CANCER SCIENCE
·
2020
·Vol. 111
·期 10
·3802-3812
·
IF 4.966
Xiaolong Zhang,Qinli Ruan,Yiqian Zhai,Dandan Lu,Chen Li,Yahan Fu,Zihui Zheng,Ying Song,Jun Guo
Baicalein, a flavonoid phytochemical, has been shown to be effective as an anti-metastatic agent for various cancers, especially for non-small-cell lung cancer (NSCLC). However, the underlying mechanism of how baicalein targets cellular processes during NSCLC cell invasion and metastasis remains elusive. In this study, we found that non-cytotoxic concentrations of baicalein still retained anti-dissemination activity both in vitro and in vivo. Using a genetic encoding tension probe based on Förster resonance energy transfer (FRET) theory, baicalein was shown to significantly decrease ezrin tension by downregulating cellular ezrin S -nitrosylation (SNO) levels in NSCLC cells in the inflammatory microenvironment. Decreased ezrin tension inhibited the formation of an aggressive phenotype of NSCLC cell and leader cell in collective migration, and subsequently suppressed NSCLC dissemination. Baicalein restrained SNO-mediated ezrin tension by decreasing iNOS expression levels. Overall this study demonstrates the novel mechanism used by baicalein to suppress NSCLC invasion and metastasis from a mechanopharmacology perspective and illustrates a new direction for drug development.
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Arabian Journal of Chemistry
·
2024
·
IF 5.3
Xiaohai Chen,Fengsheng Hong,Hualu Wu,Yuxin Shen,Hailun Xia,Ren-ai Xu,Lu Shi
The primary objective of this study was to investigate the effects of baicalein and fangchinoline on the metabolism of abemaciclib. We hypothesized that these two natural compounds could significantly affect the metabolism of abemaciclib by inhibiting the activity of the CYP3A4 enzyme, thus potentially increasing its concentration in the body. In vitro , rat liver microsomes (RLM) and human liver microsomes (HLM) were employed to explore the inhibitory effects and mechanisms of baicalein and fangchinoline on abemaciclib. In vivo , twelve healthy male Sprague-Dawley (SD) rats were randomly assigned to three groups: Group A (control group), Group B (baicalein), and Group C (fangchinoline). The concentrations of abemaciclib and its metabolite N-desethylabemaciclib (M2) were evaluated using ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS). Finally, molecular docking method was employed to understand the interaction between abemaciclib and baicalein. It was indicated by the in vitro findings that both baicalein and fangchinoline inhibited abemaciclib metabolism in RLM through a mixed mechanism of competitive and non-competitive inhibition pathway. In HLM, baicalein inhibited abemaciclib metabolism by employing a hybrid mechanism of uncompetitive and non-competitive inhibition, while fangchinoline exhibited its inhibition in a competitive manner. In vivo , pharmacokinetic experiments revealed significant increases for AUC (0-t) and AUC (0-∞) of abemaciclib in Group B and Group C when compared to Group A, while the plasma clearance (CLz/F) of abemaciclib exhibited significant reductions. Moreover, molecular docking studies showed that both abemaciclib and baicalein docked to the active pocket of CYP3A4. This study demonstrated that the co-administration of baicalein or fangchinoline significantly affected the metabolism of abemaciclib, providing valuable insights for its clinical application.
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JOURNAL OF NANOPARTICLE RESEARCH
·
2026
·Vol. 28
·期 8
·199
·
IF 3.5
Li Xiuxiu,Wu Shaoquan,Shu Ying,Tong Yuna
Acute kidney injury (AKI) is a severe clinical challenge driven by oxidative stress and inflammation. Current therapeutic options for AKI remain limited. Herein, we developed a novel metal–phenolic nanoplatform named LBP@Ga-Bai NPs. We synthesized these nanoparticles by self-assembling baicalein (Bai) with gallium (Ga3⁺), followed by surface coating with Lycium barbarum polysaccharide (LBP). These nanoparticles showed excellent colloidal stability. Our in vitro studies showed that LBP@Ga-Bai NPs protected H₂O₂-injured HK-2 cells. They effectively scavenged ROS, colocalized with mitochondria, restored membrane potential, and prevented apoptosis. In a glycerol-induced AKI mouse model, oral delivery of LBP@Ga-Bai NPs significantly reduced kidney damage. They lowered serum creatinine by 43.48% and blood urea nitrogen by 41.09%. They also reduced tubular necrosis and tissue inflammation. Transcriptomic analysis further showed that the nanoparticles reversed metabolic dysfunction. They achieved this by reactivating organic acid catabolism and restoring the TCA cycle. In conclusion, LBP@Ga-Bai NPs offer a promising multifunctional treatment for AKI. They work effectively by clearing ROS, protecting mitochondria, and restoring metabolic balance.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2026
·
IF 8.7
Kaihan Li,Can Zhao,Kunshan Wang,Hongyu Liang,Suzhen Zhou,Jinbo Fan
β-Lg can simultaneously load and protect the three flavonoid compounds, namely Isl, Gen, and Bai. • In terms of stability, the β-Lg-multilinked compound shows a better protective effect against the three types of flavonoids. • A spectroscopic approach was adopted to elucidate the binding mechanisms of three flavonoids with β-Lg. • The conformational characteristics of the complexes were investigated through molecular docking and dynamics simulations. This study elucidates the interaction mechanisms of Isoliquiritigenin (Isl), Genistein (Gen) and Baicalein (Bai) with β-lactoglobulin (β-Lg), with a focus on the protein's capacity for the co-encapsulation and stabilization of these flavonoids. The binding mechanisms were characterized using fluorescence spectroscopy, high-performance liquid chromatography, non-radiative energy transfer analysis, molecular simulations. The results demonstrated that the binding affinity ( K a ) followed the order Bai > Gen > Isl. Accordingly, the calculated binding distances for Isl, Gen and Bai were 5.36 nm, 4.49 nm, and 4.20 nm, respectively. β-Lg is capable of co-encapsulating two or three flavonoids simultaneously. The most stable ternary complex (β-Lg-Isl-Gen-Bai) formed when the flavonoids were added in the sequence of Bai, Isl, and then Gen. The β-Lg multi-ligand complex provided superior protection for Isl, Gen, and Bai compared to their respective single-ligand complexes across all tested parameters: stability, antioxidant capacity, and α-amylase inhibition. For Isl, the retention rate improvement under storage stability is the largest, reaching 73.86 ± 1.04%; for Gen, the retention rate improvement under light stability is the largest, reaching 75.22 ± 0.77%; and for Bai, the retention rate improvement under thermal stability is the largest, reaching 71.90 ± 1.02%. β-Lg simultaneously encapsulates and stabilizes three flavonoids Isl, Gen, Bai, serves as a natural and potent protein carrier for these bioactive compounds, and offers theoretical support for their protection against degradation.
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JOURNAL OF FOOD COMPOSITION AND ANALYSIS
·
2023
·
IF 4.3
Shuting Shi,Yanping Wei,Jinxia Feng,Chuanqin Zhou,Jinsong Zuo,Liangyuan Yao,Jianhua Ding,Kanghua Li,Quanguo He
A bismuth oxide-carboxylated multi-walled carbon nanotube/glassy carbon electrode (Bi 2 O 3 -CMWCNTs/GCE) was prepared for the detection of the flavonoid drug baicalein . The Bi 2 O 3 was grown on the surface of CMWCNTs by in-situ synthesis, and a simple, and efficient Bi 2 O 3 -CMWCNTs composite was prepared. The materials were characterized by XRD, SEM and EDS. CV and EIS techniques were used to study the electrochemical sensing performance of the composite electrode surface. The electrochemical performance and optimal detection conditions of baicalein on Bi 2 O 3 -CMWCNTs/GCE were investigated by LSV. The oxidation peak current of baicalein has a linear relationship with its concentration in the range of 0.01–15 μmol·L −1 , with a detection limit of 2.0 nmol·L −1 . The method is both stable and effective, and was successfully used for determination of baicalein in human urine and the Chinese herb Oroxylum indicum. It shows that the in situ synthesized materials have more stable characteristics, and have promising applications in the detection of flavonoid drugs.
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Journal of Orthopaedic Translation
·
2022
·
IF 4.889
Feng-wei Zhang,Li-yang Peng,Chuan-Jian Shi,Jian-chi Li,Feng-xiang Pang,Wei-ming Fu,Xiao-hua Pan,Jin-fang Zhang
Background Osteosarcoma (OS) is a common type of malignant bone tumor in adolescents with high risk of metastasis. However, the clinical management still remains unsatisfactory. Traditional Chinese medicine (TCM) has been widely considered as an alternative treatment, and their extracts have proved to possess great potential for drug discovery. Baicalein (BA), the active pharmaceutical ingredient of rhizoma coptidis , was proved to have anti-tumor properties in OS, but the mechanism remains poorly understood. Methods The potential anti-cancer effects on cell growth, cell cycle, apoptosis and migration were examined in OS cells. Moreover, the lncRNA-Neighboring Enhancer of FOXA2 (lncRNA-NEF) and Wnt/β-catenin signaling were detected by qPCR and Western blotting assays. The in vivo effect of GA on tumor growth was investigated using a xenograft mice model. Results In the present study, BA was found to significantly suppress tumor growth in vitro and in vivo. And it was also found to inhibit the invasion and metastasis as well. As for the mechanism investigation, lncRNA-NEF was obviously upregulated by BA in OS cells, and thus induced the inactivation of Wnt/β-catenin signaling. Moreover, lncRNA-NEF knockdown partially reversed the BA-induced anti-cancer activities; and successfully compensated the suppressive effect on Wnt/β-catenin signaling. We therefore suggested that BA induced the inactivation of Wnt/β-catenin signaling through promoting lncRNA-NEF expression. Conclusions In conclude, our results demonstrated that BA suppressed tumor growth and metastasis in vitro and in vivo through an lncRNA-NEF driven Wnt/β-catenin regulatory axis, in which lncRNA-NEF was upregulated by BA, and thus induced the inactivation of Wnt/β-catenin signaling. The Translational potential of this article The findings derived from this study validates the anti-cancer activity of BA in OS and provides a novel underlying mechanism, which suggest that BA may be a potential candidate to develop the effective drug for OS patients.
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TALANTA
·
2017
·
IF 4.162
Zhengkun Xie,Wang Lu,Lingxi Yang,Gaiping Li,Baoxian Ye
Baicalein and baicalin are the major flavonoids found in Scutellariae Radix, an essential herb which has had a presence in traditional Chinese medicine (TCMs) for more than two thousands of years. Owing to their similar characteristics and physiochemical properties, sensitive, it is a great challenge to detect both of them simultaneously. In this work, a novel, facile and sensitive electrochemical method was proposed based on tantalum oxide (Ta 2 O 5 ), niobium oxide (Nb 2 O 5 ) particles and antiseptic chitosan modified carbon paste electrode (Ta 2 O 5 -Nb 2 O 5 @CTS-CPE). Scanning electron microscope (SEM), X-ray diffraction spectroscopy (XRD), Fourier transform infrared spectroscopy (FTIR), cyclic voltammetry (CV) and electrochemical impedance spectrum (EIS) were used to characterize the properties and investigate the electrochemical response of the sensor. The electrochemical behaviors and redox mechanisms of two analytes were investigated at the target electrode. Under the optimum conditions, the highly sensitive and simultaneous determination of baicalein and baicalin was successfully achieved with a linear response range of 0.08–8.0 μM for both of them. The obtained detection limits for baicalein and baicalin were of 0.05 and 0.03 μM (S/N=3), respectively. Furthermore, the proposed sensor displayed high sensitivity, excellent stability and satisfactory results in Scutellariae Radix samples analysis and hydrolysis process analysis of baicalin in vivo .
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BIOELECTROCHEMISTRY
·
2013
·
IF 3.947
Ying Zhang,Xuejing Wang,Lei Wang,Miao Yu,Xiaojun Han
The baicalin and baicalein are the major flavonoids found in Radix Scutellariae , an essential herb in traditional Chinese medicine for thousands of years. The interactions of the baicalin and baicalein with lipid bilayer membranes were studied using cyclic voltammetry and UV–Vis spectroscopy. The thickness d of supported bilayer lipid membranes was calculated as d = 4.59(± 0.36) nm using AC impedance spectroscopy . The baicalein interacted with egg PC bilayer membranes in a dose-dependent manner. The responses of K 3 Fe(CN) 6 on lipid bilayer membrane modified Pt electrode linearly increased in a concentration range of baicalein from 6.25 μM to 25 μM with a detection limit of 0.1 μM and current-concentration sensitivity of 0.11(± 0.01) μA/μM, and then reached a plateau from 25 μM to 50 μM. However the baicalin showed much weaker interactions with egg PC bilayer membranes. UV–Vis spectroscopy also confirmed that the baicalein could interact with egg PC membranes noticeably, but the interaction of baicalin with membranes was hard to be detected. The results provide useful information on understanding the mechanism of action of Radix Scutellariae in vivo.
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CURRENT MOLECULAR MEDICINE
·
2023
·
IF 2.5
Wang Qi,Zhang Aihua
Background: Oxidative stress is a key mechanism underlying arsenicinduced
liver injury, the Kelch-like epichlorohydrin-related protein 1 (Keap1)/nuclear
factor E2 related factor 2 (Nrf2) pathway is the main regulatory pathway involved in
antioxidant protein and phase II detoxification enzyme expression. The aim of the present
study was to investigate the role and mechanism of baicalein in the alleviation of
arsenic-induced oxidative stress in normal human liver cells.
Methods: Normal human liver cells (MIHA cells) were treated with NaAsO2 (0, 5, 10,
20 μM) to observe the effect of different doses of NaAsO2 on MIHA cells. In addition,
the cells were treated with DMSO (0.1%), NaAsO2 (20 μM), or a combination of NaAsO2
(20 μM) and Baicalein (25, 50 or 100 μM) for 24 h to observe the antagonistic effect
of Baicalein on NaAsO2. Cell viability was determined using a Cell Counting Kit-8
(CCK-8 kit). The intervention doses of baicalein in subsequent experiments were determined
to be 25, 50 and 100μM. The intracellular content of reactive oxygen species
(ROS) was assessed using a 2′,7′-dichlorodihydrofluorescein diacetate (DCFH-DA)
probe kit. The malonaldehyde (MDA), Cu-Zn superoxide dismutase (Cu-Zn SOD) and
glutathione peroxidase (GSH-Px) activities were determined by a test kit. The expression
levels of key genes and proteins were determined by real-time fluorescence
quantitative polymerase chain reaction (qPCR) and Western blotting.
Results: Baicalein upregulated the protein expression levels of phosphorylated Nrf2
(p-Nrf2) and nuclear Nrf2, inhibited the downregulation of Nrf2 target genes induced by
arsenic, and decreased the production of ROS and MDA. These results demonstrate
that baicalein promotes Nrf2 nuclear translocation by upregulating p-Nrf2 and inhibiting
the downregulation of Nrf2 target genes in arsenic-treated MIHA cells, thereby enhancing
the antioxidant capacity of cells and reducing oxidative stress.
Conclusion: Baicalein alleviated arsenic-induced oxidative stress through activation
of the Keap1/Nrf2 signalling pathway in normal human liver cells.
研究领域:
毒理学
·
分子生物学
·
细胞生物学
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COLLOIDS AND SURFACES B-BIOINTERFACES
·
2026
·
IF 5.9
Nan Wang,Shiyu Ma,Fangyu Jiao,Zhe Yu,Fengshu Fei,Jianting Huang,Chuanlong Guo
RL/BAI nanomicelles (~100 nm) enhance baicalein biocompatibility. • RL/BAI triggers mitochondrial dysfunction and mtDNA release in TNBC cells. • RL/BAI activates cGAS-STING pathway to suppress tumor growth and metastasis. Triple-negative breast cancer (TNBC) remains an intractable malignancy due to the lack of specific therapeutic targets and high metastatic potential. Herein, we fabricated rhamnolipid (RL)-encapsulated baicalein (BAI) nanomicelles (RL/BAI) via a thin-film hydration method. Molecular dynamics (MD) simulations revealed that RL and BAI spontaneously assembled into stable nanomicelles (~100 nm) driven by van der Waals and hydrophobic interactions, achieving high encapsulation efficiency (~85 %) and excellent biocompatibility. In 4T1 cells, RL/BAI nanomicelles enhanced cellular uptake and achieved efficient mitochondrial colocalization, triggering mitochondrial membrane potential (MMP) collapse, excessive mitochondrial reactive oxygen species (mtROS) generation, and mitochondrial DNA (mtDNA) release. These events activated the cGAS-STING pathway, as evidenced by increased phosphorylation of STING, TBK1, and IRF-3, together with upregulation of IFN-γ and NF-κB, ultimately promoting immunogenic cell death. In 4T1 xenograft models, RL/BAI significantly inhibited primary tumor growth and lung metastasis, remodeled the pro-inflammatory tumor microenvironment by upregulating pro-inflammatory cytokines and promoting dendritic cell maturation, with no obvious systemic toxicity. Collectively, RL/BAI nanomicelles exert anti-TNBC effects through mitochondrial damage and cGAS-STING pathway activation, providing a novel natural biosurfactant-based nanomedicine strategy for TNBC treatment.
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PLACENTA
·
2025
·
IF 2.5
Caiqun Huang,E Fen Cheng,Jinping Ni,Ying Lyu
Introduction Unexplained recurrent spontaneous abortion (URSA) involves multifactorial etiologies, with regulatory T cells (Tregs) playing a pivotal role in maintaining immune tolerance during pregnancy. Baicalein, a flavonoid from Scutellaria baicalensis, exhibits anti-inflammatory and immunomodulatory properties. This study evaluates baicalein's therapeutic potential in mitigating URSA via the TLR4/NF-κB signaling pathway. Methods A URSA mouse model was used, and baicalein was administered intraperitoneally. Pregnancy outcomes, abortion rates, and placental morphology were assessed on gestational day 14 (G14). Treg cells were quantified via flow cytometry, and gene/protein expression levels were analyzed by immunohistochemistry, Western blotting, and real-time PCR. In vitro experiments on ihESCs further investigated the role of the TLR4/NF-κB pathway. Results Baicalein reduced abortion rates from 33.3 % in URSA mice to 21.6 % (low dose) and 14.8 % (high dose), improved embryonic development by altering placental structure and decidual morphology, and reduced inflammation at the maternal-fetal interface. It expanded Treg cells and enhanced the expression of IGFBP-1 and PRL, markers of endometrial decidualization, and decreased TLR4, p-P65, and P65 expression. In vitro, baicalein's effects were abrogated by TLR4 inhibition, confirming pathway specificity. Discussion Baicalein improved pregnancy outcomes by enhancing Treg function and promoting decidualization via TLR4/NF-κB pathway inhibition. These findings highlight baicalein's potential as a therapeutic agent for URSA.
研究领域:
生殖医学
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免疫学
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药理学
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CARBOHYDRATE POLYMERS
·
2025
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IF 12.5
Huizhen Han,Zhen Wang,Tong Wu,Fangzheng Zhao,Shuaibing Huang,Boxuan Peng,Chunyue Zhao,Qiqi Han,Enchang Liu,Qingyun Liu,Jinfeng Xing
A key challenge in multifunctional injectable wound dressings is the lack of integration between the appropriate mechanical strength, the effects of antibacterial, antioxidant and pro-healing properties. In this study, a pioneering research has been designed with the polymerization between oxidized dextran (ODex) and carboxymethyl chitosan (CMCS) to develop a double cross-linked injectable hydrogel (OD/CM/BP@Bai). This hierarchical structure combines a physically entangled network (providing immediate mechanical integrity) and a dynamic covalent network (enabling self-healing and injectability), resulting in a composite hydrogel with a storage modulus (G') approximately twenty times higher than that of single-network ODex pre-gel. Innovatively, black phosphorus nanosheets (BPNS) were incorporated as dual-functional elements, acting concurrently as photothermal conversion agents and nanoscale drug reservoirs. Through π–π stacking interactions, a high drug loading rate of 5.6 % was achieved for the hydrophobic drug baicalein (Bai). Incorporation of the nanoparticles further enhanced the overall mechanical properties of the hydrogel. Under near-infrared (NIR) irradiation, the hydrogel enabled synergistic and on-demand therapy. The photothermal effect not only directly eradicated bacteria but also triggered rapid Bai release. Through the synergistic interaction of functional components (CMCS/Bai/BPNS), a responsive hydrogel integrating antibacterial, anti-inflammatory, and pro-regenerative performances was constructed, which provides an innovative solution for wound treatment.
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