HPLC法测定银杏叶缓释微丸胶囊中山奈素、异鼠李素、槲皮素的含量

目的：：建立以高效液相色谱法测定银杏叶缓释微丸胶囊中山奈素、异鼠李素、槲皮素含量的方法。方法：以C 18为色谱柱,流动相为甲醇∶0.4%磷酸溶液（45∶55）,检测波长为360nm,流速为1ml/min,柱温为30℃,进样量是10μl。结果：槲皮素在0.1505～0.9030μg（r＝0.9999）浓度范围内有良好的线性关系,平均回收率为99.86％,RSD=0.4％;山奈素在0.1450～0.8940μg（r＝0.9998）浓度范围内有良好的线性关系,平均回收率为99.79％,RSD=0.5％;异鼠李素在0.0995～0.5970μg（r＝0.9998）浓度范围内有良好的线性关系,平均回收率为99.80％,RSD=0.3％。结论：本方法简便、准确、专属性强,可用于该制剂的质量控制。     

姜黄素对APPswe/PS1△9转基因小鼠空间学习与海马HSP70蛋白表达的影响

目的 探讨姜黄素对APPswe/PS1△9转基因小鼠海马热休克蛋白70(HSP70)表达及对APPswe/PS1 A9转基因小鼠空间学习能力的影响,为AD治疗提供新的理论依据.方法 实验动物分为野生小鼠组、APP/PS1转基因小鼠组、姜黄素干预组、槲皮素(HSPs抑制剂)和姜黄素共同干预组.5月龄转基因小鼠腹腔注射姜黄素150 mg·kg-1·d-1,连续4周,槲皮素和姜黄素共同干预组采用给予150mg· kg-1·d-1姜黄素腹腔注射,同时给予槲皮素50mg· kg-1 ·d-1腹腔注射,连续4周.Western blot测定APP/PS1小鼠海马区HSP70蛋白的表达,Morris水迷宫测试APP/PS1小鼠学习记忆能力,主要观察指标为小鼠找到平台的潜伏期和穿越平台次数.结果 Western blot结果显示,APP/PS1转基因小鼠海马中HSP70蛋白的表达与WT小鼠相比明显降低(OD值:APPswe/PS1△9:0.31±0.14;WT:1.14±0.51,P＜0.01).小鼠腹腔注射给予姜黄素后HSP70的表达较APP/PS1转基因鼠明显升高(OD值:姜黄素:0.91±0.20,P＜0.05).腹腔注射姜黄素或同时给予槲皮素,连续4周后,Morris水迷宫测试结果显示,与WT小鼠相比,APP/PS1小鼠找到平台的潜伏期明显延长[APPswe/PS1 △9:(82.3±6.8)s;WT:(29.5±4.4)s]、穿越平台的次数显著降低[APPswe/PS1 △9:(2.7±1.1)次;WT:(5.2±2.1)次].姜黄素给药后小鼠找到平台的潜伏期较APP/PS1小鼠明显缩短[(47.7±7.6)s],穿越平台的次数增多[(4.5±1.9)次],而小鼠同时给予姜黄素和HSPs抑制剂槲皮素后,找到平台的潜伏期较姜黄素单独给药明显延长[(69.7±9.1)s],穿越平台的次数减少[(3.2±1.6)次].结论 姜黄素可促进APP/PS1转基因小鼠海马HSP70蛋白的表达,同时可提高APP/PS1转基因小鼠的空间学习能力,这可能与姜黄素提高HSP70表达有关,结果提示姜黄素对于AD可能具有潜在的治疗价值.     

不同沙棘叶中槲皮素、山柰酚和异鼠李素的含量比较

目的 比较不同沙棘叶中主要黄酮类成分的含量.方法 采用高效液相色谱法测定槲皮素、山柰酚和异鼠李素的含量.色谱柱Shim-pack VP-ODS(4.6 mm×150 mm,5μm);流动相甲醇-0.4％磷酸(50∶50),流速1.0 mL/min;柱温30℃;检测波长370 nm.结果 槲皮素、山柰酚和异鼠李素的线性范围分别为1.67～106.60μg/mL(r=0.999 9)、0.51～32.64 μg/mL(r=0.999 6)和0.78～49.92 μg/mL(r=0.999 9);平均加样回收率分别为99.50％、98.00％和100.80％.结论 高效液相色谱法准确、简便,可用于沙棘叶的品质评价;不同基源的沙棘叶中黄酮类成分的含量差异较大.     

槲皮素减轻高糖条件下人肾小球内皮细胞损伤的实验研究

目的研究槲皮素减轻高糖条件下人肾小球内皮细胞(HRGEC)损伤的作用及其机制。方法培养HRGEC并分为对照组、高糖组、10μmol/L槲皮素组、100μmol/L槲皮素组,后3组进行高糖处理,10μmol/L及100μmol/L槲皮素组分别给予10μmol/L及100μmol/L槲皮素处理。检测细胞活力、细胞凋亡、凋亡基因mRNA表达量、氧化应激指标含量、PI3K/AKT通路分子蛋白表达量。结果与对照组比较,高糖组的细胞活力、Bcl-2的mRNA表达量、SOD及GPx的含量、p-PI3K及p-AKT的蛋白表达量降低,细胞凋亡率、Bax及Caspase-3的mRNA表达量、MDA的含量增加(P<0.05);与高糖组比较,10μmol/L及100μmol/L槲皮素组的细胞活力、Bcl-2的mRNA表达量、SOD及GPx的含量、p-PI3K及p-AKT的蛋白表达量增加,细胞凋亡率、Bax及Caspase-3的mRNA表达量、MDA的含量降低(P<0.05)且100μmol/L槲皮素组的上述变化较10μmol/L槲皮素组更为显著(P<0.05)。结论槲皮素能够减轻高糖条件下HRGEC的损伤,且这一作用与激活PI3K/AKT通路有关。     

槲皮素对肺动脉高压大鼠肺组织细胞凋亡的影响

目的:观察槲皮素对肺动脉高压肺组织细胞凋亡的影响。方法:将成年雄性SD大鼠30只,随机分为三组:正常对照组(对照组)、野百合碱(MCT)诱导的肺动脉高压组(MCT组)和槲皮素预防组(预防组),每组10只。MCT组及预防组给予野百碱造模,对照组仅以等量0.9%氯化钠液注射,预防组在造模同时每天给予槲皮素100mg/(kg.d)灌胃,21d后测肺动脉压力并计算右心肥大指数,肺组织切片用免疫组化法和免疫印迹法观察大鼠肺组织细胞凋亡(Bcl-2)情况。结果:MCT组大鼠肺动脉平均压力[MCT组(42.13±6.28)vs.对照组(14.57±1.59),P0.05;MCT组(42.13±6.28)vs.预防组(20.32±3.85),P0.05]、右心肥大指数[MCT组(0.593±0.100)vs.对照组(0.241士0.050),P0.05;MCT组(0.593±0.100)vs.预防组(0.290±0.065),P0.05]、肺组织细胞的Bcl-2蛋白相对表达量[MCT组(0.964±0.009)vs.对照组(0.684±0.014),P0.05;MCT组(0.964士0.009)vs.预防组(0.849±0.009),P0.05]显著高于对照组及预防组;同时预防组大鼠肺动脉压力[预防组(20.32士3.85)vs.对照组(14.57±1.59),P0.05]、右心肥大指数[预防组(0.290±0.065)vs.对照组(0.241±0.050),P0.05]、肺组织细胞的Bcl-2蛋白相对表达量[预防组(0.849±0.009)vs.对照组(0.684士0.014),P0.05]高于对照组。结论:槲皮素具有减缓MCT诱导肺动脉高压大鼠肺组织细胞凋亡的作用。     

基于网络药理学研究白仙风汤剂治疗类风湿性关节炎的药理机制

目的 基于网络药理学探讨白仙风汤剂治疗类风湿性关节炎的活性成分,并预测其可能机制。方法 白仙风汤剂中白芍、甘草、青风藤、威灵仙4味草药在TCMSP数据库中检索,经口服吸收率（OB）、类药性、半衰期条件筛选得到药物有效成分,并进行靶点预测;从OMIM、TTD、PharmGKB和GAD数据库对类风湿性关节炎靶点进行检索;使用Cytoscape 3.2.1软件构建药物成分靶点蛋白相互作用网络,对该网络进行拓扑学分析得到核心化学成分及核心靶点;对核心靶点基因进行GO通路分析和KEGG生物过程分析。结果 筛选得到白芍有效成分10个,甘草有效成分66个,青风藤有效成分6个,威灵仙有效成分8个,删除共有的有效成分,共有83个有效活性化合物,对这些化合物进行靶点预测,共得到260个药物靶点;对疾病相关靶点进行检索,共得到58个疾病靶点。通过对药物成分-疾病靶点网络节点的拓扑学分析得到槲皮素、β-谷甾醇、豆甾醇、甘草素等19个核心化学成分,及丝裂原活化蛋白激酶14、雌激素受体、糖皮质激素受体等9个核心靶点,对这些靶点进行通路富集发现药物治疗疾病涉及血管内皮生长因子（VEGF）信号通路、调节脂肪细胞中的脂肪分解、催乳素信号通路、雌激素信号通路、TNF信号通路等11条通路。结论 白仙风汤剂主要通过VEGF信号通路、调节脂肪细胞中的脂肪分解、催乳素信号通路等多条途径实现类风湿性关节炎的治疗作用,表现出多成分、多靶点、多通路的特点,与类风湿关节炎治疗机制相一致。     

Quercetin bioavailability is associated with inadequate plasma vitamin C status and greater plasma endotoxin in adults

ObjectiveQuercetin bioavailability exhibits high interindividual variation for reasons that remain unclear. We conducted a 24-h pharmacokinetic study to investigate whether individual differences in circulating antioxidants, oxidative stress and inflammation, and intestinal permeability affect quercetin bioavailability.MethodsHealthy adults (n = 9 M/7 F; 34.3 ± 4.5 y; 27.0 ± 1.7 kg/m²) ingested 1095 mg quercetin aglycone with a standardized meal. Plasma antioxidants, biomarkers of oxidative stress and inflammation, and endotoxin were measured at baseline (0 h), and quercetin and its methylated metabolites isorhamnetin and tamarixetin were measured at timed intervals for 24 h.ResultsPlasma pharmacokinetics of quercetin, isorhamnetin and tamarixetin were highly variable between participants (CV_inter = 37–96%). Plasma vitamin C concentrations (34.6 ± 2.5 μmol/L), but no other antioxidants, were inversely correlated to the C_max and AUC_{0 to 24 h} of total quercetin (Q_total; sum of quercetin, isorhamnetin and tamarixetin; r = −0.52 to −0.53; P < 0.05). Plasma endotoxin (0.13 ± 0.01 EU/mL), a surrogate marker of intestinal permeability, was correlated to Q_total C_max (r = 0.45; P < 0.05) and tended to be correlated to Q_total AUC_{0 to 24 h} (r = 0.38; P = 0.07). Additionally, vitamin C was inversely related to C-reactive protein, myeloperoxidase, and endotoxin (r = −0.46 to −0.55; P < 0.05), whereas endotoxin was positively correlated to C-reactive protein (r = 0.73; P < 0.05).ConclusionsThese findings suggest that vitamin C status and plasma endotoxin may be associated with interindividual variations in quercetin bioavailability. Greater quercetin absorption and bioavailability may be associated with poor vitamin C status and increased intestinal permeability in healthy adults.     

HPLC法测定银杏叶缓释微丸胶囊中山奈素、异鼠李素、槲皮素的含量

目的建立以高效液相色谱法测定银杏叶缓释微丸胶囊中山奈素、异鼠李素、槲皮素含量的方法。方法以C18为色谱柱,流动相为甲醇-0.4%磷酸溶液(45∶55),检测波长为360 nm,流速为1 m L/min,柱温为30℃,进样量是10μL。结果槲皮素在0.1505⁰.9030μg(r=0.9999)浓度范围内有良好的线性关系,平均回收率为99.86%,RSD=0.4%;山奈素在0.14500.9030μg(r=0.9999)浓度范围内有良好的线性关系,平均回收率为99.86%,RSD=0.4%;山奈素在0.1450⁰.8940μg(r=0.9998)浓度范围内有良好的线性关系,平均回收率为99.79%,RSD=0.5%;异鼠李素在0.09950.8940μg(r=0.9998)浓度范围内有良好的线性关系,平均回收率为99.79%,RSD=0.5%;异鼠李素在0.0995⁰.5970μg(r=0.9998)浓度范围内有良好的线性关系,平均回收率为99.80%,RSD=0.3%。结论本方法简便、准确、专属性强,可用于该制剂的质量控制。     

Quercetin relieves chronic lead exposure-induced impairment of synaptic plasticity in rat dentate gyrus in vivo

Increasing evidence suggests that lead (Pb) produces impairments partly through oxidative stress. Though many researchers have investigated protective effect of some antioxidant nutrients against Pb toxicity, little information is available about the effect of antioxidants on Pb-induced impairment of synaptic plasticity. Quercetin, a strong antioxidant and radical scavenger, is the representative natural flavonoid molecule abundant in fruits and vegetables. Previous studies have found that quercetin was neuroprotective in many cases. This study was designed to evaluate the effect of quercetin on chronic Pb exposure-induced impairment of synaptic plasticity in adult rat dentate gyrus (DG) area in vivo. The input/output (I/O) functions, paired-pulse reactions (PPR), excitatory postsynaptic potential (EPSP), and population spike (PS) amplitude were measured in the DG area of different groups of rats in response to stimulation applied to the lateral perforant path. The results showed that the depressed I/O, PPR, and long-term potentiation (LTP) of Pb-exposed group were significantly increased by quercetin treatment. In addition, hippocampal Pb concentration was partially reduced after quercetin treatment. These findings suggest that quercetin treatment could relieve chronic Pb exposure-induced impairment of synaptic plasticity and might be a potential therapeutic intervention to cure cognitive deficits induced by Pb.