黄芩苷预处理防止癫痫发作后认知功能障碍的实验研究

目的:评估黄芩苷对锂-皮罗卡品诱发的大鼠癫痫模型的神经元丢失和智能障碍的保护作用。方法:我们采用采用锂-匹罗卡品诱导的大鼠癫痫模型,分别在注射氯化锂及匹罗卡品前1h给予黄芩苷100mg/kg或者生理盐水腹腔注射。SE形成后,动物腹腔注射黄芩苷或等量的生理盐水连续14d或直至动物处死。并在SE后31～36d行Morris水迷宫测试,观察黄芩苷对大鼠癫痫发作后认知功能的影响。并用neuN染色评估神经元丢失。结果:黄芩苷对锂-匹罗卡品导致的海马神经元损伤有明显的神经保护,黄芩苷处理组的逃避潜伏期明显缩短。结论:黄芩苷对锂-皮罗卡品诱发的癫痫模型有神经保护作用,它有可能作为一种预防和治疗癫痫以及癫痫引起的脑损害的辅助用药值得进一步研究。

中药复方制剂中黄芩苷转移率影响因素研究

目的:考察不同剂型及其不同工序对黄芩苷转移率的影响方法:采用转移率测定法以黄芩苷的转移率为指标进行试验。结果:水提醇沉法优于醇提法加火单黄芩的转移率优于未加火单黄芩,浓缩过程极大的降低黄芩苷的转移率。结论:中药复方制剂中黄芩苷转移率的影响因素有提取方法、浓缩工艺以及黄芩的炮制方法等。

黄芩苷对ApoE基因敲除小鼠早期动脉粥样斑块中MMP-9表达的影响

目的:探讨黄芩苷对ApoE基因敲除小鼠早期动脉粥样斑块中基质金属蛋白酶-9(MMP-9)表达的影响。方法:24只8周龄ApoE-/-小鼠均给予高脂饲料喂养8周后随机分为对照组、苷低剂量和高剂量组,每组8只。灌胃8周后处死,酶法检测血清甘油三酯(TG)、总胆固醇(TC)、低密度脂蛋白胆固醇(LDL-C)和高密度脂蛋白胆固醇(HDL-C)浓度;用ELISA测血清中MMP-9的表达水平;通过RT-PCR和Western blot检测小鼠主动脉斑块组织中MMP-9的表达情况。结果:与对照组相比,干预组小鼠血清中TC水平降低(P<0.05),血清中LDL-C水平明显降低(P<0.01),高剂量组较低剂量组降低的明显(P<0.05);各组小鼠血清中HDL-C及TG含量虽有变化但无统计学意义。黄芩苷干预组血清MMP-9较对照组表达水平低,高剂量组降低更显著(P<0.05);同时,黄芩苷干预组主动脉斑块中MMP-9mRNA及蛋白水平较对照组降低明显(P<0.01),高剂量组降低尤为显著(P<0.05)。结论:黄芩苷可以降低ApoE-/-小鼠血清中血脂和MMP-9水平,并可降低动脉粥样硬化斑块中MMP-9表达,提示黄芩苷具有稳定动脉粥样硬化斑块作用。

野黄芩苷对小鼠水迷宫操作学习能力的影响

目的:研究野黄芩苷(Scutellarein,Scu)对小鼠水迷宫操作学习能力和化学性脑缺氧的影响。方法:正常昆明种小鼠连续皮下注射37.5、75和150 mg/kg野黄芩苷8 d,利用小鼠水迷宫行为学实验法,通过小鼠到达终点潜伏期和进入盲端次数,评价野黄芩苷对小鼠水迷宫学习能力的影响。同上动物连续皮下注射37.5、75和150 mg/kg野黄芩苷10d,末次给药后40 min,所有小鼠ip10 mg/kg KCN,观察并纪录所有小鼠死亡时间。结果:与空白对照组相比,37.5、75和150 mg/kg野黄芩苷都能够增加小鼠水迷宫学习能力,降低到达终点平台的潜伏期和进入盲端的次数。并且37.5、75和150 mg/kg野黄芩苷都不同程度地翻转KCN产生的死亡时间的缩短。结论:野黄芩苷能够提高小鼠学习能力。

基于AQP-4、GFAP的黄芩苷、栀子苷配伍抗脑缺血大鼠神经功能损伤的研究

目的:研究黄芩苷/栀子苷配伍(7:3)对脑缺血再灌注损伤大鼠神经功能损伤的修复作用及作用机制。方法:采用改良线栓法制作脑缺血再灌注损伤模型,造模后24 h,采用平衡木试验、大鼠抓力测定法进行评价神经功能缺损,ELISA法观察脑组织中Na^+、K+-ATP酶、Ca^(2+)、Mg^(2+)-ATP酶活性大小,尼式(Nissl)染色法检测大鼠冠状脑区皮质神经元的形态和数量,免疫组织化学检测脑组织中水通道蛋白-4((aquaporin-4,AQP-4)、胶质纤维酸性蛋白(glial fibrillary acidic protein,GFAP)的表达。结果:与模型对照组相比,黄芩苷/栀子苷配伍治疗组能降低神经功能损伤,减少进入血管外及细胞间的颗粒、减轻血管内皮细胞水肿,增加Nissl阳性细胞的数量,升高脑组织中Na^+、K+-ATP酶、Ca^(2+)、Mg^(2+)-ATP酶活力,下调AQP-4蛋白、GFAP蛋白表达,其中,黄芩苷、栀子苷配伍(42+18 mg/kg.d)组有显著性差异。结论:黄芩苷/栀子苷配伍能够减轻CIRI脑水肿,对大鼠缺血再灌注脑损伤的神经保护作用可能与增加Na^+、K+-ATP酶、Ca^(2+)、Mg^(2+)-ATP酶活力,下调AQP-4及GFAP蛋白表达有关。

Influence of Water Stress on the Physiological and Biochemical Characteristics of Scutellaria Baicalensis Georgi

Previous studies have shown that water stress can stimulate biosynthesis of secondary metabolites,and physiological and biochemical characteristics of plant can play a key role in its defense responses to water stress.So the physiological and biochemical characteristics of potted Scutellaria baicalensis Georgi plants were investigated under continuous water stress condition.The results showed that the water content in roots,stems and leaves,together with chlorophyll content of the leaves decreased as the water stress strengthened.Simultaneously,the specific leaf weight increased,and the content of proline and soluble sugar in Scutellaria baicalensis Georgi leaves increased significantly.The changing trends of the baicalin content in the roots,stems and leaves of Scutellaria baicalensis Georgi were different.It increased continuously in roots,while ascended constantly in the stems and leaves during the early days under the water stress,but decreased sharply under the heavy stress.In conclusion,proline and soluble sugar had a close correlation with the drought resistance of Scutellaria baicalensis Georgi.Moderate drought is in favor of synthesizing the secondary metabolites.

Stability of Baicalin Aqueous Solution by Validated RP-HPLC

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.

黄芩苷通过影响miRNA的表达抑制乳腺癌细胞的侵袭转移

目的:从miRNA角度探讨黄芩苷对乳腺癌侵袭与转移的影响及可能的机制。方法:黄芩苷作用于乳腺癌MCF-7细胞,运用免疫组化检测TGF-β和VEGF表达的变化,筛选最佳药物浓度;用miRNA芯片筛选受黄芩苷调控的差异miRNA,qRT-PCR对芯片结果中上调的miRNA进行验证,Western-blot检测Bcl-2、Caspase-9、Caspase-3、p-p38、p53的表达,MTT法检测细胞生存率,Transwell实验检测细胞侵袭与转移,流式细胞术检测细胞凋亡。结果:用25μmol/L、50μmol/L、100μmol/L、200μmol/L的黄芩苷作用于乳腺癌细胞,免疫组化显示TGFβ、VEGF的表达下降,筛选出最佳药物浓度为50μmol/L;黄芩苷干预后miRNA芯片筛选出miR-126表达上调最明显,并以qRT-PCR验证。黄芩苷或miR-126 mimics作用于乳腺癌细胞后Bcl-2表达水平下降,Caspase-9和Caspase-3的裂解产物、p-p38、p53表达水平提高。Transwell试验表明黄芩苷干预或转染miR-126 mimics后乳腺癌细胞的侵袭转移能力降低,MTT法显示黄芩苷或miR-126 mimics均可抑制乳腺癌细胞的增殖,流式细胞术显示黄芩苷与miR-126 mimics促进癌细胞凋亡。结论:黄芩苷能抑制乳腺癌细胞的增殖及侵袭转移,其机制可能与上调miR-126的表达有关。

Simultaneous Determination of Baicalin, Berberine and Rhein by HPLC in Traditional Chinese Patent Medicine Sanhuang Tablets

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.

黄芩苷促使细胞G2/M阻滞抑制错配修复基因缺失的结直肠癌裸鼠原位移植瘤生长

目的:探讨黄芩苷抑制错配修复基因缺失的结直肠癌裸鼠原位移植瘤生长及其机制。方法:建立错配修复基因hml H1缺失的人结肠癌HCT-116细胞裸鼠荧光原位移植瘤模型。60只模型鼠随机分为对照组和黄芩苷50mg/kg、100mg/kg、200mg/kg剂量组,每组15只,对照组采用5%NaHCO_3灌胃,黄芩苷组分别予相应剂量黄芩苷灌胃,2次/日,给药4周。流式细胞术检测肿瘤组织细胞周期,TUNEL法观察肿瘤细胞凋亡,Western blot检测hml H1、hMSH2蛋白表达,RT-PCR检测hml H1、hMSH2、PCNA、Bcl-2、Bax基因的表达,荧光多重聚合酶链反应检测微卫星标志状态。结果:黄芩苷50mg/kg、100mg/kg、200mg/kg剂量组裸鼠肿瘤细胞主要在G2/M期阻滞,与对照组比较差异有统计学意义;黄芩苷50mg/kg、100mg/kg、200mg/kg剂量组裸鼠肿瘤细胞凋亡率与对照组比较差异有统计学意义;给药一周后,与对照组比较,黄芩苷50mg/kg、100mg/kg、200mg/kg剂量组错配修复基因hml H1、hMSH2蛋白表达增强;实验终点,黄芩苷50mg/kg剂量组hml H1基因表达明显低于对照组,黄芩苷50mg/kg、100mg/kg、200mg/kg剂量组hMSH2和PCNA表达明显低于对照组;黄芩苷组和对照组均存在微卫星不稳定,组间比较差异无统计学意义;Bcl-2、Bax基因表达差异无统计学意义。结论:黄芩苷通过促使肿瘤细胞G2/M期阻滞,诱导肿瘤细胞凋亡,从而抑制错配修复基因hml H1缺失的HCT-116结肠细胞裸鼠原位移植瘤生长,其机制可能与调节错配修复基因hml H1、hMSH2和PCNA基因表达相关。

Simultaneous determination of four active compounds in Dangguilonghui tablet by high-performance liquid chromatography

A high-performance liquid chromatography （HPLC） method has been developed for the first time to simultaneously quantify the four active ingredients, namely aloha, baicalein, aloe-emodin and wogonin, in Dangguilonghui tablet. The marker compotmds were separated on the Diamonsil C18 column at a flow rate of 1.0 mL/min with a mobile phase of methanol-acetonitrile-0.3% aqueous phosphoric acid （220： 4： 200, v/v/v） and while the detection wavelength was set at 225 nm. The assay was linear over the range of 1.450 - 29.00 ug/mL （r = 0.9992） for aloin, 0.4050 - 8.100ug/mL （r = 0.9994） for baicalein, 0.1100 - 2.200 ug/mL （r = 0.9997） for aloe-emodin, 0.2160 - 4.320 ug/mL （r = 0.9991） for wogonin, respectively. The average sample recoveries at three concentration levels were 100.7% （RSD = 0.88%）, 101.0% （RSD = 0.89%）, 100.0% （RSD = 1.3%） and 100.1% （RSD = 1.1%） for these constituents, respectively. This method is suitable for the quality control of Dangguilonghui tablet.

Population pharmacokinetic analysis of baicalin after oral administration of different Shuang-Huang-Lian formulations to rats

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.

基于Hedgehog信号通路的野黄芩苷抑制HT-29细胞源性结肠肿瘤干细胞体外自我更新的研究

目的:研究半枝莲中主要成分野黄芩苷对结肠肿瘤干细胞(CSC)自我更新的影响,并从Hedgehog信号通路阐明其作用机制。方法:从HT-29人结肠腺癌上皮细胞株中分拣出结肠肿瘤干细胞(HT-29CSC),并对其进行无血清悬浮培养。用CCK-8试验研究野黄芩苷对HT-29CSC活性的影响;用干细胞球形成试验研究野黄芩苷对HT-29CSC体外自我更新的影响;用qRT-PCR研究野黄芩苷对结肠肿瘤干细胞标记物基因CD133和增殖基因ki-67表达的影响,和对结肠肿瘤干细胞中Hedgehog信号通路基因Ptch1和Gli1表达的影响。结果:终浓度为40μg/ml、80μg/ml和160μg/ml的野黄芩苷可以浓度依赖性地抑制HT-29CSC体外活性,抑制HT-29CSC体外自我更新,下调结肠肿瘤干细胞标记物基因CD133和增殖基因ki-67 mRNA水平,抑制结肠肿瘤干细胞中Hedgehog信号通路基因Ptch1和Gli1 mRNA转录。结论:野黄芩苷可以抑制结肠肿瘤干细胞活性和自我更新,其机制在于抑制Hedgehog信号通路的活性。

Synergistic effect of a novel oxymatrine-baicalin combination against hepatitis B virus replication, a smooth muscle actin expression and typeⅠcollagen synthesis in vitro

AIM： To study the effect of oxymatrine-baicalin combination （OB） against HBV replication in 2.2.15 cells and α smooth muscle actin （ α SMA） expression, type I, collagen synthesis in HSC-T6 cells. METHODS： The 2.2.15 cells and HSC-T6 cells were cultured and treated respectively. HBsAg and HBeAg in the culture supernatants were detected by ELISA and HBV DNA levels were determined by fluorescence quantitative PCR. Total RNA was extracted from HSC-T6 cells and reverse transcribed into cDNA. The cDNAs were amplified by PCR and the quantities were expressed in proportion to β actin. The total cellular proteins extracted from HSC-T6 cells were separated by electrophoresis. Resolved proteins were electrophoretically transferred to nitrocellulose membrane. Protein bands were revealed and the quantities were corrected by β actin. RESULTS： In the 2.2.15 cell culture system, the inhibitory rate against secretion of HBsAg and HBeAg in the OB group was significantly stronger than that in the oxymatrine group （HBsAg, P = 0.043; HBeAg, P = 0.026; respectively）; HBV DNA level in the OB group was significantly lower than that in the oxymatrine group （P = 0.041）. In HSC-T6 cells the mRNA and protein expression levels of α SMA in the OB group were significantly lower as compared with those in the oxymatrine group （mRNA, P = 0.013; protein, P = 0.042; respectively）; The mRNA and protein expression levels of type I collagen in the OB group were significantly lower as compared with those in the oxymatrine group （mRNA, P 〈 0.01; protein, P 〈 0.01; respectively）.CONCLUSION： OB combination has a better effect against HBV replication in 2.2.15 cells and is more effective against α SMA expression and type I collagen synthesis in HSC-T6 cells than oxymatrine in vitro.

Experimental study of therapeutic efficacy of Baicalin in rats with severe acute pancreatitis

AIM： To observe the therapeutic efficacy of Baicalin in rats with severe acute pancreatitis （SAP） and explore its therapeutic mechanisms. METHODS： The SAP rat models were randomly divided into the model control group, Baicalin treatment group, octreotide treatment group and sham operation group. All groups were randomly subdivided into 3 h, 6 h and 12 h groups with 15 rats in each group. The survival, ascites volume and pathological changes of pancreas in all rats were observed at different time points after operation. The plasma amylase content and serum TNF-α, IL-6, malonaldehyde （MDA） and PLA2 contents were also determined. RESULTS： The survival was not obviously different between the treated groups, and was significantly higher in treated groups at 12 h compared to the model control group （P 〈 0.05, 15 vs 10）. The ascites/body weight ratio at 3 h and 6 h was significantly lower in Baicalin treatment group compared to the model control group and octreotide treatment group （P 〈 0.05, 1.00 vs 2.02 and 1.43 and P 〈 0.001, 2.29 （1.21） vs 2.70 （0.80） and 2.08 （2.21）, respectively）. The contents of amylase, TNF-α, IL-6, MDA and PLA2 were significantly lower in the treated groups than in the model control group （P 〈 0.05, 4342 vs 5303, 5058 vs 6272 in amylase, P 〈 0.01, 21.90 vs 36.30, 23.80 vs 39.70, 36 vs 54.35 in MDA and 56.25 vs 76.10 in PIA2, or P 〈 0.001, 65.10 and 47.60 vs 92.15 in TNF-α, 3.03 vs 5.44, 2.88 vs 6.82, 2.83 vs 5.36 in IL-6, respectively）. The pathological scores of pancreas in the treated groups were significantly lower than that in the model control group （P 〈 0.05, 9.00 vs 10.05, 6.00 vs 9.00, 8.00 vs 10.05）, but no marked difference was found between the treated groups. CONCLUSION： The Baicalin injection has significant therapeutic effects on SAP rats, its effects are similar to those of octreotide. The Baicalin injection is also cheap and has a big application range, quite hopefully to be used in clinical treatment of SAP.

Correlation between anti-fibrotic effect of baicalin and serum cytokines in rat hepatic fibrosis

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.

Hepatoprotective effects of baicalein against CCl 4-induced acute liver injury in mice

AIM:To investigate the hepatoprotective effect of baicalein against carbon tetrachloride(CCl 4)-induced liver damage in mice.METHODS:Mice were orally administered with baicalein after CCl 4 injection,and therapeutic baicalein was given twice a day for 4 d.The anti-inflammation effects of baicalein were assessed directly by hepatic histology and serum alanine aminotranferease and aspartate aminotransferase measurement.Proliferating cell nuclear antigen was used to evaluate the effect of baicalein in promoting hepatocyte proliferation.Serum interleukin(IL)-6,IL-1β and tumor necrosis factor-α(TNF-α) levels were measured by enzyme-linked immunosorbent assay and liver IL-6,TNF-α,transforming growth factor-α(TGF-α),hepatocyte growth factor(HGF) and epidermal growth factor(EGF) genes expression were determined by quantitative real-time polymerase chain reaction.RESULTS:CCl4-induced acute liver failure model offers a survival benefit in baicalein-treated mice.The data indicated that the mRNA levels of IL-6 and TNF-α significantly increased within 12 h after CCl 4 treatment in baicalein administration groups,but at 24,48 and 72 h,the expression of IL-6 and TNF-α was kept at lower levels compared with the control.The expression of TGF-α,HGF and EGF was enhanced dramatically in baicalein administration group at 12,24,48 and 72 h.Furthermore,we found that baicalein significantly elevated the serum level of TNF-α and IL-6 at the early phase,which indicated that baicalein could facilitate the initiating events in liver regeneration.CONCLUSION:Baicalein may be a therapeutic candidate for acute liver injury.Baicalein accelerates liver regeneration by regulating TNF-α and IL-6 mediated pathways.

Baicalin inhibits PDGF-BB-stimulated vascular smooth muscle cell proliferation through suppressing PDGFRβ-ERK signaling and increase in p27 accumulation and prevents injury-induced neointimal hyperplasia

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.

Antifungal susceptibility analysis of berberine,baicalin,eugenol and curcumin on Candida albicans

Objective:To analyze the antifungal effects of Chinese herb monomers,i.e.berberine,baicalin,eugenol and curcumin,on Candida albicans.Methods:After Candida albicans strain Y01-09 was incubated for 48 h in YEPD broth which contained different concentrations of Chinese herb components,the cell cycle,fluorescent intensity and the size of cell volume were detected by flow cytometry.Results:The 4 Chinese herb monomers could affect the cell cycle of Candida albicans in different ranges.The ratio of cells in S-G2-M period decreased as the agents concentration increased,indicating that the cell division was inhibited.The fluorescent intensity of Candida albicans cells became weaker after being incubated,which reflected the loss of DNA fragments.The higher the concentration was,the weaker the fluorescent intensity became.The cell size,cell diopter and particle size changed much as the agents concentration increased.Conclusion:Chinese herb monomers play the antifungal role in inhibiting cell division.FCM could be used to determine the susceptibility of antifungal agents.

Baicalin and geniposide inhibit the development of atherosclerosis by increasing Wntl and inhibiting dickkopf-related protein-1 expression

Background Our previous study showed that the combined Chinese herbs containing scutellaria baicalensis georgi and gardenia jasminoids ellis inhibited atherosclerosis. In this study, we sought to determine if baicalin and geniposide could inhibit atherosclerosis through Wntl and dickkopf-related protein-1 （DKK1）. Methods The wild-type and ApoE-/- mice were treated with baicalin, geniposide, and baicalin plus geniposide daily by gavage for 12 weeks. Blood lipid levels were measured with an automatic biochemistry analyzer. Aortic atherosclerotic lesion areas were analyzed with Image-ProPlus software. The mRNA and protein expression of DKK1, Wntt and nuclear factor-r,B （NF-κB） were measured with RT-PCR and Westem Blot. Serum levels of interleukin-12 （IL-12） were quantified with ELISA. Results The baicalin or geniposide monotherapy as well as combination therapy inhibited the development of atherosclerotic lesions, increased Wntl and decreased DKKI expression and elevated the ratio of Wntl/DKK1 compared with high-lipid diet group. However, only baicalin or geniposide monotherapy decreased NF-κB expression. Moreover, baicalin and geniposide monoor combination therapy lowered IL-12 levels. Geniposide reduced both serum total cholesterol and low density lipoprotein levels, while baicalin either alone or in combination with geniposide did not affect serum lipid levels. In human, umbilical vein endothelial ceils stimulated by oxidized low density lipoprotein, baicalin and geniposide also increased Wntl and decreased DKK1 expression and elevated the ratio of Wntl/DKK1. Condusions Baicalin and geniposide exert inflammation-regulatory effects and may prevent atherosclerotic lesions through enhancing Wntl and inhibit- ing DKK1 expression.