MOLECULES
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2021
·Vol. 26
·期 8
·2322
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IF 4.412
Yunchang Fan,Di Wu,Sheli Zhang
Baicalin which has multiple biological activities is the main active component of the root ofScutellaria baicalensisGeorgi (SBG). Although its isolation and purification by adsorption methods have aroused much interest of the scientific community, it suffered from the poor selectivity of the adsorbents. In this work, an environmentally benign method was developed to prepare ionic liquids (ILs) grafted silica by using IL 1-butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide ([C4mim]NTf2) and ethanol as reaction media. The IL 1-propyl-3-methylimidazolium chloride ([C3mim]Cl) grafted silica ([C3mim]+Cl−@SiO2) was used to adsorb and purify baicalin from the root extract ofScutellaria baicalensisGeorgi (SBG). Experimental results indicated that the adsorption equilibrium can be quickly achieved (within 10 min). The adsorption behavior of [C3mim]+Cl−@SiO2for baicalin was in good agreement with Langmuir and Freundlich models and the adsorption was a physisorption process as suggested by Dubinin–Radushkevich model. Compared with commercial resins, [C3mim]+Cl−@SiO2showed the strongest adsorption ability and highest selectivity. After desorption and crystallization, a purity of baicalin as high as 96.5% could be obtained. These results indicated that the ILs grafted silica materials were promising adsorbents for the adsorption and purification of baicalin and showed huge potential in the purification of other bioactive compounds from natural sources.Keywords:ionic liquids (ILs);grafted silica;adsorption;baicalin;purification
研究领域:
天然产物化学
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植物化学
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产品关联
DOI
PubMed
高影响因子
Materials Today Physics
·
2021
·
IF 9.298
Xiaodan Tang,Huiyong Wang,Hongmei Yu,Brian Bui,Wei Zhang,Shaoyan Wang,Mingli Chen,Liqin Yuan,Zhizhi Hu,Wei Chen
Baicalin, a flavonoid compound extracted from the rhizome of Scutellar iae Baicalensis, plays a vital role in improving liver function after injury, reducing liver disease and treating primary liver cancer, which is also the first SARS-CoV-2 3CLpro virus inhibitor according to the latest research data published in BioRxiv. Therefore, constructing a simple and highly sensitive analytical method for the determination of baicalin is of great significance for the clinical and pharmacy settings. Herein, for the first time, carbon dots are explored for baicalin detection. Using biomass waste grape peels as the organic carbon source, nitrogen-doped fluorescent carbon dots (PT-NCDs) were fabricated, which were synthesized perfectly by a simple, environmentally friendly and one-step solid-phase thermal method without adding any other organic or acid/base reagents. Based on the synergistic effect of photo-induced electron transfer and dynamic quenching, a quenched fluorescence sensor for the determination of baicalin with a good linear range of 0.1–20 μM and a satisfactory detection limit of 43.8 nM was constructed, which successfully quantified trace amount of baicalin in baicalin capsules, human serum and urine samples. The results indicate that PT-CDs are expected to become potential sensing materials for the real-time monitoring of baicalin in organisms, which is very important for our health.
研究领域:
药理学
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分析化学
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材料科学
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产品关联
DOI
高影响因子
Viruses-Basel
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2015
·Vol. 7
·期 8
·4756-4771
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IF 3.353
Xiang Li,Yuanyuan Liu,Tingting Wu,Yue Jin,Jianpin Cheng,Changbiao Wan,Weihe Qian,Fei Xing,Weifeng Shi
Baicalin is a flavonoid compound extracted fromScutellariaroots that has been reported to possess antibacterial, anti-inflammatory, and antiviral activities. However, the antiviral effect of baicalin on enterovirus 71 (EV71) is still unknown. In this study, we found that baicalin showed inhibitory activity on EV71 infection and was independent of direct virucidal or prophylactic effect and inhibitory viral absorption. The expressions of EV71/3D mRNA and polymerase were significantly blocked by baicalin treatment at early stages of EV71 infection. In addition, baicalin could decrease the expressions of FasL and caspase-3, as well as inhibit the apoptosis of EV71-infected human embryonal rhabdomyosarcoma (RD) cells. Altogether, these results indicate that baicalin exhibits potent antiviral effect on EV71 infection, probably through inhibiting EV71/3D polymerase expression and Fas/FasL signaling pathways.Keywords:baicalin;enterovirus 71;3D polymerase;apoptosis
研究领域:
病毒学
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药理学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
Journal of Cosmetic Dermatology
·
2025
·Vol. 24
·期 2
·e70024
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IF 2.5
Liang Chen,Fudi Wang,Xiaoyun Hu,Nihong Li,Ying Gao,Fengfeng Xue,Ling Xie,Min Xie
Objective To develop a stable and efficient delivery system for baicalin, a flavonoid with potential antioxidant and antiaging properties, to overcome its limitations in solubility, stability, and skin permeability. Methods Baicalin was encapsulated using ATP synthase molecular motor technology into bio-vesicles derived from yeast/bacillus cell membranes, forming “motor baicalin” (MB). The liposome baicalin (LB), baicalin raw material (BRM), and bio-vesicles were used for comparison. The stability, transdermal penetration, and antioxidant activity of MB, LB, BRM, and bio-vesicles were evaluated through in vitro and in vivo tests. Results MB formed a stable core-shell structure, significantly enhancing the water solubility and long-term stability of baicalin. The tests confirmed superior transdermal penetration and antioxidant activity of MB, evidenced by increased expression of SOD, CAT, and GSH-Px enzymes and improved cell proliferation and migration. Clinical trials demonstrated significant reductions in wrinkle depth and improvements in skin elasticity. Conclusion This study presents a promising approach to improving the stability and transdermal delivery of baicalin. MB showcases potent antioxidant and antiaging properties, making it a valuable component in skincare products.
研究领域:
药剂学
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皮肤科学
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生物技术
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产品关联
DOI
PubMed
高影响因子
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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产品关联
DOI
PubMed
高影响因子
Frontiers in Pharmacology
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2025
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IF 4.8
Shuaifei Lu,Jiduo Shen,Xiaohui Jin,Changjing Zhang,Baoying Wang,Xianghua Liu,Ming Bai,Erping Xu,Xiangli Yan,Yucheng Li
Introduction: Dysfunction of axoplasmic transport is closely linked to depression. Baicalin, a major flavonoid in Scutellaria baicalensis, a well-known traditional Chinese medicine used in depression treatment, has demonstrated antidepressant-like effects in previous studies. However, its potential role in regulating axoplasmic transport has not been explored. This study aims to investigate the antidepressant mechanisms of baicalin through modulation of axoplasmic transport in hippocampal neurons.Methods: Male C57BL/6N mice were exposed to chronic unpredictable mild stress (CUMS) and treated with baicalin (10, 20, 40 mg/kg) or fluoxetine (20 mg/kg). Depression-like behaviors were assessed using the sucrose preference test (SPT), forced swimming test (FST), tail suspension test (TST), and locomotor activity test (LAT). Hippocampal neuronal pathology was examined using transmission electron microscopy (TEM), Nissl, and Golgi staining. Transcriptomic analysis was conducted to explore the molecular mechanisms of baicalin. HT22 cells were cultured in vitro and treated with corticosterone (CORT) and baicalin. FM1-43 was used to label vesicles and track vesicular movement. mRNA and protein levels were measured by qRT-PCR, Western blotting, and immunofluorescence.Results: Baicalin significantly alleviated CUMS-induced depressive behaviors, increasing sucrose preference, reducing immobility time in TST and FST, and increasing food intake without affecting locomotor activity. It improved hippocampal CA3 neuronal damage, increased dendritic spine density, and promoted presynaptic vesicle accumulation, particularly in glutamatergic neurons. Transcriptomic analysis revealed that baicalin upregulated vGLUT2 (encoded by the Slc17a6 gene) and significantly increased the expression of GluN2B, GluA1, and PSD95. Moreover, baicalin upregulated the expression of kinesin family member 5A (KIF5A) both in vivo and in vitro, enhancing vesicle movement along axons and increasing vesicle-associated membrane protein 2 (VAMP2) enrichment in synaptosomes.Discussion: These findings suggest that baicalin enhances anterograde axoplasmic transport by upregulating KIF5A expression, facilitating vesicular trafficking and improving synaptic function in glutamatergic neurons. This study provides novel insights into the molecular mechanisms of antidepressant effects of baicalin, highlighting KIF5A as a potential therapeutic target for depression.
研究领域:
神经科学
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药理学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
Bioactive Materials
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2022
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IF 16.874
Liping Ouyang,Baohui Chen,Xingdan Liu,Donghui Wang,Yang Li,Yun Liao,Kelvin W.K. Yeung,Xuanyong Liu
It is important to eliminate lipopolysaccharide (LPS) along with killing bacteria in periprosthetic joint infection (PJI) therapy for promoting bone repair due to its effect to regulate macrophages response. Although natural antimicrobial peptides (AMPs) offer a good solution, the unknown toxicity, high cost and exogenetic immune response hamper their applications in clinic. In this work, we fabricated a nanowire-like composite material, named [email protected] , by combining chitosan and puerarin via solid-phase reaction, which can finely mimic the bio-functions of AMPs. Chitosan, serving as the bacteria membrane puncture agent, and puerarin, serving as the LPS target agent, synergistically destroy the bacterial membrane structure and inhibit its recovery, thus endowing [email protected] with good antibacterial property. In addition, [email protected] possesses good osteoimmunomodulation due to its ability of LPS elimination and macrophage differentiation modulation. The in vivo results show that [email protected] can inhibit the LPS induced bone destruction in the Escherichia coli infected rat. [email protected] exhibits superior bone regeneration in Escherichia coli infected rat due to the comprehensive functions of its superior antibacterial property, and its ability of LPS elimination and immunomodulation. [email protected] can well mimic the functions of AMPs, which provides a novel and effective method for treating the PJI in clinic.
研究领域:
医学
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生物材料学
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DOI
PubMed
高影响因子
CHEMICAL ENGINEERING RESEARCH & DESIGN
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2025
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IF 3.9
Ze Yu Lian,Fu Zhen Gao,Run Xiang Qin,Jing Qiang Ma,Xue Zhong Wang
Baicalin as a flavonoid compound exhibits diverse and significant pharmacological activities. Nevertheless, its intrinsically poor aqueous solubility has been an obstacle to its clinical application. To overcome this limitation, this study devised an innovative crystallization strategy, thereby enabling the controllable synthesis of baicalin nanocrystals. Initially, the crystallization process of baicalin microcrystals in a stirred tank crystallizer was optimized, and the effects of parameters such as additive types, equivalents, stirring rates, and crystallization temperatures on the particle size and morphology of crystals were explored. Subsequently, technologies including X-ray diffraction (XRD), proton nuclear magnetic resonance spectroscopy (¹H NMR), online microscopy imaging, and pH monitoring were utilized to elucidate the crystallization mechanism of baicalin, thereby laying the theoretical foundation for the preparation of baicalin nanocrystals. Finally, this study innovatively introduced an impinging jet crystallizer, based on the foregoing research findings. In contrast to the traditional reactors, this device integrates the advantages of both impinging jet reactor and batch crystallizer, which can simultaneously strengthen the micro- and macro-mixing processes. This dual-scale modulation strategy achieves precise kinetic control by synchronizing nucleation enhancement with growth suppression and regulation. To identify the optimal process parameters of the impinging jet crystallizer, a computational fluid dynamics (CFD) simulation and experimental research were combined. Eventually, the baicalin nanocrystals featuring an average particle size of less than 300 nm and spherical morphology were successfully prepared.
研究领域:
药剂学
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制药工程
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材料科学
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产品关联
DOI
高影响因子
JOURNAL OF MOLECULAR LIQUIDS
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2024
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IF 5.3
Xiaoxiao Gu,Dongmei Li,Haoyang Yuan,Cailing Li,Dinghua Yu,Guowei Wang,Shuang Li
Baicalin is a flavonoid compound extracted from the Scutellaria baicalensis plant. It possesses strong free radical scavenging ability and has a wide range of medical applications in antibacterial, anti-inflammatory, and anti-tumor fields. However, its limited solubility in water restricts its application. In this study, we prepared SL-DMEA by the amidation of acidic sophorolipids and N, N-dimethylethanolamine, while SL-TMEAI was synthesized via the quaternization of SL-DMEA with iodomethane. The structures of SL-DMEA and SL-TMEAI were confirmed by 1 H NMR, FT-IR, and Mass spectra. Surface tension and micelle microenvironment indicated that SL-DMEA and SL-TMEAI exhibit superior surface activity. Furthermore, the solubility of baicalin in aqueous solutions containing SL-DMEA and SL-TMEAI was approximately 70 mg/L and 75 mg/L, while it was only 18 mg/L in SL-COOH solution, which were significantly higher than the solubility in pure water (4 mg/L). Similarly, SL-DMEA and SL-TMEAI can enhance the antioxidant activity of baicalin. Specifically, in the SL-TMEAI aqueous solution, the free radical scavenging rate of baicalin was increased by 10 %–20 %. Density functional theory calculations revealed that SL-DMEA and SL-TMEAI formed stable hydrogen bonds with baicalin molecules, which can increase the solubility of baicalin in water and expose the groups that react with free radicals in the solution, thereby enhancing the antioxidant activity. These results demonstrated that SL-DMEA and SL-TMEAI could significantly enhance the solubility and antioxidating of baicalin in water through a hydrotropy mechanism.
研究领域:
生物化学
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药物化学
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材料科学
✓ 已验证
产品关联
DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2025
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IF 8.5
Yurou Chen,Kun Sun,Yujie Lin,Jiaxuan Li,Ningzhe Wang,Qingfeng Ban,Xibo Wang
To improve the emulsion properties of soybean protein isolate (SPI), the effect of baicalin (BC) concentrations on the structure, antioxidant properties, and emulsion stability of SPI-BC conjugates were investigated. Structure analysis revealed that BC induced structural depolymerization and unfolding of SPI through the formation of covalent bonds (C N and C S), increasing hydrophilicity, stabilizing the interface, and enabling the formation of smaller oil droplets. The increase in zeta potential of SPI-BC conjugates enhanced electrostatic repulsion between droplets, preventing aggregation, while the strengthened interfacial protein network improved viscosity, shear stress, and thixotropic recovery, thereby significantly stabilizing the emulsion structure. The addition of 0.4 mg/mL BC exhibited the optimal emulsification performance, increasing emulsion stability by 35.4 %. Moreover, SPI-BC emulsions demonstrated enhanced stability against various environmental stressors (storage, heating, pH, ionic strength, and oxidation). These findings confirmed that BC covalent modification enhanced the structural properties of SPI and improved the stability of protein-based emulsions through structural regulation. This study provides new insights into the potential of BC in improving SPI functionality.
研究领域:
食品科学
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生物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
RSC Advances
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2017
·Vol. 7
·期 14
·8178-8185
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IF 3.108
Xueyang Fang,Xianlin Wu,Chang'e Li,Binwei Zhou,Xiaoyin Chen,Tianfeng Chen,Fang Yang
As a traditional Chinese medicine, baicalin exhibits high antitumor activity towards hepatitis B virus (HBV)-infected liver cancer, but low toxicity towards normal tissues. However, the properties of baicalin, including its low hydrophilicity and poor biocompatibility, have limited its clinical application. Herein, in this study, we have designed and synthesized multifunctional selenium nanoparticles (SeNPs) with baicalin (B) and folic acid (FA) surface-modifications for the targeted treatment of HBV infected liver cancer. B–SeNPs–FA showed appropriate particle size distribution, high stability, and higher cellular uptake by tumor cells than normal cells. The nanoparticles primarily targeted lysosomes in HepG2215 cells through utilization of the main pathways of caveolae-mediated endocytosis and energy-dependent endocytosis. B–SeNPs–FA induced HepG2215 cell apoptosis by down-regulating the generation of reactive oxygen species (ROS) and the expression of the HBxAg protein. In addition, B–SeNPs–FA exhibited an excellent ability to inhibit cancer cell migration and invasion. Taken together, these results suggest that baicalin-loaded selenium nanoparticles with a folic acid targeting moiety could be a promising strategy for the design and synthesis of cancer-targeted nanomaterials to treat HBV-infected liver cancer.
研究领域:
药理学
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肿瘤学
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纳米医学
✓ 已验证
产品关联
DOI
高影响因子
FOOD CHEMISTRY
·
2024
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IF 8.5
Lingyu Han,Fang Ma,Ping He,Qun Zhou,Zhanping Li,Suqin Sun
The characterization of structure of organic salts in complex mixtures has been a difficult problem in analytical chemistry. In the analysis of Scutellariae Radix (SR), the pharmacopoeia of many countries stipulates that the quality control component is baicalin (≥9% by high performance liquid chromatography (HPLC)). The component with highest response in SR was also baicalin detected by liquid chromatography-mass spectrometry (LC-MS). However, in the attenuated total reflection Fourier transform infrared spectroscopy, the carbonyl peak of glucuronic acid of baicalin did not appear in SR. The results of element analysis, time of flight secondary ion mass spectrometry, matrix assisted laser desorption ionization mass spectrometry and solid-state nuclear magnetic resonance all supported the existence of baicalin magnesium salt. Based on this, this study proposes an analysis strategy guided by infrared spectroscopy and combined with multi-spectroscopy techniques to analyze the structure of organic salt components in medicinal plant. It is meaningful for the research of mechanisms, development of new drugs, and quality control.
研究领域:
药学
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分析化学
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植物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）