RENAL FAILURE
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2026
·
IF 3.8
Chengli Lou,Yijing Zhou,Bo Feng,Xiaoping Fan,Xiuqin Xu,Pingxin Hu,Xiangjing Wang
Idiopathic membranous nephropathy (IMN) is an autoimmune glomerular disease. Current immunosuppressive therapies often cause side effects and high recurrence rates, highlighting the need for new treatments. Baicalin (BAI), a flavonoid isolated from Scutellaria baicalensis, has anti-inflammatory and antioxidant properties. This study examined effects of BAI on IMN using in vitro mouse podocyte clone-5 (MPC-5) cells treated with zymosan-activated serum (ZAS) and in vivo mouse models induced with cationic bovine serum albumin (BSA). Treatments included the BAI and advanced glycation end products/receptor for advanced glycation end products (AGE/RAGE) agonist, advanced glycation end products - bovine serum albumin (AGE-BSA). Assessments included cell viability, apoptosis, reactive oxygen species (ROS), inflammatory cytokines, oxidative stress markers, renal function, and histopathology. Potential targets and pathways involved in BAI’s effect on IMN were identified using network pharmacology. Compared to the ZAS-induced MPC-5 cell group, BAI increased cell viability and reduced apoptosis in injured cells. Meantime, BAI significantly reduced the release of pro-inflammatory cytokines tumor necrosis factor α, monocyte chemotactic protein 1, and interleukin 6 and enhanced antioxidant capacity by increasing total superoxide dismutase levels while simultaneously decreasing oxidative stress markers ROS, malondialdehyde, and lactate dehydrogenase in IMN cell models. Similarly, BAI exhibited anti-inflammatory and anti-oxidative effects in an in vitro IMN model and protected renal function in IMN mice with IMN. In addition, BAI downregulated AGE and RAGE in both IMN cell models and mice, and reduced CD68 levels in IMN mice. However, the activation of the AGE/RAGE pathway by AGE-BSA weakened the protective effects of BAI in these IMN models. Collectively, BAI mitigated inflammation and oxidative stress in IMN by repressing the AGE/RAGE pathway, suggesting its potential as a promising therapeutic agent for IMN.
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FEBS LETTERS
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2018
·Vol. 593
·期 2
·175-186
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IF 2.999
Shengnan Yang,Yuan Zhang,Fukui Shen,Xiaoyao Ma,Man Zhang,Yuanyuan Hou,Gang Bai
Baicalin is one of the main flavonoids of the dried root of Scutellaria baicalensis Georgi and is reported to exert beneficial effects on the regulation of glucose/lipid metabolism. However, understanding its specific target and unique mechanism for improving glucose utilization is a challenge. In this paper, target fishing with a baicalin probe reveals that baicalin interacts with AKT. An immunofluorescence assay further demonstrates the colocalization of baicalin with AKT in the cytoplasm. A competitive test and virtual docking show that baicalin might bind to the pleckstrin homology domain of AKT. This specific binding hampers AKT membrane translocation, activates the phosphorylation of AKT on Ser473, induces the downstream glycogen synthase kinase 3β activation, and affects glycogen synthesis.
研究领域:
药理学
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分子生物学
·
代谢
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
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2023
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IF 3.4
Jie Ma,Xiaoyu Li,Zongtong Yang,Qingming Liu,Yiming Liu,Anchang Liu
Baicalin has various neuroprotective effects in models of nervous system disease. Our study has shown baicalin could alleviate depressive-like behaviors in a neuroendocrine mouse model. But the systematic metabolic characteristic and particular targets of baicalin in regulating depressive behaviors have never been investigated. Therefore, this study aims to reveal the hippocampal metabolic profiling of chronic unpredictable mild stress (CUMS) induced depressive rats and the potential metabolic variations after baicalin treatment. We first used the sucrose preference test and open field test to access the antidepressant effects of baicalin. Then, metabolites of the hippocampus after baicalin therapy were monitored by widely-targeted metabolomics based on ultra-performance liquid chromatography-tandem mass spectrometry technology. Finally, the potential mechanism associated with neurogenesis obtained from metabolomics was verified by immunohistochemistry. The results showed that baicalin (40,80 mg/kg) could significantly alleviate depressive behaviors induced by CUMS as demonstrated by an increase in sucrose preference and movement distance and stand-up times in open field test. In the metabolomic analysis, a total of 733 metabolites were identified after baicalin treatment including 15 differential metabolites such as organic acid and its derivatives, heterocyclic compounds, fatty acid, bile acids, amino acid and its metabolites, and so on. Enrichment for differential metabolites showed that the differential metabolites might be involved in the process of folate and cofactor biosynthesis, cholesterol metabolism, primary bile acid biosynthesis, tyrosine metabolism and dopaminergic synapse. Moreover, immunohistochemical analysis confirmed baicalin could facilitate hippocampal neurogenesis of depressive rats in CUMS model. These results suggested baicalin might exert antidepressant effects through regulating the differential metabolites which might play a crucial role in inhibiting oxidative stress and improving neurogenesis. Our findings wish to discover the potential mechanism of baicalin on depression from the metabolomics perspective and promote its clinical application.
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JOURNAL OF PHARMACY AND PHARMACOLOGY
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2017
·Vol. 69
·期 6
·663-674
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IF 2.405
Li Jing,Jiang Qihua,Deng Ping,Chen Qian,Yu Mingan,Shang Jingchuan,Li Wei
ObjectivesBaicalin (BCL) has potential therapeutic benefits, but its clinical outcomes are restricted mainly because of low water solubility. This study sought to improve the water solubility of BCL by the formation of inclusion complex with β-cyclodextrin (β-CD).MethodsThe inclusion complex was studied by solubility test, differential scanning calorimeter (DSC), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), 1H Nuclear magnetic resonance (1HNMR) and scanning electron microscopy (SEM). Molecular docking was conducted to verify the experimental findings. The dissolution rate was determined by dialysis membrane method. In vivo absorption studies in rats were conducted and high-performance liquid chromatography (HPLC) was used to analyse the plasma level of BCL after oral administration.Key findingsThe DSC, FTIR, XRD, 1HNMR and SEM findings suggested the formation of inclusion complex between BCL and β-CD in 1 : 1 stoichiometry. Molecular docking demonstrated the insertion of benzene ring of BCL into β-CD cavity by hydrophobic interactions and possible H-bond formation. Moreover, β-CD markedly improved the solubility of BCL and displayed AL-type phase diagrams. The improvement in dissolution rate of the inclusion complex was reflected in the earlier Tmax, higher Cmax and larger AUC0–t than that of BCL after oral administration.Conclusionsβ-cyclodextrin complex can be used as an effective formulation strategy for development of BCL-loaded delivery system with better therapeutic outcomes.
研究领域:
药剂学
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药物化学
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TALANTA
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2017
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IF 4.162
Zhengkun Xie,Wang Lu,Lingxi Yang,Gaiping Li,Baoxian Ye
Baicalein and baicalin are the major flavonoids found in Scutellariae Radix, an essential herb which has had a presence in traditional Chinese medicine (TCMs) for more than two thousands of years. Owing to their similar characteristics and physiochemical properties, sensitive, it is a great challenge to detect both of them simultaneously. In this work, a novel, facile and sensitive electrochemical method was proposed based on tantalum oxide (Ta 2 O 5 ), niobium oxide (Nb 2 O 5 ) particles and antiseptic chitosan modified carbon paste electrode (Ta 2 O 5 -Nb 2 O 5 @CTS-CPE). Scanning electron microscope (SEM), X-ray diffraction spectroscopy (XRD), Fourier transform infrared spectroscopy (FTIR), cyclic voltammetry (CV) and electrochemical impedance spectrum (EIS) were used to characterize the properties and investigate the electrochemical response of the sensor. The electrochemical behaviors and redox mechanisms of two analytes were investigated at the target electrode. Under the optimum conditions, the highly sensitive and simultaneous determination of baicalein and baicalin was successfully achieved with a linear response range of 0.08–8.0 μM for both of them. The obtained detection limits for baicalein and baicalin were of 0.05 and 0.03 μM (S/N=3), respectively. Furthermore, the proposed sensor displayed high sensitivity, excellent stability and satisfactory results in Scutellariae Radix samples analysis and hydrolysis process analysis of baicalin in vivo .
研究领域:
分析化学
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电化学
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传统中药
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药物分析
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BIOELECTROCHEMISTRY
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2013
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IF 3.947
Ying Zhang,Xuejing Wang,Lei Wang,Miao Yu,Xiaojun Han
The baicalin and baicalein are the major flavonoids found in Radix Scutellariae , an essential herb in traditional Chinese medicine for thousands of years. The interactions of the baicalin and baicalein with lipid bilayer membranes were studied using cyclic voltammetry and UV–Vis spectroscopy. The thickness d of supported bilayer lipid membranes was calculated as d = 4.59(± 0.36) nm using AC impedance spectroscopy . The baicalein interacted with egg PC bilayer membranes in a dose-dependent manner. The responses of K 3 Fe(CN) 6 on lipid bilayer membrane modified Pt electrode linearly increased in a concentration range of baicalein from 6.25 μM to 25 μM with a detection limit of 0.1 μM and current-concentration sensitivity of 0.11(± 0.01) μA/μM, and then reached a plateau from 25 μM to 50 μM. However the baicalin showed much weaker interactions with egg PC bilayer membranes. UV–Vis spectroscopy also confirmed that the baicalein could interact with egg PC membranes noticeably, but the interaction of baicalin with membranes was hard to be detected. The results provide useful information on understanding the mechanism of action of Radix Scutellariae in vivo.
研究领域:
药理学
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生物化学
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FISH & SHELLFISH IMMUNOLOGY
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2023
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IF 4.7
Xiaojing Li,Yichen Bai,Yanju Bi,Qian Wu,Shiwen Xu
Chlorpyrifos (CPF) has caused large-scale pollution worldwide and posed a threat to non-target organisms. Baicalein (BAI) is a flavonoid extract with anti-oxidant and anti-inflammatory activities. The gills are the mucosal immune organ and the first physical barrier of fish. However, it is not clear whether BAI counteracts organophosphorus pesticide CPF exposure-caused gill damage. Therefore, we established the CPF exposure and BAI intervention models by adding 23.2 μg/L CPF in water and/or 0.15 g/kg BAI in feed for 30 days. The results showed that CPF exposure could cause gill histopathology lesions. Moreover, CPF exposure led to endoplasmic reticulum (ER) stress, caused oxidative stress and Nrf2 pathway activation, and triggered NF-κB-mediated inflammation reaction and necroptosis in carp gills. BAI adding effectively relieved the pathological changes, and lighten inflammation and necroptosis involving in the elF2α/ATF4 and ATF6 pathways through binding to GRP78 protein. Moreover, BAI could ease oxidative stress, but did not affect Nrf2 pathway in carp gills under CPF exposure. These results suggested that BAI feeding could alleviate necroptosis and inflammation against chlorpyrifos toxicity through elF2α/ATF4 and ATF6 axis. The results partially explained the poisoning effect of CPF, and showed BAI could be act as an antidote for organophosphorus pesticides.
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INTERNATIONAL JOURNAL OF IMMUNOPATHOLOGY AND PHARMACOLOGY
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2022
·
IF 3.298
Qianqian He,Xiaoqi Sun,Muqing Zhang,Li Chu,Yang Zhao,Yongchao Wu,Jianping Zhang,Xue Han,Shengjiang Guan,Chao Ding
Baicalin (BA) is a kind of flavonoid that is isolated from Scutellaria baicalensis Georgi, which has been verified to have hepatoprotective effects in some diseases. However, the role of BA in acute hepatic injury induced by arsenic trioxide (ATO) remains unclear. The aim of this study was to investigate the protective action of BA on acute hepatic injury induced by ATO and to probe its possible mechanism. Mice were pretreated with BA (50, 100 mg/kg) by gavage. After 7 h, ATO (7.5 mg/kg) was injected intraperitoneally to induce liver injury. After 7 days of treatment, serum and hepatic specimens were collected and assayed to evaluate the hepatoprotective effect of BA. Pathological sections and the liver function index indicated that ATO caused significant liver injury. The fluorescence of reactive oxygen species and oxidative stress indicators showed that ATO also increased oxidative stress. The inflammatory markers in ATO-induced mice also increased significantly. Staining of the terminal deoxynucleotidyl transferase dUTP nick end labeling and apoptotic factor assay showed that apoptosis increased. However, with BA pretreatment, these changes were significantly weakened. In addition, BA treatment promoted the expression of proteins related to the JAK2/STAT3 signaling pathway. The results suggest that BA can ameliorate acute ATO-induced hepatic injury in mice, which is related to the inhibition of oxidative stress, thereby reducing inflammation and apoptosis. The mechanism of this protection is potentially related to the JAK2/STAT3 signaling pathway.
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SENSORS AND ACTUATORS B-CHEMICAL
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2021
·
IF 7.46
Pengcheng Zhao,Linzi Huang,Hui Wang,Chenxi Wang,Jia Chen,Pingping Yang,Meijun Ni,Chao Chen,Chunyan Li,Yixi Xie,Junjie Fei
Baicalin (Bn) obtained from natural plants has been found to exhibit significant antiviral activity against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). Herein, a novel ultrasensitive Bn electrochemical sensor was proposed based on graphitized carbon-nitride - single-walled carbon nanotube nanocomposites (C 3 N 4 -SWCNTs), reduced graphene oxide (rGO) and electrodeposited cyclodextrin-metal organic framework (CD-MOF). The sensing nanomaterials were characterized by X-ray diffraction spectroscopy, X-ray photoelectron spectroscopy, Raman spectroscopy, scanning electron microscopy, and transmission electron microscopy. Under optimal conditions, the sensor exhibited sensitive detection of Bn in a wide linear range of 1 × 10 -9 –5 × 10 -7 M with an LOD of 4.6 × 10 -10 M and a sensitivity of 220 A/M, and it showed satisfactory stability and accuracy for detecting Bn in real samples (human serum and bear bile scutellaria eye drops). In addition, the electrochemical reaction sites and redox mechanism of Bn were revealed through electrochemical behavior and density functional theory. This work provided an insightful solution for detecting Bn, and extensive potential applications could be further expected.
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Neural Regeneration Research
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2021
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IF 5.135
Rui Zhao,Xue Wu,Xue-Yuan Bi,Hao Yang,Qian Zhang
Baicalin is a natural active ingredient isolated from Scutellariae Radix that can cross the blood-brain barrier and exhibits neuroprotective effects on multiple central nervous system diseases. However, the mechanism behind the neuroprotective effects remains unclear. In this study, rat models of spinal cord injury were established using a modified Allen's impact method and then treated with intraperitoneal injection of Baicalin. The results revealed that Baicalin greatly increased the Basso, Beattie, Bresnahan Locomotor Rating Scale score, reduced blood-spinal cord barrier permeability, decreased the expression of Bax, Caspase-3, and nuclear factor κB, increased the expression of Bcl-2, and reduced neuronal apoptosis and pathological spinal cord injury. SH-SY5Y cell models of excitotoxicity were established by application of 10 mM glutamate for 12 hours and then treated with 40 μM Baicalin for 48 hours to investigate the mechanism of action of Baicalin. The results showed that Baicalin reversed tight junction protein expression tendencies (occludin and ZO-1) and apoptosis-related protein expression (Bax, Bcl-2, Caspase-3, and nuclear factor-κB), and also led to up-regulation of PI3K and Akt phosphorylation. These effects on Bax, Bcl-2, and Caspase-3 were blocked by pretreatment with the PI3K inhibitor LY294002. These findings suggest that Baicalin can inhibit blood-spinal cord barrier permeability after spinal cord injury and reduce neuronal apoptosis, possibly by activating the PI3K/Akt signaling pathway. This study was approved by Animal Ethics Committee of Xi’an Jiaotong University on March 6, 2014.
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Journal of Materials Chemistry B
·
2025
·
IF 5.7
Shiyi Song,Zhiwei Ye,Dadong Jia,Mingshuang Li,Changying Yang,Mian Qin,Kaili Wu,Jiabing Ran,Liang Liang
Simultaneously restricting bacterial proliferation while mitigating inflammatory reactions and excessive reactive oxygen species (ROS)-mediated corneal damage during sleep represents a crucial therapeutic strategy for managing bacterial keratitis (BK). In this study, we developed micron-scale PCBT hydrogel beads for nocturnal BK treatment by integrating two classical ophthalmic drugs: tobramycin (TOB) as the antibacterial component and baicalin (BA) as the anti-inflammatory/antioxidant agent. The formation of hydrogel beads was facilitated by the synergistic interplay between: (i) TOB solution-induced crystallization of chitosan (CS) chains and (ii) benzene-1,4-diboronic acid (1,4-BDBA) mediated ester crosslinking of polyvinyl alcohol (PVA) chains. TOB and BA were encapsulated within the hydrogel beads, with BA molecules grafted onto PVA chains via reversible phenylboronic acid ester bonds. When applied to the inferior palpebra, mechanical friction easily transformed the beads into a smooth/soft paste that sustainedly released therapeutic concentrations of TOB and BA for over 24 hours in simulated BK microenvironments. Inhibition zone assays, macrophage (Mφ) polarization analysis, and ROS scavenging tests collectively demonstrated the simultaneous antibacterial, anti-inflammatory and anti-oxidative properties of the hydrogel beads. A Staphylococcus aureus (S. aureus) infected cornea model in rabbits was employed to assess the clinical therapeutic potential of the hydrogel beads against BK during the sleep phase. The results of visual scoring, H&E staining, Masson staining, etc. indicated that the PCBT hydrogel beads exhibited superior therapeutic efficacy compared to conventional commercial eye drops, highlighting their promising application for BK treatment during nocturnal periods.
研究领域:
眼科学
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药物递送系统
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生物材料
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纳米医学
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感染性疾病
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2026
·
IF 5.2
Yuling Wang,Jingru Li,Epiphane K. Silli,Fan Tang,Shujing Ren,Wei Liu,Huixia Lv
Atopic dermatitis (AD) is a chronic inflammatory skin disorder characterized by immune dysregulation, oxidative stress, and epidermal barrier dysfunction. Current therapies often provide incomplete long-term control and may cause adverse effects. Baicalin (BAI), a natural flavonoid with potent anti-inflammatory and antioxidant activities, is a promising candidate for AD treatment; however, its topical application is limited by poor solubility, weak skin penetration, and insufficient retention. To address these challenges, we developed a hyaluronic acid-baicalin conjugate (HA-BAI) that combines enhanced aqueous dispersibility with CD44-associated targeting and intrinsic barrier-supportive properties. HA-BAI exhibited excellent aqueous dispersibility (>220 mg/mL) across different formulation media, whereas free BAI remained poorly soluble (∼0.05 mg/mL). In vitro , HA-BAI exhibited excellent cytocompatibility, suppressed nitric oxide and pro-inflammatory cytokines, enhanced IL-10 expression, and promoted barrier-related proteins in keratinocytes. Ex vivo permeation studies demonstrated enhanced skin accumulation and prolonged retention, with 3.28-fold greater skin-associated fluorescence than the free fluorescent probe at 12 h. In a DNFB-induced AD mouse model, HA-BAI markedly alleviated dermatitis severity, reduced splenomegaly, improved histopathological features, and restored epidermal barrier homeostasis, showing superior therapeutic performance compared with the dose-normalized HA and BAI physical mixture. Collectively, HA-BAI represents a bioactive macromolecular platform that integrates targeted delivery with intrinsic therapeutic functionality for localized treatment of AD. Download: Download high-res image (409KB) Download: Download full-size image
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