ECOTOXICOLOGY AND ENVIRONMENTAL SAFETY
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2025
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IF 6.1
Jia Yu,Dahai Yu,Yong Pang,Weiyun Zhang,Shuang Liu,Xuexun Fang,Jie Zhang
Lead exposure is a well-documented environmental neurotoxin that poses a persistent threat to brain development. Excessive lead accumulation in this region impairs cognitive function and induces neuronal damage, yet effective therapeutic interventions remain limited. Baicalin, a flavonoid compound derived from Scutellaria baicalensis , exhibits antioxidant and neuroprotective activity, but its efficacy against lead-induced neural injury has not been fully elucidated. Here, we established a subchronic lead exposure model in mice and administered baicalin orally following lead treatment. Cognitive function was assessed through spatial, recognition, and avoidance learning paradigms. Lead concentrations in blood and hippocampus, as well as hippocampal structural integrity, oxidative stress markers, apoptosis signals, and neuronal autophagy, were quantitatively analyzed. In vitro studies using HT22 cells further investigated the effects of baicalin on oxidative stress, mitochondrial function, and autophagy-related signaling pathways. Baicalin treatment significantly improved cognitive performance, reduced blood and hippocampal lead concentrations, preserved hippocampal morphology, and reestablished redox homeostasis. Baicalin reduced lipid peroxidation, suppressed neuronal apoptosis, and restored autophagic flux. Mechanistically, baicalin activated AMPK, inhibited mTOR phosphorylation, and promoted ULK1-mediated autophagy. These effects were abolished by pharmacological inhibition of AMPK, confirming the pivotal regulatory role of baicalin. Collectively, these findings demonstrate that baicalin mitigates lead-induced cognitive and neuronal impairments by modulating oxidative stress, apoptosis, and autophagy via the AMPK–mTOR–ULK1 signaling axis. These results support further investigation of baicalin as a candidate neuroprotective agent for managing heavy metal-associated neurodevelopmental disorders.
研究领域:
神经毒理学
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环境健康
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分子神经科学
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药理学
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自噬研究
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高影响因子
JOURNAL OF MOLECULAR HISTOLOGY
·
2026
·Vol. 57
·期 3
·184
·
IF 2.6
Zhang Xuepu,Zhang Yue,Yang Limin,Fang Shiqiang,Mei Xifan
Diabetic foot ulcer (DFU) is a severe complication of diabetes. This study evaluated the effects and underlying mechanism of baicalin on DFU healing. High glucose (HG)-exposed HaCaT cells and streptozotocin-induced DFU rats were employed as in vitro cell models and in vivo models. Cell viability, migration, and inflammatory cytokine levels were assessed following baicalin (100 µg/mL) treatment. A baicalin-loaded carboxymethyl chitosan (CS) hydrogel was prepared, and its therapeutic effects on blood glucose and wound closure were evaluated over 14 days. Bioinformatic analysis, molecular docking, and MAPK1 knockdown were performed to elucidate the mechanism. Baicalin restored HG-reduced HaCaT cell viability ( p < 0.01) and migration ( p < 0.001), and decreased IL-6, IL-1β, and TNF-α levels. In DFU rats, the hydrogel lowered blood glucose from > 20 mM to approximately 10 mM ( p < 0.001) and accelerated wound healing ( p < 0.01). Bioinformatic analysis identified MAPK1 as a key target; molecular docking confirmed strong binding affinity (< − 6 kcal/mol). Baicalin upregulated MAPK1 expression ( p < 0.01), whereas shRNA-mediated MAPK1 knockdown attenuated the therapeutic effects in vitro and in vivo ( p < 0.001). These findings demonstrate baicalin’s potential as a DFU treatment through MAPK1 regulation and highlight the need for further research into its molecular mechanisms and clinical applications.
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高影响因子
International Journal of Nanomedicine
·
2025
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IF 6.5
Xing Liu,Wenlin Shu,Qingrui Zhong,Anqi Zeng,Yong Zeng,Huan Gu,Ping Chen,Xiaofang Li
Purpose: Prolonged exposure of the skin to ultraviolet (UV) rays from sunlight causes oxidative damage to skin cells, and prolonged exposure to UV can lead to severe sunburn and skin aging, which may increase the risk of skin cancer. Numerous natural products have been used to treat UV-induced skin damage. Baicalin (BA) has excellent antioxidant properties; however, its poor solubility hinders its direct application. Therefore, suitable formulations for dermal administration must be developed.Methods: We designed a temperature-sensitive gel drug delivery system based on baicalin liposome (BA-LP), which was first constructed using lecithin loaded with insoluble BA. Subsequently, an injectable hydrogel (BA-LG) with temperature-sensitive properties was constructed using BA-LP and chitosan (CS) with β-glycerophosphate tetrahydrate (β-GP) as a crosslinking agent.Results: BA-LP had homogeneous particle size, high EE, and good stability. BA-LG could be gelled within 2 min at 37 °C and had good spreading, adhesion, and injectability properties. The in vitro release results showed that BA-LG had a significantly slower release effect, with a cumulative release of 60% at 24 h. The effects of BA-LG on skin keratinocyte HaCaT cells were evaluated using the CCK8 method and transwell co-culture, and the results showed good cell activity and a high survival rate, indicating that the hydrogel has good biosafety. In the UVB-induced skin injury mouse model, BA-LG showed significant effects by increasing superoxide dismutase (SOD) activity, decreasing malondialdehyde (MDA) damage, and inhibiting the expression of inflammatory factors IL-6, PGE2, and TNF-α, and demonstrated a superior therapeutic effect. The analysis of histopathological sections of the skin stained with H&E and Masson revealed results consistent with those observed on the mice.Conclusion: In summary, our results suggest that BA-LG, a temperature-sensitive gel based on baicalin liposomes, has good therapeutic efficacy and potential applications in the treatment of UVB-induced skin damage.
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高影响因子
Biomedicines
·
2025
·Vol. 13
·期 1
·232
·
IF 3.9
Lu He,Min Zhu,Rui Yin,Liangli Dai,Juan Chen,Jie Zhou
Background:Heart failure (HF) is a serious public health concern. Baicalin is one of the major active ingredients of a traditional Chinese herbal medicine, Huang Qin, which is used to treat patients with chest pain or cardiac discomfort. However, the underlying mechanism(s) of the cardioprotective effect of baicalin are still not fully understood.Methods:Isoprenaline injection or transverse aortic constriction-induced animal models and isoprenaline or angiotensin 2 administration-induced cell models of heart failure were established. Baicalin (15 mg/kg/day or 25 mg/kg/day) was administered in vivo, and 10 μM baicalin was administered in vitro. Potential pharmacological targets of baicalin and genes related to heart failure were identified via different databases, which suggested that PI3K–Akt may be involved in the effects of baicalin. Molecular docking was carried out to reveal the effect of baicalin on p85a.Results:We observed significant antihypertrophic and antifibrotic effects of baicalin both in vivo and in vitro. The mean cross-sectional area of cardiomyocytes recovered from 390 μm2in the HF group to 195 μm2in the baicalin-treated group. The area of fibrosis was reduced from 2.8-fold in the HF group to 1.62-fold in the baicalin-treated group. Baicalin displayed a significant cardioprotective effect via the inhibition of the PI3K signaling pathway by binding with five amino acid residues of the p85a regulatory subunit of PI3K. The combination treatment of baicalin and an inhibitor of PI3K p110 demonstrated a stronger cardioprotective effect. The mean ejection fraction increased from 54% in the baicalin-treated group to 67% in the combination treatment group.Conclusions:Our work identified baicalin as a new active herbal ingredient that is able to treat isoprenaline-induced heart dysfunction and suggests that p85a is a pharmacological target. These findings reveal the significant potential of baicalin combined with an inhibitor of PI3K p110 for the treatment of heart failure and support more clinical trials in the future.
研究领域:
药理学
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心脏病学
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分子生物学
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高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Fengjie Liu,Fansu Meng,Xiaoshan Hong,Anil K. Giri,Mulazim Hussain Asim,Zhong Chen,Yiqi Chen,Yixuan Lin,Lulu He,Qiaowen Bu,Yong Huang,Xiaoli Sun,Zhenjiang Yang,Yu Cai
Background Baicalin (BA), a natural flavonoid compound, exhibits potential anti-breast cancer (BC) activity. However, its therapeutic efficacy is limited by biological membrane and tumor barriers. Albumin nanoparticles demonstrate excellent biocompatibility and ease of modification, making them highly advantageous for antitumor drug delivery. Despite these advantages, current preparation methods for albumin-based NPs have significant limitations, including the use of organic or toxic reagents, large and uneven particle size products, complex processes, etc. Objective The purpose of this study was to develop a novel method for preparing albumin nanoparticles (BSA NPs). Subsequently, BSA NPs were modified with folic acid (FA) and polymers and loaded with BA to construct a novel nanodrug delivery system (BA@mPEG-FA-BSA NPs) to improve the anti-breast cancer efficacy of BA. Methods Compared with the desolvation method and the thermal gelation method, the advantages of the new preparation method of BSA NPs are: less organic solvent and preparation time, greater yield, smaller particle size and uniform product. The preparation method of BSA NPs was investigated by single factor experiment. The encapsulation efficiency (EE) and drug loading (DL) of BA in BA@mPEG-FA-BSA NPs were detected by HPLC. The structural composition and physicochemical properties of the nanoparticles were characterized using transmission electron microscopy (TEM), infrared spectroscopy (FT-IR), thermogravimetric analysis (TGA), and X-ray diffraction (XRD). The anti-breast cancer efficacy of BA@mPEG-FA-BSA NPs was evaluated through cellular uptake, cytotoxicity, apoptosis, cell cycle analysis, and in vivo tumor-bearing mouse studies. Results According to the setting of process parameters, the established method can control the acquisition of uniform BSA NPs with a particle size between 20 and 300 nm. BA@mPEG-FA-BSA NPs exhibited a particle size of approximately 59.26 nm, a polydispersity index (PDI) < 0.3, EE of about 46.7 %, and DL of approximately 2.6 %. Cellular uptake experiments demonstrated that mPEG-FA-BSA NPs enhanced the uptake of free coumarin 6 in BT20 cells, with free FA showing competitive inhibition effects. Efficacy evaluation revealed that BA@mPEG-FA-BSA NPs exhibited cytotoxicity against BT20 cells, induced cell cycle arrest and apoptosis, and inhibited tumor growth in 4 T1 tumor-bearing mice. In most cases, the effects of BA@mPEG-FA-BSA NPs were superior to those of free BA, with a concentration- or dose-dependent manner observed. Conclusion This study established a novel preparation method for albumin nanoparticles, providing a new methodology for the construction of nano-drug delivery systems based on albumin materials. The developed BA@mPEG-FA-BSA NPs, with their relatively small particle size, demonstrated enhanced cellular uptake and anti-breast cancer activity of BA, highlight the potential for further optimization and clinical translation.
研究领域:
药学
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肿瘤学
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纳米医学
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PubMed
高影响因子
Green Chemistry Letters and Reviews
·
2024
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IF 5.8
Lingling Tang,Jiali Shao,Hanxue Zheng,Jixuan Chen,Guohua Xia,Huan Yang,Yaya Yang,Yuping Shen
Baicalein, usually obtained after the removal of 7-O-β-D-glucuronic acid from baicalin, has strong pharmacological activity. In this study, a novel strategy for efficient and eco-friendly preparation of baicalein was established by high-temperature-little-acid hydrolysis of baicalin. The effects of inorganic acids, solvents, solid–liquid ratio, HCl concentration and hydrolysis duration on the yield of baicalein were investigated by one-factor-at-a-time experiment. Then, an orthogonal experiment design was conducted for the optimal hydrolysis conditions, namely, baicalin was boiled in n-BuOH solution containing 0.50% HCl (w/v) at 130°C for 2.0 h with solid–liquid ratio at 1:25 (g/mL). In the 60-fold scale-up experiment, the yield of baicalein was achieved at 83.5% ± 6.3%, and its purity was increased from 74.2% to 98.7% after purification. Compared with reported methods, acid consumption per unit product of the newly developed strategy was approximately 80 times lower than that of conventional acid hydrolysis, and time consumption was substantially reduced. Overall, the novel strategy showed great prospects for a cleaner large-scale production of baicalein, which provides a new alternative desirable for the preparation of natural products with high efficiency and low consumption in the pharmaceutical industry.
研究领域:
药学
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化学工程
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天然产物化学
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高影响因子
JOURNAL OF MOLECULAR STRUCTURE
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2024
·
IF 4
Weizhao Hou,Wenjuan Guo,Zhao Dai,He Ren,Xingran Luo,Junjie Fu
Baicalin is a natural active ingredient known for its medicinal properties and a broad spectrum of pharmacological activities, including antimicrobial, antioxidant, antiviral, and anticancer effects. However, its application is hindered by its poor water-solubility. In this study, we aimed to enhance the water solubility of baicalin by embedding it within the hydrophobic cavity of hydroxypropyl-β-cyclodextrin through supramolecular assembly to form inclusion complexes. The inclusion complexes were subsequently processed into nanofiber membranes suitable for application on skin and wounds using coaxial electrostatic spinning. The inclusion complexes and nanofiber membranes were analyzed and characterized using high-performance liquid chromatography (HPLC), X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FT-IR), thermogravimetric analysis (TGA), scanning electron microscopy (SEM), and transmission electron microscopy (TEM). The combined results from XRD, FT-IR, and TGA confirmed that baicalin successfully formed inclusion complexes with cyclodextrin, resulting in an increase in water solubility from 0.0170 mg/mL to 8.9600 mg/mL, representing a 527-fold enhancement. Additionally, the inclusion complexes demonstrated superior antimicrobial activity against E. coli, S. aureus and C. albicans , as well as higher free radical scavenging rates compared to native baicalin. After the inclusion complexes were transformed into nanofiber membranes via coaxial electrospinning, their properties remained unchanged, and they continued to exhibit excellent antimicrobial and antioxidant activities. In the in vitro release assay, nearly 90 % of the drug (baicalin) was released from the nanofiber membranes over a period of time, indicating sustained release. Furthermore, the molecular docking mechanism of baicalin and cyclodextrin was elucidated through molecular docking simulations, establishing a theoretical foundation for the synthesis of inclusion complexes in the computational studies. This study reports the successful fabrication of water-soluble, antimicrobial nanofiber membranes containing bioavailable baicalin, which have potential clinical applications in the development of wound dressings and drug delivery systems utilizing plant-extracted bioactive compounds.
研究领域:
药学
·
材料科学
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高影响因子
Heliyon
·
2024
·
IF 3.4
Jiwen Zhu,Qi Liu,Yan Chen,JiaMing Zhang,Qinghua Xu,Zhengwei Wu
Neurodegenerative disorders are chronic conditions that progressively damage and destroy parts of the nervous system, and are currently considered permanent and incurable. Alternative strategies capable of effectively healing neuronal damage have been actively pursued. Here, we report the neuroprotective effects of baicalin (BA) combined with plasma-activated medium (PAM) against glutamate-induced excitotoxicity in SH-SY5Y cells. Through in vitro assays, the cell viability, inflammation, apoptosis, and oxidative stress were evaluated. The co-application of BA and PAM significantly enhanced cell viability, reduced pro-inflammatory markers (TNF-α and NF-κB), decreased apoptotic proteins (Bax and Caspase-3) and boosted antioxidative defenses (increased SOD activity and lowered ROS levels). This study confirms the potential of combining BA with PAM as an effective therapeutic strategy for mitigating the effects of excitotoxicity. PAM is a promising adjunct and potential drug delivery method in neuroprotective therapy, providing a new avenue for developing treatments for diseases characterized by neuronal damage.
研究领域:
神经科学
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药理学
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PubMed
高影响因子
BMC Cardiovascular Disorders
·
2024
·Vol. 24
·期 1
·1-12
·
IF 2
Qian Kai,Song Li,Guo Jia-Min,Fu Dan,Shi Jia,Ma Yu,Ge Zi-Jie,Li Lei,Zhang Su-qin
Background Cardiovascular disease carries the highest mortality rate among diseases, and pharmacological interventions have limited efficacy. Baicalin (Bai) promotes biological metabolic processes, eliminates oxygen free radicals, and is anti-inflammatory. This study aimed to investigate the effect of Bai on the cardiac injury model induced by isoproterenol in mice.Methods and ResultIn this study, all groups except the control received intraperitoneal injections of isoproterenol (ISO) to induce a cardiac injury model, with the drug administered continuously for 14 days. hematoxylin and eosin staining and Masson’s trichrome staining revealed that Bai significantly mitigated ISO-induced pathological changes in mouse heart tissue and alleviated myocardial hypertrophy. Echocardiography assessments demonstrated that Bai preserved cardiac function in ISO-treated mice. Furthermore, our findings indicated that Bai activated the Nrf2 signaling pathway in vivo and in vitro. To delve deeper, mice were further treated with ML385 (ML) via intraperitoneal injection to inhibit the Nrf2 pathway. Results showed that ML385 blocked the cardioprotective effects of Bai in mouse heart tissue.Conclusion Bai protects against ISO-induced cardiac injury, and its mechanism is related to activating the Nrf2/HO-1 signaling pathway to regulate cardiac ferroptosis and improve cardiac remodeling.
研究领域:
心血管疾病
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药理学
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分子生物学
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PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACOLOGY
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2020
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IF 3.263
Zi-Yuan Wang,Zheng-Meng Jiang,Ping-Ting Xiao,Ying-Qun Jiang,Wen-Jin Liu,E-Hu Liu
Obesity is one of the main causes of human cardiovascular and cerebrovascular diseases . Baicalin , a bioactive flavonoid isolated from the herbal medicine Scutellaria baicalensis Georgi, is reported to ameliorate obesity and hyperlipidemia . However, its mechanism remains unclear. Here, we used network pharmacology to explore the potential mechanism of baicalin on a system level. First, we predicted the targets of baicalin and diseases, and then protein-protein interaction (PPI) networks were constructed. Moreover, Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment was performed via the Database for Annotation, Visualization, and Integrated Discovery (DAVID) server. Lastly, we confirmed the results of the network analysis by palmitic acid (PA) treated human hepatoma cells (HepG2) in vitro . The results indicated that 37 targets related to obesity treated by baicalin were predicted by network pharmacology, and top 10 related pathways were extracted by the KEGG database. Baicalin treatment could reduce triglyceride (TG) contents and lipid droplet accumulation in PA-treated HepG2 cells. The anti-obesity effects of baicalin might be due to the up-regulation of solute carrier family 2 member 1 (SLC2A1) and down-regulation of tumor necrosis factor (TNF), nuclear factor kappa B subunit 1 (NFKB1), sterol regulatory element binding transcription factor 1 (SREBF1), peroxisome proliferator activated receptor gamma and caspase 3 (CASP3). Our results indicated that baicalin may regulate key inflammatory markers, adipogenesis process, and apoptosis for treatment of obesity.
研究领域:
药理学
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分子生物学
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细胞生物学
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生物信息学
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PubMed
高影响因子
POULTRY SCIENCE
·
2019
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IF 2.027
Y. Chen,Y. Yang,F. Wang,X. Yang,F. Yao,K. Ming,W. Yuan,L. Zeng,J. Liu
ABSTRACT Duck hepatitis A virus type 1 ( DHAV-1 ) is one of the main pathogens of ducklings and causes a high mortality rate. Baicalin ( BA ) has potent antiviral effect, but the solubility is very poor. In order to increase the absorption, solubility, and pharmacological activity, the phospholipid complex was used to modify BA in present study. Therefore, BA phospholipid complex ( BAPC ) was prepared. The anti-DHAV-1 abilities of BA and BAPC in vitro was evaluated by cell counting kit-8 and reverse transcription quantitative PCR. The curative effects of BA and BAPC on ducklings which were infected by DHAV-1 in addition to the ALT and AST levels were also detected. The results indicated the anti-DHAV-1 ability of BAPC was stronger than that of BA both in vitro and in vivo . To explore the anti-DHAV-1 mechanism, the influence of BAPC on DHAV-1 adsorption, replication, and release was studied. Furthermore, the anti-oxidative and immuno-enhancing abilities of BAPC in the treatment of infected ducklings were also determined. The results showed BAPC inhibited DHAV-1 adsorption, replication and release. Furthermore, it played anti-oxidative and immno-enhancing roles in the treatment, and the immno-enhancing role was crucial to the treatment.
研究领域:
兽医学
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病毒学
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药理学
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分子生物学
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PubMed
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
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2015
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IF 4.152
Yiyin Chen,Le Van Minh,Jianwen Liu,Borislav Angelov,Markus Drechsler,Vasil M. Garamus,Regine Willumeit-Römer,Aihua Zou
Bioavailability of baicalin (BAI), an example of traditional Chinese medicine, has been modified by loading into liposome. Several liposome systems of different composition i.e., lipid/cholesterol (L), long-circulating stealth liposome (L-PEG) and folate receptor (FR)—targeted liposome (L-FA) have been used as the drug carrier for BAI. The obtained liposomes were around 80 nm in diameter with proper zeta potentials about −25 mV and sufficient physical stability in 3 months. The entrapment efficiency and loading efficiency of BAI in the liposomes were 41.0–46.4% and 8.8–10.0%, respectively. The morphology details of BAI lipsosome systems i.e., formation of small unilamellar vesicles, have been determined by cryogenic transmission electron microscopy (cryo-TEM) and small angle X-ray scattering (SAXS). In vitro cytotoxicity of BAI liposomes against HeLa cells was evaluated by MTT assay. BAI loaded FR-targeted liposomes showed higher cytotoxicity and cellular uptake compared with non-targeted liposomes. The results suggested that L-FA-BAI could enhance anti-tumor efficiency and should be an effective FR-targeted carrier system for BAI delivery.
研究领域:
药剂学
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肿瘤学
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药物递送系统
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纳米技术
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PubMed
高影响因子
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