Journal of Functional Foods
·
2018
·
IF 3.47
Ni Zeng,Guowen Zhang,Xing Hu,Junhui Pan,Zhisheng Zhou,Deming Gong
Suppression of xanthine oxidase (XO) may contribute to control hyperuricemia and gout. In this study, baicalein and baicalin, two dietary flavones, were found to inhibit the formation of uric acid and generation of superoxide anion (O 2 − ) catalysed by XO through interaction with primary amino acid residues located in flavin adenine dinucleotides center of XO. Baicalein or baicalin binding to XO mainly facilitated by hydrophobic interactions and hydrogen bonds resulted in more compact of XO structure. The concentration profiles and pure spectra of the components extracted from highly overlapping spectral signal by multivariate curve resolution–alternating least squares chemometrics algorithm confirmed the formation of complexes and monitored the reaction kinetics process between XO and these flavones. Furthermore, the isobolographic analysis found that baicalein or baicalin exhibited a moderate synergy on the inhibition of XO when it combined with allopurinol as well as the joint use of baicalein and baicalin.
研究领域:
药理学
·
生物化学
·
医学
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DOI
高影响因子
MOLECULES
·
2023
·Vol. 28
·期 7
·3262
·
IF 4.6
Shuya Xue,Min Shi,Jinye Wang,Jiapeng Li,Guanwei Peng,Jingkun Xu,Yansha Gao,Xuemin Duan,Limin Lu
In this work, TiO2-MXene/poly (3,4-ethylenedioxythiophene): poly(styrenesulfonate) (PEDOT:PSS) composite was utilized as an electrode material for the sensitive electrochemical detection of baicalein. The in-situ growth of TiO2nanoparticles on the surface of MXene nanosheets can effectively prevent their aggregation, thus presenting a significantly large specific surface area and abundant active sites. However, the partial oxidation of MXene after calcination could reduce its conductivity. To address this issue, herein, PEDOT:PSS films were introduced to disperse the TiO2-MXene materials. The uniform and dense films of PEDOT:PSS not only improved the conductivity and dispersion of TiO2-MXene but also enhanced its stability and electrocatalytic activity. With the advantages of a composite material, TiO2-MXene/PEDOT:PSS as an electrode material demonstrated excellent electrochemical sensing ability for baicalein determination, with a wide linear response ranging from 0.007 to 10.0 μM and a lower limit of detection of 2.33 nM. Furthermore, the prepared sensor displayed good repeatability, reproducibility, stability and selectivity, and presented satisfactory results for the determination of baicalein in human urine sample analysis.Keywords:TiO2-MXene;oxygen vacancy;PEDOT:PSS;baicalein;electrochemical sensor
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PubMed
高影响因子
Biomaterials Advances
·
2025
·
IF 6
Jing Xu,Ziyan He,Yaoxin Pan,Bangming Cao,Guofang Chen
Alzheimer's disease (AD) is a progressive neurodegenerative disorder characterized by excessive amyloid-β (Aβ) accumulation, neuroinflammation, and oxidative stress. Exosomes derived from human umbilical cord mesenchymal stem cells (hUC-MSC@Exo) represent promising nanoscale carriers for targeted drug delivery. In this study, Baicalein (Bac), a potent antioxidant and anti-inflammatory flavonoid, was encapsulated into hUC-MSC-derived exosomes (Exo@Bac) to enhance its therapeutic efficacy. The neuroprotective potential of Exo@Bac was evaluated in a rat model of Aβ1–42-induced AD. Rats received intraperitoneal injections of Bac, hUC-MSC@Exo, or Exo@Bac, and cognitive performance was assessed using the passive avoidance test and Morris water maze. Exo@Bac treatment significantly improved memory deficits and elevated brain-derived neurotrophic factor (BDNF) expression compared to controls. Histopathological analyses revealed reduced neuronal damage and apoptosis, alongside decreased Aβ1–42 deposition in Exo@Bac-treated rats. Furthermore, Exo@Bac enhanced antioxidant defense (increased SOD), attenuated pro-inflammatory cytokines (TNF-α, IL-6, IL-1β), and lowered lipid peroxidation (MDA). Mechanistically, Exo@Bac promoted AMPK phosphorylation while suppressing NF-κB p65 signaling, indicating modulation of both oxidative stress and neuroinflammatory pathways. These findings demonstrate that Exo@Bac acts as a nanotherapeutic agent capable of mitigating AD pathology, highlighting its potential as a novel strategy for Alzheimer's disease therapy.
研究领域:
神经科学
·
纳米医学
·
分子生物学
·
干细胞治疗
·
神经退行性疾病
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DOI
PubMed
高影响因子
ENVIRONMENTAL POLLUTION
·
2025
·
IF 7.3
Minyi Huang,Wentao Huang,Renyan Duan,Yingfeng Huang,Yongqiang Xia
Baicalein has pharmacological functions, such as antioxidant and anti-inflammatory properties, and has been shown to alleviate damage to organs caused by environmental pollutants. However, the mechanism by which baicalein reduces the toxic effects of metals needs further research. This study used Pelophylax nigromaculatus tadpoles as a model to explore the toxicological effects of lead (Pb) on the gut-liver axis, and the mechanism by which baicalein alleviates lead toxicity. Analysis of the gut microbiota showed that baicalein alleviated abnormal changes in the gut microbiota following Pb exposure, mainly by increasing the abundance of beneficial bacterial genera, including Cetobacterium , Clostridioides , and Monoglobus . Liver metabolomics showed that compared to a natural recovery, baicalein treatment significantly increased the content of metabolites such as uridine, 17α-hydroxypregnenolone, niacin, and cucurbitacin E, and significantly reduced the content of metabolites such as linoleic, gluconic acid, and tetrahydrocortisone. These differential metabolites could be enriched in pathways such as pyrimidine metabolism, nicotinic acid and nicotinamide metabolism, and steroid hormone biosynthesis, which were beneficial for the treatment of liver injury. There was a significant correlation between the gut microbiota and the main differential metabolites in the liver with the addition of baicalein. The improvement of these metabolic pathways by baicalein is beneficial for the repair of the liver and intestines. Therefore, baicalein can increase the abundance of beneficial gut microbiota, improve liver metabolism, and thus reduce the damage of Pb exposure to the gut-liver axis.
研究领域:
环境毒理学
·
药理学
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DOI
PubMed
高影响因子
INTERNATIONAL IMMUNOPHARMACOLOGY
·
2025
·
IF 4.7
Huanqi Zhang,Xiaozhe Chen,Fuqing Liu,Yanju Bi,Meichen Gao,Xiaojing Li
Long-term environmental exposure to chlorpyrifos (CPF) can cause intestinal damage. Baicalein (BAI) helps aquatic organisms resist environmental pollution stress. Adenosine 5′-monophosphate activated protein kinase (AMPK) is a key molecule in energy regulation; however, the mechanism by which BAI inhibits CPF-induced autophagy/ferroptosis remains unclear. Based on reported environmental concentrations and IC 50 values of CPF, we established models using the midgut of carp and Epithelioma papulosum cyprini (EPC) cells exposed to CPF with or without BAI treatment. Transcriptomics and network pharmacology were used to analyze the key pathways affected by CPF and BAI. Tissue damage, cell cycle regulation, autophagy, ferroptosis, and mitochondrial function were assessed. The effect of BAI on AMPK–unc-51-like autophagy-activating kinase 1 (ULK1) binding was confirmed by molecular dynamics simulation, co-immunoprecipitation, and laser confocal analysis. In addition, the regulatory impact of an AMPK activator on the autophagy/ferroptosis axis was examined. Results indicated that BAI alleviated CPF-induced pathological changes and mitochondrial damage. CPF exposure caused tight junction disruption, mitochondrial depolarization, and reactive oxygen species and mitochondrial reactive oxygen species production. Transcriptomic analysis revealed that CPF toxicity is related to phagosomes, cell cycle regulation, and ferroptosis. By targeting AMPK, BAI prevents the formation of the AMPK–ULK1 complex and inhibits the CPF-induced cascade involving excessive autophagy, cell cycle arrest, and ferroptosis. In conclusion, BAI targets AMPK to prevent binding with ULK1, thereby suppressing the CPF-activated autophagy/ferroptosis axis, reversing mitochondrial dysfunction, and restoring intestinal homeostasis.
研究领域:
环境毒理学
·
分子生物学
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药理学
·
细胞生物学
·
生态毒理学
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DOI
PubMed
高影响因子
MOLECULAR PHARMACEUTICS
·
2024
·
IF 4.5
Huan Shi,Biaobiao Wang,Huilin Ma,Yunmei Li,Jiaqun Du,Bo Zhang,Yu Gao,Ying Liu,Chao Wu
In this study, we prepared bionic selenium–baicalein nanoparticles (ACM-SSe–BE) for the targeted treatment of nonsmall cell lung cancer. Due to the coating of the A549 membrane, the system has homologous targeting capabilities, allowing for the preparation of target tumor cells. The borate ester bond between selenium nanoparticles (SSe) and baicalein (BE) is pH-sensitive and can break under acidic conditions in the tumor microenvironment to achieve the targeted release of BE at the tumor site. Moreover, SSe further enhances the antitumor effect of BE by increasing the production of ROS in tumor cells. Transmission electron microscopy (TEM) images and dynamic light scattering (DLS) showed that the ACM-SSe–BE had a particle size of approximately 155 ± 2 nm. FTIR verified the successful coupling of SSe and BE. In vitro release experiments indicated that the cumulative release of ACM-SSe–BE at pH 5.5 after 24 h was 69.39 ± 1.07%, which was less than the 20% release at pH 7.4, confirming the pH-sensitive release of BE in ACM-SSe–BE. Cell uptake experiments and in vivo imaging showed that ACM-SSe–BE had good targeting ability. The results of MTT, flow cytometry, Western blot, and cell immunofluorescence staining demonstrated that ACM-SSe–BE promoted A549 cell apoptosis and inhibited cell proliferation. The in vivo antitumor results were consistent with those of the cell experiments. These results clearly suggested that ACM-SSe–BE will be a promising bionic nanosystem for the treatment of nonsmall cell lung cancer.
研究领域:
肿瘤学
·
药剂学
·
生物医学工程
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DOI
PubMed
高影响因子
Pharmaceutics
·
2026
·Vol. 18
·期 2
·243
·
IF 6.9
Yunshi Zhi,Li Pan,Wenjun Xiong,Thomas Chuen Lam,Huihui Xiao,Chi Wai Do
Background:Glaucoma requires therapies that extend beyond intraocular pressure (IOP)-lowering strategies, and baicalein (BA) offers dual IOP-lowering and neuroprotective potential. This study evaluated the pharmacokinetics of BA and its major metabolite baicalin (BG) in mouse eyes and serum after intravitreal (IVT) and oral administration to determine whether non-invasive oral dosing can achieve IVT-comparable ocular exposure.Methods:BA was administered via IVT injection (100 μM) or oral gavage (20 and 200 mg/kg) in mice, and concentrations of BA and BG in serum and ocular tissues were quantified using a validated ultra-performance liquid chromatography–mass spectrometry (UHPLC/MS) method.Results:After IVT, ocular BA peaked at 331.56 ± 17.75 ng/g at 5 min and declined to 7.13 ± 0.79 ng/g at 4 h, with minimal systemic exposure. Oral administration achieved comparable or higher peak ocular BA levels (380.43 ± 52.85 ng/g at 15 min for 20 mg/kg; 309.70 ± 24.75 ng/g at 5 min for 200 mg/kg), with markedly higher ocular area under the concentration–time curve (AUC: 2455.48 ± 667.83 h·ng/g for 200 mg/kg and 1224.88 ± 751.13 h·ng/g for 20 mg/kg) versus IVT (247.07 h·ng/g). Serum BA and BG peaked at 5 min after oral dosing, with systemic BG exposure substantially exceeding BA.Conclusions:Non-invasive oral BA dosing achieves ocular concentrations comparable to IVT injection, with significantly greater overall exposure and favorable pharmacokinetic profiles. This study provides the first demonstration in mice that non-invasive oral BA administration can replace invasive IVT delivery, establishing a strong rationale for its clinical development in glaucoma and retinal disease management.
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PubMed
高影响因子
Aging-US
·
2019
·
IF 5.515
Tingting Xu,Xiangting Ge,Chun Lu,Wei Dai,Hongjin Chen,Zhongxiang Xiao,Liqin Wu,Guang Liang,Songmin Ying,Yali Zhang,Yuanrong Dai
Asthma is a type of chronic lung inflammation with restrictions in effective therapy. NF-κB pathway activation has been suggested to play an important role in the pathogenesis of asthma. Baicalein, one of the major active flavonoids found in Scutellaria baicalensis , exhibits potent anti-inflammatory properties by inhibiting NF-κB activity. Herein, we report that Baicalein significantly reduces OVA-induced airway hyperresponsiveness (AHR), airway inflammation, serum IgE levels, mucus production, and collagen deposition around the airway. Additionally, western blot analysis and immunofluorescence assay showed that Baicalein attenuates the activation of NF-κB, which was mainly reflected by IκBα phosphorylation and degradation, p65 nuclear translocation and downstream iNOS expression. Furthermore, in human epithelial cells, Baicalein blocked TNF-α-induced NF-κB activation. Our study provides evidence that Baicalein administration alleviates the pathological changes in asthma through inactivating the NF-κB/iNOS pathway. Baicalein might be a promising potential therapy agent for patients with allergic asthma in the future.
研究领域:
免疫学
·
药理学
·
呼吸医学
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DOI
PubMed
高影响因子
JOURNAL OF ALLOYS AND COMPOUNDS
·
2026
·
IF 6.7
Yuan Jin,Junyuan Song,Tao Xia,Yi Liu,Nanke Ma,Guangli Li
Baicalein (BAI), exhibits diverse pharmacological activities, making its accurate and sensitive detection crucial for clinical and pharmaceutical applications. To address the need for highly sensitive and precise detection of BAI, a novel composite electrochemical sensor Bi 2 MoO 6 /GO/GCE was developed. The electrochemical analysis revealed a synergistic interplay between the catalytic properties of Bi 2 MoO 6 and the exceptional conductivity of graphene oxide (GO), resulting in the sensor exhibiting remarkable sensitivity (1.27 μA μM −1 ) and a low detection limit (0.05 μM) within the BAI concentration range of 0.1–10 μM. Mechanistic investigations demonstrated that BAI undergoes a two-electron, two-proton oxidation process at 0.2 V (vs. SCE, saturated calomel electrode). Kinetic assessments confirmed that the electrode process is governed by a combined diffusion/adsorption mechanism. Notably, Density Functional Theory (DFT) calculations revealed that neutral BAI molecules (HA state) exhibit the highest adsorption energy (E ads = −4.01 eV) and the most substantial charge transfer (Δq = 1.29 e) on the Bi 2 MoO 6 surface, offering a molecular-level rationale for the observed optimal catalytic activity at pH 6.0. The sensor demonstrated outstanding reproducibility, long-term stability (signal decay < 3% over 15 days) and successful quantification in human serum samples. This study offers a robust sensing platform for monitoring drug metabolism through an integrated materials-performance-mechanism approach.
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DOI
高影响因子
TALANTA
·
2017
·
IF 4.162
Zhengkun Xie,Gaiping Li,Yamin Fu,Mengjiao Sun,Baoxian Ye
Chrysin and baicalein are the major flavonoids found in oroxylum indicum, an essential herb in traditional Chinese medicine (TCM). Owing to their similar characteristics and physiochemical property, it is a great challenge to detect both of them simultaneously. In this work, tantalum oxide (Ta 2 O 5 ) particles and chitosan modified carbon paste electrode (Ta 2 O 5 -CTS-CPE) was prepared and characterized by scanning electron microscope (SEM), X-ray diffraction spectroscopy (XRD), Fourier transform infrared spectroscopy (FTIR), cyclic voltammetry (CV) and electrochemical impedance spectrum(EIS). Under the optimum conditions, the prepared Ta 2 O 5 -CTS-CPE exhibited excellent electrocatalytic activity toward the oxidation of chrysin and baicalein, and it could serve as the sensor for highly sensitive and simultaneous determination both of them. The linear range is 0.08–4.0 μM for both of them, and the detection limits were determined to be 0.03 and 0.05 μM (S/N=3) for chrysin and baicalein, respectively. Furthermore, the proposed electrochemical sensor displayed high sensitivity, excellent stability and got satisfactory results in oroxylum indicum samples analysis.
研究领域:
分析化学
·
中药学
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PubMed
高影响因子
FOOD CHEMISTRY
·
2022
·
IF 9.231
Jinmiao Sun,Yixin Dong,Xun Li,Fei Wang,Yu Zhang
Phytoferritin was explored as an attractive nanocarrier to encapsulate bioactive compounds due to its excellent stability and biocompatibility. In the present study, a novel phytoferritin derived from alfalfa (Medicago sativa ) was successfully expressed, purified and characterized. Results confirmed that alfalfa ferritin, self-assembled by 24 subunits, formed a spherical hollow structure. Baicalein exhibits superior antioxidant properties and nutritious values, but low bioavailability and solubility limit its application. Herein, we fabricated water-soluble chitosan-ferritin-baicalein nanoparticles to overcome its drawbacks. It was calculated that one apoferritin cage could encapsulate 52 molecules of baicalein. Moreover, chitosan-ferritin-baicalein nanoparticles prolonged the release of baicalein in simulated gastrointestinal tract digestion. Caco-2 cell monolayer absorption analysis demonstrated that baicalein encapsulated within ferritin-chitosan double layers was more efficient in cellular transportation. These results indicated that alfalfa ferritin, as a novel cage-like protein, has potential application in improving the bioavailability of insoluble bioactive molecules.
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PubMed
高影响因子
ELECTROANALYSIS
·
2022
·Vol. 34
·期 10
·1564-1571
·
IF 3.077
Bo Kong,Xiang Yang,Huiqian Dai,Yu Wu,Hong-Bing Lu,Wei Liu,Xiaoying Liu
In this work, an electrochemical sensor was developed based on the delaminated titanium carbide nanosheet (d-Ti 3 C 2 T x ) and fullerene (C 60 ) composite modified glassy carbon electrode (GCE). The composite materials d-Ti 3 C 2 T x /C 60 were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), cyclic voltammetry (CV) and electrochemical impedance spectroscopy (EIS). The prepared modified electrode (d-Ti 3 C 2 T x /C 60 /GCE) exhibited commendable electrocatalytic activity for the oxidation of baicalein. Under the optimum detection conditions, the detection of baicalin showed a wide linear range of 0.015–4.0 μM with a detection limit of 0.005 μM. In addition, the d-Ti 3 C 2 T x /C 60 /GCE showed good reproducibility, stability and anti-interference. It was also successfully used for the determination of baicalin in the commercially available Shuanghuanglian oral liquid with satisfactory results.
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高影响因子
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