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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2026 · IF 8.7

ROS-responsive multifunctional hyaluronic acid/gelatin based adhesive hydrogel encapsulating baicalin and cerium dioxide nanozymes accelerates infected diabetic wounds healing

Wei Lu,Yanming Zhao,Hao Wen,Jianxin Liu,Yulong Niu,Zhenwei Yang,Yongwei Su,Shuai Li,Nan Xia,Quan Chen

A multifunctional adhesive hydrogel with outstanding ROS-responsive release of baicalin was prepared. • The HA/Gel@CeO₂@BA hydrogel achieved dual immunomodulatory and reparative functionality. • The HA/Gel@CeO₂@BA hydrogel exhibited broad-spectrum antimicrobial efficacy • The HA/Gel@CeO₂@BA hydrogel effectively suppresses inflammation, promotes the healing of infected diabetic wounds. The management of chronic wounds in diabetic patients continues to pose a substantial clinical challenge, especially when complicated by methicillin-resistant Staphylococcus aureus (MRSA) infection, which exacerbates inflammation and impedes the healing process. To address this, we developed a Reactive Oxygen Species(ROS)-responsive, self-healing multifunctional hydrogel (HA/Gel@CeO₂@BA) incorporating baicalin (BA) and cerium dioxide (CeO₂) nanozymes with superoxide dismutase and catalase activities to synergistically provide antibacterial, antioxidant, anti-inflammatory, and pro-regenerative effects. The hydrogel comprises a dual-network structure: (1) a dynamic Schiff base-crosslinked network formed between hydrazine-modified hyaluronic acid (HA-DTPH) (containing disulfide bonds) and aldehyde-modified HA (HA-CHO), enabling tissue adhesion through amino-aldehyde bonding; and (2) a secondary network of gelatin methacrylate (GelMA) and acryloylated cyclodextrin, which anchors hydrophobic BA for sustained release. Dynamic Schiff base bonds and disulfide bonds undergo diabetes-responsive degradation via pathways involving reactive oxygen species, enabling drug release in response to the local environment. In vitro, HA/Gel@CeO₂@BA was found to scavenge ROS in macrophages, promote M2 polarization and enhance angiogenesis. It also exhibited strong antibacterial effects against Escherichia coli and S. aureus . In a diabetic rat model of infected wounds, the hydrogel significantly reduced the bacterial load and accelerated the healing process without the need for external intervention. This strategy combines ROS-triggered drug release and multifunctional therapeutic effects with biodegradability, demonstrating its high potential for clinical translation in the treatment of infected chronic wounds. Download: Download high-res image (133KB) Download: Download full-size image

✓ 已验证 DOI PubMed 高影响因子
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EUROPEAN JOURNAL OF PHARMACOLOGY · 2022 · IF 5.195

Baicalin ameliorates CUMS-induced depression-like behaviors through activating AMPK/PGC-1α pathway and enhancing NIX-mediated mitophagy in mice

Xiaohui Jin,Leilei Zhu,Shuaifei Lu,Caiyin Li,Ming Bai,Erping Xu,Jiduo Shen,Yucheng Li

Mitochondrial dysfunction has been reported to be involved in the pathogenesis of depression, and mitophagy is a key pathway for mitochondrial quality control. This study aimed to investigate the effect of baicalin on mitophagy in the hippocampus of mice exposed to chronic unpredictable mild stress (CUMS) and explore its potential mechanism. After exposure to CUMS for 6 weeks, mice were given baicalin (20 mg/kg) or fluoxetine (20 mg/kg) by oral gavage for 4 weeks, and HT22 cells were injured by corticosterone (CORT) in vitro. Depression-like behaviors were assessed by sucrose preference test and tail suspension test . The mitochondrial structure was observed by transmission electron microscopy . Detection of mitophagy and mitophagy-related protein by mitophagy kit and Western blot . The results showed that baicalin improved depressive-like behaviors in CUMS mice, and ameliorated mitochondrial structural impairment in the hippocampus neuron. Baicalin significantly down-regulated light chain 3(LC3)II/I, protein sequestosome 1 (P62), and translocase of the outer membrane 20 (TOM20), and up-regulated Nip-like protein (NIX), Adenylate activated protein kinase (AMPK), and Peroxisome proliferator-activated receptor-gamma coactivator (PGC)-1α. Furthermore, molecular docking showed that baicalin interacts with AMPK through hydrogen bonding. Baicalin increased NIX and AMPK, and improved mitophagy level and mitochondrial function in HT22 cells. Treatment with Phorbol 12-Myristate 13-acetate demonstrated that up-regulation of NIX ameliorated CORT-induced mitochondrial dysfunction in HT22 cells. In conclusion, the present study suggested that the antidepressant effect of baicalin may be related to the enhancement of NIX-mediated mitophagy through activating the AMPK/PGC-1α pathway by directly binding to AMPK.

CAS / MDL: 21967-41-9
研究领域: 神经科学 · 药理学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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NANOTECHNOLOGY · 2022 ·Vol. 33 ·期 43 ·435101 · IF 3.953

Activating caspase-8/Bid/ROS signaling to promote apoptosis of breast cancer cells by folate-modified albumin baicalin-loaded nanoparticles

Meng Lan,Zhaodi Kong,Fengjie Liu,Tengteng Zou,Lihong Li,Tiange Cai,Huaqin Tian,Yu Cai

Abnormal apoptosis can lead to uncontrolled cell growth, aberrant homeostasis or the accumulation of mutations. Therapeutic agents that re-establish the normal functions of apoptotic signaling pathways offer an attractive strategy for the treatment of breast cancer. Baicalin (BA) is one of the natural compounds with anti-proliferation and pro-apoptosis activities against numerous tumor cells. However, low bioavailability restricts the clinical application of BA. In order to improve its therapeutic efficacy and study the mechanism of actions, active targeting delivery systems were developed for targeting tumor environment and selective cell killing effects. It emphasized on the construction of folate-conjugated albumin nanoparticles loaded with baicalin (FA-BSANPs/BA) and mechanisms of which on the promotion of breast cancer apoptosis. The physicochemical properties and structural characteristics of FA-BSANPs/BA were investigated. Cell experiments were carried out to study the targeted anti-breast cancer effects of FA-BSANPs/BA and its mechanism. The results showed that FA-BSANPs/BA was successfully constructed with stable structural characteristics and sustained release effects. Cellular uptake and MTT showed that it increased targeted uptake efficiency and cytotoxicity. Flow cytometry and western blot confirmed that it promoted apoptosis by increasing the expression of caspase-8 and ROS, and decreasing the level of Bid. It is suggested that the pro-apoptotic mechanism of FA-BSANPs/BA is related to regulation of key proteins in extrinsic apoptotic pathway. In conclusion, FA-BSANPs/BA is a good delivery carrier and significantly inhibits the breast cancer growth compared with free BA. The mechanism of FA-BSANPs/BA promoting apoptosis of breast cancer may be due to its action on the caspase-8/Bid/ROS pathway.

研究领域: 肿瘤学 · 药理学 · 纳米技术 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF ELECTROANALYTICAL CHEMISTRY · 2021 · IF 4.464

Green preparation of amorphous molybdenum sulfide nanocomposite with biochar microsphere and its voltametric sensing platform for smart analysis of baicalin

Liangmei Rao,Peicong Zhou,Peng Liu,Xinyu Lu,Xuemin Duan,Yangping Wen,Yifu Zhu,Jingkun Xu

Green and sustainable development provides a new idea for solving environmental pollution issues of rural biomass wastes. Amorphous molybdenum sulfide (a-MoS x ) nanocomposite based on biochar microsphere (BM) as voltametric sensing platform for smart analysis of baicalin in real sample was facilely prepared. Pomelo peel was employed as the carbon source for improving electronic conductivity and environmental stability and electrocatalytic capacity of a-MoS x . A mixture consisted of the precursor of both a-MoS x and BM were treated by a co-hydrothermal method. The a-MoS x nanocomposite with porous BM was formed by centrifuging, washing, drying, pulverizing, and calcining. The structure and properties of the as-obtained nanocomposite were characterized, and the electrochemical behaviors of baicalin, parametric conditions and performance of the as-prepared sensor were investigated. Peak currents recorded by differential pulse voltammetry is proportional to baicalin concentrations in wide linear ranges from 10 nM to 5 μM with a low limit of detection of 2 nM. Machine learning algorithms like least squares support vector machine and artificial neural network was built to realize smart analysis and digital output for baicalin. Good cyclic stability, excellent voltammetric response, and satisfactory practicability will provide a promising electrochemical sensing platform for facile preparation of two-dimension nanomaterials functionalized with biochar derived from agroforestry biomass.

研究领域: 环境科学 · 分析化学
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EUROPEAN JOURNAL OF MEDICAL RESEARCH · 2024 · IF 2.8

Baicalin promotes the sensitivity of NSCLC to cisplatin by regulating ferritinophagy and macrophage immunity through the KEAP1-NRF2/HO-1 pathway

Yang Chen,Shujun Bao,Zhongzhao Wang,Zheng Fang,Hao Tang

Background Cisplatin (DDP) chemotherapy is commonly used in therapy for non-small cell lung cancer (NSCLC), but increased drug resistance has become a huge obstacle. Baicalin (BA) contributed to the sensitivity of NSCLC to DDP. Here, we aimed to further probe the pathophysiological mechanisms of BA in NSCLC. Methods A549 and A549/DDP cells and xenograft mice were treated with BA and DDP. Xenograft mice were treated additionally with the NRF2 inducer (Bardoxolone methyl, BM) and KEAP1 knockdown. The levels of ferritinophagy-related proteins and biomarkers were determined. The autophagosomes were observed. M1 macrophage polarization and the contents of related indicators were analyzed. The involvement of KEAP1/NRF2/HO-1 was determined. Results BA inhibited cell development, and the effect of BA and DDP on cell development was additive. The abundance of ferritinophagy-related proteins and the number of autophagosomes were induced by BA. BA also promoted the transition of GSH to GSSH. BA favored M1 macrophage polarization and affected the expression of related proteins. When BA and DDP combined, these molecular phenomena were further exacerbated. BA induced accumulation of KEAP1 and reduction of NRF2 and HO-1. However, BM and KEAP1 knockdown disrupted the synergistic effects of BA and DDP on inhibiting NSCLC growth. BM and KEAP1 knockdown reversed DDP and BA-promoted protein expression activity and M1 macrophage polarization. Conclusion Our findings suggest that BA is involved in ferritinophagy and macrophage immunity through the KEAP1-NRF2/HO-1 axis, thereby improving the DDP sensitivity in NSCLC, which could provide new candidates for treatment strategies.

研究领域: 肿瘤学 · 药理学 · 免疫学 · 分子生物学
✓ 已验证 DOI PubMed 高影响因子
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Materials · 2024 ·Vol. 17 ·期 15 ·3734 · IF 3.1

Facilely Promoting the Concentration of Baicalin in Polylactic Acid Fiber for UV Shielding and Antibacterial Functions: A Customized and Sustainable Approach

Yuyang Zhou,Peng Deng,Wei Chen

There is a significant trend towards the integration of natural substances with bio-polymers for fully bio-based functional composites. Polylactic acid is regarded as a promising biodegradable polymer for replacing synthetic polymers. Differing from the case of natural fiber, the incompatibility of polylactic acid with bio-based molecules prevents it from being used to fabricate high-quality sustainable composites. This work presents a simultaneous ultraviolet shielding and antibacterial finishing process of polylactic acid combined with bioactive baicalin and an eco-friendly ester, which is highlighted for (a) the lack of synthetic chemicals involved in such process, (b) adsorption enhancement achieved at a mild temperature, and (c) marginal color change on treated polylactic acid. A response surface methodology was adopted to analyze the impacts of various factors on the baicalin quantity in polylactic acid, and to optimize the treatment condition. The uptake ratio of baicalin in polylactic acid was drastically promoted from 8.5 mg/g to 21.1 mg/g using methyl cinnamate. The response surface methodology based on a central composite design experiment indicated that the usage of baicalin was the most significant factor followed by methyl cinnamate and temperature. After optimization, a very faint color depth of 1.2 was apparent, but UPF 50+ and 92% bacterial reduction could be achieved. In all, the success in strengthening of the functionalities of polylactic acid extends the applications of polylactic acid products.

CAS / MDL: 103-26-4
研究领域: 材料科学 · 生物医学工程
✓ 已验证 产品关联 DOI PubMed 高影响因子
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DIAMOND AND RELATED MATERIALS · 2024 · IF 4.3

Fabrication of β-CD/SiO2@rGO/MXenes composite materials with three-dimensional structures for sensitive detection of baicalin in Chinese medicine

YuXuan Xiong,Dandan Luo,Guowen He,Saiwen Liu,Jin Zhang,Chao Chen

Baicalin is a principal component of traditional Chinese medicine and plays a crucial role in treating conditions such as arthritis, respiratory tract infections, chronic and acute hepatitis, and tumors. Graphene oxide is bonded to silicon dioxide (SiO 2 ) through covalent bonds or hydrogen bonds and then reduced to SiO 2 @rGO through hydrazine hydrate to solve the problem of easy accumulation of SiO 2 and improve the conductivity of the material. Next, β-cyclodextrin (β-CD) self-assembles on SiO 2 @rGO to form a stable inclusion complex. The hydrophobic inner cavity of β-CD can effectively accommodate various guest molecules to form inclusion complexes, enhancing molecular recognition and detection capabilities. Finally, β-CD/SiO 2 @rGO is bridged and surface-loaded between clay-like Ti 3 C 2 T x (MXenes) nanosheets through electrostatic interactions to form a stable three-dimensional composite material. It is precisely because of MXenes, due to their unique layered microstructure, excellent conductivity, and extensive hydrophilic surface area, that they are conducive to self-assembly or embedding nanoparticles in aqueous solution. The composite was characterized via X-ray diffraction, X-ray photoelectron spectroscopy, and scanning electron microscopy. Under optimized conditions, the electrochemical sensor constructed from this composite exhibited a broad detection range (0.008–10 μM) and a low detection limit (0.191 nM) for baicalin. In comparison to existing methods for detecting baicalin, this approach demonstrates strong anti-interference capabilities and stability. It can efficiently, sensitively, and accurately quantify baicalin in Chinese patent medicine samples, including Scutellaria baicalensis root, Shuanghuanglian oral liquid, and Bear Bile Scutellaria baicalensis eye drops, achieving a satisfactory recovery rate. This study introduces a novel approach for the electrochemical detection of baicalin.

研究领域: 材料科学 · 中药分析 · 生物医学工程
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CNS Neuroscience & Therapeutics · 2019 ·Vol. 25 ·期 5 ·575-590 · IF 3.394

Baicalin mitigates cognitive impairment and protects neurons from microglia-mediated neuroinflammation via suppressing NLRP3 inflammasomes and TLR4/NF-κB signaling pathway

Xin Jin,Ming-Yan Liu,Dong-Fang Zhang,Xin Zhong,Ke Du,Ping Qian,Wei-Fan Yao,Hua Gao,Min-Jie Wei

Summary Aims Baicalin (BAI), a flavonoid compound isolated from the root of Scutellaria baicalensis Georgi, has been established to have potent anti-inflammation and neuroprotective properties; however, its effects during Alzheimer's disease (AD) treatment have not been well studied. This study aimed to investigate the effects of BAI pretreatment on cognitive impairment and neuronal protection against microglia-induced neuroinflammation and to explore the mechanisms underlying its anti-inflammation effects. Methods To determine whether BAI plays a positive role in ameliorating the memory and cognition deficits in APP (amyloid beta precursor protein)/PS1 (presenilin-1) mice, behavioral experiments were conducted. We assessed the effects of BAI on microglial activation, the production of proinflammatory cytokines, and neuroinflammation-mediated neuron apoptosis in vivo and in vitro using Western blot, RT-PCR, ELISA, immunohistochemistry, and immunofluorescence. Finally, to elucidate the anti-inflammation mechanisms underlying the effects of BAI, the protein expression of NLRP3 inflammasomes and the expression of proteins involved in the TLR4/NF-κB signaling pathway were measured using Western blot and immunofluorescence. Results The results indicated that BAI treatment attenuated spatial memory dysfunction in APP/PS1 mice, as assessed by the passive avoidance test and the Morris water maze test. Additionally, BAI administration effectively decreased the number of activated microglia and proinflammatory cytokines, as well as neuroinflammation-mediated neuron apoptosis, in APP/PS1 mice and LPS (lipopolysaccharides)/Aβ-stimulated BV2 microglial cells. Lastly, the molecular mechanistic study revealed that BAI inhibited microglia-induced neuroinflammation via suppression of the activation of NLRP3 inflammasomes and the TLR4/NF-κB signaling pathway. Conclusion Overall, the results of the present study indicated that BAI is a promising neuroprotective compound for use in the prevention and treatment of microglia-mediated neuroinflammation during AD progression.

CAS / MDL: 13718-50-8
研究领域: 神经科学 · 药理学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Acta Pharmaceutica Sinica B · 2014 · IF 0

Combined use of phospholipid complexes and self-emulsifying microemulsions for improving the oral absorption of a BCS class IV compound, baicalin

Huiyi Wu,Xiaoying Long,Fei Yuan,Li Chen,Sujing Pan,Yunjun Liu,Yoshiko Stowell,Xiaoling Li

The aim of this study was to develop a formulation to improve the oral absorption of baicalin (BA) by combining a phospholipid complex (PC) and self-emulsifying microemulsion drug delivery system (SMEDDS), termed BA–PC–SMEDDS. BA–PC was prepared by a solvent evaporation method and evaluated by complexation percentage (CP). The physicochemical properties of BA–PC were determined. The synergistic effect of PC and SMEDDS on permeation of BA was studied in vitro with Caco-2 cells and in situ with a single pass intestinal perfusion model. The improved bioavailability of BA in BA–PC–SMEDDS was confirmed in an in vivo rat model. The CP of BA–PC reached 100% when the molar ratio of drug to phospholipid (PP) was ≥1:1. The solubility of BA–PC increased in both water and octanol, and the log   P o/w of BA–PC was increased significantly. BA–PC–SMEDDS could be dispersed more evenly in water, compared to BA and BA–PC. Both the Caco-2 cell uptake and single-pass intestinal perfusion models illustrated that transport of BA in BA–PC was lower than that of free BA, while improved significantly in BA–PC–SMEDDS. The relative bioavailability of BA–PC(1:2)–SMEDDS was 220.37%. The combination system of PC and SMEDDS had a synergistic effect on improving the oral absorption of BA.

CAS / MDL: 56-81-5
研究领域: 药剂学 · 药物代谢动力学
✓ 已验证 产品关联 DOI PubMed
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PHYTOTHERAPY RESEARCH · 2022 ·Vol. 36 ·期 10 ·3969-3987 · IF 6.388

Potential mechanism of oral baicalin treating psoriasis via suppressing Wnt signaling pathway and inhibiting Th17/IL-17 axis by activating PPARγ

Yi Chen,Shasha Song,Yongfang Wang,Jia Zhu,Xinyu Li

Psoriasis (PSO), an immune-mediated chronic inflammatory skin disease, has seriously affected the quality of patients' life. It is urgent to find effective medicines with lower costs and less side effects. Baicalin (HQG) is the main bioactive substance from Scutellaria baicalensis with effects of anti-inflammation and immunoregulation. Herein, we explored the effect of oral HQG treating PSO and its potential mechanism. Firstly, network pharmacology was used to predict that HQG may act on Estrogen, TNF-alpha (tumor necrosis factor, TNF), interleukin-17 (IL-17) signaling pathways and Th17 cell differentiation, especially the key targets including TNF, Proto-oncogene tyrosine-protein kinase Src, Peroxisome proliferator-activated receptor gamma and Matrix metalloproteinase-9. Imiquimod (IMQ)-induced mice were then used to study the effects of HQG treating PSO. HQG could significantly ameliorate the skin lesions, decrease the level of inflammatory factors and inhibit Th1/Th17 cell differentiation in IMQ-induced mice. Finally, transcriptome analysis of skin lesions integrated with the prediction of network pharmacology further demonstrated that the potential mechanism may be associated with suppressing Wnt signaling pathway and inhibiting Th17/IL-17 axis by activating PPARγ. In conclusion, this study suggested that HQG may be a promising agent for further studies in the search for therapeutic strategies to treat PSO in the future.

CAS / MDL: 21967-41-9
研究领域: 药理学 · 免疫学 · 皮肤科 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF SOLID STATE ELECTROCHEMISTRY · 2024 ·Vol. 28 ·期 8 ·2959-2971 · IF 2.6

The core–shell structure ZIF-67/MIL-101 (Fe)-modified carbon paper electrode: high sensitivity and selectivity for the determination of baicalin

Gao Yali,Pang Wanyu,Chang Xile,Hu Zhiyong,Hu Tuoping,Ma Xuemei

Baicalin (Bn) is one of the flavonoids with various biological activities, and its accurate determination is of great significance to clinical medicine. The new “MOF-on-MOF” materials have a broad application prospect. ZIF-67 and MIL-101(Fe) are typical metal–organic frame (MOF) materials, which have the advantages of flexible structure, large specific surface area, large porosity, and adjustable pore size. In this paper, a disposable and sensitive Bn electrochemical sensor based on ZIF-67/MIL-101(Fe) composite modified carbon paper (CP) electrode was developed for the first time. The sensing nanomaterials were characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), X-ray diffraction spectroscopy (XRD), and X-ray photoelectron spectroscopy (XPS). Cyclic voltammetry (CV) was used to evaluate the electrochemical behavior of Bn on different modified electrodes. The results showed that ZIF-67/MIL-101(Fe)/CP exhibited a well-defined redox peak compared with bare CP, ZIF-67/CP, and MIL-101(Fe)/CP, which was attributed to the synergistic effect of ZIF-67 and MIL-101(Fe). Under optimal conditions, the electrochemical sensor was able to quantify Bn in the ranges of 0.01 ~ 3 µM and 3 ~ 6 µM with a detection limit (LOD) as low as 0.009 µM (S/N = 3). In addition, the sensor was successfully used for the quantitative analysis of Bn in Dual yellow oral liquid with reliable results.

研究领域: 分析化学 · 药物分析 · 生物医学工程
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Frontiers in Immunology · 2022 · IF 8.786

Baicalin Induces a Potent Innate Immune Response to Inhibit Respiratory Syncytial Virus Replication via Regulating Viral Non-Structural 1 and Matrix RNA

Qin Sheng,Huang Xianzhang,Qu Shaogang

Respiratory syncytial virus (RSV) infection is the most frequent cause of hospitalization in pediatric patients. Current systemic treatment and vaccines are not curative and re-infection is often associated with a more drastic incidence of the disease. Baicalin is a flavonoid isolated from Scutellaria baicalensis with potent anti-viral characteristics, namely against RSV. However, its precise mechanism of action remains unclear. Here, using in vitro methods and an in vivo murine model of RSV infection, we showed that baicalin inhibits RSV replication induces translational upregulation of type I interferons (IFNs), IFN-α and IFN-β, and reverses epithelial thickening in lung tissues. Moreover, baicalin inhibits transcription of the RSV non-structural proteins NS1 and NS2. Molecular docking and surface plasmon resonance-based affinity analysis showed that baicalin also binds to the α3 helix of the NS1 protein with an affinity constant of 1.119 × 10−5 M. Polysome profiling showed that baicalin inhibits translation of the RSV matrix protein (M) RNA. Baicalin mediates increased release of the ribosomal protein L13a from the large ribosomal subunit, where the extra ribosomal subunit L13a inhibits M RNA translation. These results comprehensively establish the multiple mechanisms by which baicalin induces a potent innate immune response against RSV infection.

CAS / MDL: 21967-41-9
研究领域: 病毒学 · 免疫学 · 药理学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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