International Journal of Nanomedicine
·
2024
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IF 6.6
Dong Zhang,Mogen Zhang,Huiping Fan,Rui Sun,Jiayun Liu,Weiyuan Ma
Background Melanoma is an aggressive skin tumor with limited therapeutic options due to rapid proliferation, early metastasis, and poor prognosis. Baicalin (BA), a natural flavonoid, shows promise in inducing ferroptosis and apoptosis but faces challenges of poor solubility and bioavailability. To address these issues, we developed a multifunctional drug delivery system: manganese-doped ZIF-8 nanoparticles (ZIF(Mn)) loaded with BA and modified with folic acid (FA) and polyethylene glycol (PEG). FA targets melanoma cells by exploiting folate receptor overexpression, while PEG enhances biocompatibility and systemic circulation. Manganese enables magnetic resonance (MR) imaging for real-time, non-invasive therapy monitoring.Methods BA-loaded ZIF(Mn)/FA-PEG nanoparticles were synthesized via a one-pot method, enabling drug encapsulation, Mn²+ incorporation, and surface modification. The nanoparticles were comprehensively characterized (particle size, Zeta potential, FTIR, and XRD). Cytotoxicity and cellular uptake were evaluated in B16-F10 melanoma cells, and in vivo experiments in C57BL/6J mice investigated MR imaging capability, antitumor efficacy, and biosafety.Results BA@ZIF(Mn)/FA-PEG nanoparticles demonstrated excellent stability, a BA loading capacity of 33.50 ± 0.04%, and pH-responsive release, with accelerated drug release under acidic tumor conditions. Mn²+ provided strong T1-weighted MR imaging contrast. Cellular and animal studies showed enhanced uptake, reduced premature drug release, and improved compatibility. Mechanistically, the nanoparticles induced significant ferroptosis and apoptosis in melanoma cells, leading to potent antitumor effects.Conclusion The BA@ZIF(Mn)/FA-PEG nanoplatform effectively integrates targeted delivery, imaging guidance, and dual ferroptosis-apoptosis induction, offering a promising strategy for improving melanoma treatment outcomes.
研究领域:
药剂学
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肿瘤学
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医学影像学
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DOI
PubMed
高影响因子
ELECTROCHIMICA ACTA
·
2026
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IF 5.8
Yuchuan Zhu,Xinyu Huang,Ruoxi Yang,Ruoyao Tong,Changqing Lu,Ruirui Yue
One-pot synthesis of rGO/PEDOT:PSS/Ru composite for targeted flavonoid sensing. • PEDOT:PSS prevents rGO restacking and enables uniform Ru nanoparticle dispersion. • Interfacial coupling downshifts Ru d-band center to accelerate oxidation kinetics. • Ternary architecture greatly minimizes charge-transfer resistance at the interface. Flavonoid quantification is essential for pharmaceutical and food quality control, yet direct electrochemical detection is hindered by sluggish heterogeneous electron-transfer kinetics and limited current responses at trace concentrations on unmodified electrodes. We report an electrochemical sensing platform based on an rGO/PEDOT:PSS/Ru nanocomposite. Structural characterization indicates that π-π stacking between rGO and PEDOT:PSS prevents graphene restacking, enabling uniform Ru nanoparticle distribution. Crucially, interfacial electronic coupling within the ternary network downshifts the d-band center of the Ru nanoparticles, thereby accelerating the electro-oxidation kinetics. Electrochemical kinetic analyses reveal that the analytes undergo an adsorption-controlled, two-electron and two-proton (2e - /2H + ) transfer pathway. This architecture significantly minimizes charge-transfer resistance and expands the electroactive surface area. Differential pulse voltammetry delivered linear ranges of 0.006–65.0 μM (rutin), 0.05–70.0 μM (quercetin), and 0.02–50.0 μM (baicalin), with detection limits of 3.7, 17.3, and 6.3 nM, respectively. The sensor maintained consistent responses over 15 days and exhibited reliable selectivity against common interferents. Recovery studies in Sophora japonica, onion, and Scutellaria baicalensis extracts correlated with UV–Vis reference data, illustrating how coupling conducting polymers with redox-active nanoparticles can modulate interfacial electron-transfer pathways for targeted electrochemical sensing. Download: Download high-res image (354KB) Download: Download full-size image
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高影响因子
Frontiers in Pharmacology
·
2025
·
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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DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2025
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IF 5.4
Zhen-yan Song,Wen-jing Yu,Yi-jie Jin,Meng-fen Zhou,Chun-xiang He,Ze Li,Jia-wei He,Qi Chen,Ping Li,Yaqiao Yi,Shao-wu Cheng
Ethnopharmacological relevance Derived from the plant Scutellaria baicalensis Georgi, baicalin is a naturally occurring flavonoid, has demonstrated anti-inflammatory, neuroprotective, hypoglycemic, and lipid-lowering properties. While its effects on Alzheimer's disease (AD) or type 2 diabetes mellitus (T2DM) have been studied individually, its therapeutic role in AD comorbid with T2DM remains unclear. Aim of the study This study aims to explore the potential therapeutic mechanisms associated with baicalin through a rat model featuring AD combined with T2DM. Materials and methods A dual-pathology rat model was developed using a streptozotocin (STZ) and a high-fat dietary regimen injections to induce T2DM, followed by intracerebroventricular STZ to induce AD pathology. Behavioral tests, biochemical assays, histological analyses, qPCR, and Western blotting were used to evaluate baicalin's effects. Untargeted metabolomics was applied to profile metabolic alterations, while network pharmacology and molecular docking were integrated to predict key targets and pathways. Finally, cellular thermal shift assay (CETSA) was conducted to validate the direct binding of baicalin to core proteins. Results Baicalin significantly improved cognitive performance, ameliorated glucose and lipid metabolism, and suppressed neuroinflammation in AD-T2DM rats. Metabolomics identified disruptions in energy metabolism, amino acid metabolism, and purine metabolism pathways. Network pharmacology analysis revealed ALDH2, NOS2, GOT1, GPT, and XDH as key targets associated with these metabolic disturbances. Molecular docking demonstrated strong binding affinities between baicalin and the identified targets. qPCR confirmed the regulation of ALDH2 and NOS2 gene expression by baicalin, and CETSA experiments further validated the thermal stabilization of these proteins, supporting direct interactions in vivo. Conclusions Baicalin exerts therapeutic effects by targeting ALDH2 and NOS2 to modulate arginine and proline metabolism and regulate key metabolites such as GABA and L-arginine. This mechanism improves neuronal function and insulin sensitivity, highlighting baicalin as a promising multi-target treatment for AD with T2DM.
研究领域:
药理学
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神经科学
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内分泌学
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代谢组学
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民族药理学
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分子生物学
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DOI
PubMed
高影响因子
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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2025
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IF 5.4
Fu-Qiang Shi,Yuan Zhu,Bo-Wen Li,Zi-Yi Guo,Hang Li,Xiao-Li Sun,Qing-Sheng Zhao
To enhance the extraction efficiency of baicalin (BA) from Scutellariae Radix （SR） and improve the solubility, bioactivity and stability of Scutellaria Extract (SE), a glycyrrhizic acid (GA)-assisted green extraction process for BA was developed and optimized. The results demonstrated that GA-assisted extraction significantly elevated BA yield, achieving 1.7-fold higher extraction rates and 2.1-fold higher BA content in the extracts compared to the conventional 70 % ethanol extraction method. Characterization studies confirmed the formation of an inclusion complex (SE-GA) between GA and BA, which markedly improved SE solubility and bioavailability. Notably, SE-GA exhibited reduced cytotoxicity and enhanced antibacterial and antioxidant activities relative to unmodified SE. Stability assessments further revealed superior preservation of bioactive compounds in SE-GA. Mechanistic analysis suggested that SE penetrates the GA cavity, thereby protecting its bioactive components.
研究领域:
药学
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天然产物化学
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绿色化学
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药理学
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分析化学
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DOI
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2025
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IF 8.5
Fansu Meng,Panpan Wang,Lina Yang,Junjie Yan,Anil K. Giri,Jaiwoo Lee,Kosuke Kusamori,Makiya Nishikawa,Shoko Itakura,Honghui Gu,Qi Li,Zhong Chen,Zhenjiang Yang,Detang Li,Yu Cai
Breast cancer (BC) stands as one of the primary malignancies threatening women's health. Baicalin (BA) exhibits anti - BC effects, yet it is plagued by issues such as low water solubility and poor bioavailability. To enhance the anti-BC efficacy of BA, this study developed a pH - responsive albumin nanoparticle loaded with BA (BA-AN-FA@mPEG). The optimized BA-AN-FA@mPEG features an average particle size of (185.8 ± 2.36) nm, a Zeta potential of (−32.70 ± 1.27) mV, an encapsulation efficiency of approximately 73.82 %, and a drug loading of about 5.68 %. The aqueous solution of BA-AN-FA@mPEG demonstrates excellent stability at 4 °C, with no significant drug leakage occurring within 12 weeks. BA-AN-FA@mPEG shows a certain sustained - release effect, and the drug release rate is faster under acidic conditions. The results of efficacy evaluation indicate that the half - maximal inhibitory concentration of BA-AN-FA@mPEG against MDA-MB-231 cells is 26.34 μg/mL. It can promote cellular uptake, effectively induce apoptosis, and cause cell cycle arrest. In summary, BA-AN-FA@mPEG is a promising tumor - targeted therapeutic formulation that can improve drug stability, tumor delivery efficiency, and therapeutic efficacy.
研究领域:
药剂学
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纳米技术
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肿瘤学
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药物递送
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生物医学工程
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产品关联
DOI
PubMed
高影响因子
Pharmaceuticals
·
2025
·Vol. 18
·期 10
·1458
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IF 4.8
Xin Meng,Zhiyun Yu,Chao Ning,Mingtong Sun,Mengna Kang,Haiyong Guo
Background:The treatment of methicillin-resistantStaphylococcus aureus(MRSA) infections is extremely challenging due to its antibiotic resistance, and the combination of plant active ingredients with antibiotics represents a potential strategy to address this issue.Methods:We determined the combinatorial relationship between baicalin (BA) and kanamycin (KM) using the checkerboard dilution method. The antibacterial activity of the baicalin–kanamycin (BA/KM) combination was evaluated through growth curve determination assays and scanning electron microscopy (SEM). The effects of the BA/KM combination on the cell membrane and cell wall of MRSA were analyzed using reactive oxygen species (ROS) detection assays, intracellular protein leakage experiments, alkaline phosphatase (AKP) activity assays, laser scanning confocal microscopy (LSCM) observations, and molecular docking simulations. The antibiofilm activity and related mechanisms of the BA/KM combination were elucidated via crystal violet staining, MTT assay, phenol-sulfuric acid method, congo red staining, staphyloxanthin determination assays, and quantitative real-time polymerase chain reaction (qPCR). The safety of the BA/KM combination was assessed through hemolytic activity analysis, and its anti-MRSA efficacy was evaluated on lettuce.Results:BA/KM combination showed a synergistic antibacterial effect on MRSA USA300. Mechanistic studies revealed that BA may interact with amino acid residues of peptidoglycan synthetase PBP2a to hinder peptidoglycan synthesis, thereby facilitating KM penetration through the cell wall. Subsequently, BA binds to amino acid residues of the membrane transporter NorA, leading to disruption of cell membrane homeostasis and enhancing KM’s ability to induce intracellular ROS accumulation in MRSA. Furthermore, the BA/KM combination reduced MRSA biofilm formation by 77.85% and decreased the metabolic activity of biofilm cells by 42.93% through inhibiting the synthesis of biofilm components EPS and PIA. Additionally, this combination suppressed the synthesis of staphyloxanthin and downregulated the expression ofagrAandagrCgenes. When 1/8 MIC BA was combined with 1/4 MIC KM, the count of MRSA on lettuce surfaces was reduced by 0.88 log CFU/cm2, an effect comparable to that of 0.2% (v/v) hydrogen peroxide.Conclusions:According to these findings, the BA/KM combination may offer a promising option for enhancing antibacterial efficacy through synergism, reducing antibiotic usage concentrations, and limiting MRSA transmission in fresh agricultural products.
研究领域:
微生物学
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药理学
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分子生物学
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植物天然产物
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抗生素联合疗法
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食品安全
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产品关联
DOI
PubMed
高影响因子
Bioactive Materials
·
2025
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IF 20.3
Rui Yuan,Sa Du,Siyu Pan,Zhuoyuan Lin,Nan Zhang,Chenxi Zhang,Qiang Zeng,Yen Wei,Yuwei Wu,Lei Tao
The post-radiotherapy wounds are common in patients. The irradiation-induced reactive oxygen species (ROS) accumulation, nucleic acid damage, and inflammation greatly hinder wound healing. The irradiation-induced immunosuppression may further cause bacterial infection. At present, few dressings are available for infected wounds after radiotherapy (IWAR). In this study, a multifunctional hydrogel for IWAR has been developed by combining a positively-charged antioxidant polymer with the natural product baicalin. This hydrogel can smartly release baicalin under IWAR-like microenvironment and possesses broad-spectrum antibacterial properties. It has effectively prevented irradiation-induced intracellular ROS and nucleic acid damage to protect fibroblasts for tissue repair. In mice treated with IWAR, this hydrogel has inhibited infection caused by drug-resistant Pseudomonas aeruginosa , downregulated inflammation, and significantly accelerated wound healing (to more than 10 times the rate of untreated IWAR), achieving full-layer regeneration. This study obtains a multifunctional hydrogel for IWAR, and provides insights into the development of radiotherapy-related biomaterials.
研究领域:
生物材料
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放射治疗
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伤口修复
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纳米医学
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抗菌治疗
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组织工程
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产品关联
DOI
PubMed
高影响因子
TOXICOLOGY AND APPLIED PHARMACOLOGY
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2021
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IF 4.219
Huilong Xiang,Huan Lei,Ziyuan Liu,Yongjie Liu,Yang Li,Yinsheng Qiu,Lingyun Xu
Oxidative stress and inflammation in kidney are the main causes for hyperuricemic nephropathy (HN). Baicalin and baicalein , two flavonoids , have anti-inflammatory and anti-oxidative effects and they are interconvertible in the body. In this study, both baicalin and baicalein were administered by intragastric administration (i.g.) or intraperitoneal injection (i.p.) at the dose of 50 mg kg −1 , once a day for 15 consecutive days to HN mice, a model established by i.g. of yeast extract combined with i.p. of potassium oxonate . In HN mice, baicalin and baicalein reduced serum uric acid (SUA) levels and protected kidneys by anti-inflammatory and anti-oxidative effects. Mechanistically, the effect of baicalin and baicalein on reducing SUA levels might due to their inhibitory effect on xanthine oxidase (XO) activity in vivo and in vitro . Furthermore, the mechanisms of baicalin and baicalein against HN were analyzed with network pharmacology and molecular docking technology . The network pharmacology indicated that the protective effects of baicalin and baicalein against HN were mainly related to their down-regulating effects on TLRs , NF-κB, MAPK, PI3K/AKT and NOD-like receptor signaling pathways. Molecular docking indicated high binding affinity of baicalin/baicalein to targets such as AKT1 and MAPK1 . In summary, baicalin and baicalein are promising drug candidates for the treatment of HN by inhibiting XO activity, reducing inflammation and cell apoptosis through down-regulating TLRs/NLRP3/NF-κB, MAPK, PI3K/AKT/NF-κB pathways.
研究领域:
药理学
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分子生物学
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肾病学
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DOI
PubMed
高影响因子
Journal of Immunology Research
·
2021
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IF 4.818
Lin Zhang,Lukun Yang,Xiaowei Xie,Hongyue Zheng,Hangsheng Zheng,Lizong Zhang,Cuizhe Liu,Ji-Gang Piao,Fanzhu Li
Baicalin (BA) magnesium salt (BA-Mg) is a good water-soluble ingredient extracted from Scutellaria baicalensis Georgi, a commonly used traditional Chinese medicine. This study is aimed at investigating whether BA-Mg could exert a better protective effect on lipopolysaccharide- (LPS-) induced acute lung injury (ALI) in mice and illuminate the underlying mechanisms in vivo and in vitro. Mice were intraperitoneally administrated with equimolar BA-Mg, BA, and MgSO4 before LPS inducing ALI. Lung tissues and bronchoalveolar lavage fluid were collected for lung wet/dry ratio, histological examinations, cell counts, and biochemical analyses at 48 h post-LPS exposure. Meanwhile, the protein expressions of TLR4/NF-κB signaling pathway and proinflammatory cytokines in lung tissues and lung bronchial epithelial cells (BEAS-2B) were detected. The results showed BA-Mg pronouncedly ameliorated LPS-induced inflammatory response and histopathological damages, elevated antioxidant enzyme activity (SOD), and downregulated myeloperoxidase (MPO) and malonaldehyde (MDA) levels through the inhibition of TLR4/NF-κB signaling pathway activation. Moreover, the effect of BA-Mg was significantly better than that of BA and MgSO4 in ameliorating symptoms. Overall, BA-Mg can effectively relieve inflammatory response and oxidative stress triggered by LPS, indicating it may be a potential therapeutic candidate for treating ALI.
研究领域:
药理学
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免疫学
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肺病学
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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 DRUG DELIVERY SCIENCE AND TECHNOLOGY
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2021
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IF 3.981
Fansu Meng,Fengjie Liu,Meng Lan,Tengteng Zou,Lihong Li,Tiange Cai,Yu Cai
Baicalin (BA) has been shown to be one of the natural compounds with anti-proliferative activity against numerous cancer cell lines, but its application is restricted due to its rapid metabolism and non-targeting to specific tissues. This study exploited folic acid (FA)-conjugated bovine serum albumin (BSA) nanoparticles (NPs) loaded with baicalin (FA-BSANPs/BA) by desolvation crosslinking method to improve its bioavailability and therapeutic efficacy. The optimized FA-BSANPs/BA showed spherical shape and uniform distribution. The average particle size, zeta potential , encapsulation efficiency (EE) and drug loading (DL) of FA-BSANPs/BA were 228.41 ± 2.36 nm , −32.70 ± 1.27 mV, 76.88 ± 0.59% and 7.41 ± 0.23%, respectively. X-ray diffraction (XRD) and thermogravimetric (TG) analysis exhibited that the drug was amorphous in the particles. The results of drug release behavior in vitro demonstrated that FA-BSANPs/BA releases BA slowly and continuously. In vitro cytotoxicity test results suggested that the IC 50 of FA-BSANPs/BA and BA on MCF-7 cells was 16.7 and 75.96 μg/mL, respectively. The uptake efficiency of FA-BSANPs was significantly higher than that of BSANPs, which leads to a stronger potential for apoptosis . In vivo antitumor studies showed that FA-BSANPs/BA can greatly inhibit tumor growth compared with BA and exhibited the ability to target tumors in MCF-7 xenograft tumor-bearing nude mice . In conclusion, FA-BSANPs/BA improves therapeutic efficacy of BA and reduces side effects by targeting tumors, providing a promising strategy for breast cancer therapy.
研究领域:
药学
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纳米技术
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肿瘤学
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药物递送系统
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产品关联
DOI
高影响因子
FOOD CHEMISTRY
·
2021
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IF 7.514
Shaobing Lu,Junyu Tao,Xinfei Liu,Zhen Wen
To investigate antibacterial properties and application in food preservation of nanofibrous films (NFs), baicalin-liposomes (BCL-LPs) were loaded into polyvinyl alcohol-chitosan (PVA-CS) substrates to form NFs using electrospinning technology. The microstructure and phase identification of the NFs were characterized. The antibacterial properties and cytotoxicity of NFs were determined. The preservation of the NFs to mushrooms was evaluated. The results showed that smooth and uniform NFs were formed through molecular interaction between BCL-LPs and PVA-CS matrix. The NFs exhibited good antibacterial effects on Escherichia coli and Staphylococcus aureus due to the bacterial destruction resulting from the BCL delivery to bacterial cells by liposomes. In addition, the NFs were compatible with L929 fibroblasts. The BCL-LPs/PVA-CS NFs inhibited weight loss, browning, rancidity and bacterial growth as well as maintained the nutrients of mushrooms. The results show BCL-LPs/PVA-CS NFs possessed effective antibacterial properties, non-cytotoxicity and preservation performance, indicating the potential utilization as food-active packing.
研究领域:
材料科学
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食品科学
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生物技术
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）