COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
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2025
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IF 5.4
Jingtao Wu,Xiaodong Yue,Tianyu Wang,Yafeng Zhang,Yuan Jin,Guangli Li
Excessive intake of baicalein (BA) may lead to many adverse heathy risks. Hence, it is highly desirable to develop a convenient and sensitive method for the determination of BA. Herein, a low-cost and highly sensitive electrochemical sensor was fabricated for determination of BA in herbal medicine based on shuttle-shape α-Fe 2 O 3 nanoparticles decorated multiwalled carbon nanotubes (s-Fe 2 O 3 /MWCNTs). Various microscopic and spectroscopic methods confirmed the successful formation of s-Fe 2 O 3 /MWCNTs. CV and EIS techniques revealed that the s-Fe 2 O 3 /MWCNTs significantly improved the electroactive surface area and electron transport ability. Owing to the synergistic interactions between s-Fe 2 O 3 NPs and MWCNTs, the s-Fe 2 O 3 /MWCNTs exhibited superior electrocatalytic toward BA oxidation through a two electrons two protons pathway. Under optimal experimental conditions (accumulation potential of 0 V, accumulation time of 120 s, and pH of 6.0), The s-Fe 2 O 3 /MWCNT/GCE displayed a wide detection range from 0.001 to 10 μM with an ultrahigh sensitivity (6.154 μA μM −1 ) and extremely low limit of detection (0.2 nM). The s-Fe 2 O 3 /MWCNTs demonstrated strong anti-interfering ability against common potential interfering substances even at high concentration, and maintained stable peak current responses for at least 2 weeks. Furthermore, the s-Fe 2 O 3 /MWCNTs achieved the reliable detection of BA in traditional herbal medicine with satisfactory recovery (97 − 105 %). Considering their low cost, convenient operation, and comprehensive sensing performance, the s-Fe 2 O 3 /MWCNTs have demonstrated promising application prospects in sensitive detection of flavonoids.
研究领域:
分析化学
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药物分析
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材料科学
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DOI
高影响因子
Natural Product Communications
·
2019
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IF 0.554
Chengyun He,Xiaoling Liu,Junliang Sun
Baicalein is one of the main bioactive compounds in Scutellaria baicalensis. In this study, its inhibitory mechanism against α-glucosidase from Saccharomyces cerevisiae was clarified based on experimental and molecular simulation methods. According to HPLC analysis, the α-glucosidase inhibitory activity of S. baicalensis (IC50, 6.75 ± 0.08 μg mL−1) was superior to that of acarbose (IC50, 2.52 ± 0.12 mg mL−1). The fluorescence results suggested that baicalein could form a complex with α-glucosidase at the molar ratio of 1 under the drive of hydrogen bonding and van der Waals force. Molecular docking showed that baicalein could form hydrogen bonds with Trp391, Arg428, Gly566,and Glu771 of α-glucosidase, and interacted with Phe385, Phe389, Arg387, Glu429, Phe444, Trp789, and Trp710 by hydrophobic force, which coincided with the experimental results. It can be concluded that baicalein is a potential α-glucosidase inhibitor for controlling the postprandial blood glucose level of diabetics.
研究领域:
药理学
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生物化学
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DOI
高影响因子
Frontiers in Microbiology
·
2025
·
IF 4.5
Mengmin Liang,Qingwen Hu,Junhao Yu,Heng Zhang,Sijie Liu,Jiangrong Huang,Yi Sun
Background: Invasive fungal infections (IFIs) constitute a significant health challenge, particularly among immunocompromised individuals, characterized by a high prevalence and associated mortality rates. The synergistic administration of Baicalein (BE) with azole antifungal agents could potentially herald a novel therapeutic paradigm.Materials and methods: 54 Aspergillus strains and 23 strains of dematiaceous fungi were selected. The standard M38-A2 microbroth dilution method was used to test the minimum inhibitory concentration (MIC) and the fractional inhibitory concentration index (FICI) of fungi when BE combined with itraconazole (ITC), voriconazole (VRC), posaconazole (POS) and Isavuconazole (ISV).Results: BE shows synergistic effects with POS and ITC, with 89.61% and 25.97% of fungal strains. The BE/POS regimen exerted synergistic effects in 87.04% of Aspergillus and an impressive 95.65% of dematiaceous fungi. In comparison, the BE/ITC combination showed significantly lower synergy, affecting 33.33% of Aspergillus and a mere 8.70% of dematiaceous strains. Antagonistic interactions were sporadically observed with BE in combination with ITC, VRC, POS and ISV. Within the azole class, the BE/POS pairing stood out for its frequent synergistic activity, in contrast to the absence of such effects when BE was paired with VRC or ISV. Highlighting the potential of BE/POS as a notably effective antifungal strategy.Conclusion: In vitro, BE/POS combination emerged as the most effective antifungal strategy, exhibiting synergistic effects in the majority of Aspergillus and dematiaceous fungi strains, whereas BE/ITC showed significantly less synergy, and BE with VRC or ISV displayed no synergistic activity.
研究领域:
医学
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微生物学
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药理学
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产品关联
DOI
PubMed
高影响因子
Microbiology Spectrum
·
2023
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IF 3.7
Yuhang Wang,Junfeng Su,Ziyan Zhou,Jie Yang,Wenjuan Liu,Yafen Zhang,Pengyu Zhang,Tingting Guo,Guocai Li
As multidrug-resistant pathogens emerge and spread rapidly, novel antibiotics urgently need to be discovered. With a dwindling antibiotic pipeline, antibiotic adjuvants might be used to revitalize existing antibiotics. In recent decades, traditional Chinese medicine has occupied an essential position in adjuvants of antibiotics. This study found that baicalein potentiates doxycycline against multidrug-resistant Gram-negative pathogens. Mechanism studies have shown that baicalein causes membrane disruption by attaching to phospholipids on the Gram-negative bacterial cytoplasmic membrane and lipopolysaccharides on the outer membrane. This process facilitates the entry of doxycycline into bacteria. Through collaborative strategies, baicalein can also increase the production of reactive oxygen species and inhibit the activities of multidrug efflux pumps and biofilm formation to potentiate antibiotic efficacy. Additionally, baicalein attenuates the lipopolysaccharide-induced inflammatory response in vitro. Finally, baicalein can significantly improve doxycycline efficacy in mouse lung infection models. The present study showed that baicalein might be considered a lead compound, and it should be further optimized and developed as an adjuvant that helps combat antibiotic resistance.IMPORTANCE Doxycycline is an important broad-spectrum tetracycline antibiotic used for treating multiple human infections, but its resistance rates are recently rising globally. Thus, new agents capable of boosting the effectiveness of doxycycline need to be discovered. In this study, it was found that baicalein potentiates doxycycline against multidrug-resistant Gram-negative pathogens in vitro and in vivo. Due to its low cytotoxicity and resistance, the combination of baicalein and doxycycline provides a valuable clinical reference for selecting more effective therapeutic strategies for treating infections caused by multidrug-resistant Gram-negative clinical isolates.
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DOI
PubMed
高影响因子
JOURNAL OF PHARMACEUTICAL SCIENCES
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2015
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IF 2.59
Yanting Huang,Bowen Zhang,Yuan Gao,Jianjun Zhang,Limin Shi
ABSTRACT The purpose of this study was to investigate the effect of preparation methods on cocrystallization between baicalein (BE) and nicotinamide (NCT), their intermolecular interaction, and to demonstrate that BE–NCT cocrystal can achieve the simultaneous enhancement in solubility, dissolution, and oral bioavailability of BE. The cocrystals from three preparation methods have the similar differential scanning calorimetry thermograms and X-ray powder diffraction patterns. Compared with crystalline BE, BE–NCT cocrystal has significantly improved the solubility and dissolution of BE. In addition, the cocrystal exhibits a 2.49-fold higher peak plasma concentration ( C max ) and 2.80-fold higher area under the curve ( AUC ) in rats. This prominent improvement in oral bioavailability is even greater than the previously reported BE nanocrystal . This investigation enriched the present understanding of cocrystals on their behavior in vitro and in vivo , and built the groundwork for future development of BE as a promising compound into efficacious drug products. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:2330–2337, 2014
研究领域:
药学
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药物化学
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生物药剂学
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2025
·
IF 5.2
Wanbing Pan,Rong Sun,Yaoyuan Yu,Yuxin Liu,Yinling Mu,Hanyan Gong,Hongxia Fan,Yingchao Zhang,Lutong He,Haibing He,Jingxin Gou,Xing Tang,Tian Yin,Yu Zhang
Effective management of posterior ocular segment disorders necessitates sustained retinal drug delivery and rational therapeutic selection. Despite significant advances, developing drug delivery systems that simultaneously achieve deep tissue penetration and prolonged ocular surface retention remains challenging. To bridge this gap, we engineered a borneol- decorated baicalein nanoemulsion in-situ gel (Bor/Bai-N@GEL) ophthalmic formulation for dry age-related macular degeneration (d-AMD). The system integrates a borneol-decorated baicalein nanoemulsion with an ion- sensitive hydrogel. Comparative analysis revealed Bor/Bai-N@GEL’s superior therapeutic performance, attributable to the prolonged ocular residence time and enhanced transcorneal permeability. Pharmacodynamic profiling demonstrated marked attenuation of inflammatory cytokines, oxidative markers, and apoptotic signaling in murine d-AMD models. In summary, our work provided a meaningful delivery strategy and research basis to treat fundus diseases. This approach offers the potential to conveniently treat early-stage d-AMD at home, improving patient adherence and overall treatment outcomes.
研究领域:
药剂学
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眼科医学
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生物医学工程
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DOI
PubMed
高影响因子
Microbiology Spectrum
·
2022
·Vol. 10
·期 4
·
IF 9.043
Liping Li,Hui Lu,Xuan Zhang,Malcolm Whiteway,Hao Wu,Shanlun Tan,Jianye Zang,Shujuan Tian,Cheng Zhen,Xianlei Meng,Wanqian Li,Dazhi Zhang,Min Zhang,Yuanying Jiang
Baicalein (BE) is a promising antifungal small-molecule compound with an extended antifungal spectrum, good synergy with fluconazole, and low toxicity, but its target protein and antifungal mechanism remain elusive. In this study, we found that BE can function against Candida albicans by disrupting glycolysis through targeting Eno1 and inhibiting its function. Eno1 acts as a key therapeutic target of the drug, as BE had no antifungal activity against the eno1 null mutant in a Galleria mellonella model of C. albicans infection. To investigate the mechanism of action, we solved the crystal structure of C. albicans Eno1(CaEno1) and then compared the difference between this structure and that of Eno1 from humans. The predicted primary binding site of BE on CaEno1 is between amino acids D261 and W274, with D263, S269, and K273 playing critical roles in the interaction with BE. Both positions S269 and K273 have different residues in the human Eno1 (hEno1). This finding suggests that BE may bind selectively to CaEno1, which would limit the potential for side effects in humans. Our findings demonstrate that Eno1 is a target protein of BE and thus may serve as a novel target for the development of antifungal therapeutics acting through the inhibition of glycolysis.IMPORTANCE Baicalein (BE) is a promising antifungal agent which has been well characterized, but its target protein is still undiscovered. The protein Eno1 plays a crucial role in the survival of Candida albicans. However, there are few antifungal agents which inhibit the functions of Eno1. Here, we found that BE can function against Candida albicans by disrupting glycolysis through targeting Eno1 and inhibiting its function. We further solved the crystal structure of C. albicans Eno1(CaEno1) and predicted that the primary binding site of BE on CaEno1 is between amino acids D261 and W274, with D263, S269, and K273 playing critical roles in the interaction with BE. Our findings will be helpful to get specific small-molecule inhibitors of CaEno1 and open the way for the development of new antifungal therapeutics targeted at inhibiting glycolysis.
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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结构生物学
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DOI
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
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2025
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IF 5.6
Ruqi Wang,Qishu Jin,Zhaoxu Meng,Xiaodong Cao,Yihao Wu,Chen Yang,Jiandong Yuan
Oxidative stress is increasingly recognized as a key pathological driver of skeletal degeneration in diabetes, aging, trauma, and other orthopedic disorders, where excessive reactive oxygen species (ROS) compromise osteoblast and bone marrow mesenchymal stem cell (BMSC) function while promoting osteoclast activity. Natural polyphenols such as baicalein (BA) exhibit potent antioxidant effects but are hindered by poor solubility and limited stability. Here, we report a series of BA-X self-assembled nanoparticles, in which X represents osteogenic metal ions including Mg 2+ , Mn 2+ , Cu 2+ , Zn 2+ , and Sr 2+ . Among these, BA-Mn demonstrated the most robust radical-scavenging activity in DPPH, ABTS, and multiple ROS-targeted assays. BA-Mn exhibited nanoscale dimensions, uniform coordination, and excellent cytocompatibility, significantly reducing intracellular ROS and protecting H 2 O 2 -injured BMSCs. Functionally, BA-Mn restored osteogenic differentiation under oxidative stress, enhancing alkaline phosphatase activity, mineral deposition, and osteogenic gene expression. Transcriptomic analysis further revealed concurrent activation of cell cycle, PI3K-Akt, and MAPK signaling pathways, alongside suppression of ferroptosis and ROS-related carcinogenesis. Collectively, these findings establish BA-Mn as a multifunctional nanoplatform that integrates antioxidant defense with osteogenic stimulation, offering a promising therapeutic approach for oxidative stress-related bone disorders.
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PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2023
·
IF 5.8
Fang Zheng,Yujia Luo,Yuanqi Liu,Yuanyuan Gao,Wenyu Chen,Kun Wei
Cancer-associated fibroblasts constitute a significant component in the tumor microenvironment, playing a pivotal role in tumor proliferation, invasion, migration, and metastasis. Consequently, therapy combining chemotherapeutic agents with tumor microenvironment (TME) modulators appears to be a promising avenue for cancer treatment. In this paper, a tumor microenvironment-based mPEG-PLGA nanoparticle loaded with baicalein (PMs-Ba) was constructed for the purpose of improving the tumor microenvironment in cases of triple-negative breast cancer. The results demonstrate that, on the one hand, PMs-Ba was able to inhibit the transforming growth factor β(TGF-β) signaling pathway to avoid the activation of cancer-associated fibroblasts (CAFs), thereby influencing the interstitial microenvironment of the tumor. On the other hand, the agent led to an increase in the infiltration of cytotoxic T cells, activating the tumor immune microenvironment. Meanwhile, in the murine breast cancer model, an intravenous injection of PMs-Ba combined with doxorubicin nanoparticles (PMs-ADM) significantly improved the antitumor effectiveness. These results suggest that baicalein encapsulated in nanoparticles may be a promising strategy for modulating the TME and for adjuvant chemotherapy, signifying a potential TME-remodeling nanoformulation that could enhance the antitumor efficacy of nanotherapeutics.
研究领域:
肿瘤学
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药学
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纳米技术
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免疫学
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DOI
PubMed
高影响因子
JOURNAL OF SUPERCRITICAL FLUIDS
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2015
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IF 2.371
Tingxuan Yan,Yue Cheng,Zhixiang Wang,Dechun Huang,Honggang Miao,Yi Zhang
Baicalein, a bioactive flavonoid, exhibits various pharmacological activities and other beneficial effects, but its poor solubility and dissolution rate restrict its oral intestinal absorption rate and bioavailability. In this study, micronized baicalein was prepared by utilizing the technique of solution-enhanced dispersion by supercritical fluids (SEDS). Preparation, characterization, and the potential use of microparticles to improve the in vitro release of baicalein were studied. In vitro characterization data were obtained through Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X-ray powder diffractometry (XRD), and scanning electron microscopy (SEM). The in vitro dissolution of the prepared microparticles was investigated and compared with raw powder. The results demonstrated that the prepared baicalein microparticles appeared as small flake shapes with a mean particle size (PS) of 0.614 μm under the appropriate conditions (solvent mixture of DCM and DMSO (5/1, v/v), drug concentration = 7 mg/mL, pressure = 16 MPa, and temperature = 308 K) without an observed change in the crystal form. Additionally, the reduced PS of baicalein microparticles contributed to the enhanced dissolution rate.
研究领域:
药剂学
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药物化学
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DOI
高影响因子
ARCHIVES OF MICROBIOLOGY
·
2024
·Vol. 206
·期 8
·1-26
·
IF 2.3
Li Can,Wang Jun,Li Hao,Wang Yemei,Wu Hui,Wei Wenfan,Wu Daqiang,Shao Jing,Wang Tianming,Wang Changzhong
Candida auris , a rapidly spreading multi-drug‐resistant fungus, is causing lethal infections under certain conditions globally. Baicalin (BE), an active ingredient extracted from the dried root of Scutellaria baicalensis Georgi, exhibits antifungal activity. However, studies have shown the distinctive advantages of Traditional Chinese medicine in combating fungal infections, while the effect of BE, an active ingredient extracted from the dried roots of Scutellaria baicalensis Georgi, on C. auris, remains unknown. Therefore, this study aims to evaluate the potential of BE as an antifungal agent against the emerging multidrug‐resistant C. auris . Various assays and models, including microbroth dilution, time growth curve analysis, spot assays, adhesion tests, flocculation test, cell surface hydrophobicity assay, hydrolase activity assays, XTT assay, violet crystal assay, scanning electron microscope (SEM), confocal laser scanning microscope (CLSM), flow cytometry, Live/dead fluorescent staining, reactive oxygen species (ROS), cell wall assay, aggregation assay, porcine skin model, Galleria mellonella larvae ( G. mellonella larvae) infection model, and reverse transcription–quantitative polymerase chain reaction (RT-PCR) were utilized to investigate how baicalein suppresses C. auris through possible multifaceted mechanisms. The findings indicate that BE strongly inhibited C. auris growth, adhesion, and biofilm formation. It also effectively reduced drug resistance and aggregation by disrupting the cell membrane and cell wall while reducing colonization and invasion of the host. Transcriptome analysis showed significant modulation in gene expression related to different virulence factors post‐BE treatment. In conclusion, BE exhibits significant effectiveness against C. auris , suggesting its potential as a viable treatment option due to its multifaceted suppression mechanisms. Graphical abstract Schematic representation of this study. Baicalein (BE) can effectively hinder the growth and colonization of C. auris by disrupting the expression of multiple virulence factors. This results in a strong antifungal effect, providing protection to the host from infection.
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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传染病学
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DOI
PubMed
高影响因子
PHYTOMEDICINE
·
2024
·
IF 6.7
Shanshan Guo,Lang Zhou,Xueqi Liu,Li Gao,Yuanyuan Li,Yonggui Wu
Background In acute kidney injury (AKI), ferroptosis is the main mechanism of cell death in the renal tubular epithelium. Baicalein, a traditional Chinese medicine monomer, plays a protective role in various kidney diseases; however, the effect of baicalein on ferroptosis in AKI still needs further exploration. Purpose In this study, we explored the role of baicalein and its specific mechanism in mediating ferroptosis in cisplatin-induced AKI. Methods We used a cisplatin-induced AKI model to study the effects of baicalein on renal tissue and tubular epithelial cell injury. The effects of baicalein on tubular epithelial cell ferroptosis were detected in cisplatin-induced AKI and further verified by folic acid-induced AKI. The Swiss Target Prediction online database was used to predict the possible mechanism by which baicalein regulates ferroptosis, and the specific target proteins were further verified. Molecular docking and SPR were used to further determine the binding potential of baicalein to the target protein. Finally, RNA interference (RNAi) technology and enzymatic inhibition were used to determine whether baicalein regulates ferroptosis through target proteins. Results Baicalein alleviated cisplatin- and folic acid-induced renal dysfunction and pathological damage and improved cisplatin-induced HK2 cell injury. Mechanistically, baicalein reduced the expression of 12-lipoxygenase (ALOX12), which inhibits phospholipid peroxidation and ferroptosis in AKI. Molecular docking and SPR demonstrated direct binding between baicalein and ALOX12. Finally, we found that silencing ALOX12 had a regulatory effect similar to that of baicalein. Comparable results were also obtained with the ALOX12 inhibitor ML355. Conclusion This was the first study to confirm that baicalein regulates ferroptosis both in vitro and in vivo in cisplatin-induced AKI and to verify the regulatory effect of baicalein in folic acid-induced AKI. Our results reveal the critical role of ALOX12 in kidney damage and ferroptosis caused by cisplatin and emphasize the regulatory effect of baicalein on renal tubular epithelial cell ferroptosis mediated by ALOX12. Baicalein is an effective drug for treating AKI, and ALOX12 is a potential drug target.
研究领域:
药理学
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肾病学
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细胞生物学
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分子生物学
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药物发现
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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）