EUROPEAN JOURNAL OF PHARMACOLOGY
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2022
·
IF 5.195
Yang Lin,Zi-Yuan Wang,Ma-Jie Wang,Zheng-Meng Jiang,Ya-Qiu Qin,Tian-Qing Huang,Yu Song,Hui-Ting Liang,E-Hu Liu
In this work, we examined whether baicalin (BC), a bioactive flavonoid in Scutellaria baicalensis Georgi, can reduce high-fat diet (HFD)-induced metabolic syndrome (MetS) in mice. The UPLC-QTOF/MS was used for metabolome profiles analysis, and an analysis of bacterial 16S rDNA in feces was used to examine the effects of BC on gut microbiota composition. Our results showed that BC (400 mg/kg) could reduce the body weight gain, decrease hepatic fat accumulation and abnormal blood lipids, and increase insulin sensitivity after 8 weeks of treatment. BC could reverse the alteration of 7 metabolites induced by HFD and the metabolic pathways responsive to BC intervention including citrate cycle, alanine , aspartate and glutamate metabolism, glycerophospholipid metabolism, and aminoacyl-tRNA biosynthesis. 16S rDNA analysis demonstrated that BC altered the composition and function of gut microbiota in MetS mice. Notably, we found that the change in succinic acid was negatively associated with the changes in Bacteroides and Sutterella , and positively associated with the change in Mucispirillum . Moreover, we confirmed that succinic acid displayed a metabolic protective effect on MetS mice. The antibiotic treatment verified that BC exert s metabolic protection through gut microbiota. Our findings suggested BC may be a potential therapeutic drug to ameliorate diet induced MetS and gut microbiome may be a novel mechanistic target of BC for treatment of MetS.
研究领域:
药理学
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代谢组学
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微生物学
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营养学
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DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2025
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IF 5.4
Si-yu Liu,Chang-qing Wang,Tong-tong Luo,Gui-juan Cui,Yuan Zhang,Xing-ju Zou,Zi-jian Zhang,Wen-xiu Liu,Chen Sun,Cheng Peng
Ethnopharmacological relevance Scutellaria baicalensis , a traditional Chinese medicine herb, has been classically used to treat diarrhea and dysentery caused by damp heat in Traditional Chinese Medicine. And it has been demonstrated to alleviate colonic mucosal inflammation in ulcerative colitis. However, the mechanism through which its main active ingredient, baicalin, alleviates ulcerative colitis remains unclear. Aim of the study This study investigated whether baicalin regulates macrophages to ameliorate ulcerative colitis through the JAK1/STAT1/SOCS1 pathway. Materials and methods LPS-induced RAW264.7 cells were used to investigate the anti-inflammatory and regulatory effects of baicalin on macrophage polarization. The NO content was assessed by a Griess assay, and label-free optical diffraction tomography for live-cell imaging and confocal imaging were conducted to observe macrophage polarization and analyze the expression of CD86 and CD206. The protective effect of baicalin on DSS-induced colitis mice was evaluated through the Disease Activity Index (DAI) system, endoscopy, enzyme-linked immunosorbent assay (ELISA), hematoxylin and eosin (HE) staining, Alcian Blue periodic acid Schiff (AB-PAS) staining, and immunofluorescence. Macrophages in the lamina propria of the colon were analyzed by tiling light sheet microscopy imaging and flow cytometry. Western blotting (WB) was used to evaluate the expression of JAK1/STAT1/SOCS1 pathway members, and the expression of the downstream transcription factors were quantified through qPCR. Key results Baicalin markedly inhibited NO levels induced by LPS and delayed the timing and quantity of macrophage polarization toward the M1 phenotype. Furthermore, baicalin ameliorated the symptoms of colitis in mice, such as diarrhea, hematochezia, weight loss, colon shortening, decreased spleen weight, pathological changes, intestinal mucosal barrier dysfunction, and decreased DAI and inflammatory factor levels. Moreover, baicalin promoted macrophage polarization toward the M2 phenotype and inhibited the polarization of M1 macrophages in the intestinal lamina propria. Mechanistically, baicalin inhibited the phosphorylation of JAK1 and STAT1 and restored the negative feedback inhibition of JAK1/STAT1 by upregulating SOCS1. In addition, baicalin reduced the mRNA levels of downstream genes. Conclusions and implications Baicalin can alleviate intestinal inflammation, ameliorate intestinal barrier damage, and regulate macrophage polarization by inhibiting M1 macrophage polarization in an ulcerative colitis model. This protective effect was achieved through the JAK1/STAT1/SOCS1 pathway.
研究领域:
药理学
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免疫学
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民族药理学
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分子生物学
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胃肠病学
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DOI
PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
·
2026
·Vol. 40
·期 8
·e70534
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IF 1.7
Ruyang Cheng,Weining Song,Yu Wang,Yehao Wang,Xiaomin Xu,Fang Lu,Donghua Yu,Pingping Chen,Shumin Liu
In this study, we explored the therapeutic effects and mechanisms of baicalin (BA) in a dibutyltin dichloride (DBTC)–induced chronic pancreatitis (CP) rat model using metabolomics and network pharmacology. The results showed that BA significantly reduced inflammatory cell infiltration and fibrosis in pancreatic tissues, lowered serum levels of interleukin (IL)-1β, IL-6, tumor necrosis factor-alpha (TNF-α), amylase (AMS), and lipopolysaccharide (LPS) and thereby decreased expression of alpha-smooth muscle actin (α-SMA) and fibronectin (FN) in pancreatic tissues. Metabolomic analyses revealed that BA influences multiple metabolic pathways, including glycerophospholipid and arachidonic acid metabolism, in serum and urine. Network pharmacology identified key targets, such as phospholipase A2 group IVA (PLA2G4A) and transient receptor potential vanilloid 4 (TRPV4), which are primarily involved in IL-17 signaling, as well as other pathways beyond inflammation. Further integrated analysis demonstrated that BA inhibits pancreatic stellate cell activation and reduces pancreatic fibrosis by regulating metabolites, such as arachidonic acid, that act on the PLA2G4A/TRPV4 and transforming growth factor-beta 1 (TGF-β1)/SMAD family member 3 (SMAD3) pathways. Molecular docking studies confirmed that BA binds strongly to these targets. In summary, BA exerts anti-inflammatory and antifibrotic effects through multiple targets and pathways, thereby alleviating the pathological progression of CP.
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PubMed
高影响因子
THERIOGENOLOGY
·
2026
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IF 2.9
Lin-Feng Li,Hao Shen,Zhi-Min Qi,Tian Luo,Sheng-Ming Liu,Li-Li Ou,Chang-Long Xu,Yu Liu
Repeated superovulation is widely applied in livestock reproduction programs to enhance ovulation rate and embryo yield, but increasing evidence indicates that intensive stimulation may disrupt ovarian homeostasis and impair oocyte quality. This study evaluated whether baicalin, a bioactive flavonoid, can mitigate ovarian dysfunction induced by repeated superovulation. Female mice were subjected to four cycles of superovulation with or without baicalin treatment. Physiological parameters and reproductive outcomes were recorded. Ovarian and fecal metabolomic profiles, as well as gut microbiota composition, were analyzed by LC–MS and 16S rRNA sequencing. Histological and molecular analyses were performed to assess ovarian morphology, steroidogenesis, AMPK/Foxo3a-mediated glycolysis, and oocyte quality. Repeated superovulation induced follicular atresia, metabolic disturbances characterized by excessive glycolysis, suppression of AMPK/Foxo3a signaling, gut microbial dysbiosis, and reduced MII oocyte quality. Baicalin markedly alleviated these alterations by restoring metabolic and signaling homeostasis, improving microbial balance, and preserving oocyte maturation and spindle integrity. Collectively, these findings provide new insights into the metabolic basis of ovarian dysfunction induced by repeated superovulation and suggest that baicalin may help preserve ovarian function and oocyte quality under conditions of intensive ovarian stimulation, with potential relevance to the sustainability of donor animals in livestock reproduction programs.
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PubMed
高影响因子
Animals
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2025
·Vol. 15
·期 16
·2457
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IF 2.7
Qirong Lu,Xuwen Liu,Junke Tian,Pu Guo,Chun Ye,Shulin Fu,Yu Liu,Yinsheng Qiu
Simple SummaryGlaesserella parasuis(GPS), a Gram-negative bacterium that colonizes piglets’ upper respiratory tracts, causes Glässer’s disease including peritonitis under stress, though the peritonitis mechanism remains unclear. Baicalin, a main active component of Huangqin (Scutellaria baicalensis), exhibits significant anti-inflammatory effects. This study aimed to investigate the mechanism by which baicalin alleviatesGPS-induced peritonitis in piglets. We examined the effects of baicalin on inflammatory responses and key signaling molecules in both porcine peritoneal mesothelial cells (PPMCs) in vitro and the peritoneum ofGPS-infected piglets in vivo. Our results showed that baicalin significantly reducedGPS-induced expression of pro-inflammatory cytokines (tumor necrosis factor alpha, interleukin-1 beta, and interleukin-6) and inhibited the upregulation of disintegrin and metalloproteinase 17 (ADAM17), phosphorylated epidermal growth factor receptor (EGFR)/EGFR, and phosphorylated extracellular signal-regulated kinase (ERK)/ERK. Mechanistically, baicalin inhibited ADAM17 overexpression-induced upregulation of this pathway and cytokines in PPMCs, while ADAM17 small interfering RNA attenuatedGPS-induced effects. These findings demonstrate that baicalin mitigatesGPS-induced peritonitis by suppressing the ADAM17/EGFR axis and the subsequent cytokine production, thus providing a theoretical basis for novelGPScontrol strategies and the development of novel non-antibiotic strategies, including phytochemical therapeutics and feed additives.Glaesserella parasuis(GPS) is a Gram-negative, pathogenic bacterium that colonizes the upper respiratory tract of piglets and causes Glässer’s disease with peritonitis under stress conditions. The mechanism underlying GPS-induced peritonitis in piglets remains unclear. Baicalin is one of the main active ingredients of Huangqin (Scutellaria baicalensis), which has a significant anti-inflammatory effect on inflammatory diseases. Therefore, this study aimed to elucidate the molecular mechanism by which baicalin alleviatesGPS-induced peritonitis in piglets, specifically focusing on the role of the ADAM17/EGFR signaling axis. We investigated the effects of baicalin in vitro using porcine peritoneal mesothelial cells (PPMCs) and in vivo in GPS-infected piglets. Our results showed that baicalin reduced the expression of the pro-inflammatory cytokines tumor necrosis factor alpha (TNF-α), interleukin-1 beta (IL-1β), and interleukin-6 (IL-6) in PPMCs and the peritoneum of piglets afterGPSinfection. Concurrently, baicalin significantly reduced the upregulation of disintegrin and metalloproteinase 17 (ADAM17), phosphorylated epidermal growth factor receptor (p-EGFR)/EGFR, and phosphorylated extracellular signal-regulated kinase (p-ERK)/ERK induced byGPSinfection in PPMCs and the peritoneum of piglets. Crucially, in vitro mechanistic investigations revealed that baicalin can significantly reduce the upregulation of ADAM17, p-EGFR/EGFR, p-ERK/ERK, TNF-α, IL-1β, and IL-6 induced by ADAM17 overexpression in PPMCs. Furthermore, ADAM17 small interfering RNA can significantly reduce the upregulation of ADAM17, p-EGFR/EGFR, p-ERK/ERK, TNF-α, IL-1β, and IL-6 induced byGPSinfection in PPMCs. These findings demonstrate that baicalin can inhibit the expression of inflammatory factors TNF-α, IL-1β, and IL-6 through the ADAM17/EGFR axis, and then alleviate the peritonitis caused byGPSin piglets. This provides a theoretical basis for developing novel non-antibiotic strategies, including phytochemical therapeutics and feed additives, for preventing and controlling GPS.
研究领域:
兽医学
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微生物学
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药理学
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免疫学
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分子生物学
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畜牧学
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PubMed
高影响因子
RSC Advances
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2015
·Vol. 5
·期 52
·41377-41384
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IF 3.84
Xiaoli Gu,Hongliang He,Chong-zhi Wang,Yankun Gao,Hongjuan Zhang,Junli Hong,Shuhu Du,Lina Chen,Chun-su Yuan
Surface molecularly imprinted polymers (MIP@SBA-15) imprinted on the surface of hybrid nanostructured organic/inorganic materials (SBA-15) were prepared for the selective extraction and detection of baicalin (BA) in biological samples. The surface morphologies and characteristics of the imprinted and non-imprinted polymers were characterized by Fourier transform infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), transmission electron microscopy (TEM), thermogravimetric analysis (TGA) and nitrogen adsorption–desorption isotherms. The results indicated that the polymers were successfully grafted onto the surface of SBA-15 and possessed a highly ordered mesoporous structure. In binding tests, MIP@SBA-15 reached saturated adsorption within 80 min and exhibited significant specific recognition toward BA with a large adsorption capacity. In addition, the prepared MIP@SBA-15 was used as a selective sorbent for solid-phase extraction of BA from biological samples. Recoveries of BA from the liver and spleen ranged from 90.6% to 90.9% with RSD <3.7%. All these results reveal that this method is simple, rapid and sensitive for effectively extracting and detecting trace BA in biological samples.
研究领域:
分析化学
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药物分析
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材料科学
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PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
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IF 7.7
Yucheng Yan,Safdar Ali Amur,Hong Liu,Ruoyao Shen,Huaiqing Sun,Yunlin Pei,Chaowan Guo,Hao Liang
With the extensive application of baicalein in the treatment of cardiovascular and cerebrovascular diseases, its clinical and market demand has gradually expanded. But the natural yield of baicalein is very low, and it is mainly prepared by the deglycosylation of baicalin. However, the insolubility of baicalin in water significantly limits the deglycosylation of it under biocatalysis. To make biocatalysis of baicalin more efficient and environmental, a strategy was designed to enhance its water solubility through the solubilization mechanism of endogenous biological macromolecules, and the effect on the activity of glucuronidase was further explored. The results showed that wrapping with Scutellaria baicalensis polysaccharide (SBP) significantly improved the solubility of baicalin in water (the water solubility of baicalin increased by 23 times, BI/SBP = 1/12, w/w ). It was not only contributed to the efficient production of baicalein by one-pot method, but also effectively improved the deglycosylation rate of baicalin (increase by 47.04 % in aqueous solution). With the help of the solubilization of endogenous polysaccharide on baicalin in aqueous solution, a green, low-cost and efficient method (one-pot method) was designed to simultaneously extract and enzymatic hydrolyze baicalin to prepare baicalein. Under the same conditions, the yield of one-pot method is 87.17 %, which was much higher than that of the conventional method (29.38 %). In addition, one-pot method with the aid of endogenous polysaccharide could simply and conveniently prepare aglycone of other insoluble natural flavonoids, which has a wide range of industrial application value.
研究领域:
药理学
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生物技术
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化学工程
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DOI
PubMed
高影响因子
PHYTOMEDICINE
·
2023
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IF 7.9
Yi Cai,Shisheng Jiang,Chaoming Huang,Ao Shen,Xuan Zhang,Wanling Yang,Yichuan Xiao,Shuhan Gao,Rong Du,Guodong Zheng,Tingdong Yan,Chunpeng (Craig) Wan
Background The conserved sirtuin protein sirtuin 3 (SIRT3) is a vital protective protein for cardiac hypertrophy. Inhibition of SIRT3 accelerated the development of heart hypertrophy. On the other hand, myocardial hypertrophy was prevented by overexpressing SIRT3. SIRT3 has been proposed as a potential therapeutic target for managing or averting heart hypertrophy. Baicalin, a flavonoid extracted from the Scutellaria baicalensis plant, has anti-cardiovascular properties, including protection against cardiac hypertrophy. However, the molecular mechanism of the anti-hypertrophic effect of baicalin is not well known. Purpose In this study, we aim to investigate the effect of baicalin on cardiac hypertrophy and explored its underlying molecular mechanisms. Study-design/methods Abdominal aortic constriction (AAC)-induced mouse cardiac hypertrophy and angiotensin II (Ang II)-induced cardiomyocyte hypertrophy models were established. After baicalin treatment, cardiac hypertrophy was monitored by detecting the expression of hypertrophic genes and cell surface area. Echocardiogram was performed to check the heart function in vivo . Moreover, the protein expression of the SIRT3-dependent pathway was detected by Western blotting. Results In this work, we demonstrated that baicalin might suppress the cell surface area and the expression of the Ang II -induced myosin heavy chain β (β-MHC), brain natriuretic polypeptide (BNP), and atrial natriuretic factor (ANF). Additionally, it reduced the AAC rats' hypertrophic impact. We also found that baicalin prevents cardiac hypertrophy by regulating SIRT3/LKB1/AMPK signaling pathway. Moreover, we showed that baicalin upregulated the SIRT3 protein expression by inhibiting proteasome and by the activation of 20 S proteasome subunit beta type-5 (PSMB5). Conclusion These results offer the first proof that baicalin inhibits cardiac hypertrophy due to its effect on the SIRT3-dependent signaling pathway, indicating its potential for treating cardiac hypertrophy and heart failure. The present study provides a preliminary experimental basis for the clinical application of baicalin and baicalin-like compounds.
研究领域:
心脏病学
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药理学
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分子生物学
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PubMed
高影响因子
Drug Design Development and Therapy
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2022
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IF 4.319
Nan Li,Zhenzhen Han,Lin Li,Bing Zhang,Zhidong Liu,Jiawei Li
Purpose The objective of this study was to investigate the effects of the solid lipid nanoparticles of baicalin (BA-SLNs) on an experimental cataract model and explore the molecular mechanism combined with bioinformatics analysis.Materials and methods The transparency of lens was observed daily by slit-lamp and photography. Lenticular opacity was graded. Two-dimensional gel electrophoresis (2-DE) was employed to analyze the differential protein expression modes in each group. Proteins of interest were subjected to protein identification by nano-liquid chromatography tandem mass spectrometry (LC–MS/MS). Bioinformatics analysis was performed using the Ingenuity Pathway Analysis (IPA) online software to comprehend the biological implications of the proteins identified by proteomics.Results At the end of the sodium selenite-induced cataract progression, almost all lenses from the model group developed partial nuclear opacity; however, all lenses were clear and normal in the blank group. There was no significant difference between the BA-SLNs group and the blank group. Many protein spots were differently expressed in 2-DE patterns of total proteins of lenses from each group, and 65 highly different protein spots were selected to be identified between the BA-SLNs group and the model group. A total of 23 proteins were identified, and 12 of which were crystalline proteins.Conclusion We considered crystalline proteins to play important roles in preserving the normal expression levels of proteins and the transparency of lenses. The general trend in the BA-SLN-treated lenses’ data showed that BA-SLNs regulated the protein expression mode of cataract lenses to normal lenses. Our findings suggest that BA-SLNs may be a potential therapeutic agent in treating cataract by regulating protein expression and may also be a strong candidate for future clinical research.
研究领域:
药理学
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眼科学
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生物化学
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分子生物学
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DOI
PubMed
高影响因子
NEPHROLOGY
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2023
·
IF 2.5
Ziyuan Liu,Huilong Xiang,Qin Deng,Wanting Fu,Yang Li,Zejun Yu,Yinsheng Qiu,Zhinan Mei,Lingyun Xu
Aim Inflammation and apoptosis are main pathological processes that lead to the development of hyperuricemic nephropathy (HN). This study aims to explore whether baicalin (BA) and baicalein (BAI) can relieve the damage through PI3K/AKT/NF-κB signal pathway and provide more reliable and precise evidence for the treatment of HN. Methods HN mice were induced by yeast extract with potassium oxonate (PO), and HK-2 cells were induced by monosodium urate (MSU). Molecular docking, western blot, q-PCR, and other methods were used to explore the changes of various indicators in HN mice and HK-2 cells. Results Molecular docking results showed that BA and BAI had good binding ability with PI3K, AKT, p65 and IκBα. BA and BAI significantly ameliorated the levels of renal function, decreased the p-PI3K, p-AKT and p-p65 expression, down-regulated the BAX/BCL2 and CASP3, and blunted the mRNA levels of tumour necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-18 in both renal tissue of HN mice and HK-2 cells induced by MSU. BA and BAI also decreased the oxidative stress level of MSU-induced HK-2 cells. Conclusion BA and BAI were confirmed to attenuate HN through alleviating renal inflammatory and apoptosis in cells and tissues by inhibiting PI3K/AKT/NF-κB pathway. BA and BAI were expected to be developed as new anti-HN drugs.
研究领域:
药理学
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肾病学
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分子生物学
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细胞生物学
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DOI
PubMed
高影响因子
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
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2025
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IF 2.5
Mingming Wang,Zan Sun,Jian Hu,Qiaoyan Huang,Weifeng Long,Zhengjia Shen,Ya Li,Ping Wang
Baicalin is a flavonoid glycoside with substantial biological activity and pharmacological effects, primarily extracted from Scutellaria baicalensis Georgi. However, its clinical implementation has been impeded by suboptimal aqueous solubility and unfavorable bioavailability. This study employed a supercritical anti-solvent (SAS) process to prepare amorphous solid dispersions of baicalin, aiming to enhance its dissolution and bioavailability. The effects of supercritical temperature, supercritical pressure, and CO2 flow rate on encapsulation were thoroughly investigated using the Box-Behnken Design (BBD) response surface methodology. SEM, FTIR, DSC, and XRD analyses confirmed that the baicalin solid dispersion prepared via the SAS method was in an amorphous state. In vitro dissolution tests indicated that the solubility of baicalin in the solid dispersion was 9.4 times (pH = 6.8) greater than that of the raw baicalin particles. Furthermore, rat experiments revealed that the bioavailability of baicalin in the solid dispersions was 1.8 times higher than that in traditional particles. Notably, BASD exhibited strong inhibitory effects on the growth of Bacillus subtilis and Escherichia coli. Consequently, a solid dispersion of baicalin was successfully prepared using the BBD-optimized SAS process, significantly enhancing the performance of baicalin.
研究领域:
药剂学
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药物递送
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超临界流体技术
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药用材料科学
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生物药剂学
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DOI
PubMed
高影响因子
Food Frontiers
·
2026
·Vol. 7
·期 6
·e70370
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IF 6.3
Jingzheng Li,Honglin Jiang,Jianwen He,Wen Yao
Lactation represents one of the most metabolically demanding physiological states in mammals, characterized by heightened bioenergetic flux that increases electron transport chain (ETC) activity. This metabolic feature renders the maternal liver highly susceptible to mitochondrial redox imbalance under heat stress (HS). Baicalin (BAI), a nature food-derived flavonoid from Scutellaria baicalensis , is known for its antioxidant and hepatoprotective properties, but its mechanism in lactational HS has not been fully elucidated. Here, we demonstrate that BAI exerts its hepatoprotective effects by targeting the Sirt3–NDUFS1 axis to preserve mitochondrial complex I redox homeostasis in lactating mammals. Using a lactational HS mouse model and AML-12 hepatocytes, we demonstrate that BAI attenuates HS-induced hepatic injury, oxidative stress, and mitochondrial dysfunction. Mechanistically, BAI restored the expression of the mitochondrial deacetylase Sirt3, which was suppressed by HS. This led to deacetylation of the complex I core subunit NDUFS1, thereby rescuing complex I activity and limiting mitochondrial reactive oxygen species (mtROS) overproduction. BAI also attenuated secondary excessive Pink/PARKIN-dependent mitophagy triggered by mitochondrial respiratory failure, revealing coordinated recovery of electron transport function and downstream mitochondrial quality control. Pharmacological inhibition of Sirt3 abolished the protective effects of BAI on mitochondrial respiration and redox balance, confirming Sirt3 dependence. These findings reveal a BAI–Sirt3–NDUFS1 axis maintaining mitochondrial complex I redox homeostasis, thereby enhancing maternal hepatic resilience to HS. Distinct from previous Sirt3 research in nonreproductive disease models, this work establishes a natural nutritional target strategy specialized for HS lactating subjects, with great potential for maternal nutritional intervention and functional food development.
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高影响因子
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