Advanced Composites and Hybrid Materials
·
2024
·Vol. 7
·期 6
·1-16
·
IF 23.2
Jiang Youwei,Sima Yingyu,Alomar Taghrid S.,AlMasoud Najla,El-Bahy Zeinhom M.,Feng Jinxia,Wan Kun,Toktarbay Zhexenbek,He Quanguo,Ding Jianhua,Wang Jingfeng,Wang Wu
The pursuit of rapid and sensitive detection methods for bioactive compounds in traditional Chinese medicine (TCM) is a continuous quest in the field of natural product chemistry. Herein, we report the development of a novel nanocomposite material comprising bismuth molybdate (Bi 2 MoO 6 ) and multi-walled carbon nanotubes (MWCNTs), which has been successfully applied to the ultrasensitive and simultaneous detection of the bioactive flavonoids baicalein and chrysin. These compounds, known for their potent anticancer and antioxidant properties, are prevalent in TCM and nutraceuticals. The Bi 2 MoO 6 -MWCNTs nanocomposite was meticulously characterized using X-ray diffraction (XRD), scanning electron microscopy (SEM), electrochemical impedance spectroscopy (EIS), and cyclic voltammetry (CV), revealing its structural and functional attributes. The optimized electrochemical sensor, based on a glassy carbon electrode modified with the nanocomposite, demonstrated remarkable sensitivity with a linear response range of 0.001–5.0 μmol·L −1 for baicalein and 0.007–3.0 μmol·L −1 for chrysin, alongside impressively low detection limits of 0.2 nmol·L −1 and 1.4 nmol·L −1 , respectively. The sensor’s performance was further validated through its application in the analysis of human serum and Scutellaria baicalensis extracts, showcasing its robust repeatability, selectivity, and stability. This work not only advances the field of TCM analysis but also opens new horizons for the integration of hollow bimetallic oxides with carbon-based materials in electrochemical sensing, offering a strategic approach to the rapid assessment of bioactive constituents in complex matrices.
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MICROCHEMICAL JOURNAL
·
2020
·
IF 3.594
Dandan Wang,Xinxin Luo,Yike Huang,Min Wang,Zhining Xia
A ternary deep eutectic solvent (DES) was applied as a novel functional monomer for synthesis of molecularly imprinted polymers (MIPs) to separate baicalein from the Scutellaria baicalensis Georgi ( S. baicalensis ). For rapid separation from the complex systems, modified Fe 3 O 4 particles were used as the magnetic cores to prepare magnetic deep eutectic solvent molecularly imprinted polymers (DES-MMIPs). The prepared DES-MMIPs were characterized by scanning electron microscopy, transmission electron microscopy, dynamic light scattering, Fourier transform infrared spectra, x-ray diffraction, thermal gravimetric analysis, vibrating sample magnetometer and BET analysis. Moreover, the adsorption capability and selectivity of DES-MMIPs to baicalein were investigated systematically. The results of adsorption experiments demonstrated that DES-MMIPs showed excellent binding capacity to baicalein and the selectivity of DES-MMIPs to baicalein was much higher than that of structure analogues (quercetin, hesperetin and keampferol). Finally, DES-MMIPs were applied in selective extraction of baicalein in the S. baicalensis by magnetic separation. The analysis was conducted by high performance liquid chromatography. The recoveries of baicalein in the S. baicalensis ranged from 91.6% to 99.3%. It had been proven that the DES-MMIPs were an innovative and effective adsorbent for selective recognition and separation of baicalein in complex systems.
研究领域:
药用植物化学
·
分析化学
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CELL BIOLOGY AND TOXICOLOGY
·
2026
·Vol. 42
·期 1
·68
·
IF 5.7
Li Ting,Feng Mengxiao,Wang Ping,Jiang Miao,Cui Jaiyu,Jin Mengxia,Song Congying,Lin Liying,Lu Yuan-Qiang
Baicalein, a naturally occurring flavonoid with well-documented anti-inflammatory and neuroprotective effects, has shown therapeutic promise in multiple models of neurological disorders. However, whether baicalein can counteract diquat-induced neurotoxicity remains uncertain. This study reveals that baicalein alleviates diquat-induced neuroinflammation and microglial pyroptosis in mice in a gut microbiota (GM)-dependent manner. In the in vivo experiments, multi-omics analyses demonstrated that baicalein elevates the GM-derived metabolite indole-3-propionic acid (IPA), which was sufficient to suppress pyroptosis. In parallel, IPA was identified as a critical mediator of baicalein's neuroprotective effects, as exogenous IPA administration recapitulated baicalein's protection, and baicalein treatment significantly elevated IPA levels. Mechanistically, through inhibiting the DEAD-box helicase 3 X-linked / GTPase-activating protein (SH3 domain) binding protein 1 pathway by in vitro experiments. Our study demonstrated that baicalein mitigates diquat-induced neuroinflammation, underscoring the therapeutic potential of targeting the GM to counteract herbicide-related neurotoxicity. Graphical
The alternative text for this image may have been generated using AI.
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JOURNAL OF MOLECULAR LIQUIDS
·
2023
·
IF 6
Jing Kong,Mingyuan Li,Yutong Li,Min Liu,Qian Zhang,Jie Liu,HongZhuan Xuan
A surfactant that can regulate interactions between drugs and proteins would be a material that is medicinally excipient and biomimetic that has great theoretical and practical significance. Thus, the interactions and binding mechanism of flavonoid isomers [galangin (Gal) and baicalein (Bai)] and hemoglobin (HB) under physiological conditions were studied using multispectral methods, dynamic light scattering (DLS), and antioxidant, antibacterial, and cytotoxicity assay techniques. Then, one bile salt biosurfactant [sodium taurodeoxycholate (NaTDC)] was added to explore the effects that it has on the interactions and functional properties of Gal-HB and Bai-HB systems. For Gal-HB and Bai-HB systems, the fluorescence quenching mechanism of flavonoids on HB was always a static quenching. Driven mainly by electrostatic forces, the conformation of HB became loose, and its secondary structure changed as a result of the presence of Gal or Bai. Three adjacent hydroxyl groups on the A-ring had an obvious binding interaction with protein, and thus, Bai had a stronger binding affinity with HB than Gal, and this has a greater influence on the secondary structure of HB than Gal. In the presence of NaTDC, the binding constants were significantly increased for both systems; also, the antioxidant character, stability, solubility, antibacterial properties, and cancer cell growth inhibition of flavonoids were improved to a certain extent. These findings help us understand the pharmacokinetics, pharmacodynamic function and mechanism of Gal and Bai at the molecular level and also lay the scientific foundation for the design of flavonoid-based foods and drugs.
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Journal of Biomedical Nanotechnology
·
2022
·Vol. 18
·期 10
·2350-2363
·
IF 3.641
Ji Shun-Li,Zhang Chun-Yan,Yin Xiao-Qin,Wang Jing,Wang Jia-Peng,Xu Xin
Due to low aqueous solubility and poor bioavailability of the flavone baicalein (BIC), a nano-micelle of delivery system was developed. Preparation of BIC-loaded crown ether-mPEG-PLGA micelle (BCPP-M) was performed via thin-film hydration method. Characterization of micellar excipients
was accomplished with 1H NMR, while evaluation of the optimal BCPP-M formulation was appropriately carried out through zeta potential (ZP), size of particles (PS), efficiency of encapsulation (EE) and capacity of drug loading (DL). We evaluated BIC release In-Vitro and profile
of In-Vivo pharmacokinetics. Evaluation of the anti-breast cancer property of BCPP-M using MCP-7 cells cytotoxicity and mice model was performed. Particles of BCPP-M were homogenously and spherically shaped with smaller average PS, coupled with higher EE and DL, good stability and polydispersity
index (PDI). The accumulative release of BCPP-M was obviously higher than free-BIC. Significantly, oral biological availability of BCPP-M was improved comparable to free BIC. Besides, half maximum inhibitory concentration (IC50) of BCPP-M in MCP-7 cells was lower than free-BIC. Animal experiments
also showed targeting, long circulation and antitumor potential of BCPP-M. Successful incorporation of BIC into long-acting and targeting micellar system could have enhanced solubility in aqueous media, oral In-Vivo availability and antitumor property of BIC.
研究领域:
药学
·
纳米技术
·
肿瘤学
·
生物药剂学
·
药理学
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BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
·
2025
·
IF 2.2
Han Lin,Yunlong Lv,Huacheng Liu,Zheng Lin,Ning Zhu,Bingwu Huang
Background As a persistent gastrointestinal disorder, irritable bowel syndrome (IBS) influences the gut-brain connection, leading to abdominal pain and altered bowel irregularities. Baicalein, a flavonoid extracted from Scutellaria baicalensis, is frequently utilized in anti-inflammatory treatments. This study aimed to explore baicalein's effectiveness in mitigating IBS symptoms triggered by both chronic and acute stress (CAS) and to uncover its fundamental mechanisms. Methods Sprague-Dawley rats were employed to develop an IBS rat model by inducing CAS for five weeks. Each rat was randomly allocated to one of four experimental groups: model (M), low-dose baicalein (L), high-dose baicalein (H), and control (C). Baicalein was orally administered throughout the experiment. Behavioral assessments were conducted, including forced swimming, marble-burying, intestinal motility, and visceral sensitivity tests. Colonic tissues were collected for histopathological examination, evaluation of oxidative stress (MDA and SOD levels), and analysis of inflammatory cytokines, and ODC1/NF-κB pathway activation using Western blot assay, ELISA, and immunofluorescence. Results Baicalein treatment notably ameliorated IBS-like symptoms, such as fecal pellet output and AWR scores, by alleviating stress-induced behavioral changes. Baicalein bolstered antioxidant defenses through boosting SOD activity and lowering MDA levels. Moreover, baicalein inhibited inflammatory responses, targeting IL-6, IL-1β, and TNF-α, while suppressing the expression of ODC1 and restraining NF-κB p65 phosphorylation within the colon. These results indicate that baicalein modulates oxidative stress and inflammation in CAS-associated IBS. Conclusion Baicalein demonstrates protection against CAS-induced IBS by diminishing intestinal inflammation, oxidative damage, and visceral hypersensitivity via suppression of the ODC1/NF-κB pathway. These findings underscore baicalein's potential as a therapeutic approach for IBS.
研究领域:
药理学
·
胃肠病学
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PROCESS BIOCHEMISTRY
·
2021
·
IF 3.757
Lingqi Wang,Changyong Cai,Jiajia Liu,Zhijian Tan
To explore convenient and efficient techniques for the extraction and separation of the active ingredients in medicinal plants is still ongoing. As a new class of molten salt, ionic liquids (ILs) are widely used in the extraction of bioactive compounds from plant resources. In this work, the IL-based biphasic system was developed for the extraction and separation of the homologues of baicalin and baicalein from Scutellaria baicalensis Georgi. The IL-water biphasic system is superior to the other organic solvents-water systems for the extraction and separation of baicalin and baicalein. The phase volume ratio of the IL-water biphasic system was studied, and the other influencing parameters of solid–liquid ratio, extraction temperature, extraction time, and ultrasonic time were optimized through the single factor experiments. The results revealed that the extraction yields were 43.3 mg/g and 14.3 mg/g for baicalin (aqueous phase) and baicalein (IL phase), respectively; and the distribution coefficients were 23.8 and 13.7 for baicalin and baicalein, respectively under the optimized conditions. Finally, the IL can be easily recycled and reused by means of its temperature-responsive characteristic. This study provides a green and efficient method for the selective separation of the homologues in natural plant resources.
研究领域:
药用植物学
·
分离科学与技术
·
绿色化学
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Pharmacology Research & Perspectives
·
2022
·Vol. 10
·期 1
·e00928
·
IF 2.963
Siyuan Cao,Min Zhang,Minyan Yuan,Dan Yang,Mei Zhao,Shuo Zhang,Pengjiao Wang,Rongping Zhang,Xiuli Gao
The bioavailability of drugs is often related to intestinal metabolism and transport mechanisms. In previous studies, pharmaceutical excipients were recognized as inert substances in clinical safety evaluations. However, a large number of studies have shown that pharmaceutical excipients regulate the metabolism and transport of drugs in the body and improve the bioavailability. The pharmaceutical excipient polyethylene glycol 400 (PEG400) as a good solubilizer and surfactant has the potential to improve the bioavailability of drugs. The combined action of UDP-glucuronosyltransferases (UGTs) and efflux transport proteins is responsible for the intestinal disposition and poor bioavailability of baicalein. Our aim is to study the effect of PEG400 on the absorption of baicalein on the Caco-2 monolayer, and confirm the interaction of PEG400 with UGTs (UGT1A8 and UGT1A9) and efflux transports. We initially found that baicalein in the Caco-2 monolayer would be metabolized into glucuronide conjugates BG and B6G under the action of UGT1A8 and UGT1A9 on the endoplasmic reticulum membrane, and then mainly excreted to different sides by acting of MRP and BCRP. The addition of PEG400 significantly accelerated the metabolism of B in Caco-2 cells and increased the penetration of BG and B6G. Furthermore, PEG400 also significantly decreased the efflux ratio of BG and B6G, which was the evidence of the interaction with the efflux transporters. In the in vitro intestinal microsome regeneration system, low concentration PEG400 decreased the K m value of UGT1A8 and UGT1A9 (key enzymes that mediate the production of BG and B6G); high concentration PEG400 enhanced the V max value of UGT1A8 and UGT1A9. In conclusion, our results determined that PEG400 interacted with some UGTs and efflux transporters, which were the main factors affecting the absorption of baicalein.
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Advanced Healthcare Materials
·
2025
·
IF 9.6
Yuhui Lu,Liying Zhou,Alu Ouyang,Xin Wang,Xiaoyang Wei,Shangping Xing,Feifei Nong,Jinquan Lin,Haotong Wang,Yuan Li,Jie Deng,Yilu Bao,Jie Yang,Ronghua Jin,Zhuo Luo
Herpes simplex virus type 1 (HSV-1) is a prevalent human pathogen primarily transmitted through skin-to-skin contact. Traditional antiviral drugs like acyclovir (ACV) have limitations due to viral resistance and side effects, necessitating the development of alternative therapeutic strategies. Drug-loaded hydrogels have emerged as a promising approach for managing various skin infections. Considering the low-pH microenvironment following HSV-1 infection, a pH-responsive baicalein@chitosan (B@C) hydrogel is developed for the topical treatment of HSV-1 skin infections. This hydrogel is synthesized by incorporating baicalein, a natural flavonoid, into a chitosan matrix modified with 4-formylphenylboronic acid and protocatechualdehyde to achieve potent anti-HSV-1 activity and pH-responsiveness. In vitro results demonstrated the hydrogel's pH-dependent inhibitory effect on HSV-1 infections, including ACV-resistant strains. Subsequent investigations confirmed its efficacy in multiple murine infection models. Mechanistically, the B@C hydrogel inhibited viral replication by modulating the phosphorylation of inhibitor of nuclear factor kappa-B kinase subunit beta, promoted collagen synthesis, and decreased reactive oxygen species generation. Ultra-high-performance liquid chromatography-tandem mass spectrometry analysis revealed a sustained release of baicalein from the hydrogel, ensuring long-term drug retention in HSV-1-infected skin tissues. Collectively, these findings suggest that the B@C hydrogel holds significant potential for the therapeutic management of HSV-1 skin infections.
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Antioxidants
·
2021
·Vol. 10
·期 6
·976
·
IF 6.313
Chongshan Dai,Hui Li,Yang Wang,Shusheng Tang,Tony Velkov,Jianzhong Shen
This study investigates the protective effect of baicalein on carbon tetrachloride (CCl4)-induced acute liver injury and the underlying molecular mechanisms. Mice were orally administrated baicalein at 25 and 100 mg/kg/day for 7 consecutive days or ferrostatin-1 (Fer-1) at 10 mg/kg was i.p. injected in mice at 2 and 24 h prior to CCl4injection or the vehicle. Our results showed that baicalein or Fer-1 supplementation significantly attenuated CCl4exposure-induced elevations of serum alanine aminotransferase and aspartate aminotransferase, and malondialdehyde levels in the liver tissues and unregulated glutathione levels. Baicalein treatment inhibited the nuclear factor kappa-B (NF-κB) pathway, activated the erythroid 2-related factor 2 (Nrf2)/heme oxygenase 1 (HO-1) pathway in liver tissues, and markedly improved CCl4-induced apoptosis, inflammation and ferroptosis in liver tissues exposed with CCl4. In vitro, baicalein treatment improved CCl4-induced decreases of cell viabilities and knockdown ofNrf2and arachidonate 12-lipoxygenase (ALOX12) genes partly abolished the protective effect of baicalein on CCl4-induced cytotoxicity in HepG2 cells. In conclusion, our results reveal that baicalein supplementation ameliorates CCl4-induced acute liver injury in mice by upregulating the antioxidant defense pathways and downregulating oxidative stress, apoptosis, inflammation and ferroptosis, which involved the activation of Nrf2 pathway and the inhibition of ALOX12 and NF-κB pathways.Keywords:baicalein;oxidative stress;ferroptosis;acute liver injury;ALOX12 pathway;Nrf2 pathway
研究领域:
药理学
·
肝病学
·
分子生物学
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PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY
·
2022
·
IF 5.201
Lina Ruan,Kaiyu Guan,Yue Wang,Ming Gu,Yue Chen,Lisha Cai,Ruixuan Ye,Zhengwei Huang,Anqi Guo,Zhengkang Su,Xi Li,Jianchun Pan
Post-traumatic stress disorder (PTSD) is a serious mental disease featured by a stress dysfunction that occurs after an individual has faced intense mental stress, often accompanied by anxiety and chronic pain. Currently, the mainstream drug for PTSD is serotonin reuptake inhibitors (SSRIs), however, their pain management for patients is limited. Baicalein , a Chinese traditional herbal medicine, has shown promising results in treating anxiety, depression, and pain. In this study, we found that baicalein may alleviate single prolonged stress (SPS)-induced PTSD-like behaviors in mice without altering baseline nociceptive sensitivity or activity. Meanwhile, baicalein increased the noradrenaline (NE) and serotonin (5-HT) content and decreased the ratio of 5-hydroxyindoleacetic acid (5-HIAA)/5-HT by inhibiting the activity of monoamine oxidase A (MAO-A) in SPS-induce mice. The anxiolytic and antinociceptive effects induced by baicalein were totally abolished by 5-HT depleting agents. Moreover, the anxiolytic effects of baicalein could be abolished by the 5-HT 1A receptor antagonist WAY-100635, and the analgesic effects could be abolished by delta-opioid receptor antagonists in the spinal. Taken together, our study provides compelling evidence that baicalein reversed anxiety-like behaviors and neuropathic pain in PTSD through serotonergic system and spinal delta-opioid receptors.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2022
·
IF 8.025
Shuoshuo Yang,Guoqi Ni,Mengyang Xia,Hailing Li,Zhonghong Gao
Oxidative stress is associated with most traumatic or pathological bone defects, and seriously affects the effect of implantation. The construction of antioxidative and osteogenic coatings is of great significance to accelerate the bone regeneration of implants. In this study, baicalein (BAI), a nature flavonoid drug, was loaded in bovine serum albumin (BSA) by desolvent method to prepare BAI-BSA composite protein, and tannic acid (TA)/BAI-BSA coatings were further built via layer by layer self-assembly technology. BAI-BSA possesses good biocompatibility that showed no cytotoxicity to osteoblasts and erythrocytes, and helps to enhance the activity of alkaline phosphatase (ALP) and promote the formation of osteogenic mineralized calcium nodules. After assembled with TA, BAI-BSA coating significantly promoted cell adhesion and in vitro osteogenic mineralization of MC3T3-E1. Moreover, BAI drug loading improved the antioxidative function of BSA coatings effectively. The scavenging rates of (TA/BAI-BSA-10) 4 for ABTS +• and DPPH • free radicals were 69.6 ± 16.1 % and 53.4 ± 2.4 %, respectively. At cellular level, the TA/BAI-BSA coating effectively inhibited the impact of oxidative stress on the oxidative damage of osteoblasts. The drug-loaded protein coatings possess both great antioxidative and osteogenic functions, which have important potential in the field of bone repair.
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