Frontiers in Immunology
·
2022
·
IF 8.786
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.
研究领域:
病毒学
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免疫学
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药理学
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DOI
PubMed
高影响因子
Frontiers in Pharmacology
·
2024
·
IF 4.4
Huan Yu,Dan Zhou,Wei Wang,Qingxia Wang,Min Li,Xiaoyun Ma
Background and Purpose: The damage or apoptosis of retinal ganglion cells (RGCs) is one of the leading causes of various blinding eye diseases, such as glaucoma, diabetic retinopathy, optic neuritis, and ischemic optic neuropathy. Oxidative stress is involved in RGCs death. Baicalin, a flavonoid compound extracted from Scutellaria baicalensis, has various beneficial effects, including anti-inflammatory, anti-apoptotic, and antioxidant properties. However, the effects of baicalin on RGCs and the underlying mechanisms require further investigation.Methods: In this study, a glutamate-induced oxidative stress damage model of R28 cells and a rat retinal injury model were established to investigate the effects of baicalin on oxidative stress damage to RGCs and try to elucidate the underlying mechanism.Results: In vitro experiments demonstrated that the survival rate of R28 cells after glutamate treatment dropped to 33.4%, while 10 μM baicalin significantly inhibited glutamate-induced damage in RGCs (P < 0.001) and enhanced cell viability through decreasing ROS levels, increasing antioxidant enzyme activity, and suppressing the expression of inflammatory factors iNOS, TNF-α, IL-6, and IL-1β (P < 0.001). In vivo, baicalin effectively mitigated structural damage to retinal tissue and RGCs morphology induced by glutamate, increasing the thickness of the retinal ganglion cell layer, improving RGCs density, and reducing overall retinal thinning in rats (P < 0.001) in a time- and dose-dependent effects. Mechanistic studies revealed that glutamate evaluated the phosphorylation levels of JAK/STAT, while baicalin effectively inhibited the activation of the JAK/STAT signaling pathway.Conclusion: This study confirmed that baicalin protects against glutamate-induced oxidative stress damage in RGCs. It effectively alleviates oxidative stress and inflammatory responses, reduces cell apoptosis, and improves the pathological changes in the retina of rat models of RGCs damage, thereby decreasing RGCs death. Further exploration of its mechanism revealed that baicalin effectively inhibits the JAK/STAT signaling pathway, protecting RGCs from oxidative stress damage. This provides an experimental basis for the application of baicalin in the treatment of RGCs damage.
研究领域:
眼科学
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药理学
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细胞生物学
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神经科学
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PubMed
高影响因子
Biology-Basel
·
2026
·Vol. 15
·期 18
·1639
·
IF 4.3
Chao Ning,Jiale Zhou,Zhiyun Yu,Yuxuan Yang,Mengna Kang,Zhiyao Dong,Yantong Sun,Xin Meng,Haiyong Guo
Simple SummaryMethicillin-resistantStaphylococcus aureus(MRSA) infections present significant therapeutic challenges and constitute a major public health hazard. While the synergistic application of phytochemicals alongside conventional antibiotics offers a promising strategy to suppress bacterial growth with a reduced risk of triggering resistance, the precise mechanisms underlying this antibacterial effect and its in vivo efficacy remain poorly understood. Our study demonstrates that co-administration of baicalin and oxacillin sodium facilitates the intracellular buildup of reactive oxygen species (ROS). Furthermore, this combination reduces the levels of extracellular polymeric substances (EPSs) and total protein within biofilms, suppresses the metabolic functions of biofilm cells, and hinders the production of key virulence factors, specifically lipase and staphyloxanthin. These observed anti-biofilm and anti-virulence effects are likely attributable to the downregulation ofsarAgene expression induced by the baicalin-oxacillin sodium mixture. Building on these findings, we further assessed the in vivo anti-infective potential of this combined therapy. The results indicated that this combined therapy significantly decreased the infiltration of inflammatory cells within the peritoneal cavity of murine models, suppressed the production of pro-inflammatory mediators, and reduced bacterial burdens in tissues. Furthermore, it facilitated the restoration of pathological tissue injuries and exhibited protective properties for both hepatic and renal functions. In conclusion, the synergistic application of baicalin and sodium oxacillin effectively impedes MRSA biofilm development and virulence factor synthesis, thereby attenuating pathogenicity in a mouse model of peritonitis induced by MRSA USA300 strain. These findings validate the anti-infective efficacy of integrating plant-derived compounds with conventional antibiotics, offering novel experimental support for clinical strategies aimed at managing peritonitis caused by drug-resistant pathogens.Over the past few years, considerable scholarly interest has been directed toward the synergistic application of natural compounds alongside conventional antibiotics to address infections stemming from multidrug-resistant (MDR) pathogens. The primary objective of this research is to investigate the efficacy of baicalin (BA), an extract obtained fromScutellaria baicalensis, when used in conjunction with oxacillin sodium (OXS). Specifically, the study evaluates their combined impact on biofilm formation and toxicity reduction in methicillin-resistantStaphylococcus aureus(MRSA) strain USA300. Furthermore, a murine peritonitis model induced by MRSA USA300 was developed to determine the therapeutic potential of this combination therapy against infection. Experimental data indicate that the co-administration of BA and OXS does not induce hemolysis in vitro. In comparison to treatments involving either BA or OXS alone, the combined regimen significantly enhances the accumulation of intracellular reactive oxygen species (ROS) within MRSA USA300. Additionally, this synergistic approach suppresses the production of extracellular polymeric substances (EPSs), decreases the overall protein content within the biofilm matrix, and impairs the metabolic functions of biofilm cells. The investigation also revealed that the synergistic application of BA and OXS intensifies the suppression of key virulence determinants, specifically lipase activity and staphyloxanthin production, while simultaneously downregulating the transcription ofsarA(a global regulator of virulence). These findings substantiate the anti-virulence efficacy of the BA-OXS combination. In a murine model of peritonitis established using MRSA USA300, the healthy mice group, the MRSA USA300 group, the BA group, the OXS group, the combined group of BA and OXS, and the VAN group were set up, with eight mice in each group. The results showed that the combined therapy significantly mitigated body weight reduction, decreased the circulating counts of inflammatory cells, including leukocytes and lymphocytes, and suppressed the secretion of pro-inflammatory mediators such as TNF-α, IL-6, and IL-1β, thereby demonstrating potent anti-inflammatory properties. Furthermore, the co-administration of BA and OXS reduced bacterial burden in the abdominal organs of infected mice and alleviated associated histopathological injuries. Importantly, the treatment regimen exhibited no hepatorenal toxicity in the peritonitis mice, effectively maintaining normal levels. In the plasma of mice suffering from peritonitis, the concentration of malondialdehyde (MDA), a marker of oxidative stress, was reduced, while the activities of catalase (CAT) and superoxide dismutase (SOD) were elevated. This modulation contributes to anti-infective effects. These findings offer a theoretical foundation for subsequent investigations into the synergistic application of natural compounds and conventional antibiotics against MRSA.
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高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
·
IF 8.5
Qianwen Li,Fansu Meng,Mengjie Xie,Makiya Nishikawa,Kosuke Kusamori,Anil K. Giri,Lina Yang,Qi Li,Honghui Gu,Zhong Chen,Zhenjiang Yang,Jiajia Qin,Yu Cai
To address tamoxifen (TAM) resistance in estrogen receptor α (ERα)-positive breast cancer and enhance the bio availability of baicalin (BA), this research developed pH/folate dual-responsive bovine serum albumin (BSA)-based nanoparticles (NPs) to improve TAM sensitivity. Four BA-loaded BSA NPs were engineered: non-targeted (BA@BSA NPs), folate-targeted (BA@FA BSA NPs), pH-sensitive (BA@mPEGA BSA NPs), and dual-responsive (BA@mPEGA FA BSA NPs). Physicochemical characterization included TEM, dynamic light scattering (size, PDI, zeta potential), encapsulation efficiency, drug loading, FTIR, TGA and stability. pH-dependent drug release profiles (pH 5.0, 6.5, 7.4) were evaluated. Cellular uptake (fluorescence imaging via FRα targeting) and cytotoxicity (pH 6.5 vs. 7.4) were assessed in TAM-resistant LCC9 cells. In vivo efficacy was determined through hemocompatibility, tumor-targeting efficiency (fluorescence imaging), and xenograft tumor suppression. Four BA-loaded BSA NPs exhibited uniform morphology (80–120 nm), low PDI (<0.2), negative zeta potential (−13 to −16 mV), high encapsulation efficiency (>85 %), and drug loading (>0.5 %). FTIR confirmed successful fabrication. BA@mPEGA FA BSA NPs showed superior thermal stability (1.29 % mass loss at 40–110 °C vs. 1.73–4.23 % for other four BA-loaded BSA NPs),the nanoparticles demonstrated good stability when stored at 4 °C for three months and pH-responsive BA release (87.74 ± 0.55 % at pH 5.0 vs. 58.11 ± 1.18 % at pH 6.5 and 14.81 ± 1.58 % at pH 7.4 over 48 h). Combined with TAM, BA@mPEGA FA BSA NPs reduced LCC9 cell IC 50 by 2.29-fold (pH 6.5) versus free BA+TAM.FRα-mediated BA@mPEGA FA BSA NPs cellular uptake was 7.20-fold higher than free FA + BA@mPEGA FA BSA NPs ( p < 0.0001). In vivo, NPs showed low hemolysis (<5 %) and tumor targeting. BA@mPEGA FA BSA NPs MD+ TAM achieved 82.06 ± 3.67 % tumor suppression, significantly outperforming controls (p < 0.0001), and demonstrated favorable safety profiles. The dual-responsive BA@mPEGA FA BSA NPs effectively overcome BA delivery limitations and resensitize ERα + breast cancer to TAM, offering a clinically translatable strategy to combat endocrine therapy resistance.
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高影响因子
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
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分离科学与技术
·
绿色化学
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DOI
高影响因子
DYES AND PIGMENTS
·
2026
·
IF 3.9
Jiahong Zuo,Ruizhi Liu,Minghui Qiu,Shenghong Tu,Xiangrong Wang,Xiaoyan Hu,Yuyang Zhou
A fully bio-based photo-stable CCM is fabricated via ‘zero-length’ coupling strategy. • The exhaustion of CCM Mod on silk descends with pH due to ion−ion interaction. • The lightfastness of dyed silk follows: CCM Mod > BCL/CCM blends > CCM. • The K/S loss of CCM Mod dyed silk is 42.74% less than half of that of CCM dyed silk. • Silk fabric dyed with CCM Mod attains a UPF value of 50+. Utilizing low-cost bio-resources for developing textile dyestuffs promotes the progress of sustainable textile industry. Curcumin (CCM) stands out as one of the most promising yellow bio-colorants owing to its high color value and bioactivities; however, its application in large-scale dyeing industry is significantly hindered by issues of photo-fading and hydrophobicity. Although mordant dyeing, chemical modification, and compound dyeing have demonstrated their effectiveness, notable but unavoidable drawbacks persist, including substantial color changes, the introduction of hazardous moieties, and dyeing competition. In this study, a fully bio-based, photo-stable, and water-soluble CCM derivative (CCM Mod ) is synthesized through a ‘zero-length’ coupling strategy employing baicalin (BCL) as dual functional UV absorber and antioxidant. The structure of CCM Mod is verified using FTIR, UV-Vis absorption spectroscopy, and HPLC-MS. The investigation of adsorption kinetics reveals that CCM Mod initially undergoes rapid adsorption onto fiber, followed by a gradual diffusion into fiber until an equilibrium is reached. The pseudo-second-order kinetic model provides a superior description of the adsorption behavior compared to the pseudo-first-order kinetic model, indicating that chemical interactions predominantly govern the process. Silk fabric dyed with CCM Mod exhibits a significantly enhanced light fastness, improving from level 1.5 to 3, along with improved washing and rubbing fastness, in comparison to fabric dyed with CCM. After 20 h of exposure to artificial light, the K/S loss for silk dyed with CCM Mod is 42.74%, which is less than half of that observed for silk dyed with CCM (87.16%). The UPF value of silk dyed with CCM Mod (5% owf) reaches 50+. The proposed facile coupling strategy not only addresses the photo-fading limitations of CCM but also offers a transferable approach for modifying other bio-colorants, thereby expanding their applications in food, cosmetics, etc. Download: Download high-res image (427KB) Download: Download full-size image
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高影响因子
Frontiers in Pharmacology
·
2020
·
IF 4.225
Ma Chongyang,Wang Xueqian,Xu Tian,Zhang Shuang,Liu Shuling,Zhai Changming,Wang Zisong,Mu Jie,Li Changxiang,Cheng Fafeng,Wang Qingguo
Stroke is the second leading cause of death after heart disease globally and cerebral ischemic stroke accounts for approximately 70% of all incident stroke cases. We selected four main compounds from a patent Chinese medicine, Qingkailing (QKL) injection, including baicalin from Scutellaria baicalensis Georgi (Huang Qin), geniposide from Gardenia jasminoides J. Ellis (Zhizi), and cholic acid and hyodeoxycholic acid from Bovis Calculus (Niuhuang) with a ratio of 4.4:0.4:3:2.6 m/m, to develop a more efficacious and safer modern Chinese medicine injection against ischemic stroke, refined QKL (RQKL). In this study, we investigated multiple targets, levels, and pathways of RQKL by using an integrative pharm\acology combining experimental validation approach. In silica study showed that RQKL may regulate PI3K-Akt, estrogen, neurotrophin, HIF-1, MAPK, Hippo, FoxO, TGF-beta, NOD-like receptor, apoptosis, NF-kappa B, Wnt, chemokine, TNF, Toll-like receptor signaling pathways against ischemic stroke. The experimental results showed that RQKL improved neurological function and prevented infract volume and blood-brain-barrier damage. RQKL inhibited microgliosis and astrogliosis, and protected neurons from ischemic/reperfusion injury. RQKL also inhibited cell apoptosis and affecting the ratio of the anti-apoptosis protein B-cell lymphoma-2 (Bcl2) and pro-apoptosis protein Bcl2-associated X protein (Bax). Western blot analysis showed that RQKL activated AKT/PI3K signaling pathway and antibody array showed RQKL inhibited inflammatory response and decreased proinflammatory factor Tnf, Il6, and Il1b, and chemokines Ccl2, Cxcl2, and Cxcl3, and increased anti-inflammatory cytokine Il10. In conclusion, RQKL protected tissue against ischemic stroke through multiple-target, multiple signals, and modulating multiple cell-types in brain. This study not only promoted our understanding of the role of RQKL against ischemic stroke, but also provided a pattern for the study of Chinese medicine combining pharmaceutical Informatics and system biology methods.
研究领域:
药理学
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神经科学
·
中医药
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整合生物学
·
实验验证
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DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
·
2022
·
IF 5.112
Le-Yuan Shang,Ming-Hao Zhou,Si-Yuan Cao,Min Zhang,Peng-Jiao Wang,Shuo Zhang,Xiao-Xia Meng,Qi-Mei Yang,Xiu-Li Gao
Baicalin (BG) is a bioactive flavonoid extracted from the dried root of the medicinal plant, Scutellaria radix (SR) (dicotyledonous family, Labiatae), and has several biological activities. Polyethylene glycol 400 (PEG400) has been used as a suitable solvent for several traditional Chinese medicines (TCM) and is often used as an excipient for the compound preparation of SR. However, the drug–excipient interactions between BG and PEG400 are still unknown. Herein, we evaluated the effect of a single intravenous PEG400 administration on the BG levels of rats using pharmacokinetic and tissue distribution studies. A liver microsome and recombinant enzyme incubation system were used to further confirm the interaction mechanism between PEG400 and UDP-glucuronosyltransferases (UGTs) (UGT1A8 and UGT1A9). The pharmacokinetic study demonstrated that following the co-intravenous administration of PEG400 and BG, the total clearance (CL z ) of BG in the rat plasma decreased by 101.60% ( p < 0.05), whereas the area under the plasma concentration-time curve (AUC) 0-t and AUC 0-inf increased by 144.59% ( p < 0.05) and 140.05% ( p < 0.05), respectively. Additionally, the tissue distribution study showed that the concentration of BG and baicalein-6-O-β-D-glucuronide (B6G) in the tissues increased, whereas baicalein (B) in the tissues decreased, and the total amount of BG and its metabolites in tissues altered following the intravenous administration of PEG400. We further found that PEG400 induced the UGT1A8 and UGT1A9 enzyme activities by affecting the maximum enzymatic velocity (V max ) and Michaelis–Menten constant (K m ) values of UGT1A8 and UGT1A9. In conclusion, our results demonstrated that PEG400 interaction with UGTs altered the pharmacokinetic behaviors and tissue distribution characteristics of BG and its metabolites in rats.
研究领域:
药理学
·
生物化学
·
药物化学
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中药学
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DOI
PubMed
高影响因子
Iranian Journal of Basic Medical Sciences
·
2023
·
IF 2.2
Junyuan Li,Gang Wang,Yehao Zhang,Xiaodi Fan,Mingjiang Yao
Objective(s): To explore the ability and underlying molecular mechanisms involved in the protective effects of Baicalin (BA) against L-Glutamate-induced mouse hippocampal neuron cell line HT-22. Materials and Methods: The cell injury model of HT-22 cells was induced by L-glutamate, and cell viability and damage were detected by CCK-8 and LDH assays. Generation of intracellular reactive oxygen species (ROS) was measured by DCFH-DA in situ fluorescence method. The SOD activity and MDA concentration in the supernatants were determined by WST-8 and colorimetric method, respectively. Furthermore, Western blot and real-time qPCR analysis were utilized to detect the expression levels of the Nrf2/HO-1 signaling pathway and NLRP3 inflammasome proteins and genes. Results: L-Glutamate exposure induced cell injuries in HT-22 cells, and the concentration of 5 mM L-Glutamate was chosen to be the modeling condition. Co-treatment with BA significantly promoted cell viability and reduced LDH release in a dose-dependent manner. In addition, BA attenuated the L-Glutamate-induced injuries by decreasing the ROS production and MDA concentration, while increasing the SOD activity. Moreover, we also found that BA treatment up-regulated the gene and protein expression of Nrf2 and HO-1, and then inhibited the expression of NLRP3. Conclusion: Our study found that BA could relieve oxidative stress damage of HT-22 cells induced by L-Glutamate, and the mechanism might be related to the activation of Nrf2/HO-1 and inhibition of NLRP3 inflammasome.
研究领域:
药理学
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神经科学
·
细胞生物学
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分子生物学
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PubMed
高影响因子
Inorganic Chemistry Frontiers
·
2023
·
IF 7
Yafeng Liu,Chenxi Jiang,Liang Peng,Zhimin Li,Jintao Wang,Xiangwen Liao,Wenying Guo
Antimicrobial resistance is a major public health concern. Many drug development strategies focus on metal complexes because they have different inhibitory mechanisms and are less prone to drug resistance than traditional antibiotics. In this study, we investigated the antibacterial properties of Radix scutellariae (Huangqin), a traditional Chinese medicine. Using acid methanol solutions, we identified metal complexes in aqueous extracts of Huangqin, in which baicalin, oroxindin, and scutellarin function as ligands. Mn2+ increased the antibacterial activity of the aqueous extract through metal ion addition. We investigated the mechanism and structure of the baicalin–manganese complex (BCM) obtained by hydrothermal synthesis. Reaction products containing BCM at a ratio of 1 : 1 and 2 : 1 were significantly more effective against bacteria than baicalin alone. The antibacterial activity of the BCM against Staphylococcus aureus was eight times higher than that of baicalin. The antibacterial mechanisms included altering the morphological structure of bacteria, disrupting the integrity of their cell membrane and wall, and causing the cells to produce large amounts of reactive oxygen species. Importantly, after continuous cultivation of S. aureus for 20 generations in drug-containing cultures, the minimum inhibitory concentrations (MIC) of amikacin, azithromycin, and clindamycin were 32, eight, and four times greater than those in the first generation, respectively, whereas the MIC of BCM was maintained. BCM could reverse S. aureus resistance to amikacin and azithromycin. In conclusion, during the decoction of Huangqin, the organic components form complexes with metal ions, producing compounds with good antibacterial activity and a low tendency to cause resistance.
研究领域:
药理学
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微生物学
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中药学
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无机化学
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高影响因子
HISTOLOGY AND HISTOPATHOLOGY
·
2024
·
IF 2.5
Jinfeng Xie,Yonggui Liao,Dile Wang
Background: Deep vein thrombosis (DVT) is the third most prevalent vascular disease worldwide, seriously threatening human health. Baicalin, a flavonoid isolated from the roots of Scutellaria baicalensis , has been identified to play a crucial role in various vascular diseases. The study aimed to explore the efficacy and underlying mechanisms of baicalin in DVT. Methods: Endothelial progenitor cells (EPCs) were differentiated from peripheral blood mononuclear cells isolated from rat bone marrow. Dil-ac-LDL/FITC-UEA-1 double staining and flow cytometry analysis were conducted for the identification of EPCs. The angiogenesis and migration of EPCs in vitro were tested by a tube formation assay and Transwell assay, respectively. DVT rat models were established by stenosis of the inferior vena cava (IVC). After the euthanasia of rats, thrombi in the IVC were collected and weighed, and histological alterations in IVC tissue were measured by H&E staining. The protein levels of SIRT1, p-P65, and p65 in rat IVC tissues were quantified via western blotting. Results: EPCs used in this study displayed a spindle-like shape and were positive for endothelial cell-specific markers, suggesting the phenotypic characteristics of EPCs. Baicalin enhanced the migratory and angiogenetic abilities of EPCs in vitro . For in vivo experiments, baicalin reduced thrombus weight and mitigated DVT formation in model rats. Moreover, baicalin activated SIRT but repressed NF-κB signaling in IVC tissues of DVT rats. Conclusion: Baicalin facilitates migration and angiogenesis of EPCs but impedes thrombus formation via regulation of SIRT1/NF-κB signaling in DVT model rats.
研究领域:
药理学
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血管生物学
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心血管疾病
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PubMed
高影响因子
Chemical Biology & Drug Design
·
2024
·Vol. 103
·期 4
·e14522
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IF 3.2
Wanting Fu,Ziyuan Liu,Yingzhou Wang,Xindi Li,Xiang Yu,Yang Li,Zejun Yu,Yinsheng Qiu,Zhinan Mei,Lingyun Xu
Pyroptosis is a programmed cell death process that frequently occurs in many diseases, including hyperuricemic nephropathy (HN). In HN, a range of stimuli mediates inflammation, leading to the activation of inflammasomes and the production of gasdermin D (GSDMD). Baicalin (BA), a natural flavonoid renowned for its antioxidant and anti-inflammatory properties, was investigated for its role in HN in this study. Initially, HN-like inflammation and pyroptosis were induced in HK-2 cells with treatment of monosodium urate (MSU), followed by the BA treatment. The expression of pyroptosis-associated genes, Panx-1 and P2X7, at both mRNA and protein levels was assessed through real-time polymerase chain reaction (RT-qPCR) and Western blotting (WB) without or with BA treatment. The results showed that expression of Panx-1 and P2X7 at mRNA and protein levels was increased in MSU-treated HK-2 cells, which subsequently decreased upon the BA treatment. Further experiments showed that BA could combine NLRP3 inflammasome and GSDMD, destabilizing GSDMD protein. Moreover, BA protected the cell membrane from MSU-induced damage, as evidenced by Hoechst 33342 and PI double staining, lactate dehydrogenase (LDH) assays, and electron microscopy observations. These results suggest that BA is involved in the regulating Panx-1/P2X7 pathways and thus inhibits pyroptosis, highlighting its potential therapeutic effect for HN.
研究领域:
药理学
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细胞生物学
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分子生物学
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肾病学
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PubMed
高影响因子
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