Inorganics
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2024
·Vol. 12
·期 6
·154
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IF 3.1
Yujia Cheng,Yan Huang,Guang Yu
Carbon dots (CDs) have emerged as significant fluorescent nanomaterials due to their bright, stable fluorescence, good biocompatibility, facile synthesis, etc. They are widely used in various scientific and practical applications, particularly in combination with mesoporous, florescent, or magnetic nanomaterials to enhance their properties. Recent research has focused on employing CDs and their composites in drug analysis, drug loading, biological imaging, disease diagnosis, and temperature sensing, with a growing interest in their biological and medical applications. In this study, we synthesized blue-fluorescent S, N-co-doped CDs (cys-CDs) using hydrothermal synthesis with L-cysteine and sodium citrate. These resulting cys-CD particles were approximately 3.8 nm in size and exhibited stable fluorescence with a quantum yield of 0.66. By leveraging the fluorescence quenching of the cys-CDs, we developed a rapid and sensitive method for baicalein detection, achieving high sensitivity in the low micromolar range with a detection limit for baicalein of 33 nM. Our investigation revealed that the fluorescence-quenching mechanism involved static quenching and inner-filter effect components. Overall, cys-CDs proved to be effective for accurate quantitative baicalein detection in real-world samples.
研究领域:
材料科学
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生物医学
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DOI
高影响因子
Frontiers in Chemistry
·
2020
·
IF 3.693
Zhang Jianming,Teng Chao,Li Caolong,He Wei
Macrophages are potent to modulate inflammation via phenotypic switch and production of inflammatory factors. Baicalein (BCL) is frequently used to alleviate inflammation; however, its application is always hindered due to low solubility. Herein, BCL nanocrystals (BNRs) were prepared to improve its delivery to macrophages. The prepared BNRs have a diameter of 150 nm with a rod-like structure. The nanocrystals could be well-taken up by macrophages via the caveolar pathway and, therefore, promote the polarization switch from proinflammatory phenotype to anti-inflammatory macrophages and alleviate the inflammation via reducing production cytokine IL-12. In conclusion, the crystallization strategy is promising for the improvement of the solubility of BCL and promotion of its anti-inflammatory activities.
研究领域:
药理学
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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
Clinical and Translational Medicine
·
2020
·Vol. 10
·期 4
·e154
·
IF 7.919
Xiaoxuan Yu,Hui Li,Po Hu,Yingjie Qing,Xiangyuan Wang,Mengyuan Zhu,Hongzheng Wang,Zhanyu Wang,Jingyan Xu,Qinglong Guo,Hui Hui
Background Although targeting histone deacetylases (HDACs) may be an effective strategy for core binding factor-acute myeloid leukemia (CBF-AML) harboring t(8;21) or inv(16), HDAC inhibitors are reported to be limited by drug-resistant characteristic. Our purpose is to evaluate the anti-leukemia effects of Baicalein on CBF-AML and clarify its underlying mechanism. Methods Enzyme activity assay was used to measure the activity inhibition of HDACs. Rhodamine123 and RT-qPCR were employed to evaluate the distribution of drugs and the change of ATP-binding cassette (ABC) transporter genes. CCK8, Annexin V/PI, and FACS staining certified the effects of Baicalein on cell growth, apoptosis, and differentiation. Duolink and IP assay assessed the interaction between HDAC-1 and ubiquitin, HSP90 and AML1-ETO, and Ac-p53 and CBFβ-MYH11. AML cell lines and primary AML cells-bearing NOD/SCID mice models were used to evaluate the anti-leukemic efficiency and potential mechanism of Baicalein in vivo. Results Baicalein showed HDAC-1/8 inhibition to trigger growth suppression and differentiation induction of AML cell lines and primary AML cells. Although the inhibitory action on HDAC-1 was mild, Baicalein could induce the degradation of HDAC-1 via ubiquitin proteasome pathway, thereby upregulating the acetylation of Histone H3 without promoting ABC transporter genes expression. Meanwhile, Baicalein increased the acetylation of HSP90 and lessened its connection to AML1/ETO, consequently leading to degradation of AML1-ETO in t(8;21)q(22;22) AML cells. In inv(16) AML cells, Baicalein possessed the capacity of apoptosis induction accompanied with p53-mediated apoptosis genes expression. Moreover, CBFβ-MYH11-bound p53 acetylation was restored via HDAC-8 inhibition induced by Baicalein contributing the diminishing of survival of CD34 + inv(16) AML cells. Conclusions These findings improved the understanding of the epigenetic regulation of Baicalein, and warrant therapeutic potential of Baicalein for CBF-AML.
研究领域:
肿瘤学
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分子生物学
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药理学
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表观遗传学
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DOI
PubMed
高影响因子
PHYTOMEDICINE
·
2020
·
IF 4.268
Yanyu Chen,Zean Zhao,Yongmei Li,Yang Yang,Lu Li,Yu Jiang,Cuiting Lin,Ying Cao,Pingzheng Zhou,Yuanxin Tian,Ting Wu,Jianxin Pang
Background Insufficient renal urate excretion and/or overproduction of uric acid (UA) are the dominant causes of hyperuricemia . Baicalein (BAL) is widely distributed in dietary plants and has extensive biological activities , including antioxidative, anti-inflammatory and antihypertensive activities. Purpose: To investigate the anti-hyperuricemic effects of BAL and the underlying mechanisms in vitro and in vivo . Methods We investigated the inhibitory effects of BAL on GLUT9 and URAT1 in vitro through electrophysiological experiments and 14 C-urate uptake assays . To evaluate the impact of BAL on serum and urine UA, the expression of GLUT9 and URAT1, and the activity of xanthine oxidase (XOD), we developed a mouse hyperuricemia model by potassium oxonate (PO) injection. Molecular docking analysis based on homology modeling was performed to explain the predominant efficacy of BAL compared with the other test compounds. Results BAL dose-dependently inhibited GLUT9 and URAT1 in a noncompetitive manner with IC 50 values of 30.17 ± 8.68 μM and 31.56 ± 1.37 μM, respectively. BAL (200 mg/kg) significantly decreased serum UA and enhanced renal urate excretion in PO-induced hyperuricemic mice. Moreover, the expression of GLUT9 and URAT1 in the kidney was downregulated, and XOD activity in the serum and liver was suppressed. The docking analysis revealed that BAL potently interacted with Trp336, Asp462, Tyr71 and Gln328 of GLUT9 and Ser35 and Phe241 of URAT1. Conclusion These results indicated that BAL exerts potent antihyperuricemic efects through renal UA excretal promotion and serum UA production. Thus, we propose that BAL may be a promising treatment for the prevention of hyperuricemia owing to its multitargeted inhibitory activity.
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PubMed
高影响因子
Advances in Pharmacological and Pharmaceutical Sciences
·
2024
·Vol. 2024
·期 1
·2869332
·
IF 2.1
Dong Yuan,Wenbo Xu,Faisal Raza,Hajra Zafar,Shuangxian Guan,Zhen Wang,Kamran Hidayat Ullah,Hongchao Shi
High mortality and disability have been principally linked with traumatic brain injury (TBI) with this condition being a principal issue in public health. Currently, there is no reliable pharmaceutical agent to salvage the damage caused by TBI. Baicalein (BCL), a traditional Chinese medicine active ingredient, has preliminarily shown repair activity on brain injury. However, BCL has poor water solubility and bioavailability, which culminates in rapid elimination in vivo. Herein, we sought to solve the above-mentioned challenges that are associated with the application of this flavonoid by preparing BCL-loaded long-circulating liposomes (BLC-Lips) via thin-film hydration method. Subsequently, BLC-Lips were applied to TBI model mice to evaluate their effect on brain injury repair. The results showed that the prepared BLC-Lips exhibited smaller sized nanoparticles, excellent polydispersed index (PDI), and zeta ( ζ )-potential with stable property. After loading of BCL into the liposomes, we estimated the physicochemical properties of BLC-Lips to be roughly 87.98% (encapsulation efficiency [EE]) and 7.56% (loading capacity of the drug). Administration of BLC-Lips through oral route increased aqueous solubility, bioavailability, and time for in vivo circulation of BCL. Moreover, the BLC-Lips could improve outcomes of histological and neurological motor function and reduce inflammatory cytokines and neurotoxicity after TBI. Taken together, the long-circulating liposomes may serve as a new approach to potentially prolong drug circulation in vivo and increased bioavailability of BCL for TBI treatment.
研究领域:
药学
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神经科学
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生物技术
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药理学
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DOI
PubMed
高影响因子
FASEB JOURNAL
·
2026
·Vol. 40
·期 19
·e72336
·
IF 4.3
Zengfeng Guo,Ningfeng Zhang,Junshen Huang,Wang Zhang,Yawei Hu,Shaochu Chen,Ming Gong,Jianhua Zhou,Jiancheng Yang,Jiawen Wu
Postmenopausal osteoporosis (PMOP) is frequently complicated by iron accumulation, which exacerbates bone loss. Baicalein, a natural flavonoid with iron-chelating and antioxidant properties, has shown bone-protective effects, but its role in iron-overloaded PMOP remains unclear. This study investigated whether baicalein ameliorates iron-accumulated PMOP by inhibiting osteoclastogenesis via Nrf2 activation. In vitro, bone marrow-derived macrophages (BMMs) were induced into osteoclasts with RANKL under iron overload. Baicalein (10 μM) suppressed osteoclast differentiation, F-actin ring formation, and bone resorption, reduced intracellular and mitochondrial ROS, lowered Fe 2+ and total iron content, and upregulated Nrf2 nuclear translocation and HO-1 expression. These effects were abrogated by the Nrf2 inhibitor ML385 or Nrf2 siRNA. In vivo, an ovariectomized (OVX) mouse model with iron dextran injection (100 mg/kg/week) was used. Oral baicalein treatment (100 mg/kg/day) significantly prevented bone loss, improved bone microarchitecture and biomechanical properties, reduced iron deposition in bone, liver and spleen, lowered serum ferritin and bone ROS, and activated Nrf2 signaling in bone tissue. Co-administration of ML385 reversed these protective effects. Collectively, baicalein ameliorates iron-accumulated postmenopausal osteoporosis by activating the Nrf2 pathway, thereby inhibiting osteoclast differentiation and bone resorption. Baicalein represents a promising multi-target candidate for treating PMOP, especially in patients with concomitant iron accumulation. Graphical Baicalein inhibits osteoclastogenesis in vitro and attenuates iron accumulation-associated postmenopausal osteoporosis in vivo. Mechanistically, baicalein targetedly activates Nrf2, subsequently leading to the activation of antioxidant enzymes, which facilitates the elimination of intracellular ROS. The reduced ROS levels attenuate RANKL-induced NFATc1 expression, thereby suppressing the transcription of osteoclast-related genes and ultimately inhibiting osteoclastogenesis.
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DOI
PubMed
高影响因子
Journal of Materials Chemistry B
·
2026
·
IF 6.2
Mengting Chen,Lu Han,Sai Li,Yuji Pu,Bin He,Qingqing Pan
Natural bioactive compounds possess significant antioxidant and anti-inflammatory activity, offering a promising natural alternative or complement to current immunosuppressive therapies for ulcerative colitis (UC). However, achieving effective colon-targeted delivery of these compounds remains a significant challenge due to premature drug release and limited local retention. In this study, we present a nanoparticle–hydrogel composite system, BZH@HCE, designed to enhance the therapeutic efficacy of baicalein (BA) for UC treatment. Zein and oxidized hyaluronic acid-based nanoparticles (BZH) provide a high loading capacity for BA and prevent premature drug release in the upper gastrointestinal tract. BZH encapsulation within an epigallocatechin gallate (EGCG)-containing hydrogel matrix (HCE) further sustains BA release and amplifies its antioxidant and anti-inflammatory effects through synergistic action with EGCG. The adhesive hydrogel matrix ensures prolonged colon retention for up to 24 hours in colitis mice. In vivo studies using a dextran sulfate sodium-induced murine colitis model demonstrates that BZH@HCE significantly alleviates intestinal inflammation, promotes epithelial barrier repair, and shows excellent biocompatibility, outperforming both free BA and BZH nanoparticles. These findings position BZH@HCE as a versatile and effective platform for UC therapy, highlighting its potential as a natural, bioactive compound-based treatment.
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DOI
PubMed
高影响因子
JOURNAL OF SUPERCRITICAL FLUIDS
·
2025
·
IF 4.4
Zhongfeng Geng,Mingyu Yan,Yongxin Feng,Huisheng Lv
Baicalein, which exhibits antioxidant activity and wogonin, with anticancer activity, can be extracted from Scutellaria baicalensis Georgi. Their similar structures pose a challenge to further isolation. Supercritical Fluid-Simulated Moving Bed (SF-SMB) can function as a large-scale green separation process based on the adsorptive difference between them. The adsorption data of baicalein and wogonin on ZorBax SB-CN column in supercritical carbon dioxide/methanol were determined using the Elution by Characteristic Points method and could be well fitted by Langmuir model. At lower temperature or lower density of mobile phase, the adsorption capacity increased, with the maximum being 70.10 kg/m 3 for baicalein and 45.25 kg/m 3 for wogonin. The diffusion coefficients of the baicalein and wogonin were determined by the Taylor-Aris peak broadening method. They decreased with higher pressure, lower temperature, or higher density of the mobile phase. This work offers basic data support for the design of SF-SMB systems and industrial platform technology.
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高影响因子
Frontiers in Microbiology
·
2025
·
IF 4.5
Reng Qiu,Jun Li,Changjun Jiang,Yang Yu,Dandan Li,Xuehan Xie,Yang Lei,Lunguang Yao
Introduction: Aeromonas hydrophila (AH) is a pathogenic bacterium commonly found in aquatic organisms, particularly in fish products. Baicalein, a bioactive flavonoid derived from traditional Chinese herbal medicine, possesses a wide range of pharmacological properties, including anticancer, antibacterial, antiviral, antioxidant, hepatoprotective, and anti-inflammatory effects.Methods: In vitro, the Oxford cup method was employed to assess the antibacterial activity of baicalein, while the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were determined using the microtiter broth dilution technique. Biofilm formation and bacterial motility were evaluated through the crystal violet assay and swimming assay, respectively. The impact of baicalein on bacterial membrane permeability and morphology was observed using the Live/Dead BacLight kit and transmission electron microscopy. In vivo, grass carp were used as the model organism to evaluate the effect of baicalein on AH proliferation, while the expression of pro-inflammatory cytokines and antioxidant factors was quantified by qRT-PCR.Results: This study demonstrated the antibacterial activity of baicalein against AH infection. Baicalein exhibited bacteriostatic effects in vitro, with an MIC of 40 μg/mL and an MBC of 80 μg/mL. Time-kill assays confirmed its bactericidal properties. Additionally, baicalein inhibited biofilm formation and reduced bacterial motility. The antibacterial mechanism of baicalein involved increased membrane permeability and structural disruption of AH cells. In vivo studies in grass carp revealed a dose-dependent reduction in AH burden following baicalein administration. Moreover, baicalein suppressed the expression of pro-inflammatory cytokines, including interleukin-1β (IL-1β), interleukin-8 (IL-8), and tumor necrosis factor-α (TNF-α), while enhancing the expression of antioxidant-related genes, such as catalase (CAT), glutathione reductase (GR), and superoxide dismutase (SOD). These findings indicate that the antibacterial and anti-inflammatory effects of baicalein contribute to its protective role against AH infection in vivo.Discussion: Baicalein effectively inhibits the proliferation of AH both in vitro and in vivo, highlighting its potential as a promising pharmacotherapeutic agent for the prevention of AH infections in fish.
研究领域:
微生物学
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药理学
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水产养殖
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免疫学
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分子生物学
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鱼类疾病
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产品关联
DOI
PubMed
高影响因子
DYES AND PIGMENTS
·
2026
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IF 3.9
Xuemei Sun,Jiahao Li,Suyu Jiang,Lin Zang,Rong-Mei Kong,Yan Zhao,Weiheng Kong
The escalating incidence of antibacterial resistance presents a formidable challenge in managing bacterial infections. Traditional Zn-based antibacterial agents face limitations due to their reliance on ultraviolet activation and potential neurotoxicity. The combination of nanotechnology and traditional Chinese medicine (TCM) not only reduces the side effects of Zn 2+ but also enhances therapeutic efficacy. In this study, we synthesized Zn-baicalein nanoparticles (Zn-BE NPs) that self-assemble through chemical coordination, offering broad-spectrum antibacterial capabilities. The Zn component exhibited inherent antibacterial properties by disrupting the synthesis of bacterial metabolic enzymes and destroying genetic factors. Baicalein (BE), derived from Scutellaria , enhanced the NPs’ antibacterial efficacy by disrupting bacterial membranes and facilitating Zn 2+ influx, leading to cell wall rupture and metabolic disruption. In addition, Zn-BE NPs exhibited excellent photothermal conversion efficiency, enabling effective bactericidal action under near-infrared irradiation. This triple synergistic mechanism not only overcame the limitations of conventional Zn-based therapies but also sustained long-term antibacterial activity by preventing rapid bacterial metabolism. Our findings demonstrated that Zn-BE NPs could achieve complete bacterial eradication, showcasing expected potential in addressing antibacterial resistance. This research laid a foundation for the development of safer and more effective antibacterial agents, with implications for future applications in combating resistant infections.
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高影响因子
JSFA Reports
·
2024
·
IF 0
Rui-Yan Peng,Meng-Yao Hu,Hai-Xia Xu,Wen-Jun Wang,Zhong-Ping Yin,Ji-Guang Chen,Qing-Feng Zhang
Background Obesity is increasing seriously worldwide. Inhibiting pancreatic lipase (PL) is an important way to prevent obesity. Baicalein, a dietary flavone, shows various physiological activities and has anti-obesity potential. Therefore, the inhibitory activity of baicalein on PL was investigated in present study. Results Baicalein exhibited a significant inhibitory effect on PL with IC 50 value of 68 μg/mL. Inhibition kinetics indicated that baicalein was a mixed-type inhibitor of PL. Fluorescence titration showed that baicalein could induce fluorescence quenching of PL. The binding constant (logK a ) and number of binding sites were calculated as 5.40 and 1.11, respectively. In addition, synchronous fluorescence analysis revealed that the quenching ratio of baicalein to tryptophan was greater than that of tyrosine. Circular dichroism (CD) spectrum showed that the binding of baicalein affected the secondary structure of the enzyme protein. Through molecular docking analysis, it confirmed that baicalein could interact with amino acid residues in lipase, thus reducing the enzyme catalytic activity. In vivo studies showed that oral administration of baicalein with a does of 50 mg/kg bwt significantly reduced fat absorption and increased its fecal excretion in rats. Conclusion Baicalein showed inhibitory activity on PL in both in vitro and in vivo studies. It may be a safe and effective dietary supplement for obesity prevention.
研究领域:
生物化学
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药理学
·
营养学
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DOI
LIFE SCIENCES
·
2020
·
IF 3.647
Meifang Wang,Yinping Dong,Jing Wu,Hongyan Li,Yuanyang Zhang,Saijun Fan,Deguan Li
Aims Ionizing radiation (IR) induces injuries to the hematopoietic and intestinal systems, which are the leading cause of death. Baicalein, a plant-derived flavonoid, shows anti-oxidative stress, anti-apoptosis, anti-inflammation effects in many diseases. In this study, we evaluated the effects and mechanism of baicalein on IR induced intestinal and hematopoietic injuries. Main methods Mice were divided into three groups: Control, IR and IR + Baicalein. All of mice were intraperitoneally administered with 100 mg/kg baicalein or normal saline for 1 h before IR, and then a day post-IR. The changes in intestinal structure, function and molecular expression were observed by pathological experiments and western blot. 16S rRNA gene sequencing was performed to analyze gut microbiota and further predicted metabolic pathways through Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis. Hematopoietic function was evaluated by peripheral blood cells count and by flow cytometry analysis of hematopoietic cells composition. Key findings Baicalein improved intestinal structure and the ability of proliferation and regeneration after mice exposed to IR, in which the rebalance of gut microbial composition played an important role. KEGG results showed that p53-related apoptotic pathways played important roles in the composition changes of gut microbiota. Then we observed that baicalein inhibited the activation of p53 and p53 mediated mitochondrial apoptosis and death receptor apoptosis in the intestine. In addition, IR induced injuries to hematopoietic system also could be ameliorated by baicalein. Significance These results provide new insights into the mechanism of baicalein and support the potential of baicalein as a radioprotective medicine.
研究领域:
药理学
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放射生物学
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免疫学
·
微生物学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
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