JOURNAL OF MATERIALS SCIENCE & TECHNOLOGY
·
2024
·
IF 11.2
Dongliang Xie,Yi Kuang,Bingnan Yuan,Yunlong Zhang,Chenyu Ye,Yuyi Guo,Hua Qiu,Juanna Ren,Saud O. Alshammari,Qamar A. Alshammari,Zeinhom M. El-Bahy,Kui Zhao,Zhanhu Guo,Qingqing Rao,Shengxiang Yang
As a typical bioflavonoid, diosmetin is desirable in the field of natural medicine, healthy food, and cosmetics by anti-cancer, antibacterial, antioxidant, estrogen-like and anti-inflammatory activities, and it comes from a wide range of sources in traditional Chinese medicine like spider fragrance, spearmint and chrysanthemum, as well as in Citrus fruit. However, traditional analytical methods such as silica gel column chromatography face multiple challenges in the selective extraction of diosmetin from biological materials and traditional Chinese medicinal materials. Therefore, it is urgent to develop a new type of absorbent with high efficiency, recyclability and good specificity to diosmetin. In this investigation, a magnetic surface molecularly imprinted polymer (labeled as Diosmetin/SMIPs) was synthesized employing magnetic nanoparticles as the carrier and 4-vinylpyridinyl (4-VP) as the functional monomer by surface imprinting technology. The functional monomer was screened by the binding energy (ΔE) between functional monomers and template molecules via computational simulation. The Diosmetin/SMIPs had a high level of specific recognition and adsorption capability towards diosmetin with a 20.25 mg g -1 adsorption capacity and an imprinting factor (IF) of 2.28. Additionally, it demonstrated excellent regeneration performance with 8 adsorption/desorption cycles. In addition, 91.20 %–94.16 % of spiked diosmetin was recovered from the lemon peel samples. The strategy of constructing Diosmetin/SMIPs based on computational simulation can effectively enhance the specific adsorption performance of diosmetin. Meanwhile, Diosmetin/SMIPs synthesized by imprinting polymerization showed excellent anti-interference and reusability, and realized efficient targeted extraction of diosmetin from lemon peel samples. The results of this investigation provide a promising adsorbent for selective enrichment of diosmetin from Citrus fruit and complicated materials.
研究领域:
天然药物化学
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材料科学
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分析化学
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DOI
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2025
·
IF 6.2
Mingwei Peng,Jicheng Fu,Yingjie Song,Meiqi Lu,Baoshun Zhang
Cerebral ischemia-reperfusion (I/R) injury involves brain tissue damage caused by a temporary interruption of blood flow followed by reperfusion, leading to inflammation, oxidative stress, and neuronal death. Diosmetin, a flavonoid with known anti-inflammatory and antioxidant properties, has been shown to mitigate I/R injury, but its impact on systemic inflammation is not fully understood. In this study, we investigated its protective effects on I/R injury and the mechanisms mediated through the microbiota-gut-brain axis. Using MCAO-induced rats and OGD/R-induced PC12 cells, we employed multiomics sequencing and molecular biology techniques. The results showed that the IL-6/pJAK1/pSTAT3 signaling pathway was the key mechanism influenced by tryptophan metabolites. Diosmetin alleviated intestinal and systemic inflammation by modulating tryptophan metabolism and gut microbiota dysbiosis. Microbiota transplantation from diosmetin-treated rats produced similar protective effects. In conclusion, diosmetin mitigated I/R injury by influencing tryptophan metabolism through the microbiota-gut-brain axis, offering potential therapeutic strategies for I/R injury.
研究领域:
神经科学
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药理学
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微生物学
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代谢组学
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分子生物学
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DOI
PubMed
高影响因子
MICROCHEMICAL JOURNAL
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2024
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IF 4.9
Chang Tang,Rui Tong,Guoqing Deng,Jing Yang,Yi Zhang,Zhifeng Cai
In this paper, a single signal fluorescent sensor of nitrogen-doped carbon dots (N-CQDs) was established for the micro-determination of diosmetin. In this determination platform, the as-developed N-CQDs with yellow fluorescence were prepared through a facile hydrothermal method with p-phenylenediamine and ascorbic acid as the precursors containing nitrogen and carbon. The as-developed N-CQDs had a classical surface structure and surprising fluorescence stability. The maximum excitation and emission peaks were located at 372 and 528 nm, respectively. Under the optimal sensing conditions, the as-prepared N-CQDs held preeminent immunity towards possible interfering substances. The determination platform’s fluorescence intensity was quenched because of the static quenching and inner filter effect. The fluorescence weakening changes displayed an attractive linear relationship with diosmetin in range of 0.5–150 μM, and the linear equation was ln(F 0 /F) = 0.014[Q]–0.055 with the R 2 of 0.9975 and the detection limit of 0.049 μM. The determination platform could be applied for the trace detection of diosmetin in river water and bovine serum samples. The corresponding recovery rate was 94.8 %–108.8 %, exhibiting that it was a facile and efficient fluorescence sensing strategy.
研究领域:
分析化学
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生物医学工程
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DOI
高影响因子
Chemical Biology & Drug Design
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2024
·Vol. 103
·期 4
·e14529
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IF 3.2
Aihong Yang,Xiaoyue Yi,Hongwei Zhang,Rui Shen,Xiaodi Kou
With the increasing aging population, rational design of drugs for Alzheimer's disease (AD) treatment has become an important research area. Based on the multifunctional design strategy, four diosmetin derivatives ( 1 – 4 ) were designed, synthesized, and characterized by 1 H NMR, 13 C NMR, and MS. Docking study was firstly applied to substantiate the design strategies and then the biological activities including cholinesterase inhibition, metal chelation, antioxidation and β-amyloid (Aβ) aggregation inhibition in vitro were evaluated. The results showed that 1–4 had good acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibition, metal chelation (selective chelation of Cu 2+ ions), antioxidation, self-induced, Cu 2+ -induced, and AChE-induced Aβ aggregation inhibition activities, and suitable blood–brain barrier (BBB) permeability. Especially, compound 3 had the strongest inhibitory effect on AChE (10 −8 M magnitude) and BuChE (10 −7 M magnitude) and showed the best inhibition on AChE-induced Aβ aggregation with 66.14% inhibition ratio. Furthermore, compound 3 could also reduce intracellular reactive oxygen species (ROS) levels in Caenorhabditis elegans and had lower cytotoxicity. In summary, 3 might be considered as a potential multifunctional anti-AD ligand.
研究领域:
药物化学
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神经科学
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生物化学
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DOI
PubMed
高影响因子
TOXICOLOGY AND APPLIED PHARMACOLOGY
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2017
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IF 3.791
Jun-Jun Chen,Jing-Xian Zhang,Xiang-Qi Zhang,Mei-Juan Qi,Mei-Zhi Shi,Jiao Yang,Ke-Zhi Zhang,Cheng Guo,Yong-Long Han
Diosmetin (3′, 5, 7-trihydroxy-4′-methoxyflavone), a natural flavonoid from traditional Chinese herbs, has been used in various medicinal products because of its anticancer, antimicrobial, antioxidant, estrogenic and anti-inflammatory activity. However, flavonoids could affect the metabolic enzymes and cause drug-drug interactions (DDI), reducing the efficacy of co-administered drugs and potentially resulting in serious adverse reactions. To evaluate its potential to interact with co-administered drugs, the IC 50 value of phase I cytochrome P450 enzymes (CYPs), phase II UDP-glucuronyltransferases (UGTs) and hepatic uptake transporters (organic cation transporters (OCTs), organic anion transporter polypeptides (OATPs) and Na + -taurocholate cotransporting polypeptides (NTCPs)) were examined in vitro by LC-MS/MS. Diosmetin showed strong inhibition of CYP1A2 in a concentration-dependent manner. The intensity of the inhibitory effect was followed by CYP2C8 , CYP2C9 , CYP2C19 and CYP2E1 . For CYP2A6 , CYP2B6 , CYP2D6 and CYP3A4 , diosmetin was found to have no significant inhibitory effects, and the induction effect on CYPs was not significant. For UGTs, diosmetin had a minimal inhibitory effect. In addition, the inhibitory effects of diosmetin on OATP and OCT1 were weak, and it had little effect on NTCP. This finding indicated that drug-drug interactions induced by diosmetin may occur through co-administration of drugs metabolized by CYP1A2.
研究领域:
药理学
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毒理学
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生物化学
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DOI
PubMed
高影响因子
NEW JOURNAL OF CHEMISTRY
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2020
·Vol. 44
·期 17
·6799-6809
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IF 3.288
Yongjie Liu,Hao Chen,Huilong Xiang,Huan Lei,Di Zhang,Yinsheng Qiu,Lingyun Xu
Diosmetin, as a methoxyflavone compound, was investigated for its interaction and mechanism with xanthine oxidase (XOD), which is a key enzyme catalyzing xanthine to uric acid and finally causing hyperuricemia. Using a kinetic analysis method, diosmetin was shown to possess a strong inhibitory activity for XOD in a reversibly competitive manner with an IC50 value of (5.08 ± 0.48) × 10−6 mol L−1. The results of fluorescence titrations showed that the combination of diosmetin with XOD gave spontaneous, exothermic static quenching, and hydrogen bonding and van der Waals forces were the main driving forces. It was suggested that diosmetin increased the polarity of the tyrosine and tryptophan microenvironment of XOD by synchronous fluorescence analysis. The results of ultraviolet absorption spectroscopy, circular dichroism and molecular docking showed that diosmetin could bind to the active site of XOD to form a new diosmetin–XOD complex. In these experiments, diosmetin reduced the content of α-helices, β-sheets and β-turns of XOD, which led to the instability of the XOD structure and the decrease of its catalytic function. Furthermore, the 4′-methoxy group of diosmetin had a higher affinity for XOD than the 4′-hydroxyl group of luteolin. To the best of our knowledge, this is the first comprehensive report to present the inhibitory activities of diosmetin against XOD.
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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DOI
高影响因子
CARBOHYDRATE POLYMERS
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2025
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IF 12.5
Yuanyuan Chen,Qian Zhou,Yue Zhou,Jinlan Huang,Renjie Niu,Jian Ming,Mingfu Wang
Oral delivery of natural antioxidants represents a promising therapeutic strategy for ulcerative colitis (UC), yet their therapeutic efficacy is hindered by instability and poor accumulation at inflamed sites. To address this, we developed Galectin-3 (Gal-3)-targeted nanoparticles (ZDP-NPs) by encapsulating diosmetin within zein complexes modified with a galactose- and rhamnogalacturonan-I (RG-I)-rich pectin (PMTP, Mw: 228.8 kDa, DM: 34.21 %, RG-I content: 43 %) extracted from Premna microphylla Turcz leaves. Surface plasmon resonance (SPR) analysis confirmed a strong binding affinity between PMTP and Gal-3 (KD = 2.83 μM). ZDP-NPs exhibited uniform spherical morphology (~170 nm), high drug loading (87.9 %) and colloidal stability. Under simulated gastrointestinal conditions, ZDP-NPs showed reduced Dio release (45.6 %) compared to PMTP-free nanoparticles (ZD-NPs, 75.6 %). In vitro studies showed that PMTP surface modification significantly enhanced nanoparticle uptake by LPS-induced macrophages via Gal-3-mediated endocytosis. In vivo colitis experiment of mice revealed that ZDP-NPs selectively accumulated in inflamed colons via Gal-3 targeting, prolonged retention, and significantly alleviated colonic damage by reducing oxidative stress, suppressing pro-inflammatory cytokines, and restoring epithelial barrier integrity. Biocompatibility assays confirmed minimal toxicity of ZDP-NPs. This study presented a food-derived pectin-based nanoplatform for precise colitis intervention through Gal-3 targeting, offering a multifaceted strategy to break the inflammation-oxidative stress cycle.
研究领域:
纳米医学
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药理学
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胃肠病学
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生物化学
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炎症性肠病研究
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植物来源药物
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DOI
PubMed
高影响因子
ONCOGENE
·
2023
·Vol. 42
·期 29
·2278-2293
·
IF 8
Chen Yihuan,Dai Xiaoshuo,Chen Wei,Qiao Yan,Bai Ruihua,Duan Xiaoxuan,Zhang Kai,Chen Xinhuan,Li Xin,Mo Saijun,Cao Wenbo,Li Xiang,Liu Kangdong,Dong Ziming,Lu Jing
Cisplatin (CDDP) is the first-line drug in the clinical treatment of esophageal squamous cell carcinoma (ESCC), which has severe nephrotoxicity. Diosmetin (DIOS) can protect kidney from oxidative damage, however, its function in ESCC is unknown. This study aims to explore the effect and mechanism of DIOS on ESCC and its combined effect with CDDP. Herein, we found that DIOS significantly inhibited the progression of ESCC in vitro and in vivo. Furthermore, the anti-tumor effect of DIOS was not statistically different from that of CDDP. Mechanically, transcriptomics revealed that DIOS inhibited the E2F2/RRM2 signaling pathway. The transcriptional regulation of RRM2 by E2F2 was verified by luciferase assay. Moreover, docking model, CETSA, pull-down assay and CDK2 inhibitor assay confirmed that DIOS directly targeted CDK2, leading to significant suppression of ESCC. Additionally, the patient-derived xenografts (PDX) model showed that the combination of DIOS and CDDP significantly inhibited the growth of ESCC. Importantly, the combined treatment with DIOS and CDDP significantly reduced the mRNA expression levels of kidney injury biomarkers KIM-1 and NGAL in renal tissue, as well as the levels of blood urea nitrogen, serum creatinine and blood uric acid compared to the single treatment with CDDP. In conclusion, DIOS could be an effective drug and a potential chemotherapeutic adjuvant for ESCC treatment. Furthermore, DIOS could reduce the nephrotoxicity of CDDP to some extent.
研究领域:
肿瘤学
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药理学
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分子生物学
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DOI
PubMed
高影响因子
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
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2024
·
IF 2.7
Yuqing Zhang,Yaping Li,Yuhan Zhai,Xing Zhao,Mingxing Lv,Shaoxuan Yu,Haifang Xiao,Yuanda Song
Inhibition of α-glucosidase activity is a promising method to prevent postprandial hyperglycemia. The inhibitory effect and interaction of chrysin and diosmetin on α-glucosidase were studied in this study. The results of inhibition kinetics showed that chrysin and diosmetin reversibly inhibited α-glucosidase activity with IC50 value of 26.445 ± 1.406 μmol L−1 and 18.380 ± 1.264 μmol L−1, respectively. Further research revealed that chrysin exhibited a mixed-type inhibitory pattern against α-glucosidase, while diosmetin was noncompetitive inhibitory with Ki value of (2.6 ± 0.04) ×10−4 mol L−1. Fluorescence spectroscopy showed that both chrysin and diosmetin could quench the intrinsic fluorescence of α-glucosidase, the maximum emission wavelength of tyrosine (Tyr) and tryptophan (Trp) were not moved by chrysin, but red shifted by diosmetin. UV-Vis, fourier transform infrared spectroscopy (FT-IR) and circular dichroism (CD) measurements showed that the secondary structure and microenvironment of α-glucosidase were changed by chrysin and diosmetin. Further analysis of molecular docking showed that chrysin and diosmetin could bind with α-glucosidase and might cause the decrease of α-glucosidase activity. The results of molecular dynamics (MD) simulation showed that the stability of chrysin (or diosmetin)-α-glucosidase complex system was changed during binding process. In conclusion, chrysin and diosmetin are good α-glucosidase inhibitors.Communicated by Ramaswamy H. Sarma
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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DOI
PubMed
高影响因子
Pharmaceutics
·
2025
·Vol. 17
·期 3
·302
·
IF 5.5
Jing Zhang,Min Zha,Anping Wan,Satya Siva Kishan Yalamarty,Nina Filipczak,Xiang Li
Background Despite many studies on polymer-incorporated nanocarriers for ophthalmic drug delivery, few have thoroughly explored the relationship between coating composition and performance. This study aimed to evaluate the effects of three commonly used cationic polymers—distearoyl phosphatidylethanolamine-polyethylene glycol 1000-poly(amidoamine) (DSPE-PEG1000-PAMAM), trimethyl chitosan (TMC), and (2,3-dioleoyloxypropyl) trimethylammonium chloride (DOTAP)—on the corneal behaviors and anti-cataract efficacy of diosmetin (DIO)-loaded micelles (D-M-P, D-M-T, and D-M-D, respectively). Methods The DIO-loaded micelles were prepared using the thin-film dispersion method and incorporated with the three polymers through hydrophobic interactions and electrostatic adsorption. Structural characterization was demonstrated by TEM imaging and particle size analyzer. In vitro release behavior was detected by the dialysis method. Cell viability of D-M-P, D-M-T, and D-M-D on L929 cells was detected by CCK-8 assays, with cellular uptake performed using coumarin 6 as the fluorescence indicator. Precorneal retention behaviors of these three vesicles were observed by In Vivo Imaging System. Transcorneal permeability was determined by modified Franz diffusion method and the permeation routes of the vesicles are investigated. Selenite-induced cataract model was established. The anti-cataract effects of three different DIO-loaded micelles were evaluated by the observation of lens opacity and antioxidant enzyme activities. Eye Irritation of the DIO in different preparations was estimated using the Draize test, along with H&E staining of the corneas. Results Structural characterization of DIO-loaded micelles revealed that the vesicles were spherical, with a uniform size distribution of around 28 nm, a similar surface potential of approximately 6.0 mV, and a high DIO entrapment efficiency of about 95%. Compared to the DIO suspension, all three formulations exhibited a significant sustained-release effect. They showed no signs of irritation and demonstrated increased IC50 values in L929 cells, indicating improved biocompatibility. Cellular uptake in human lens epithelial cells (HLECs) was assessed using confocal laser scanning microscopy. C-M-T displayed the highest fluorescence signals, with a cellular internalization 3.2 times greater than that of the solution group. Both C-M-T and C-M-P enhanced vesicle retention on the corneal surface by at least 47.8% compared to the Cou-6 solution. Furthermore, TMC facilitated the paracellular transport of vesicles into the deepest layers of the cornea and delivered DIO across the cornea, with a P app value 3.11 times and 1.49 times those of D-M-D and D-M-P, respectively. In terms of therapeutic efficacy, D-M-T demonstrated the most significant attenuation of lens opacity, along with enhanced antioxidant enzyme activities and inhibition of lipid peroxidation. Conclusion The modification of micelle vesicles with different cationic polymers significantly influences their performance in ocular drug delivery. Among the tested formulations, D-M-T stands out due to its multiple advantages, including enhanced transcorneal drug delivery, therapeutic efficacy for DIO, and safety, making it the most promising candidate for ophthalmic applications.
研究领域:
药剂学
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眼科学
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产品关联
DOI
PubMed
高影响因子
FASEB JOURNAL
·
2026
·Vol. 40
·期 6
·e71679
·
IF 4.3
Jie Wang,Yuxin Shi,Yan Jia,Jie Peng
Diosmetin is a bioactive flavonoid that exhibits well-documented antioxidant, anti-inflammatory, and anti-tumor properties. However, its potential to attenuate acute pancreatitis (AP) progression through gut microbiota modulation has not yet been elucidated. In this study, mice were pretreated with varying oral doses of diosmetin for 1 week before AP induction via intraperitoneal (i.p.) caerulein injections. The therapeutic efficacy and optimal dosage were determined through histopathological analysis of pancreatic tissue and serological biomarker assessment. Additionally, transcriptomic profiling and western blot were employed to elucidate the underlying signaling pathways. Furthermore, based on integrated metagenomic and metabolomic analyses, a core gut microbiota-metabolite-gene interaction network modulated by diosmetin was constructed. Finally, fecal microbiota transplantation (FMT) experiments validated the critical role of gut microbiota in the effects of diosmetin against AP. The results showed that medium-dose diosmetin treatment significantly attenuated pancreatic histopathological damage and acinar cell apoptosis in AP mice, while suppressing the activation of the MAPK inflammatory signaling pathway. Notably, diosmetin treatment was associated with restored microbial diversity, altered bacterial community structure, and changes in key metabolic pathways, reversing gut microbiota dysbiosis. Specifically, a diosmetin-responsive interaction network was constructed, highlighting associations between core bacterial taxa ( Butyricimonas faecalis , Enterocloster bolteae , Roseburia intestinalis ), key metabolites (3-indoleacrylic acid, 2-methoxy-4-vinylphenol, nitrite), and MAPK pathway-related genes. Finally, the protective effect of diosmetin was further substantiated by FMT, suggesting a potential role of the gut microbiota in this process. In conclusion, diosmetin ameliorated pancreatic injury in a murine model of caerulein-induced AP by modulating gut microbiota composition and associated metabolic profiles. These findings suggested that diosmetin represented a promising therapeutic option for AP, offering a scientific foundation for its clinical application and the underlying mechanisms involved. Graphical This study integrates transcriptomic, metagenomic, and metabolomic analyses to systematically elucidate the protective mechanisms of diosmetin against acute pancreatitis through the “microbiota-metabolite-inflammation” axis. Results show that diosmetin effectively inhibits pancreatic MAPK overactivation, reduces systemic inflammation, restores gut microbiota homeostasis, and reverses caerulein-induced metabolic alterations.
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PubMed
高影响因子
AAPS PHARMSCITECH
·
2022
·Vol. 23
·期 4
·1-16
·
IF 4.026
Gu Zhengqing,Xue Yuanyuan,Li Shuang,Adu-Frimpong Michael,Xu Ying,Yu Jiangnan,Xu Ximing,Zhu Yuan
Diosmetin (DIOS) is a functional compound with poor water solubility, bad permeability, and crystal form. Self-microemulsifying drug delivery system (SMEDDS) was an effective formulation to overcome these shortcomings. In this study, liquid SMEDDS was prepared using Capmul® MCM C8 EP/NF, Cremophor EL, and PEG 400 (2:5.6:2.4, w/w/w) as excipients. Then, the novel technology of electrospray solidified liquid SMEDDS and prepared solid SMEDDS for inhibiting crystallization. Polyvinyl pyrrolidone (PVP) was used as carrier to construct DIOS-loaded solid SMEDDS, with polyethylene oxide (PEO) contributing to the formation of regular sphere in the process of spinning. The particle size of solid SMEDDS (194 ± 5 nm) was much bigger than of liquid SMEDDS (25 ± 1 nm), while DIOS-loaded solid SMEDDS showed greater dissolution rates in pH 1.2 and pH 6.8 media through in vitro drug release study. The solid nanoparticles were smooth and uniform from the graph of a scanning electron microscope (SEM). The graph of a transmission electron microscope (TEM) showed that small droplets were loaded in the matrix. Furthermore, DIOS was encapsulated by matrix in amorphous state via differential scanning calorimetry (DSC) and attenuated total reflection Fourier transform infrared (ATR-FTIR). The crystalline of DIOS was not formed in solid SMEDDS due to the characteristic peaks of DIOS disappeared in X-ray diffraction (XRD) pattern. Therefore, the oral bioavailability of DIOS improved significantly compared with liquid SMEDDS (4.27-fold). Hence, solid SMEDDS could improve the solubility and bioavailability of DIOS, through transfer of the state of crystalline to amorphous by electrospray technology.
研究领域:
药剂学
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
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