Foods
·
2022
·Vol. 11
·期 2
·165
·
IF 5.561
Ang Li,Lei Chen,Weijie Zhou,Junhui Pan,Deming Gong,Guowen Zhang
Two flavonoids with similar structures, baicalein (Bai) and chrysin (Chr), were selected to investigate the interactions with β-lactoglobulin (BLG) and the influences on the structure and functional properties of BLG by multispectral methods combined with molecular docking and dynamic (MD) simulation techniques. The results of fluorescence quenching suggested that both Bai and Chr interacted with BLG to form complexes with the binding constant of the magnitude of 105L·mol−1. The binding affinity between BLG and Bai was stronger than that of Chr due to more hydrogen bond formation in Bai–BLG binding. The existence of Bai or Chr induced a looser conformation of BLG, but Chr had a greater effect on the secondary structure of BLG. The surface hydrophobicity and free sulfhydryl group content of BLG lessened due to the presence of the two flavonoids. Molecular docking was performed at the binding site of Bai or Chr located in the surface of BLG, and hydrophobic interaction and hydrogen bond actuated the formation of the Bai/Chr–BLG complex. Molecular dynamics simulation verified that the combination of Chr and BLG decreased the stability of BLG, while Bai had little effect on it. Moreover, the foaming properties of BLG got better in the presence of the two flavonoids compounds and Bai improved its emulsification stability of the protein, but Chr had the opposite effect. This work provides a new idea for the development of novel dietary supplements using functional proteins as flavonoid delivery vectors.Keywords:baicalein;chrysin;β-lactoglobulin;functional property;spectrophotometry;molecular dynamics simulation
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EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
·
2021
·
IF 4.384
Meng Tong,Xiaoyan Wu,Shuya Zhang,Di Hua,Shukun Li,Xiangyu Yu,Jing Wang,Zhenhai Zhang
The oral bioavailability and efficacy of baicalein is dramatically limited by its low solubility and effect of efflux. In our study, we chose PVP-VA64 as a carrier and TPGS as a plasticizer and efflux inhibitor to prepare a solid dispersion of baicalein using hot-melt extrusion technology to improve its solubility and bioavailability. The hot-melt process and formulation were optimized, and a BAC-PVP VA64-TPGS solid dispersion (BPT-SD) was prepared. BAC exists in an amorphous or molecular state in BPT-SD. BPT-SD comprised irregular lumps and small particles without BAC or carrier characteristics. The dissolution efficiency of BPT-SD improved under sink conditions. FTIR showed a strong hydrogen bond between BAC and PVP-VA64 in BPT-SD. BPT-SD maintained good physical stability for 6 months. The apparent permeability coefficient of BAC in the Caco-2 cell model confirmed that BPT-SD had higher gastrointestinal membrane permeability. A rat pharmacokinetic study showed that BPT-SD had higher C max and AUC 0- 24h, shorter T max , and 2.88-fold higher bioavailability than BAC. A behavioral experiment in chronic unpredictable mild stress (CUMS) mice confirmed the antidepressant efficacy of BAC. BPT-SD reversed depression-like behavior in CUMS mice and improved BAC bioavailability. BAC preparation into a solid dispersion significantly enhanced dissolution performance and bioavailability.
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Natural Product Communications
·
2021
·
IF 0.986
Wenyu Xin,Ming Jing,Junjie Yang,Meiling Wang,Guige Hou,Qiaoyun Wang,Leiming Zhang,Chunhua Wang
Emerging evidence indicates that NOD-like receptor protein 3 (NLRP3) inflammasome-induced inflammation plays a critical role in the pathogenesis of Parkinson’s disease (PD). Baicalein has been considered as a possible option for PD treatment based on its anti-neuroinflammatory effects. However, no studies have elucidated the precise mechanisms underlying the anti-neuroinflammatory activity of baicalein, particularly inflammasome-mediated effects. In this present study, rotenone-induced PD mice and BV2 microglia were used to investigate the anti-neuroinflammatory effects of baicalein and explore its underlying mechanism in vivo and in vitro. The results demonstrated that baicalein alleviated motor impairments and attenuated several inflammatory responses in rotenone-induced PD mice. Also, baicalein inhibited the expression of NLRP3 and activated caspase-1 in brain tissues. Correspondingly, baicalein prominently suppressed the inflammatory response in BV2 microglia induced by rotenone. Furthermore, in vitro data showed that baicalein suppressed the expression of NLRP3 and activated caspase-1 by abrogating the upregulation of ROS, as well as by inhibiting the TLR4/NF-κB signaling cascade. Overall, the results of the present study indicated that baicalein exerted anti-neuroinflammatory effects partly by inhibiting activation of the NLRP3 inflammasome, and targeting NLRP3 inflammasome signaling offers a novel therapeutic strategy for PD treatment.
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Food Bioscience
·
2024
·
IF 4.8
Qiuyan Jiang,Tiehua Zhang,Yuan Liang,Jie Zhang
The role of the pregnane X receptor (PXR) extended beyond regulating drug metabolism and transport, it also played a crucial part in lipid metabolism. Baicalein, a flavonoid derived from Scutellaria baicalensis , was demonstrated anti-inflammatory, anti-cancer, and anti-oxidative stress properties. Recent investigations reported its capacity to enhance lipid metabolism disorders. This study aimed to clarify the mechanism via which baicalein exerted its positive effects on lipid metabolism disorders by targeting PXR. The findings indicated that baicalein facilitated the nuclear translocation of PXR and controlled the expression of its target genes. In HepG2 cells with oleic acid and palmitic acid-induced lipid accumulation, baicalein treatment reduced the production of triglycerides, total cholesterol, and lipid droplets. In addition, it decreased the expression of sterol regulatory element-binding protein 1 (SREBP1), as well as lipogenic enzymes fatty acid synthase (FAS) and stearoyl-CoA desaturase-1 (SCD1). The results of computer simulation indicated that baicalein was a natural ligand of PXR. In conclusion, baicalein might potentially alleviate lipid metabolism disorders by targeting the PXR pathway.
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Heliyon
·
2024
·
IF 3.4
Guo-qiang Liang,Wei Mu,Chun-bo Jiang
Evidence indicates that Baicalein can ameliorate renal interstitial fibrosis by inducing myofibroblast apoptosis and inhibit the RLS3-induced ferroptosis in melanocytes. However, the relationship between renal interstitial fibrosis and anti-ferroptosis affected by Baicalein remains unclear. In our study, the anti-fibrosis and anti-ferroptosis effects of Baicalein were assessed in a rat model induced by the UUO method in vivo , and the effects of Baicalein on Erastin-induced ferroptosis of renal MPC-5 cells were examined by Western blot of fibrosis-related and ferroptosis-related proteins in vitro . In the UUO-induced rat model, Baicalein decreased kidney weight loss, improved renal function assessed the biomarks of urinary albumin excretion, serum creatine, and BUN levels, and reduced renal tubular injury. Furthermore, Baicalein inhibited renal ferroptosis by reducing ROS and MDA levels and increasing SOD and GSH levels in the UUO rat model. In addition, Baicalein potently reduced the expression of fibrosis-related proteins such as TGF-β1, a-SMA, and Smad-2 to prevent renal interstitial fibrosis, and increased the expression of ferroptosis-related proteins such as SLC7A11, GPX4, and FTH to inhibit ferroptosis both in vitro and in vivo . Taken together, Baicalein exerts anti-fibrosis activity by reducing the ferroptosis response on the UUO-induced rat model and renal MPC5 cells. Therefore, Baicalein, as a novel therapeutic method on kidney diseases with strong activity in suppressing ferroptosis, could be a potential alternative treatment for renal interstitial fibrosis.
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Chinese Herbal Medicines
·
2025
·
IF 8.9
Fuyun Chi,Wenshuang Wang,Shanshan Zhai,Man Zhang,Yuanyuan Hou,Gang Bai
Objective To explore novel anti-inflammatory strategies by targeting prostaglandin E2 (PGE2) overexpression, aiming to overcome the limitations of conventional cyclooxygenase-1/2 (COX-1/2) inhibitors such as nonsteroidal anti-inflammatory drugs (NSAIDs). Methods A correlation analysis of the anti-inflammatory activities of 24 exterior- releasing herb medicines, including NF- κ B, COX2, and PGE2 activities, was conducted, and the key active ingredients in the herbs showing significant associations were screened. Using a self-assembly technique, baicalein-2,4-decadienal (BD) were formulated into stable and homogeneous carrier-free nanoparticles to enhance drug solubility and targeting. Subsequently, disease models associated with PGE2 overexpression—fever, pneumonia and rheumatoid arthritis were established to evaluate the antipyretic, analgesic and anti-inflammatory properties of BD nanomedicines. Their targeting capability and drug release profile were also investigated. Results BD nanomedicines exhibited a synergistic inhibitory effect on PGE2 production by concurrently targeting COX2 and microsomal prostaglandin E synthase-1 (mPGES1), thereby producing antipyretic, analgesic, and anti-inflammatory effects superior to those observed with either agent alone. Furthermore, BD nanoparticles demonstrated preferential accumulation in macrophages implicated in the inflammatory response and facilitated pH-responsive drug release within the inflammatory microenvironment. This targeted delivery approach not only enhances therapeutic efficacy but also enables dose reduction and mitigates the risk of adverse effects, representing a promising strategy for the treatment of PGE2-mediated inflammatory diseases. Conclusion The findings provide new insights into drug development for inflammatory diseases caused by PGE2 overexpression, emphasizing the advantages of carrier-free supramolecular bioactive materials derived from natural products in the treatment of such diseases.
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FOOD CHEMISTRY
·
2026
·
IF 10.4
Jingjing Zhang,Hui Cao,Bing Li,Fuying Wang,Qin Duan,Yaru Li,Jinjin Pei,Hui Wang,Juan Carlos Mejuto,Jesús Simal-Gándara,Haolin Zhang
Heterocyclic amines (HCAs) are carcinogenic contaminants formed during meat thermal processing, and the traditionally recognized inhibitory effects of flavonoids on HCA formation remain controversial. Dihydromyricetin (DMY) and baicalein (BAI) both exhibited dose-dependent bidirectional effects on PhIP formation in a PhIP chemical model. At low concentrations (DMY 125–250 μM, BAI 125–1000 μM), PhIP levels gradually increased to nearly 210% and 300% of control, respectively, mainly driven by amination-related reactions of flavonoid thermal degradation products that promoted phenylacetaldehyde accumulation. At high concentrations (≥2000 μM), PhIP was suppressed to <50% (DMY) and <20% (BAI) of control via potent radical scavenging and phenylacetaldehyde trapping. The bidirectional regulation may be governed by a dynamic balance between amination-driven promotion and the dual inhibitory pathways for PhIP formation. This study explains how flavonoids lead to contradictory effects on HCA formation in cooked meat and provides a mechanistic foundation for their application.
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Smart Medicine
·
2026
·Vol. 5
·期 3
·e70047
·
IF 12.8
Zhiqiang Luo,Lingbao Zeng,Xinyu Zhu,Yuanjin Zhao
Synergy therapy of Chinese herbs is an effective strategy for wound repair and its further development focuses on the chronological release of specific herbs with healing proceeding. Herein, we report a novel asiatic acid/baicalein nanocarrier integrated microcapsule with spatiotemporal release feature from microfluidic electrospray for wound healing. Benefiting from advantages of both nanocarrier formulation and integration capacity of microfluidic electrospray, synthesized baicalein-tannic acid nanoparticles are integrated into the shell of microcapsule while fabricated asiatic acid liposomes are located at the core region. This design enables chronological release: baicalein is first released to kill bacteria, followed by releasing asiatic acid liposomes to enhance cell migration and granulation tissue formation. In vitro tests confirm the excellent biocompatibility, antibacterial and pro-migration property of microcapsules. The results from in vivo wound healing studies showed the outcomes of reduced inflammation and accelerated wound closure in microcapsules-treated wounds. Therefore, it is believed that this herbal microcapsule with spatiotemporal and hierarchical release of baicalein and asiatic acid is an effective therapeutic platform for clinical wound treatment. Highlights AA liposomes were derived from concentrated extrusion of AA and phospholipid molecule. Baicalein-tannic acid nanoparticles (BTANPs) were synthesized by solvent exchange. AA liposomes and BTANPs were integrated into ABNM by microfluidic electrospray. ABNM could chronologically release BTANPs and AA liposomes with their biodegradation. ABNM were highly curative to the healing of wounds.
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OPTICAL MATERIALS
·
2026
·
IF 4.3
Zhipeng Wang,Leyu Gao,Qifubo Geng,Zhuang Peng,Yang Gao,Xinrui Zhang,Huiyu Yang,Shengbo Zhang,Bo Su,Hailin Cui,Cunlin Zhang
Carbamazepine (CBZ) suffers from low solubility and dose-dependent hepatotoxicity. Baicalein (BAI), a liver-protective flavonoid, shares similar solubility limitations. Here we report the first synthesis of a CBZ-BAI cocrystal in a 1:1 M ratio via slow evaporation. The cocrystal was comprehensively characterized using terahertz time-domain spectroscopy from 0.2 to 2.2 THz, Raman spectroscopy from 50 to 2000 cm −1 , powder X-ray diffraction, and differential scanning calorimetry. Density functional theory DFT calculations were performed to assign the vibrational modes. The THz absorption spectrum shows the disappearance of the characteristic peaks of CBZ at 1.22 and 1.81 THz and of BAI at 1.21 and 2.18 THz. Importantly, a new peak emerges at 1.90 THz, which DFT assigns to hydrogen bonding vibrations between the –CONH 2 group of CBZ and the C O group of BAI, thus confirming cocrystal formation. Raman spectroscopy further supports this through changes in the 724 to 1310 cm −1 region. In simulated intestinal fluid at pH 6.8, the cocrystal improves CBZ solubility by 18% from 150.0 to 177.1 μg/mL and makes practically insoluble BAI detectable at 0.12 μg/mL. CCK-8 assays on mouse hepatocytes NCTC 1469 show that the cocrystal increases cell viability from 59.6% for CBZ alone to 76.1% at 12 h and from 61.9% to 68.3% at 24 h, indicating that cocrystal formation markedly reduces CBZ-induced hepatotoxicity. The CBZ-BAI cocrystal thus represents a promising strategy to simultaneously enhance solubility and mitigate drug-induced hepatotoxicity.
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Antioxidants
·
2026
·Vol. 15
·期 5
·544
·
IF 8.2
Lin Jiang,Xiaolei He,Yuxing Wang,Yang Liu,Xiubo Li,Fei Xu
Streptococcus agalactiae, also known asGroup B Streptococcus(GBS), is a major pathogen responsible for mastitis in dairy cows. It causes persistent and difficult-to-treat mammary infections, leading to reduced milk production. Baicalein, a flavonoid compound, exhibits anticancer, anti-inflammatory, and antibacterial activities; however, its specific mechanism of action against GBS remains unclear. This study aimed to investigate the mechanism by which baicalein inhibits GBS invasion of bovine mammary epithelial cells (bMECs). The results showed that baicalein at concentrations of 4 μg/mL or higher effectively inhibited 50% of the invasion of bMECs by GBS strain HB31 and exerted a concentration-dependent inhibitory effect on bacterial adhesion. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of baicalein against HB31 were both greater than 1024 μg/mL. Therefore, the antibacterial effect of baicalein alone may not fully account for its mechanism; other pathways likely contribute to the reduced invasiveness of GBS. To elucidate the mechanism by which baicalein inhibits GBS invasiveness, this study investigated both bacterial metabolism and gene expression. Metabolomic analysis revealed that baicalein treatment led to the downregulation of amino acid metabolites, including alanine and aspartic acid, as well as nucleotide metabolites such as adenine and UMP in GBS HB31. Additionally, the NADH/NAD+ratio increased while ATP levels decreased, indicating that the overall metabolic activity of GBS was suppressed. Transcriptomic analysis focused on changes in invasion-associated virulence genes. The results showed that the expression ofpbsP, an invasion-associated virulence gene, was significantly reduced, while the expression ofhylBandcfbshowed downward trends that did not reach statistical significance. In contrast, the expression ofcylEand the two-component systemvicKRwas upregulated. The upregulation ofcylEmay be related to baicalein-induced oxidative stress in HB31. Furthermore, HB31 suppressedNrf2-HO-1mRNA expression, whereas baicalein activated theNrf2signaling pathway and reduced HB31-inducedIL-6andNF-κBmRNA expression. These findings provide new insights for the development of anti-virulence therapeutic strategies targeting GBS.
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MOLECULES
·
2023
·Vol. 28
·期 7
·3262
·
IF 4.6
Shuya Xue,Min Shi,Jinye Wang,Jiapeng Li,Guanwei Peng,Jingkun Xu,Yansha Gao,Xuemin Duan,Limin Lu
In this work, TiO2-MXene/poly (3,4-ethylenedioxythiophene): poly(styrenesulfonate) (PEDOT:PSS) composite was utilized as an electrode material for the sensitive electrochemical detection of baicalein. The in-situ growth of TiO2nanoparticles on the surface of MXene nanosheets can effectively prevent their aggregation, thus presenting a significantly large specific surface area and abundant active sites. However, the partial oxidation of MXene after calcination could reduce its conductivity. To address this issue, herein, PEDOT:PSS films were introduced to disperse the TiO2-MXene materials. The uniform and dense films of PEDOT:PSS not only improved the conductivity and dispersion of TiO2-MXene but also enhanced its stability and electrocatalytic activity. With the advantages of a composite material, TiO2-MXene/PEDOT:PSS as an electrode material demonstrated excellent electrochemical sensing ability for baicalein determination, with a wide linear response ranging from 0.007 to 10.0 μM and a lower limit of detection of 2.33 nM. Furthermore, the prepared sensor displayed good repeatability, reproducibility, stability and selectivity, and presented satisfactory results for the determination of baicalein in human urine sample analysis.Keywords:TiO2-MXene;oxygen vacancy;PEDOT:PSS;baicalein;electrochemical sensor
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Biomed Research International
·
2018
·
IF 2.583
Xinggui Tian,Huaji Jiang,Yuhui Chen,Xiang Ao,Chuan Chen,Wentao Zhang,Feilin He,Xiaoqing Liao,Xiaocheng Jiang,Tao Li,Zhongmin Zhang,Xintao Zhang
Background. Tendon-bone healing is a reconstructive procedure which requires a tendon graft healing to a bone tunnel or to the surface of bone after the junction injury between tendon, ligament, and bone. The surgical reattachment of tendon to bone often fails due to regeneration failure of the specialized tendon-bone junction. Materials and Methods. An extra-articular tendon-bone healing rat model was established to discuss the effect of the baicalein 10 mg/(kg·d) in accelerating tendon-bone healing progress. Also, tendon-derived stem cells (TDSCs) were treated with various concentrations of baicalein or dickkopf-1 (DKK-1) to stimulate differentiation for 14 days. Results. In vivo, tendon-bone healing strength of experiment group was obviously stronger than the control group in 3 weeks as well as in 6 weeks. And there were more mature fibroblasts, more Sharpey fibers, and larger new bone formation area treated intragastrically with baicalein compared with rats that were treated with vehicle for 3 weeks and 6 weeks. In vitro, after induction for 14 days, the expressions of osteoblast differentiation markers, that is, alkaline phosphatase (ALP), runt-related transcription factor 2 (Runx2), osteocalcin (OCN), osterix (OSX), and collagen I, were upregulated and Wnt/β-catenin signaling pathway was enhanced in TDSCs. The effect of DKK-1 significantly reduced the effect of baicalein on the osteogenic differentiation. Conclusion. These data suggest that baicalein may stimulate TDSCs osteogenic differentiation via activation of Wnt/β-catenin signaling pathway to accelerate tendon-bone healing.
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