These findings provide mechanistic and structural support for the further preclinical evaluation of vitexin in preventing gastric cancer progression.
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PubMed
高影响因子
Food Science & Nutrition
·
2026
·Vol. 14
·期 6
·e71925
·
IF 5
Shu-Yu Wu,Kai-Wen Kang,Dan-Yu Huang,Shu-Ying Li,Hao Zheng,Ri-Hui Wu,Hui-Qing Lv,Wan-Bin Song,Jing Chen,Cheng-Ping Wen,Li-She Gan,Xiao Yuan
This study identified vitexin as one of the primary active flavonoids in hawthorn that ameliorate hyperuricemia by targeting the PPARγ/ABCG2 pathway. UPLC–MS/MS analysis indicated 17 flavonoid structures in total flavonoids of hawthorn (TFH), while SwissADME calculation then suggested vitexin as the prime candidate for further mechanistic and pharmacodynamic validation. Network pharmacology and molecular docking predicted PPARγ/ABCG2 as one of the key pathways for these flavonoids, which was confirmed by favorable binding with both PPARγ and ABCG2 and stable complex formation of vitexin with PPARγ in molecular dynamics studies. This hypothesis was validated in an HUA mouse model. Vitexin treatment effectively reduced serum uric acid by inhibiting hepatic XOD and ADA activities, and more notably, markedly upregulating renal and intestinal ABCG2 expression to near-normal levels, along with modulation of OAT1 and GLUT9, thereby significantly enhancing urate excretion. The compound also alleviated HUA-induced liver, kidney, and intestinal injuries, restored epithelial barrier integrity, and reduced oxidative stress and inflammation. These findings demonstrate that vitexin exerts multi-target protective effects against HUA by simultaneously suppressing urate production, enhancing its excretion, and mitigating tissue damage. This mechanism of action is consistent with the predicted pathways and supports its potential as a natural therapeutic candidate.
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高影响因子
FOOD RESEARCH INTERNATIONAL
·
2026
·
IF 8.8
Qianqian Wang,Yue Zhang,Zirui Xu,Yingwu Su,Xinyu Fu,Xiao Guan,Sen Li
Mannose-glycosylated soy peptide nanoparticles were developed for vitexin delivery. • Vitexin was amorphously encapsulated with a high efficiency over 94%. • M-SPAV regulated the polarization of macrophage via targeted delivery. • M-SPAV enhanced the cellular uptake of Vitexin and blocked the TLR4/MyD88/NF-κB signaling axis. • The system provides a novel oral delivery strategy for hydrophobic bioactives. Soy peptide aggregates (SPA) are the hydrolysate products of soy protein isolate, which possess good biocompatibility and self-assembly properties, making them excellent materials for nanocarriers. In this study, a green, food-grade nanocarrier based on mannose-modified soy peptide aggregates (M-SPAV) was developed for the efficient encapsulation and targeted delivery of vitexin, a bioactive polyphenol, which has poor water solubility and low bioavailability. The mannose modification of the soy peptide aggregates was performed via a mild and feasible glycosylation method to achieve macrophage targeting. The results demonstrated that nanoparticles prepared at a mannose-to-soy protein aggregate mass ratio of 1:1 exhibited a minimum particle size of 142 nm and achieved an encapsulation efficiency as high as 93.46%. Notably, M-SPAV displayed excellent stability across a broad pH range (3.0–8.0), under high ionic strength conditions and prolonged storage, while effectively protecting vitexin and maintaining antioxidant capacity throughout simulated gastrointestinal digestion. Furthermore, mannose modification not only improved the physicochemical properties of the soy protein aggregates but also endowed the nanoparticles with specific macrophage-targeting capability through receptor recognition. This nanoparticle system substantially enhanced the cellular uptake efficiency of vitexin. Consequently, M-SPAV significantly reduced intracellular reactive oxygen species (ROS) levels in LPS-stimulated macrophages compared to free vitexin, and anti-inflammatory activity by inhibiting the TLR4 / MyD88 / NF-κB signaling axis and regulating macrophage polarization. In summary, M-SPAV provides a promising food-grade nanoplatform for precision immunomodulatory intervention in macrophage-associated inflammatory diseases. Download: Download high-res image (194KB) Download: Download full-size image
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高影响因子
NEW JOURNAL OF CHEMISTRY
·
2025
·
IF 2.5
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.
研究领域:
药剂学
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材料科学
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药理学
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纳米技术
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DOI
高影响因子
Food & Function
·
2024
·
IF 5.1
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.
研究领域:
药理学
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心脏病学
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分子生物学
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营养学
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PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2023
·
IF 6.1
Nan Li,Ruiyan Wang,Wenwen Li,Qian Du,Zeyuan deng,Yawei Fan,Liufeng Zheng
Vitexin, which exists in various medicinal plants and food sources, has recently received increasing attention because of its anti-inflammatory properties. This study aims to identify the protein target of vitexin that ameliorates dextran sulfate sodium (DSS)-induced colitis. The results showed that vitexin not only alleviated the clinical symptoms and colonic damage in mice with DSS-induced colitis but also suppressed the colonic production of inflammatory cytokines (IL-1β, IL-6, ICAM, and VCAM) and enhanced the expression of barrier-associated proteins (ZO-1, Occludin, and E-cadherin). Based on tissue thermal proteome profiling (Tissue-TPP) and molecular docking, OLA1 was creatively identified as a potential protein target for vitexin. Further siRNA-mediated knockdown of the OLA1 gene in Caco-2 cells demonstrated the ability of OLA1 to increase Nrf2 protein expression and, thus, mediated the anti-inflammatory effects of vitexin. Interaction of the OLA1–vitexin complex with Keap1 protein to disrupt the Keap1-Nrf2 interaction may be required for activating Nrf2. Our findings revealed a novel role for OLA1 as a protein target of vitexin that contributes to its anti-inflammatory action by activating Nrf2, which may provide a promising molecular mechanism for novel therapeutic strategies to treat colitis and the associated systemic inflammation.
研究领域:
药理学
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免疫学
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分子生物学
·
胃肠病学
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PubMed
高影响因子
危险品化学品经营许可证（带存储）