AQUACULTURE
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2025
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IF 3.9
Feiran Li,Guangyao Hu,Mengsha Zhou,Liqun Lu
Spring viremia of carp virus (SVCV) inflicts substantial economic damage on global cyprinid farming operations, primarily affecting common carp and koi carp. Currently, no effective control measures exist. Baicalein, a flavonoid derived from Scutellaria baicalensis , exhibits broad-spectrum antiviral activity. This study investigated baicalein's inhibitory effects against SVCV in vitro and in vivo. Cytotoxicity assays demonstrated no observable toxicity in EPC cells at concentrations of 1–25 μg/mL. Transcriptome analysis and biochemical assays revealed that baicalein enhances innate immunity via the NF-κB pathway while concurrently suppressing SVCV-induced apoptosis. In SVCV-infected koi, baicalein treatment significantly reduced viral replication, attenuated pathogenicity, and improved survival rates. Pharmacokinetic studies in koi carp indicated favorable properties: rapid absorption (Tmax = 4 h), sustained plasma presence (t 1/2 z/h > 7 h), and dose-proportional exposure (AUC 0-t ). These findings establish baicalein as a novel therapeutic candidate against SVCV in aquaculture.
研究领域:
水产养殖
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病毒学
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药理学
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鱼类健康
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抗病毒研究
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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
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2019
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IF 2.931
Jun Zhang,Danyang Nan,Shuang Pan,Hui Liu,Huan Yang,Xiaoli Hu
In this work, nitrogen and sulfur dual-doped CDs (N,S-CDs) were prepared via a facile one-pot hydrothermal method from citric acid and N -acetyl-L-cysteine with a high quantum yield (QY) of 49%. As-fabricated N,S-CDs had a size around 2.5 nm and exhibited excitation-independent emission and excellent luminescent properties. The fluorescent sensor based on the N,S-CDs showed a highly sensitive detection of baicalein with a detection limit (LOD) of 0.21 μmol L −1 in the linear range from 0.69 to 70.0 μmol L −1 . The fluorescence of the N,S-CDs could be effectively quenched by baicalein based on static quenching. In addition, the temperature sensor based on the synthesized N,S-CDs showed a good linear relationship between temperature and fluorescence (FL) intensity with a temperature range from 5 °C to 75 °C. Furthermore, the synthesized N,S-CDs were successfully applied to the measurement of baicalein in real samples. In a word, the N,S-CDs had great potential to be worked as fluorescence sensors to monitor the concentration of baicalein and temperature.
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Frontiers in Pharmacology
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2018
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IF 3.831
Xu Peng,Zhou Hua,Li Ya-Zhuo,Yuan Zhong-Wen,Liu Chang-Xiao,Liu Liang,Xie Ying
Although hepatoprotective properties of silybin are well documented, the clinical therapeutic efficacy is limited by its low bioavailability due to absorption rates, extensive phase II metabolism, and biliary excretion. As our previous study indicated that metabolic enzymes may have limited effects on the pharmacokinetic (PK) behavior of silymarin, here, we intended to increase the oral bioavailability and bio-efficacy of silybin through the inhibition of active efflux. In Caco-2 and transfected MDCKII cell models, flavone baicalein significantly inhibited the efflux of silybin as a BCRP and MRP2 inhibitor. In addition, baicalein reduced the biliary excretion index (BEI) and biliary clearance of silybin conjugates in the sandwich-cultured rat hepatocyte (SCH) model, indicating the inhibition of baicalein in biliary excretion of conjugated silybin metabolites. PK study demonstrated that baicalein significantly increased the area under the curve (AUC) and Cmax of silybin and its conjugates, suggesting enhanced absorption in vivo. Moreover, coadministration of silybin with baicalein boosted the liver protective, antioxidant, and anti-inflammatory effects of silybin in the carbon tetrachloride (CCl4)-induced liver injury model in comparison with silybin given alone. In summary, efflux transporters play a critical role in the low bioavailability of silybin, while inhibition of breast cancer resistance protein (BCRP) and multi-drug resistance protein 2 (MRP2) by baicalein can significantly increase the absorption and bio-efficacy of silybin, which provides a new combination therapeutic approach for the treatment of chronic liver diseases.
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INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
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2024
·Vol. 25
·期 7
·3654
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IF 4.9
Wencheng Zhao,Huizi Cui,Kaifeng Liu,Xiaotang Yang,Shu Xing,Wannan Li
Type 2 diabetes mellitus (T2DM) is marked by persistent hyperglycemia, insulin resistance, and pancreatic β-cell dysfunction, imposing substantial health burdens and elevating the risk of systemic complications and cardiovascular diseases. While the pathogenesis of diabetes remains elusive, a cyclical relationship between insulin resistance and inflammation is acknowledged, wherein inflammation exacerbates insulin resistance, perpetuating a deleterious cycle. Consequently, anti-inflammatory interventions offer a therapeutic avenue for T2DM management. In this study, a herb called Baikal skullcap, renowned for its repertoire of bioactive compounds with anti-inflammatory potential, is posited as a promising source for novel T2DM therapeutic strategies. Our study probed the anti-diabetic properties of compounds from Baikal skullcap via network pharmacology, molecular docking, and cellular assays, concentrating on their dual modulatory effects on diabetes through Protein Tyrosine Phosphatase 1B (PTP1B) enzyme inhibition and anti-inflammatory actions. We identified the major compounds in Baikal skullcap using liquid chromatography–mass spectrometry (LC–MS), highlighting six flavonoids, including the well-studied baicalein, as potent inhibitors of PTP1B. Furthermore, cellular experiments revealed that baicalin and baicalein exhibited enhanced anti-inflammatory responses compared to the active constituents of licorice, a known anti-inflammatory agent in TCM. Our findings confirmed that baicalin and baicalein mitigate diabetes via two distinct pathways: PTP1B inhibition and anti-inflammatory effects. Additionally, we have identified six flavonoid molecules with substantial potential for drug development, thereby augmenting the T2DM pharmacotherapeutic arsenal and promoting the integration of herb-derived treatments into modern pharmacology.
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2026
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IF 4.9
Aiju Chen,Qiulu Wang,Xiangtai Wang,Lixia Yuan,Hui Yan,Lingfeng Gao,Min Liu
Baicalein (Bai), a flavonoid with multiple pharmacological effects, suffers from poor solubility and low stability, limiting its therapeutic application. To overcome these limitations, biocompatible solvents with high solvation capacity present a simple and efficient strategy. In this work, three natural deep eutectic solvents (NADES) were prepared from choline chloride (ChCl) and structurally comparable organic acids: levulinic acid (LevA), lactic acid (LacA), and malic acid (MalA). These NADES exhibited good biocompatibility and were mixed with water to improve the solubility and stability of Bai. The solubility enhancement of Bai in these solvents followed the order: ChCl-LevA > ChCl-LacA > ChCl-MalA > water. Thermodynamic analysis revealed an entropy-driven dissolution process. To delve deeper into the dissolution mechanism, density measurements, FTIR spectroscopy, and molecular dynamics simulations were conducted to elucidate solvent-solvent and solute-solvent interactions. Additionally, the storage stability, photostability, and pH stability of Bai in NADES were also investigated. The results indicated that the differences in intermolecular interactions caused by different NADES exerted varying effects on the stability of Bai. The DPPH free radical scavenging assay was used to investigate the synergistic or antagonistic antioxidant effects between Bai and NADES, with the data analyzed by response surface methodology. These results are expected to provide a theoretical basis for the development of NADES-based solubilizers or drug carriers in pharmaceutical and food science.
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Biomaterials Science
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2023
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IF 6.6
Limei Liu,Weisong Wu,Siqi Li,Li Ma,Yunting Liu,Xiaoli Wang,Yanjun Jiang
Orally administrating baicalein-decorated zinc phosphates (ZnBM) were engineered for mucosal barrier improvement and intestinal inflammation relief. ZnBM with a size of 1.78 µm comprised 5.58 wt% of baicalein and 13.17 wt% of Zn. The incorporation of baicalein endowed ZnBM with excellent radical scavenging activities. ZnBM exhibited good stability with negligible zinc re-lease in PBS solution for 2 days, and 32.82% of zinc could reach the gut. In addition, ZnBM polar-ized macrophages into anti-inflammatory M2 type and effectively scavenged intracellular ROS of LPS-treated RAW264.7. Meanwhile, ZnBM effectively scavenged intracellular ROS of PMA-induced Caco-2 cells and exerted a reparative effect on LPS-damaged Caco-2 monolayer, causing obvious improvement of barrier function. Reduced systemic exposure to FITC-dextran was observed to illustrate barrier restoration by ZnBM, which was achieved through upregula-tion of tight junction proteins expression. Notably, the commonly used clinical drug, 5-aminosalicylic acid was toxic to liver and kidney, and commercial ZnO caused death of mice during treatment. Apparently, the therapeutic effect of ZnBM was significantly better than that of baicalein alone in chronic colitis. Overall, ZnBM exhibited outstanding therapeutic efficacy and was expected to be used in the clinical treatment of colitis due to its effectiveness, biosecuri-ty, facile preparation, and easy storage.
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PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
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2023
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IF 4.7
Qian Wu,Wenrui Yang,Yanju Bi,Yujie Yao,Chengzhi Li,Xiaojing Li
Chlorpyrifos (CPF), a widely used organophosphate pesticide that has caused large-scale contamination globally, has become a major concern. Baicalein (BAI), as a flavonoid extract, shows anti-inflammatory as well as antioxidant activities . The kidneys of fish serve to excrete toxins and are major target organs for environmental contaminants. However, it is not obvious whether BAI can counteract the damage caused by CPF exposure to fish kidneys . Therefore, we conducted a 30-day simulation of CPF poisoning and/or BAI treatment by adding 23.2 μg/L CPF to water and/or 0.15 g/kg BAI to feed. In the transmission electron microscopy results, we observed obvious phenomenon of autophagy and apoptosis in the CPF group, and the TUNEL staining and immunofluorescence of LC3B and p62 double-staining results confirmed that CPF induced autophagy and apoptosis in the kidney of common carp . Furthermore, CPF induced the increase of ROS level and inhibition of PI3K and Nrf2 pathways, which in turn triggered oxidative stress , autophagy and apoptosis in carp kidney according to western blot , RT-qPCR and kit assays. However, addition of BAI significantly alleviated oxidative stress , autophagy and apoptosis due to binding to PI3K protein. Additionally, through phylogenetic tree and structural domain analyses, we also found that the binding sites of BAI and PI3K are conserved in a variety of representative species. These results suggest that BAI antagonizes CPF-caused renal impairments in carp involving the PI3K/AKT pathway and the Nrf2 pathway. Our findings provide new insights into the nephrotoxicity effects of CPF and the potential use of BAI as a detoxification agent for CPF intoxication.
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BIOCHEMICAL PHARMACOLOGY
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2020
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IF 4.96
Junke Song,Li Zhang,Yanfeng Xu,Dezhi Yang,Li Zhang,Shiying Yang,Wen Zhang,Jinhua Wang,Shuo Tian,Shengqian Yang,Tianyi Yuan,Ailin Liu,Qi Lv,Fengdi Li,Hongqi Liu,Biyu Hou,Xiaozhong Peng,Yang Lu,Guanhua Du
Baicalein is the main active compound of Scutellaria baicalensis Georgi, a medicinal herb with multiple pharmacological activities, including the broad anti-virus effects. In this paper, the preclinical study of baicalein on the treatment of COVID-19 was performed. Results showed that baicalein inhibited cell damage induced by SARS-CoV-2 and improved the morphology of Vero E6 cells at a concentration of 0.1 μM and above. The effective concentration could be reached after oral administration of 200 mg/kg crystal form β of baicalein in rats. Furthermore, baicalein significantly inhibited the body weight loss, the replication of the virus, and relieved the lesions of lung tissue in hACE2 transgenic mice infected with SARS-CoV-2. In LPS-induced acute lung injury of mice, baicalein improved the respiratory function, inhibited inflammatory cell infiltration in the lung, and decreased the levels of IL-1β and TNF-α in serum. In conclusion, oral administration of crystal form β of baicalein could reach its effective concentration against SARS-CoV-2. Baicalein could inhibit SARS-CoV-2-induced injury both in vitro and in vivo. Therefore, baicalein might be a promising therapeutic drug for the treatment of COVID-19.
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SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
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2021
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IF 4.098
Rui Wang,Jian Li,De-Bao Niu,Fei-Yue Xu,Xin-An Zeng
In this work, the protective effect of baicalein on DNA oxidative damage and its possible protection mechanisms were investigated. 2-thiobarbituric acid (TBA) colorimetry and agarose gel electrophoresis study found that baicalein protected the deoxyribose residue and double-stranded backbone of DNA from the damage of hydroxyl radicals. Antioxidant analysis results showed that baicalein has excellent radicals scavenging effects and Fe 2+ chelating ability, which might be the mechanism of baicalein protecting DNA. DNA binding studies indicated that baicalein bound to the minor groove of DNA with moderate binding affinity ( K = (7.35 ± 0.91) × 10 3 M −1 ). Hydrogen bonding and van der Waals forces played a major role in driving the binding process. Molecular docking further confirmed the experimental results. This binding could stabilize DNA double helix structure, thereby protecting DNA from oxidative damage. This study may provide theoretical basis for designing new functional foods of baicalein for DNA damage protection.
研究领域:
药理学
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分子生物学
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生物化学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2025
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IF 8.5
Kunshan Wang,Yingao Zhai,Zenghui Yu,Xuan Zhang,Suzhen Zhou,Jinbo Fan
To mitigate postprandial hyperglycemia, acarbose's excessive α-amylase (AMY) inhibition causes gastrointestinal side effects. Baicalein (Bai), genistein (Gen), and isoliquiritigenin (Isl), featuring 5,6-dihydroxyflavone structures, mildly inhibit AMY. In this study, the inhibitory mechanism of Bai, Gen, and Isl on AMY was determined by integrating multiple analytical techniques and molecular simulation technologies. The results showed that Bai/Gen/Isl exhibited strong inhibitory activity against AMY with IC 50 values of 22.44 ± 0.92 μmoL·L −1 , 24.78 ± 1.91 μmoL·L −1 , and 26.78 ± 1.79 μmoL·L −1 , respectively, which belonged to the mixed inhibition type dominated by competitive inhibition. The three form a ground state complex with AMY through a static quenching mechanism, and the order of binding constants is Bai > Gen > Isl. Their binding significantly changed the microenvironment polarity of Trp residues in AMY and induced secondary structure rearrangement. Differential scanning calorimetry (DSC), X-ray diffraction (XRD), and scanning electron microscopy (SEM) showed that the relative crystallinity of AMY increased, forming dense aggregates and increasing thermal stability. Molecular simulation showed that the interactions between AMY and Bai/Gen were dominated by van der Waals forces or hydrogen bonds, while the interactions with Isl were dominated by hydrophobic interactions. By employing a novel integrative approach combining fluorescence/UV–Vis/FTIR spectroscopy, DSC-XRD-SEM characterization, and 120 ns molecular dynamics simulation, this study overcomes the single-technique limitations of previous research and provides a theoretical basis for the development of blood glucose control agents based on natural products.
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Biomaterials Science
·
2025
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IF 5.7
Yan Wang,Suyuan Su,Chaofeng Wang,Congyang Mao,Xiangmei Liu,Hanpeng Liu,Zhaoyang Li,Shengli Zhu,Hui Jiang,Zhenduo Cui,Yufeng Zheng,Shuilin Wu
Persistent bacterial infections and the imbalance in immune regulation induced by oxidative stress present a significant challenge in diabetic wound healing. In this study, we developed a novel dual-network hydrogel system composed of chitosan/polyacrylic acid (PEC) and polyoxometalate PMo12 (PMo12-PEC) loaded with baicalein (BA), designated as PMo12-BA-PEC, for the treatment of methicillin-resistant Staphylococcus aureus (MRSA)-infected diabetic wounds. The hydrogel demonstrated enhanced mechanical strength and elasticity, facilitating effective wound adherence and accommodating tissue movement. Upon 808 nm near-infrared (NIR) light irradiation, the photothermal properties of PMo12 enabled controlled low-temperature hyperthermia and accelerated BA release. Remarkably, the hydrogel achieved an antibacterial efficacy of 99.45% ± 0.12% against MRSA following 5 minutes of NIR exposure, while exhibiting potent antioxidant and anti-inflammatory capabilities to scavenge reactive oxygen species and mitigate inflammatory responses. Comprehensive evaluation revealed that the PMo12-BA-PEC hydrogel significantly promoted angiogenesis, enhanced collagen deposition, inhibited bacterial growth, and modulated immune regulation, thereby accelerating the wound healing process in diabetic rat models. These findings suggest that the PMo12-BA-PEC hydrogel represents a promising biomaterial platform for clinical management of diabetic wounds and potential treatment of oxidative stress-related disorders.
研究领域:
生物医学工程
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药理学
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免疫学
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NEUROTOXICOLOGY
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2021
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IF 4.294
Qingxin Song,Shanxin Peng,Xiaosong Zhu
Baicalein, a major bioactive flavone constituent isolated from Scutellaria baicalensis Georgi, has neuroprotective properties in several neurological disorders. Many studies suggest that oxidative stress plays a central role in the pathogenesis of Parkinson’s disease (PD). Baicalein has also been shown to have antioxidant effects. Therefore, the current study was designed to investigate whether baicalein could protect against MPP + /MPTP-induced neurotoxicity via suppressing oxidative stress in vitro and in vivo . In vitro , our results showed that baicalein increased cell viability in MPP + -treated SH-SY5Y cells. Treatment with baicalein could reversed the increased MDA and ROS levels, and the decreased GSH levels in MPP + -treated SH-SY5Y cells. In MPTP-treated mice, baicalein ameliorated MPTP-induced motor impairment and suppressed the MPTP-induced accumulation of iron and lipid peroxides. Besides, baicalein improved the neurotoxicity induced by MPTP as seen by a significant raise of tyrosine hydroxylase (TH) and simultaneous decrease of monoamine-oxidase-B (MAO-B). The inhibitory effect of baicalein on oxidative stress probably was partially governed by inhibition of ERK activation. In conclusion, our results suggest that baicalein could prevent MPP+/MPTP-induced neurotoxicity via suppressing oxidative stress.
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