Background:Diquat,a commonly employed bipyridyl herbicide,is recognized for its hepatotoxic effects attributed to the generation of reactive oxygen species.Baicalin(BAI),a flavonoid derivative,has garnered significant...Background:Diquat,a commonly employed bipyridyl herbicide,is recognized for its hepatotoxic effects attributed to the generation of reactive oxygen species.Baicalin(BAI),a flavonoid derivative,has garnered significant research interest for its hepatoprotective properties.Nevertheless,the clinical application of BAI is constrained by its limited water solubility and poor bioavailability.To address these challenges,BAI-nanoliposome(BAI-NL)has emerged as a novel drug delivery platform aimed at enhancing therapeutic outcomes.Methods:We used diquat-induced liver injury mouse model and AML12 hepatocytes to test the pro-tective effect of BAI and BAI-NL on liver inflammation,oxidative stress,and mitochondrial function.The parameters included histological,biochemical,and molecular biological analyses.Results:In the diquat-induced model,both BAI and BAI-NL exhibited effectiveness on attenuating liver inflammation.Ex vivo analyses further indicated that BAI-NL was superior to BAI in preserving mito-chondrial membrane potential,reducing oxidative stress,and modulating the phosphatase and tensin homolog-induced putative kinase 1(PINK1)/Parkin RBR E3 ubiquitin-protein ligase(Parkin)signaling pathway.These findings enhanced mitophagy and facilitated the removal of damaged mitochondria.Conclusions:BAI-NL exhibited superior hepatoprotective effects compared to free BAI,possibly by re-ducing inflammation,preserving mitochondrial homeostasis,and reinstating autophagic balance through modulation of the PINK1/Parkin signaling pathway.These outcomes indicate a groundbreaking method for addressing liver diseases and underscore the potential of nanoliposome technology in augmenting the efficacy of natural compounds.展开更多
[Objectives]To establish a high-performance liquid chromatography(HPLC)method for the simultaneous determination of forsythin,baicalin,and chlorogenic acid in a traditional Chinese medicine spray disinfectant.[Methods...[Objectives]To establish a high-performance liquid chromatography(HPLC)method for the simultaneous determination of forsythin,baicalin,and chlorogenic acid in a traditional Chinese medicine spray disinfectant.[Methods]The chromatographic separation was performed on a GL Sciences(19H0044724)-C_(18)column(4.6 mm×250 mm,5μm)with a mobile phase of acetonitrile-0.05%formic acid solution at a flow rate of 1 mL/min.The injection volume was 10μL,detection wavelength was set at 280 nm,and column temperature was maintained at 25℃.[Results]The linear ranges of forsythin,baicalin,and chlorogenic acid were 10.5-52.5,20.6-103,and 14.2-71μg/mL,respectively,with good linear relationships between concentration and peak area(R^(2)=0.9999).The relative standard deviations(RSD s)for precision and repeatability tests were all≤1.0%.The average recoveries were 98.51%,98.48%,and 97.71%for the three components,with RSD s of 0.96%,0.97%,and 0.73%,respectively.[Conclusions]This method demonstrates strong specificity,high precision,excellent accuracy,and simplicity of operation,making it suitable for the simultaneous quantification of forsythin,baicalin,and chlorogenic acid in traditional Chinese medicine spray disinfectants.It provides a reliable basis for quality control and practical applications in animal breeding environments.展开更多
Objective:To explore the potential mechanisms of a baicalin-geniposide combination against cerebral ischemia using a network pharmacology strategy.Method:We used network pharmacology integrating drug-target-disease in...Objective:To explore the potential mechanisms of a baicalin-geniposide combination against cerebral ischemia using a network pharmacology strategy.Method:We used network pharmacology integrating drug-target-disease interactions to identify key pathways which were validated in a rat middle cerebral artery occlusion model treated with baicalin(55 mg/kg),geniposide(5 mg/kg),or their 11:1 combination.Therapeutic efficacy and mechanistic insights were evaluated using triphenyltetrazolium chloride staining,Evans blue assay,enzyme-linked immunosorbent assay,and Western blot.Results:The results revealed that the nuclear factor-kappa B(NF-κB)signaling pathway is inhibited in combination treatment of cerebral ischemia.Ten targets were identified as key nodes in the protein-protein interaction network:interleukin 6(IL-6),interleukin-1β,interleukin 18,C-C motif ligand 2,C-C motif ligand 4,interleukin 10,interferon-γ-inducible protein 10,C-C motif ligand 3,tumor necrosis factor-α(TNF-α),interleukin-1α.The baicalin-geniposide combination significantly reduced infarct volume,improved neurological deficits,and alleviated brain edema/blood-brain barrier leakage compared with monotherapy.Additionally,it significantly inhibited toll-like receptor 4(TLR4)/NF-κB signaling and downregulated pro-inflammatory cytokines TNF-αand IL-6 levels.Conclusion:The baicalin-geniposide combination alleviated cerebral ischemia-reperfusion injury by synergistically suppressing the TLR4/NF-κB pathway and its downstream inflammatory factors.展开更多
Background:Baicalin(BC)and geniposide(GD)are effective components of natural remedies,and studies have shown that they protect against cerebral ischemic stroke(CIS).Transient receptor potential vanilloid 4(TRPV4)is a ...Background:Baicalin(BC)and geniposide(GD)are effective components of natural remedies,and studies have shown that they protect against cerebral ischemic stroke(CIS).Transient receptor potential vanilloid 4(TRPV4)is a calcium-permeable channel that plays important roles in vascular function and vasodilation.However,no studies are available on the effect of BC/GD on the TRPV4 channel and rat cerebral basilar artery(CBA).This study examined the effect of the combination of BC/GD(7:3)on cerebral vascular function after CIS.Methods:We used western blotting to determine TRPV4 protein levels and live cell fluorescence Ca 2+imaging and patch clamp to determine how BC/GD activates TRPV4 channels.Isolated vessel experiments were used to observe the dilatory effects of BC/GD on CBA under different conditions.Laser Doppler imaging was used to measure cerebral blood flow in rats.Triphenyl tetrazolium chloride and Nissl stainings were used to determine the infarct area in the rat brain and neuronal damage,respectively.Results:BC/GD significantly boosted TRPV4 protein levels in vascular smooth muscle cells(VSMCs)during oxygen-glucose deprivation and increased[Ca 2+]i in TRPV4-HEK 293 cells and VSMCs.This effect was not observed in vector-HEK 293 cells.In patch clamp experiments,BC/GD increased Ca 2+currents in TRPV4-HEK 293 cells,whereas no significant changes were observed in vector-HEK 293 cells.BC/GD dilated CBA contractions induced by U46619 and KCl,with a concentration-dependent increase of the dilatory effect.In the middle cerebral artery occlusion model,cerebral blood flow in the ischemic side significantly decreased,whereas BC/GD intervention significantly increased cerebral blood perfusion in the ischemic side,reduced the infarct area,and improved neurological function scores and neuronal damage.Conclusion:BC/GD activates the TRPV4 channel,leading to Ca ^(2+) influx,which in turn activates the intermediate conductance calcium-activated potassium channels channel to regulate vasodilation in vascular smooth muscle.展开更多
Background:Scutellaria root(root of Scutellaria baicalensis),which has potent anti-inflammatory effects,is a component of useful traditional formulaes.Albeit a low frequency,it has been reported to cause severe inters...Background:Scutellaria root(root of Scutellaria baicalensis),which has potent anti-inflammatory effects,is a component of useful traditional formulaes.Albeit a low frequency,it has been reported to cause severe interstitial pneumonia and liver dysfunction.Importantly,the hepatotoxicity induced by Scutellaria root can be controlled by the baicalin content,one of its major constituents.This study aimed to clarify the role of MRP2 in modulating baicalin-induced cytotoxicity in HepG2 cells,providing insights that inform safer use and assessment of baicalin.Methods:Cytotoxicity of HepG2 and MDCK cells was assessed using a cell counting kit-8 assay in the presence and absence of MK571,an MRP2 inhibitor.MRP2 expression levels were confirmed using agarose gel electrophoresis,and intracellular baicalin concentrations were measured using LC/MS.Results:Baicalin exhibited concentration-dependent cytotoxicity,with higher toxicity observed in MRP2-negative MDCK cells than in MRP2-positive HepG2 cells.Pre-treatment with MK571 increased baicalin-induced cytotoxicity in HepG2 cells and doubled the intracellular baicalin concentration.Conclusion:Our results indicated that MRP2 plays an important role in reducing baicalin-induced hepatocyte toxicity by decreasing intracellular baicalin levels.Monitoring MRP2 activity could serve as a critical predictive biomarker to identify individuals at higher risk of baicalin-induced hepatotoxicity,enabling personalized dosing strategies and minimizing adverse effects associated with Scutellaria root-containing formulae.展开更多
Baicalin,a major flavonoid compound found in Scutellariae radix,is the first SARS-CoV-23CLpro virus inhibitor.Therefore,developing an accurate and reliable strategy to detect baicalin in biological systems is vital.He...Baicalin,a major flavonoid compound found in Scutellariae radix,is the first SARS-CoV-23CLpro virus inhibitor.Therefore,developing an accurate and reliable strategy to detect baicalin in biological systems is vital.Herein,we report the first indolyl-lanthanide metal-organic framework(MOF)materials and their application as baicalin sensors.The results of this study indicate that the new crystal structure has good stability and luminous performance.The detection limits of baicalin in serum and urine are 0.05 and 0.04μmol/L,respectively,suggesting high sensitivity and selectivity.Various background substances present in practical samples,such as anions,cations,and amino acids,do not interfere with the photoluminescence analytical signal of Eu^(3+).We identified that the quenching of the Eu-MOF is due to the inner filter effect,absorption energy competition,and photoinduced electron transfer among the baicalin,ligand,and MOF through powder X-ray diffraction analysis,Fourier transform infrared spectroscopy,luminescence lifetimes,ultraviolet studies,and computational analysis.Thus,we designed a convenient,sensitive,and facile detection method using the Eu-MOF and demonstrate that Eu^(3+)-based materials are promising sensors for baicalin detection in actual serum and urine.Additionally,the prepared Eu-MOF@polyvinyl alcohol composite matrix membrane test film has considerable practical application value for the portable detection of baicalin.展开更多
Background Intestinal inflammation is a common and serious health problem in piglet production,especially enteritis caused by pathogenic Escherichia coli(E.coli).This condition often leads to high mortality,slow weigh...Background Intestinal inflammation is a common and serious health problem in piglet production,especially enteritis caused by pathogenic Escherichia coli(E.coli).This condition often leads to high mortality,slow weight gain,and significant economic losses.Results In this study,we isolated an E.coli strain,SKLAN202302,from the colon of diarrheal piglets to create an intestinal inflammation model for evaluating the protective effects of baicalin.Piglets infected with E.coli exhibited significant reductions in body weight,feed intake,small intestine length,and ileal goblet cell count(P<0.05),along with deteriorated ileal morphology.However,baicalin supplementation resulted in body weights,feed intake,and intestinal morphology similar to those of the control group.Notably,there was a significant increase in the colonization of Lactobacillus species,particularly Lactobacillus_reuteri,Lactobacillus_amylovorus,and Lactobacillus_johnii,compared to the E.coli group(P<0.05).At the metabolic and transcriptional levels,E.coli infection increased inflammatory mediators,including eicosanoids(leukotriene F4,prostaglandin F1a,leukotriene E4,thromboxane B2,prostaglandin G2,and PGH2),monosaccharides,and TCA cycle intermediates(oxoglutaric acid,glutaric acid,adipic acid,citric acid,and isocitric acid)in the ileum.It also promoted the expression of genes related to autoimmune diseases and the Th17 differentiation signaling pathway(CTLA4,IFN-ALPHA-8,IL12RB2,TRAV3,TRAV16,FOS,and VEGFA),as well as inflammatory factors.Conversely,baicalin supplementation not only counteracted these effects but also enhanced the presence of metabolites such as phospholipids[including lyso PC(P-18:1(9Z)/0:0),PC(17:0/0:0),lyso PC(16:1(9Z)/0:0),PC(18:0/0:0),lyso PC(18:0/0:0),PA(10:0/i-16:0),and PA(10:0/8:0)]and amino acids.It also regulated genes within the IL-17 signaling pathway(IL4,CCL17,CXCL10,IFNG,and CXCL2),suggesting a mechanism by which baicalin mitigates E.coli-induced intestinal and microbial disturbances.Subsequent flow cytometry analysis showed that E.coli infection increased the numbers of CD3+and Foxp3+cells,decreased IL-17A+cells,and reduced Th17/Treg ratios.Baicalin supplementation restored these parameters to control levels.Conclusions Baicalin supplementation effectively alleviates E.coli-induced intestinal inflammation and microbial disturbances in piglets by enhancing beneficial Lactobacillus colonization,counteracting inflammatory mediators,and regulating immune-related gene expression and the Th17/Treg balance.These findings highlight baicalin's potential in alleviating intestinal inflammation.展开更多
Background Baicalin and probiotic cocktails are promising feed additives with broad application prospects.While probiotic cocktails are known to enhance intestinal health,the potential synergistic impact of combining ...Background Baicalin and probiotic cocktails are promising feed additives with broad application prospects.While probiotic cocktails are known to enhance intestinal health,the potential synergistic impact of combining baicalin with probiotic cocktails on the gut health of broiler chickens remains largely unexplored.Therefore,this study aims to investigate the influence of the combined administration of baicalin and probiotic cocktails on the composition of ileal and cecal microbiota in broiler chickens to elucidate the underlying mechanisms responsible for the healthpromoting effects.Results A total of 3201-day-old male Arbor Acres broilers were divided into 4 groups,each with 8 replicates of 10 chicks per replicate.Over a period of 42 d,the birds were fed a basal diet or the same diet supplemented with 37.5 g/t baicalin(BC),1,000 g/t probiotic cocktails(PC),or a combination of both BC(37.5 g/t)and PC(1,000 g/t).The results demonstrated that BC+PC exhibited positive synergistic effects,enhancing intestinal morphology,immune function,and barrier function.This was evidenced by increased VH/CD ratio,sIgA levels,and upregulated expression of occludin and claudin-1(P<0.05).16S rRNA analysis indicated that PC potentiated the effects of BC,particularly in the ileum,where BC+PC significantly increased theα-diversity of the ileal microbiota,altered itsβ-diversity,and increased the relative abundance of Flavonifractor(P<0.05),a flavonoid-metabolizing bacterium.Furthermore,Flavonifractor positively correlated with chicken ileum crypt depth(P<0.05).While BC+PC had a limited effect on cecal microbiota structure,the PC group had a very similar microbial composition to BC+PC,suggesting that the effect of PC at the distal end of the gut overshadowed those of BC.Conclusions We demonstrated the synergistic enhancement of gut health regulation in broiler chickens by combining baicalin and probiotic cocktails.Probiotic cocktails enhanced the effects of baicalin and accelerated its metabolism in the ileum,thereby influencing the ileal microbiota structure.This study elucidates the interaction mechanism between probiotic cocktails and plant extract additives within the host microbiota.These findings provide compelling evidence for the future development of feed additive combinations.展开更多
Natural product-based antiviral candidates have received significant attention.However,there is a lack of sufficient research in the field of antivirals to effectively combat patterns of drug resistance.Baicalein and ...Natural product-based antiviral candidates have received significant attention.However,there is a lack of sufficient research in the field of antivirals to effectively combat patterns of drug resistance.Baicalein and its glucuronide derivative baicalin are two main components extracted from Scutellaria baicalensis Georgi.They have proven to be effective against a broad range of viruses by directly killing virus particles,protecting infected cells,and targeting viral antigens on their surface,among other mechanisms.As natural products,they both possess the advantage of lower toxicity,enhanced therapeutic efficacy,and even antagonistic effects against drug-resistant viral strains.Baicalein and baicalin exhibit promising potential as potent pharmacophore scaffolds,demonstrating their antiviral properties.However,to date,no review on the antiviral effects of baicalein and baicalin has been published.This review summarizes the recent research progress on antiviral effects of baicalein and baicalin against various types of viruses both in vitro and in vivo with a focus on the dosages and underlying mechanisms.The aim is to provide a basis for the rational development and utilization of baicalein and baicalin,as well as to promote antiviral drug research.展开更多
Recent studies have shown that stress can substantially facilitate breast cancer metastasis,which can be reduced by nonselective β1/β2-adrenergic receptor(β1/β2-AR)blocker.However,several side effects were identif...Recent studies have shown that stress can substantially facilitate breast cancer metastasis,which can be reduced by nonselective β1/β2-adrenergic receptor(β1/β2-AR)blocker.However,several side effects were identified.Thus,it is extremely warranted to explore more effective and better-tolerated β2-AR blocker.Currently,we demonstrated that baicalin(BA),a major bioactive component of Scutellaria baicalensis Georgi,could significantly attenuate stress hormones especially epinephrine(Epi)-induced breast cancer cell migration and invasion in vitro.Mechanistically,we identified that β2-AR was a direct target of BA via the drug affinity responsive target stability(DARTS)combined with mass spectrum assay,and BA photoaffinity probe with pull-down assay,which was further confirmed by a couple of biophysical and biochemical assays.Furthermore,we demonstrated that BA could directly bind to the Phe193 and Phe-289 of β2-AR,subsequently inhibit cyclic adenosine monophosphate-protein kinase A-focal adhesion kinase(cAMP-PKA-FAK)pathway,and thus impede epithelial-mesenchymal transition(EMT),thereby hindering the metastatic progression of the chronic stress coupled with syngeneic and xenograft in vivo orthotopic and tail vein mouse model.These findings firstly identify BA as a potential b2-AR inhibitor in the treatment of stress-induced breast cancer metastasis.展开更多
[Objectives]To study the effect and mechanism of baicalin on the activation of NLRP3 inflammasome in human fibroblast like synoviocytes of rheumatoid arthritis(HFLS-RA).[Methods]To confirm that baicalin alleviated the...[Objectives]To study the effect and mechanism of baicalin on the activation of NLRP3 inflammasome in human fibroblast like synoviocytes of rheumatoid arthritis(HFLS-RA).[Methods]To confirm that baicalin alleviated the activation of NLRP3 inflammasome in HFLS-RA,the expression of NLRP3 before and after baicalin treatment was observed by immunofluorescence.Western blot was used to detect the protein expression of p-PI3K,p-Akt,NF-κB p65,NLRP3,ASC and caspase-1 after baicalin treatment for 48 h,and the contents of IL-1 and IL-18 in the supernatents were detected by ELISA.In order to explore the mechanism of baicalin alleviating the activation of NLRP3 inflammasome,the corresponding relationship between let-7i-3p and PIK3CA was verified by double luciferin and Westen blot analysis.The expression of let-7i-3p and PI3K before and after baicalin intervention was detected by RT-qPCR.let-7i-3p interference was used to verify whether baicalin mitigated the activation of enhanced NLRP3 inflammasome.[Results]Baicalin(50 and 100 mg/L)significantly reduced the activation of NLRP3 inflammasome,inhibited the protein expressions of p-PI3K,p-Akt,NF-κB p65,NLRP3,ASC and caspase-1,and the secretion of IL-1 and IL-18.let-7i-3p and PIK3CA had a targeted correspondence,and baicalin up-regulated the expression of let-7i-3p and down-regulated the expression of PIK3CA.Baicalin attenuated the activation of NLRP3 inflammasome enhanced by let-7i-3p interference.[Conclusions]Baicalin can up-regulate let-7i-3p expression,inhibit PI3K/Akt/NF-κB signal transduction,and thus reduce the activation of NLRP3 inflammasome in HFLS-RA.展开更多
Aim In the present study a RP-HPLC method was developed and validated toinvestigate the stability of baicalin aqueous solution. Methods The influences of temperature and pHon the stability of baicalin aqueous solution...Aim In the present study a RP-HPLC method was developed and validated toinvestigate the stability of baicalin aqueous solution. Methods The influences of temperature and pHon the stability of baicalin aqueous solution were investigated by classic homoiothermicacceleration test, and the pH for the most stable solution was determined. Results The time whenbaicalin suffered 10% loss was found to be 18.1 h, and the degradation activation energy of baicalinwas 79.1 kJ·moL^(-1) . The pH at which baicalin is most stable is 4.28. Conclusion The temperatureshould be kept at a lower level and the pH should be adjusted to near that for the most stablesolution in the production of baicalin preparations.展开更多
Aim To establish a reversed phase liquid chromatographic method forsimultaneous determination of three main medicinal constituents, baicalin, berberine and rhein, inSanhuang tablets. Methods The separation was perform...Aim To establish a reversed phase liquid chromatographic method forsimultaneous determination of three main medicinal constituents, baicalin, berberine and rhein, inSanhuang tablets. Methods The separation was performed on a Kromasil C_(18) column with TEA-adjusted0.02 mol·L^(-1) H_3PO_4 (pH 6.78)-acetonitrile-methanol (40 : 9 : 7) as mobile phase at aflow-rate of 1.0 mL·min^(-1), with detection at 254 ran. Considering interaction between acidic andalkaline compounds, three standard markers were added respectively and the volume of samplesolution was doubled in recovery experiments. Results Three regression equations revealed excellentlinear relationship between the peak areas and concentrations and the correlation coefficients allsurpassed 0.999 8. The average recovery was 96.1% (RSD = 2.1%) baicalin, 98.5% (RSD = 2.4%) forberberine, and 101.5% (RSD =1.3%) for rhein. Conclusion The method developed can be used to controlthe quality of Sanhuang tablets comprehensively.展开更多
To investigate pharmacokinetics ofbaicalin after an oral administration of different Shuang-Huang-Lian （SHL） formulations to rats. Different SIlL formulations were orally administered to rats. The concentrations of ...To investigate pharmacokinetics ofbaicalin after an oral administration of different Shuang-Huang-Lian （SHL） formulations to rats. Different SIlL formulations were orally administered to rats. The concentrations of baicalin in rat plasma were determined by HPLC, the non-compartmental pharmacokinetic parameters and population pharmacokinetic parameters of baicalin were estimated by WinNonlin and NONMEM. The plasma concentration profiles of baicalin demonstrated double-peak phenomenon except for group microemulsion prescription 2. Population pharmacokinetic model developed includes four covariates, which were the effect of formulation （FORM） on CL/F and V/F, the effect of body weight （BW） on Ka, and the effect of gender （GEND） on V/F. Numbers 1 to 6 denote SHL formulation decoction, oral liquid, colloidal solution, microemulsion prescription 1, microemulsion prescription 2 and granule, respectively. The equations for the parameters are as following： CL/F = （0.432 ＋ 0.529）. e^ηCl L/h if formulation was 2 or 6, otherwise CL/F = 0.432. e^ηCl L/h ; V/F = （11.3- 4.03 - 3.87. GEND）. e^ηv L if formulation was 5, otherwise V/F = （11.3 - 3.87. GEND）. e^ηv L ; Ka = 0.475. [1 - 0.0223. （BW - 195.1）]. e^ηKah^-1. SHL formulations have significant effects on the nharmacokinefic narameters.展开更多
AIM: To evaluate the role of baicalin in ulcerative colitis (UC) with regard to the CD4<sup>+</sup>CD29<sup>+</sup> T helper cell, its surface markers and serum inflammatory cytokines.
OBJECTIVE:To evaluate the effects of baicalin in human gastric cancer cells, including apoptosis-inducing effects, and to investigate its underlying mechanisms of action.METHODS:Cell proliferation and apoptosis assays...OBJECTIVE:To evaluate the effects of baicalin in human gastric cancer cells, including apoptosis-inducing effects, and to investigate its underlying mechanisms of action.METHODS:Cell proliferation and apoptosis assays were performed to investigate the anti-proliferation effects of baicalin in human gastric cancer BGC-823 and MGC-803 cells.Real time-quantitative polymerase chain reaction and Western blotting analysis were performed to elucidate the molecular mechanisms underlying the anti-tumor properties of baicalin.RESULTS:In BGC-823 and MGC-803 gastric cancer cells treated with 80, 120, and 160 μmol/L baicalin for 48 h, a 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide assay showed that baicalin significantly inhibited cell proliferation in a dose-dependent manner, while flow cytometric analysis demonstrated that baicalin could induce apoptosis, also in a dose-dependent manner.Moreover, baicalin up-regulated the expression of caspase-3, caspase-9, and B cell lymphoma(Bcl-2)-associated X protein and down-regulated the expression of Bcl-2 at both the m RNA and protein level.CONCLUSION:Baicalin has potential as a therapeutic agent for gastric cancer by inducing apoptosis in cancer cells.展开更多
The increased proliferation and migration of vascular smooth muscle cells （VSMCs） are key events in the development of atherosclerotic lesions. Baicalin, an herb-derived flavonoid compound, has been previously shown...The increased proliferation and migration of vascular smooth muscle cells （VSMCs） are key events in the development of atherosclerotic lesions. Baicalin, an herb-derived flavonoid compound, has been previously shown to induce apoptosis and growth inhibition in cancer cells through multiple pathways. However, the potential role of baicalin in regulation of VSMC proliferation and prevention of cardiovascular diseases remains unexplored. In this study, we show that pretreatment with baicalin has a dose-dependent inhibitory effect on PDGF-BB-stimulated VSMC pro- liferation, accompanied with the reduction of proliferating cell nuclear antigen （PCNA） expression. We also show that baicalin-induced growth inhibition is associated with a decrease in cyclin E-CDK2 activation and increase in p27 level in PDGF-stimulated VSMCs, which appears to be at least partly mediated by blockade of PDGF recep- tor [~ （PDGFR~）-extracellular signal-regulated kinase 1/2 （ERK1/2） signaling. In addition, baicalin was also found to inhibit adhesion molecule expression and cell migration induced by PDGF-BB in VSMCs. Furthermore, using an animal carotid arterial balloon-injury model, we found that baicalin significantly inhibited neointimal hyperplasia. Taken together, our results reveal a novel function of baicalin in inducing growth arrest of PDGF-stimulated VSMCs and suppressing neointimal hyperplasia after balloon injury, and suggest that the underlying mechanism involves the inhibition of cyclin E-CDK2 activation and the increase in p27 accumulation via blockade of the PDGFR^-ERK1/2 signaling cascade.展开更多
Objetive:To investigate the nerve protective effect and mechanism of baicalin on newborn rats with hypoxic ischemic brain damage(HIBD).Methods:A total of 64 SD newborn rats were randomlu divided into control group.mod...Objetive:To investigate the nerve protective effect and mechanism of baicalin on newborn rats with hypoxic ischemic brain damage(HIBD).Methods:A total of 64 SD newborn rats were randomlu divided into control group.model group.nerve growth factor group and baicalin group.with 16 in each group.Left carotid artery ligation method was adopted to establish the HIBD model except fou in control group,which was treatde with intraperitoneal injection of salin e10mL/kg for 3 d.After oxygen recovery on hypoxia ischemia rats.intraperitoneal injectionof salin 10mL/kg was adopted in model group for 3 d.Intraperitoneal injection of nerve growth factor injection50μg/kg per day was adopted in nerve growth factor group for 3 d:intraperitoneal injection of radix scutellariae 16mg/kg per day was adopted in baicalin group for 3 d after modeeling.Four rats of each group were sacrificed at Day 1,2,3,7 for microscopic observation of pathological morphological changes in brain tissus aften HE staining,S-P immunohistochemical method was used for observation of Fas and FasL expression in brain cells.Results:Neat structure of cells was observed in control group;edema cells in disordered arrangement was observed in model group,with some cells necrosis and cavity change;tissue injury in nerve growth factor group and baicalin group was significantly lighter than that in model group;Fas and FasL expression in model group,nerve growth factor group and baicalin group were significantiy higher than that in control group at different time points(P<0.05):Fas and FasL expression in nerve growth factor group and baicalin group were significantly lower than that in model group at different time points(P<0.05):There was no statistical diggerence of Fas,FasL expression at each time point between nerve growth factor group and baicalin group(P>0.05).Conclusions:Baicalin can reduce expression of Fas and FasL in HIBD rats,inhibit apoptosis of nerve cells,thus achieve the protective effect on HIBD rat nerves.展开更多
AIM： To investigate the correlation between the antifibrotic effect of baicalin and serum cytokine production in rat hepatic fibrosis, METHODS： Forty male Sprague-Dawley rats were divided randomly into four groups：...AIM： To investigate the correlation between the antifibrotic effect of baicalin and serum cytokine production in rat hepatic fibrosis, METHODS： Forty male Sprague-Dawley rats were divided randomly into four groups： normal control group, model group, baicalin-treated group, and colchicine-treated group. Except for the normal control group, all rats in the other groups were administered with carbon tetrachloride to induce hepatic fibrosis. At the same time, the last two groups were also treated with baicalin or colchicine. At the end of the 8 wk, all animals were sacrificed. Serum alanine aminotransferase （ALl＇）, aspartate aminotransferase （AST）, transforming growth factor （TGF）-β1, tumor necrosis factor （TNF）-α, interleukin （IL）-6 and IL-10 were measured. Liver index, hepatic hydroxyproline content and the degree of liver fibrosis were also evaluated. RESULTS： The levels of ALT, AST and liver index in the baicalin-treated group were markedly lower than those in the model group （ALT： 143.88 ± 14.55 U/L vs 193.58± 24.35 U/L; AST： 263.66 ± 44.23 U/L vs 404.37± 68.29 U/L; liver index： 0.033 ± 0.005 vs 0.049± 0.009, P 〈 0.01）. Baicalin therapy also significantly attenuated the degree of hepatic fibrosis, collagen area and collagen area percentage in liver tissue （P 〈 0.01）. Furthermore, the levels of serum TGF-β1, TNF-α and IL-6 were strikingly reduced in the baicalin-treated group compared with the model group, while the production of IL-10 was up-regulated： （TGF-β1：260.21 ± 31.01 pg/mL vs 375.49 ± 57.47 pg/mL; TNF-α： 193.40±15.18 pg/mL vs 260.04 ± 37.70 pg/mL; IL-α：339.87 ± 72.95 pg/mL vs 606.47 ± 130.73 pg/mL; IL-10：506.22 ± 112.07 pg/mL vs 316.95 ± 62.74 pg/mL, P 〈 0.01）. CONCLUSION： Baicalin shows certain therapeutic effects on hepatic fibrosis, probably by immunoregulating the imbalance between profibrotic and antifibrotic cytokines.展开更多
基金supported by grants from the National Key Re-search and Development Program of China(2023YFC3603100 and 2023YFC3603105)“Leading Goose”R&D Program of Zhejiang Province(2022C03076-4).
文摘Background:Diquat,a commonly employed bipyridyl herbicide,is recognized for its hepatotoxic effects attributed to the generation of reactive oxygen species.Baicalin(BAI),a flavonoid derivative,has garnered significant research interest for its hepatoprotective properties.Nevertheless,the clinical application of BAI is constrained by its limited water solubility and poor bioavailability.To address these challenges,BAI-nanoliposome(BAI-NL)has emerged as a novel drug delivery platform aimed at enhancing therapeutic outcomes.Methods:We used diquat-induced liver injury mouse model and AML12 hepatocytes to test the pro-tective effect of BAI and BAI-NL on liver inflammation,oxidative stress,and mitochondrial function.The parameters included histological,biochemical,and molecular biological analyses.Results:In the diquat-induced model,both BAI and BAI-NL exhibited effectiveness on attenuating liver inflammation.Ex vivo analyses further indicated that BAI-NL was superior to BAI in preserving mito-chondrial membrane potential,reducing oxidative stress,and modulating the phosphatase and tensin homolog-induced putative kinase 1(PINK1)/Parkin RBR E3 ubiquitin-protein ligase(Parkin)signaling pathway.These findings enhanced mitophagy and facilitated the removal of damaged mitochondria.Conclusions:BAI-NL exhibited superior hepatoprotective effects compared to free BAI,possibly by re-ducing inflammation,preserving mitochondrial homeostasis,and reinstating autophagic balance through modulation of the PINK1/Parkin signaling pathway.These outcomes indicate a groundbreaking method for addressing liver diseases and underscore the potential of nanoliposome technology in augmenting the efficacy of natural compounds.
基金Supported by Shandong Province Major Agricultural Technologies Collaborative Promotion Project(SDNYXTTG-2024-04)National Key Laboratory for Quality Control of Chinese Medicinal Materials and Decoction Pieces Project(2024GSMPA-KL16)Weifang Municipal Science and Technology Bureau Project(2021GX031).
文摘[Objectives]To establish a high-performance liquid chromatography(HPLC)method for the simultaneous determination of forsythin,baicalin,and chlorogenic acid in a traditional Chinese medicine spray disinfectant.[Methods]The chromatographic separation was performed on a GL Sciences(19H0044724)-C_(18)column(4.6 mm×250 mm,5μm)with a mobile phase of acetonitrile-0.05%formic acid solution at a flow rate of 1 mL/min.The injection volume was 10μL,detection wavelength was set at 280 nm,and column temperature was maintained at 25℃.[Results]The linear ranges of forsythin,baicalin,and chlorogenic acid were 10.5-52.5,20.6-103,and 14.2-71μg/mL,respectively,with good linear relationships between concentration and peak area(R^(2)=0.9999).The relative standard deviations(RSD s)for precision and repeatability tests were all≤1.0%.The average recoveries were 98.51%,98.48%,and 97.71%for the three components,with RSD s of 0.96%,0.97%,and 0.73%,respectively.[Conclusions]This method demonstrates strong specificity,high precision,excellent accuracy,and simplicity of operation,making it suitable for the simultaneous quantification of forsythin,baicalin,and chlorogenic acid in traditional Chinese medicine spray disinfectants.It provides a reliable basis for quality control and practical applications in animal breeding environments.
基金supported by grants from the National Natural Science Foundation of China(U21A20400,81973789,82004327).
文摘Objective:To explore the potential mechanisms of a baicalin-geniposide combination against cerebral ischemia using a network pharmacology strategy.Method:We used network pharmacology integrating drug-target-disease interactions to identify key pathways which were validated in a rat middle cerebral artery occlusion model treated with baicalin(55 mg/kg),geniposide(5 mg/kg),or their 11:1 combination.Therapeutic efficacy and mechanistic insights were evaluated using triphenyltetrazolium chloride staining,Evans blue assay,enzyme-linked immunosorbent assay,and Western blot.Results:The results revealed that the nuclear factor-kappa B(NF-κB)signaling pathway is inhibited in combination treatment of cerebral ischemia.Ten targets were identified as key nodes in the protein-protein interaction network:interleukin 6(IL-6),interleukin-1β,interleukin 18,C-C motif ligand 2,C-C motif ligand 4,interleukin 10,interferon-γ-inducible protein 10,C-C motif ligand 3,tumor necrosis factor-α(TNF-α),interleukin-1α.The baicalin-geniposide combination significantly reduced infarct volume,improved neurological deficits,and alleviated brain edema/blood-brain barrier leakage compared with monotherapy.Additionally,it significantly inhibited toll-like receptor 4(TLR4)/NF-κB signaling and downregulated pro-inflammatory cytokines TNF-αand IL-6 levels.Conclusion:The baicalin-geniposide combination alleviated cerebral ischemia-reperfusion injury by synergistically suppressing the TLR4/NF-κB pathway and its downstream inflammatory factors.
基金supported by the Chinese Medicine"Dual Chain Integration"Young and Middle-aged Scientific Research and Innovation Teams(No.2022-SLRH-YQ-006)the Key R&D Programme Projects of Xianyang Municipality(No.L2023-ZDYF-SF-014)+1 种基金the Shaanxi University of Traditional Chinese Medicine Science,Education and Research Collaborative Educational Achievement Transformation Project(No.2024KC03)the open research topic from the Key Laboratory of Neurological Diseases in Traditional Chinese Medicine,Shaanxi Province(No.KF202315).
文摘Background:Baicalin(BC)and geniposide(GD)are effective components of natural remedies,and studies have shown that they protect against cerebral ischemic stroke(CIS).Transient receptor potential vanilloid 4(TRPV4)is a calcium-permeable channel that plays important roles in vascular function and vasodilation.However,no studies are available on the effect of BC/GD on the TRPV4 channel and rat cerebral basilar artery(CBA).This study examined the effect of the combination of BC/GD(7:3)on cerebral vascular function after CIS.Methods:We used western blotting to determine TRPV4 protein levels and live cell fluorescence Ca 2+imaging and patch clamp to determine how BC/GD activates TRPV4 channels.Isolated vessel experiments were used to observe the dilatory effects of BC/GD on CBA under different conditions.Laser Doppler imaging was used to measure cerebral blood flow in rats.Triphenyl tetrazolium chloride and Nissl stainings were used to determine the infarct area in the rat brain and neuronal damage,respectively.Results:BC/GD significantly boosted TRPV4 protein levels in vascular smooth muscle cells(VSMCs)during oxygen-glucose deprivation and increased[Ca 2+]i in TRPV4-HEK 293 cells and VSMCs.This effect was not observed in vector-HEK 293 cells.In patch clamp experiments,BC/GD increased Ca 2+currents in TRPV4-HEK 293 cells,whereas no significant changes were observed in vector-HEK 293 cells.BC/GD dilated CBA contractions induced by U46619 and KCl,with a concentration-dependent increase of the dilatory effect.In the middle cerebral artery occlusion model,cerebral blood flow in the ischemic side significantly decreased,whereas BC/GD intervention significantly increased cerebral blood perfusion in the ischemic side,reduced the infarct area,and improved neurological function scores and neuronal damage.Conclusion:BC/GD activates the TRPV4 channel,leading to Ca ^(2+) influx,which in turn activates the intermediate conductance calcium-activated potassium channels channel to regulate vasodilation in vascular smooth muscle.
基金supported by the JSPS KAKENHI(Grant Number:JP22K06676)。
文摘Background:Scutellaria root(root of Scutellaria baicalensis),which has potent anti-inflammatory effects,is a component of useful traditional formulaes.Albeit a low frequency,it has been reported to cause severe interstitial pneumonia and liver dysfunction.Importantly,the hepatotoxicity induced by Scutellaria root can be controlled by the baicalin content,one of its major constituents.This study aimed to clarify the role of MRP2 in modulating baicalin-induced cytotoxicity in HepG2 cells,providing insights that inform safer use and assessment of baicalin.Methods:Cytotoxicity of HepG2 and MDCK cells was assessed using a cell counting kit-8 assay in the presence and absence of MK571,an MRP2 inhibitor.MRP2 expression levels were confirmed using agarose gel electrophoresis,and intracellular baicalin concentrations were measured using LC/MS.Results:Baicalin exhibited concentration-dependent cytotoxicity,with higher toxicity observed in MRP2-negative MDCK cells than in MRP2-positive HepG2 cells.Pre-treatment with MK571 increased baicalin-induced cytotoxicity in HepG2 cells and doubled the intracellular baicalin concentration.Conclusion:Our results indicated that MRP2 plays an important role in reducing baicalin-induced hepatocyte toxicity by decreasing intracellular baicalin levels.Monitoring MRP2 activity could serve as a critical predictive biomarker to identify individuals at higher risk of baicalin-induced hepatotoxicity,enabling personalized dosing strategies and minimizing adverse effects associated with Scutellaria root-containing formulae.
基金Project supported by Jilin Province Science and Technology Development Plan Project(20210201061GX)。
文摘Baicalin,a major flavonoid compound found in Scutellariae radix,is the first SARS-CoV-23CLpro virus inhibitor.Therefore,developing an accurate and reliable strategy to detect baicalin in biological systems is vital.Herein,we report the first indolyl-lanthanide metal-organic framework(MOF)materials and their application as baicalin sensors.The results of this study indicate that the new crystal structure has good stability and luminous performance.The detection limits of baicalin in serum and urine are 0.05 and 0.04μmol/L,respectively,suggesting high sensitivity and selectivity.Various background substances present in practical samples,such as anions,cations,and amino acids,do not interfere with the photoluminescence analytical signal of Eu^(3+).We identified that the quenching of the Eu-MOF is due to the inner filter effect,absorption energy competition,and photoinduced electron transfer among the baicalin,ligand,and MOF through powder X-ray diffraction analysis,Fourier transform infrared spectroscopy,luminescence lifetimes,ultraviolet studies,and computational analysis.Thus,we designed a convenient,sensitive,and facile detection method using the Eu-MOF and demonstrate that Eu^(3+)-based materials are promising sensors for baicalin detection in actual serum and urine.Additionally,the prepared Eu-MOF@polyvinyl alcohol composite matrix membrane test film has considerable practical application value for the portable detection of baicalin.
基金supported by the National Natural Science Foundation of China(32102582)the Youth innovation of Chinese Academy of Agricultural Sciences(Y2023QC09)+1 种基金Zhejiang Province Traditional Chinese Medicine Science and technology Project(2022ZB270)the Agricultural Science and Technology Innovation Program(ASTIPIAS07,cxgc-ias-16)。
文摘Background Intestinal inflammation is a common and serious health problem in piglet production,especially enteritis caused by pathogenic Escherichia coli(E.coli).This condition often leads to high mortality,slow weight gain,and significant economic losses.Results In this study,we isolated an E.coli strain,SKLAN202302,from the colon of diarrheal piglets to create an intestinal inflammation model for evaluating the protective effects of baicalin.Piglets infected with E.coli exhibited significant reductions in body weight,feed intake,small intestine length,and ileal goblet cell count(P<0.05),along with deteriorated ileal morphology.However,baicalin supplementation resulted in body weights,feed intake,and intestinal morphology similar to those of the control group.Notably,there was a significant increase in the colonization of Lactobacillus species,particularly Lactobacillus_reuteri,Lactobacillus_amylovorus,and Lactobacillus_johnii,compared to the E.coli group(P<0.05).At the metabolic and transcriptional levels,E.coli infection increased inflammatory mediators,including eicosanoids(leukotriene F4,prostaglandin F1a,leukotriene E4,thromboxane B2,prostaglandin G2,and PGH2),monosaccharides,and TCA cycle intermediates(oxoglutaric acid,glutaric acid,adipic acid,citric acid,and isocitric acid)in the ileum.It also promoted the expression of genes related to autoimmune diseases and the Th17 differentiation signaling pathway(CTLA4,IFN-ALPHA-8,IL12RB2,TRAV3,TRAV16,FOS,and VEGFA),as well as inflammatory factors.Conversely,baicalin supplementation not only counteracted these effects but also enhanced the presence of metabolites such as phospholipids[including lyso PC(P-18:1(9Z)/0:0),PC(17:0/0:0),lyso PC(16:1(9Z)/0:0),PC(18:0/0:0),lyso PC(18:0/0:0),PA(10:0/i-16:0),and PA(10:0/8:0)]and amino acids.It also regulated genes within the IL-17 signaling pathway(IL4,CCL17,CXCL10,IFNG,and CXCL2),suggesting a mechanism by which baicalin mitigates E.coli-induced intestinal and microbial disturbances.Subsequent flow cytometry analysis showed that E.coli infection increased the numbers of CD3+and Foxp3+cells,decreased IL-17A+cells,and reduced Th17/Treg ratios.Baicalin supplementation restored these parameters to control levels.Conclusions Baicalin supplementation effectively alleviates E.coli-induced intestinal inflammation and microbial disturbances in piglets by enhancing beneficial Lactobacillus colonization,counteracting inflammatory mediators,and regulating immune-related gene expression and the Th17/Treg balance.These findings highlight baicalin's potential in alleviating intestinal inflammation.
基金funded by National Key R&D Program of China(2022YFD1300403,2021YFD1300404)China Agriculture Research System program(CARS-40,CARS-41-G11)Beijing Natural Science Foundation(6222036).
文摘Background Baicalin and probiotic cocktails are promising feed additives with broad application prospects.While probiotic cocktails are known to enhance intestinal health,the potential synergistic impact of combining baicalin with probiotic cocktails on the gut health of broiler chickens remains largely unexplored.Therefore,this study aims to investigate the influence of the combined administration of baicalin and probiotic cocktails on the composition of ileal and cecal microbiota in broiler chickens to elucidate the underlying mechanisms responsible for the healthpromoting effects.Results A total of 3201-day-old male Arbor Acres broilers were divided into 4 groups,each with 8 replicates of 10 chicks per replicate.Over a period of 42 d,the birds were fed a basal diet or the same diet supplemented with 37.5 g/t baicalin(BC),1,000 g/t probiotic cocktails(PC),or a combination of both BC(37.5 g/t)and PC(1,000 g/t).The results demonstrated that BC+PC exhibited positive synergistic effects,enhancing intestinal morphology,immune function,and barrier function.This was evidenced by increased VH/CD ratio,sIgA levels,and upregulated expression of occludin and claudin-1(P<0.05).16S rRNA analysis indicated that PC potentiated the effects of BC,particularly in the ileum,where BC+PC significantly increased theα-diversity of the ileal microbiota,altered itsβ-diversity,and increased the relative abundance of Flavonifractor(P<0.05),a flavonoid-metabolizing bacterium.Furthermore,Flavonifractor positively correlated with chicken ileum crypt depth(P<0.05).While BC+PC had a limited effect on cecal microbiota structure,the PC group had a very similar microbial composition to BC+PC,suggesting that the effect of PC at the distal end of the gut overshadowed those of BC.Conclusions We demonstrated the synergistic enhancement of gut health regulation in broiler chickens by combining baicalin and probiotic cocktails.Probiotic cocktails enhanced the effects of baicalin and accelerated its metabolism in the ileum,thereby influencing the ileal microbiota structure.This study elucidates the interaction mechanism between probiotic cocktails and plant extract additives within the host microbiota.These findings provide compelling evidence for the future development of feed additive combinations.
基金supported by National Natural Science Foundation of China(No.81573585)the Innovative Practice of Undergraduate Project of Naval Medical University(No.FH2021104)。
文摘Natural product-based antiviral candidates have received significant attention.However,there is a lack of sufficient research in the field of antivirals to effectively combat patterns of drug resistance.Baicalein and its glucuronide derivative baicalin are two main components extracted from Scutellaria baicalensis Georgi.They have proven to be effective against a broad range of viruses by directly killing virus particles,protecting infected cells,and targeting viral antigens on their surface,among other mechanisms.As natural products,they both possess the advantage of lower toxicity,enhanced therapeutic efficacy,and even antagonistic effects against drug-resistant viral strains.Baicalein and baicalin exhibit promising potential as potent pharmacophore scaffolds,demonstrating their antiviral properties.However,to date,no review on the antiviral effects of baicalein and baicalin has been published.This review summarizes the recent research progress on antiviral effects of baicalein and baicalin against various types of viruses both in vitro and in vivo with a focus on the dosages and underlying mechanisms.The aim is to provide a basis for the rational development and utilization of baicalein and baicalin,as well as to promote antiviral drug research.
基金supported by the Matching Grant of National Natural Science Foundation of China from Nanjing University of Chinese Medicine(Grant Nos.:NZY81903857,and NZY81703765)the National Natural Science Foundation of China(Grant No.:21877062)+1 种基金the Opening Project of Chinese Materia Medica FirstClass Discipline of Nanjing University of Chinese Medicine(Grant No.:2020YLXK020)Postgraduate Research&Practice Innovation Program of Jiangsu Province(Grant Nos.:SJCX21_0707,KYCX21_1772,and KYCX22_2039).
文摘Recent studies have shown that stress can substantially facilitate breast cancer metastasis,which can be reduced by nonselective β1/β2-adrenergic receptor(β1/β2-AR)blocker.However,several side effects were identified.Thus,it is extremely warranted to explore more effective and better-tolerated β2-AR blocker.Currently,we demonstrated that baicalin(BA),a major bioactive component of Scutellaria baicalensis Georgi,could significantly attenuate stress hormones especially epinephrine(Epi)-induced breast cancer cell migration and invasion in vitro.Mechanistically,we identified that β2-AR was a direct target of BA via the drug affinity responsive target stability(DARTS)combined with mass spectrum assay,and BA photoaffinity probe with pull-down assay,which was further confirmed by a couple of biophysical and biochemical assays.Furthermore,we demonstrated that BA could directly bind to the Phe193 and Phe-289 of β2-AR,subsequently inhibit cyclic adenosine monophosphate-protein kinase A-focal adhesion kinase(cAMP-PKA-FAK)pathway,and thus impede epithelial-mesenchymal transition(EMT),thereby hindering the metastatic progression of the chronic stress coupled with syngeneic and xenograft in vivo orthotopic and tail vein mouse model.These findings firstly identify BA as a potential b2-AR inhibitor in the treatment of stress-induced breast cancer metastasis.
基金Supported by the National Natural Science Foundation of China(82360802):the Natural Science Foundation of Ningxia Province,China(2022AAC 03152).
文摘[Objectives]To study the effect and mechanism of baicalin on the activation of NLRP3 inflammasome in human fibroblast like synoviocytes of rheumatoid arthritis(HFLS-RA).[Methods]To confirm that baicalin alleviated the activation of NLRP3 inflammasome in HFLS-RA,the expression of NLRP3 before and after baicalin treatment was observed by immunofluorescence.Western blot was used to detect the protein expression of p-PI3K,p-Akt,NF-κB p65,NLRP3,ASC and caspase-1 after baicalin treatment for 48 h,and the contents of IL-1 and IL-18 in the supernatents were detected by ELISA.In order to explore the mechanism of baicalin alleviating the activation of NLRP3 inflammasome,the corresponding relationship between let-7i-3p and PIK3CA was verified by double luciferin and Westen blot analysis.The expression of let-7i-3p and PI3K before and after baicalin intervention was detected by RT-qPCR.let-7i-3p interference was used to verify whether baicalin mitigated the activation of enhanced NLRP3 inflammasome.[Results]Baicalin(50 and 100 mg/L)significantly reduced the activation of NLRP3 inflammasome,inhibited the protein expressions of p-PI3K,p-Akt,NF-κB p65,NLRP3,ASC and caspase-1,and the secretion of IL-1 and IL-18.let-7i-3p and PIK3CA had a targeted correspondence,and baicalin up-regulated the expression of let-7i-3p and down-regulated the expression of PIK3CA.Baicalin attenuated the activation of NLRP3 inflammasome enhanced by let-7i-3p interference.[Conclusions]Baicalin can up-regulate let-7i-3p expression,inhibit PI3K/Akt/NF-κB signal transduction,and thus reduce the activation of NLRP3 inflammasome in HFLS-RA.
文摘Aim In the present study a RP-HPLC method was developed and validated toinvestigate the stability of baicalin aqueous solution. Methods The influences of temperature and pHon the stability of baicalin aqueous solution were investigated by classic homoiothermicacceleration test, and the pH for the most stable solution was determined. Results The time whenbaicalin suffered 10% loss was found to be 18.1 h, and the degradation activation energy of baicalinwas 79.1 kJ·moL^(-1) . The pH at which baicalin is most stable is 4.28. Conclusion The temperatureshould be kept at a lower level and the pH should be adjusted to near that for the most stablesolution in the production of baicalin preparations.
基金Innovation Fund of Chinese Academy of Sciences(KGCX2 SW 213 05)
文摘Aim To establish a reversed phase liquid chromatographic method forsimultaneous determination of three main medicinal constituents, baicalin, berberine and rhein, inSanhuang tablets. Methods The separation was performed on a Kromasil C_(18) column with TEA-adjusted0.02 mol·L^(-1) H_3PO_4 (pH 6.78)-acetonitrile-methanol (40 : 9 : 7) as mobile phase at aflow-rate of 1.0 mL·min^(-1), with detection at 254 ran. Considering interaction between acidic andalkaline compounds, three standard markers were added respectively and the volume of samplesolution was doubled in recovery experiments. Results Three regression equations revealed excellentlinear relationship between the peak areas and concentrations and the correlation coefficients allsurpassed 0.999 8. The average recovery was 96.1% (RSD = 2.1%) baicalin, 98.5% (RSD = 2.4%) forberberine, and 101.5% (RSD =1.3%) for rhein. Conclusion The method developed can be used to controlthe quality of Sanhuang tablets comprehensively.
基金National Natural Science Foundation of China (Grant No. 30472195)
文摘To investigate pharmacokinetics ofbaicalin after an oral administration of different Shuang-Huang-Lian （SHL） formulations to rats. Different SIlL formulations were orally administered to rats. The concentrations of baicalin in rat plasma were determined by HPLC, the non-compartmental pharmacokinetic parameters and population pharmacokinetic parameters of baicalin were estimated by WinNonlin and NONMEM. The plasma concentration profiles of baicalin demonstrated double-peak phenomenon except for group microemulsion prescription 2. Population pharmacokinetic model developed includes four covariates, which were the effect of formulation （FORM） on CL/F and V/F, the effect of body weight （BW） on Ka, and the effect of gender （GEND） on V/F. Numbers 1 to 6 denote SHL formulation decoction, oral liquid, colloidal solution, microemulsion prescription 1, microemulsion prescription 2 and granule, respectively. The equations for the parameters are as following： CL/F = （0.432 ＋ 0.529）. e^ηCl L/h if formulation was 2 or 6, otherwise CL/F = 0.432. e^ηCl L/h ; V/F = （11.3- 4.03 - 3.87. GEND）. e^ηv L if formulation was 5, otherwise V/F = （11.3 - 3.87. GEND）. e^ηv L ; Ka = 0.475. [1 - 0.0223. （BW - 195.1）]. e^ηKah^-1. SHL formulations have significant effects on the nharmacokinefic narameters.
基金Supported by National Natural Science Foundation of Chinunder Grant No.30772701
文摘AIM: To evaluate the role of baicalin in ulcerative colitis (UC) with regard to the CD4<sup>+</sup>CD29<sup>+</sup> T helper cell, its surface markers and serum inflammatory cytokines.
基金Supported by the Natural Science Foundation of Gansu Province(No.148RJZA073)the Health Industry Scientific Research Project of Gansu Province(No.GWGL 2013-40)the Openning Plan Project of Key Laboratory for Transfer of Dunhuang Medicine at the Provincial and Ministerial Level(No.DHYX1213-008)
文摘OBJECTIVE:To evaluate the effects of baicalin in human gastric cancer cells, including apoptosis-inducing effects, and to investigate its underlying mechanisms of action.METHODS:Cell proliferation and apoptosis assays were performed to investigate the anti-proliferation effects of baicalin in human gastric cancer BGC-823 and MGC-803 cells.Real time-quantitative polymerase chain reaction and Western blotting analysis were performed to elucidate the molecular mechanisms underlying the anti-tumor properties of baicalin.RESULTS:In BGC-823 and MGC-803 gastric cancer cells treated with 80, 120, and 160 μmol/L baicalin for 48 h, a 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide assay showed that baicalin significantly inhibited cell proliferation in a dose-dependent manner, while flow cytometric analysis demonstrated that baicalin could induce apoptosis, also in a dose-dependent manner.Moreover, baicalin up-regulated the expression of caspase-3, caspase-9, and B cell lymphoma(Bcl-2)-associated X protein and down-regulated the expression of Bcl-2 at both the m RNA and protein level.CONCLUSION:Baicalin has potential as a therapeutic agent for gastric cancer by inducing apoptosis in cancer cells.
基金We are grateful to Dr Guan KL （Moore＇s Cancer Center, La Jolla, CA, USA） for the gift of pCMV-MEKca. This study was supported by the National Natural Science Foundation of China （30770787 and 90919035）, the National Basic Research Program of China （2005CB523301）, and the International Cooperation in Science and Technology Projects （2006DFB32460） and the Hebei Province Natural Science Foundation （C2007000831）.
文摘The increased proliferation and migration of vascular smooth muscle cells （VSMCs） are key events in the development of atherosclerotic lesions. Baicalin, an herb-derived flavonoid compound, has been previously shown to induce apoptosis and growth inhibition in cancer cells through multiple pathways. However, the potential role of baicalin in regulation of VSMC proliferation and prevention of cardiovascular diseases remains unexplored. In this study, we show that pretreatment with baicalin has a dose-dependent inhibitory effect on PDGF-BB-stimulated VSMC pro- liferation, accompanied with the reduction of proliferating cell nuclear antigen （PCNA） expression. We also show that baicalin-induced growth inhibition is associated with a decrease in cyclin E-CDK2 activation and increase in p27 level in PDGF-stimulated VSMCs, which appears to be at least partly mediated by blockade of PDGF recep- tor [~ （PDGFR~）-extracellular signal-regulated kinase 1/2 （ERK1/2） signaling. In addition, baicalin was also found to inhibit adhesion molecule expression and cell migration induced by PDGF-BB in VSMCs. Furthermore, using an animal carotid arterial balloon-injury model, we found that baicalin significantly inhibited neointimal hyperplasia. Taken together, our results reveal a novel function of baicalin in inducing growth arrest of PDGF-stimulated VSMCs and suppressing neointimal hyperplasia after balloon injury, and suggest that the underlying mechanism involves the inhibition of cyclin E-CDK2 activation and the increase in p27 accumulation via blockade of the PDGFR^-ERK1/2 signaling cascade.
基金supported by Yantai Science and Technology Projects(GrantNo:2004221)
文摘Objetive:To investigate the nerve protective effect and mechanism of baicalin on newborn rats with hypoxic ischemic brain damage(HIBD).Methods:A total of 64 SD newborn rats were randomlu divided into control group.model group.nerve growth factor group and baicalin group.with 16 in each group.Left carotid artery ligation method was adopted to establish the HIBD model except fou in control group,which was treatde with intraperitoneal injection of salin e10mL/kg for 3 d.After oxygen recovery on hypoxia ischemia rats.intraperitoneal injectionof salin 10mL/kg was adopted in model group for 3 d.Intraperitoneal injection of nerve growth factor injection50μg/kg per day was adopted in nerve growth factor group for 3 d:intraperitoneal injection of radix scutellariae 16mg/kg per day was adopted in baicalin group for 3 d after modeeling.Four rats of each group were sacrificed at Day 1,2,3,7 for microscopic observation of pathological morphological changes in brain tissus aften HE staining,S-P immunohistochemical method was used for observation of Fas and FasL expression in brain cells.Results:Neat structure of cells was observed in control group;edema cells in disordered arrangement was observed in model group,with some cells necrosis and cavity change;tissue injury in nerve growth factor group and baicalin group was significantly lighter than that in model group;Fas and FasL expression in model group,nerve growth factor group and baicalin group were significantiy higher than that in control group at different time points(P<0.05):Fas and FasL expression in nerve growth factor group and baicalin group were significantly lower than that in model group at different time points(P<0.05):There was no statistical diggerence of Fas,FasL expression at each time point between nerve growth factor group and baicalin group(P>0.05).Conclusions:Baicalin can reduce expression of Fas and FasL in HIBD rats,inhibit apoptosis of nerve cells,thus achieve the protective effect on HIBD rat nerves.
基金Supported by Grants from National Key Technologies R&D Program of 11th five-year plan, 2009ZX09501-015
文摘AIM： To investigate the correlation between the antifibrotic effect of baicalin and serum cytokine production in rat hepatic fibrosis, METHODS： Forty male Sprague-Dawley rats were divided randomly into four groups： normal control group, model group, baicalin-treated group, and colchicine-treated group. Except for the normal control group, all rats in the other groups were administered with carbon tetrachloride to induce hepatic fibrosis. At the same time, the last two groups were also treated with baicalin or colchicine. At the end of the 8 wk, all animals were sacrificed. Serum alanine aminotransferase （ALl＇）, aspartate aminotransferase （AST）, transforming growth factor （TGF）-β1, tumor necrosis factor （TNF）-α, interleukin （IL）-6 and IL-10 were measured. Liver index, hepatic hydroxyproline content and the degree of liver fibrosis were also evaluated. RESULTS： The levels of ALT, AST and liver index in the baicalin-treated group were markedly lower than those in the model group （ALT： 143.88 ± 14.55 U/L vs 193.58± 24.35 U/L; AST： 263.66 ± 44.23 U/L vs 404.37± 68.29 U/L; liver index： 0.033 ± 0.005 vs 0.049± 0.009, P 〈 0.01）. Baicalin therapy also significantly attenuated the degree of hepatic fibrosis, collagen area and collagen area percentage in liver tissue （P 〈 0.01）. Furthermore, the levels of serum TGF-β1, TNF-α and IL-6 were strikingly reduced in the baicalin-treated group compared with the model group, while the production of IL-10 was up-regulated： （TGF-β1：260.21 ± 31.01 pg/mL vs 375.49 ± 57.47 pg/mL; TNF-α： 193.40±15.18 pg/mL vs 260.04 ± 37.70 pg/mL; IL-α：339.87 ± 72.95 pg/mL vs 606.47 ± 130.73 pg/mL; IL-10：506.22 ± 112.07 pg/mL vs 316.95 ± 62.74 pg/mL, P 〈 0.01）. CONCLUSION： Baicalin shows certain therapeutic effects on hepatic fibrosis, probably by immunoregulating the imbalance between profibrotic and antifibrotic cytokines.
