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Baicalin
SENSORS AND ACTUATORS B-CHEMICAL · 2021 · IF 7.46

An ultrasensitive high-performance baicalin sensor based on C3N4-SWCNTs/reduced graphene oxide/cyclodextrin metal-organic framework nanocomposite

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 · 2021 · IF 5.135

Baicalin attenuates blood-spinal cord barrier disruption and apoptosis through PI3K/Akt signaling pathway after spinal cord injury

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.

CAS / MDL: 97232-16-1
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FEBS LETTERS · 2018 ·Vol. 593 ·期 2 ·175-186 · IF 2.999

The flavonoid baicalin improves glucose metabolism by targeting the PH domain of AKT and activating AKT/GSK3β phosphorylation

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.

CAS / MDL: 2183473-25-6
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BIOELECTROCHEMISTRY · 2013 · IF 3.947

Interactions of the baicalin and baicalein with bilayer lipid membranes investigated by cyclic voltammetry and UV–Vis spectroscopy

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.

CAS / MDL: 491-67-8 21967-41-9
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TALANTA · 2017 · IF 4.162

A voltammetry sensor platform for baicalein and baicalin simultaneous detection in vivo based on Ta2O5-Nb2O5@CTS composite

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 .

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JOURNAL OF PHARMACY AND PHARMACOLOGY · 2017 ·Vol. 69 ·期 6 ·663-674 · IF 2.405

The formation of a host-guest inclusion complex system between β-cyclodextrin and baicalin and its dissolution characteristics

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.

CAS / MDL: 21967-41-9 151-21-3
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Heliyon · 2024 · IF 3.4

Baicalin reduced injury of and autophagy-related gene expression in RAW264.7 cells infected with H6N6 avian influenza virus

Xin Yang,Junxian Li,Chunlan Shan,Xuqin Song,Jian Yang,Hao Xu,Deyuan Ou

In the present study, we investigated whether baicalin could reduce the damage caused to RAW264.7 cells following infection with H6N6 avian influenza virus. In addition, we studied the expression of autophagy-related genes. The morphological changes in cells were observed by hematoxylin and eosin (H&E) staining, and the inflammatory factors in the cell supernatant were detected by enzyme-linked immunosorbent assay (ELISA). Transmission electron microscopy (TEM) was used to detect the levels of RAW264.7 autophagosomes, and western blotting and immunofluorescence were used to detect the protein expression of autophagy marker LC3. Quantitative reverse transcriptase-polymerase chain reaction (qRT-PCR) was used to detect the mRNA transcription levels of autophagy key factors. The results showed that different doses of baicalin significantly reduced the H6N6 virus-induced damage of RAW264.7 cells. The contents of interleukin (IL)-1β, IL-2, IL-6, and tumor necrosis factor (TNF)-α in the cell supernatant significantly decreased. In addition, the protein expression of LC3 and Beclin-1, ATG12, ATG5 the mRNA levels were significantly decreased. This study showed that baicalin can reduce cell damage and affect the H6N6-induced autophagy level of RAW264.7 cells.

CAS / MDL: 21967-41-9
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JOURNAL OF NANOBIOTECHNOLOGY · 2024 ·Vol. 22 ·期 1 ·1-19 · IF 10.6

Baicalin nanodelivery system based on functionalized metal-organic framework for targeted therapy of osteoarthritis by modulating macrophage polarization

Huang Lanli,Yao Yi,Ruan Zhuren,Zhang Shengqing,Feng Xianjing,Lu Chun,Zhao Jinmin,Yin Feiying,Cao Cunwei,Zheng Li

Intra-articular drugs used to treat osteoarthritis (OA) often suffer from poor pharmacokinetics and stability. Nano-platforms as drug delivery systems for drug delivery are promising for OA therapy. In this study, we reported an M1 macrophage-targeted delivery system Bai@FA-UIO-66-NH2 based on folic acid (FA) -modified metal-organic framework (MOF) loaded with baicalin (Bai) as antioxidant agent for OA therapy. With outstanding biocompatibility and high drug loading efficiency, Bai@FA-UIO-66-NH2 could be specifically uptaken by LPS-induced macrophages to serve as a potent ROS scavenger, gradually releasing Bai at the subcellular level to reduce ROS production, modulate macrophage polarization to M2, leading to alleviation of synovial inflammation in OA joints. The synergistic effect of Bai@FA-UIO-66-NH2 on macrophage polarization and ROS scavenging significantly improved the therapeutic efficacy of OA, which may provide a new insight into the design of OA precision therapy.

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APPLIED SURFACE SCIENCE · 2025 · IF 6.9

Synergistic depression of copper-activated pyrite by Fe2+/baicalin system: a novel strategy for selective Zn-S flotation

Cuihuan Lv,Jinpeng Cai,Guohui Wang,Jiuxiu Chen,Hao Lai,Peilun Shen,Dianwen Liu

Organic depressants often exhibit low selectivity at high dosages, and introduce risks of concentrate dewatering. The combined depressants composed of inorganic and organic substances can significantly reduce reliance on organic depressant dosage, providing a promising solution to this challenge. In order to achieve highly efficient separation of sphalerite and pyrite in the CuSO 4 -butyl xanthate (PBX) flotation system, the combined depressant Fe 2+ / baicalin (BCL) was innovatively employed to inhibit copper-activated pyrite. The flotation tests indicate that compared with the single depressant BCL, the combined depressant Fe 2+ /BCL demonstrates superior selective inhibitory effects on copper-activated pyrite. For artificially mixed ores, a zinc concentrate is obtained with a zinc grade of 62.33 % and a zinc recovery of 93.86 % when the combined depressant of 10 mg/L Fe 2+ and 5 mg/L BCL are used, and the separation efficiency is significantly improved from 40.66 to 79.69 %. Adsorption characteristic studies indicated that BCL exhibits stronger affinity for copper-activated pyrite than for sphalerite. The introduced Fe 2+ provide additional active sites, thereby enhancing the depression effect on copper-activated pyrite. Following Fe 2+ /BCL modification, the adsorption of PBX on copper-activated pyrite was hindered, while having no substantial impact of that on sphalerite, which is also confirmed by molecular dynamics simulations. Therefore, the combined depressant Fe 2+ /BCL markedly widened the hydrophobicity difference between sphalerite and pyrite, creating the potential for their effective separation.

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APPLIED SURFACE SCIENCE · 2025 · IF 6.9

Effective flotation separation of dolomite and apatite utilizing baicalin as a green depressant: a mechanistic and experimental study

Pan Yu,Lingpan Du,Menglai Wang,Fengting Zhao,Runzhe Liu,Xiang Gong,Hongyu Lu,Fuhua Luo,Qi Zuo,Shuming Wen,Shaojun Bai

To address the challenge of separating dolomite from apatite via flotation, this research firstly employed Baicalin (BA) as an environment-friendly depressant and examined the underlying depression mechanism on apatite and dolomite in a sodium oleate (NaOL) collector system. Micro-flotation findings demonstrated effective separation of apatite and dolomite under conditions of 50 mg/L BA and 120 mg/L NaOL at pH 11.0. Zeta potential, adsorption capacity, FT-IR, and SEM-EDS analyses indicated that the dolomite surface exhibited a greater affinity for BA adsorption. Contact angle measurements showed that BA prominently reduced the surface hydrophobicity of dolomite while having a minimal impact on apatite’s surface hydrophobicity. XPS analysis confirmed that BA adsorption on the dolomite surface mainly involved chemisorption between –COO − groups and Ca and Mg sites, whereas a weaker physical adsorption occurred on the apatite surface. Molecular dynamics simulations (MDS) analysis showed that BA exhibited a greater affinity on the dolomite surface relative to apatite, thereby rendering the dolomite surface more hydrophilic than apatite. This study presents a novel methodology for the efficient and sustainable removal of dolomite from apatite, thereby advancing the theoretical understanding of flotation separation in apatite-dolomite systems.

CAS / MDL: 21967-41-9
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JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY · 2026 · IF 5.2

Hyaluronic acid-baicalin conjugate for CD44-Targeted topical therapy of atopic dermatitis with enhanced skin retention and barrier restoration

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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Coatings · 2026 ·Vol. 16 ·期 8 ·967 · IF 3.4

Baicalin-Ternary LDH-Modified Magnesium Alloy with Anti-Corrosion and pH-Responsive Controlled Release, Near-Infrared-Enhanced Catalytic Property

Yuhan Liang,Lijie Chen,Mingyue Feng,Tong Zhang,Rongbang Sun,Yang Liu,Yifu Fu,Yunxiang Chen,Lan Chen

HighlightsWhat are the main findings?The Mg-Mn-Fe LDH grown in situ on the PEO coating-modified Mg alloy effectively blocks pores and introduces metal catalytic active sites.Baicalin achieves stable immobilization by forming coordination bonds with the metal ions in LDH through the oxygen-containing functional groups.The LDH/BA composite coating significantly improved corrosion resistance, along with pH-responsive drug release and near-infrared-enhanced enzyme-like catalytic performance.What are the implications of the main findings?A multi-functional modification strategy integrating “corrosion resistance, drug loading and control release” was established, which provides a novel technical solution for the long-term corrosion protection of magnesium alloys.The revealed interfacial coordination immobilization mechanism can provide theoretical references for the structural design of organic–inorganic composite protective coatings.The synergy of corrosion resistance and microenvironment stimulus-responsive functions is realized, which expands the application of LDH coatings in the modification of metal implants.Aiming at the rapid corrosion of degradable magnesium alloys in physiological environments and the insufficient long-term protection of single plasma electrolytic oxidation (PEO) coatings, Mg-Mn-Fe layered double hydroxide (LDH) and baicalin (BA)-loaded LDH/BA composite coatings were prepared in situ on PEO-pretreated ZE21C magnesium alloy substrates. BA was stably anchored on the LDH surface via coordination bonds between its oxygen-containing functional groups and laminate metal sites. Benefiting from the physical barrier of the LDH lamellar structure and the corrosion inhibition effect of baicalin, the LDH/BA coating significantly improved the corrosion resistance of the magnesium alloy matrix. The composite coating exhibited peroxidase-like catalytic activity for reactive oxygen species generation, which could be enhanced by near-infrared irradiation. It also possessed stable photothermal conversion performance and pH-responsive drug release behavior under acidic conditions. Biological characterization demonstrated that BA-loaded LDH composite coatings exert potent inhibitory effects on 143B cell proliferation. This work integrates long-term corrosion resistance, controlled drug release, and photoresponsive catalytic functions onto magnesium alloy surfaces, providing an effective strategy for developing high-performance biodegradable magnesium alloys.

CAS / MDL: 21967-41-9 54827-17-7
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