水飞蓟宾对D-半乳糖诱导衰老大鼠抑制糖氧化应激反应及改善学习记忆作用

目的:观察水飞蓟宾对D-半乳糖(D-gal)诱导衰老大鼠糖化氧化应激反应及学习记忆作用的影响。方法:采用D-gal诱导衰老大鼠模型;采用Morris水迷宫测定法检测大鼠学习记忆能力。实验结束后测定大鼠血浆糖化血红蛋白(HbA1c)、血浆非酶糖基化终产物(AGEs)和果糖胺(FRA)含量、红细胞醛糖还原酶(AR)活性及脑组织超氧化物歧化酶(SOD)活性和丙二醛(MDA)、AGEs含量。结果:水飞蓟宾150mg/kg和75mg/kg均能明显抑制D-gal诱导的AR活性增高(P<0.01),降低FRA、HbA1c和AGEs含量(P<0.01或P<0.05),能不同程度地降低大鼠脑组织AGEs和MDA含量,提高SOD活性(P<0.01)。结论:水飞蓟宾对D-半乳糖所致衰老大鼠学习记忆障碍具有保护作用,能增强学习记忆能力,其机制可能与抑制糖氧化应激反应有关。     

甘草中黄酮类化合物的网络药理学研究

目的:分析、预测甘草中黄酮类化合物的潜在药理作用及可能作用机制。方法:采用网络药理学方法,依据中药整合药理学计算平台(TCMSP)等数据库,以化合物的口服药物生物利用度(OB)>30%和类药性(DL)>0.18为标准,筛选甘草中的黄酮类化合物。采用药效团匹配与PharmMapper数据库预测其潜在的作用靶点,随后借助生物学信息注释数据库V 6.8(DAVID V 6.8)分析工具对获得的靶点蛋白进行京都基因与基因组数据库(KEGG)信号通路分析和基因本体(GO)生物过程富集分析(以P<0.05为标准判断相关),并运用Cytoscape 3.5.1软件构建甘草中黄酮类化合物-靶点蛋白-信号通路网络图。结果:共从甘草中筛选出了19个黄酮类化合物(如甘草苷、异甘草苷、甘草素等),涉及细胞视黄酸结合蛋白2、脑啡肽酶等78个靶点蛋白(共188次),以及胰岛素信号通路、磷脂酰肌醇3激酶-丝氨酸/苏氨酸激酶(PI3K-Akt)等40条信号通路(其中与癌症相关的通路8条、与内分泌系统相关的通路7条、与信号转导相关的通路6条、与传染病相关的通路5条、与代谢相关的通路3条等);所建黄酮类化合物-靶点蛋白-信号通路网络图显示,甘草中黄酮类化合物可通过多个靶点作用于不同的疾病代谢通路。结论:甘草中黄酮类化合物对癌症、内分泌系统、传染病、代谢系统等方面疾病可能具有治疗作用,且可能有潜在的抗帕金森症作用。     

晚期糖基化终产物裂解剂C24对糖尿病大鼠心血管作用

目的研究新型化合物C24裂解晚期糖基化终产物(AGEs)蛋白交联结构及其对糖尿病大鼠心血管功能的作用,从而为开发新型AGEs裂解剂提供实验依据。方法酶联免疫吸附测定(ELISA)法测定C24体外裂解AGEs交联结构作用。通过血流动力学实验观察C24对长期糖尿病大鼠心血管的作用,观察C24对大鼠尾胶原溶解性的影响。结果C24能够裂解体外形成的AGEBSA胶原交联结构,能够显著增加糖尿病大鼠心输出量(P<0.05)、降低总外周阻力(P<0.01)、提高动脉顺应性(P<0.05)。生化检测表明,C24能够显著增加糖尿病大鼠尾胶原溶解性(P<0.05),裂解体内AGEs交联结构。结论C24能够裂解体内及体外AGEs交联结构,改善糖尿病大鼠心血管功能。     

葛根素对糖尿病大鼠肾脏非酶糖基化和氧化应激的抑制作用

目的 研究葛根素对糖尿病大鼠氧化应激反应和非酶糖基化的抑制作用。方法糖尿病大鼠用葛根素治疗后，评价葛根素对糖尿病大鼠的非酶糖基化终末期产物、氧化应激及。肾脏结构的影响。结果与对照组比较，糖尿病大鼠糖化血清蛋白(GSP)、糖基化终末期产物-肽链(AGE-P)、。肾小球AGEs含量及肾小球截面积明显上升，同时丙二醛(MDA)显升高，而葛根素治疗组可明显降低糖尿病大鼠GSP、AGE-P、MDA含量，明显降低。肾小球内AGE含量及肾小球截面积。结论葛根素能抑制糖尿病大鼠肾脏非酶糖基化和氧化应激。     

丹知青娥方抑制大鼠下尿路症状

目的探究补阳调阴兼活血化瘀的丹知青娥方(DZQE)是否有抑制下尿路症状的作用,并探讨其可能的作用机制。方法用膀胱灌流法检测DZQE对正常雄性Wistar大鼠排尿参数的影响;分离正常大鼠膀胱逼尿肌肌条,用体外张力法检测对本底水平和KCl诱导的肌条收缩舒张的调节作用;通过TCMSP和ETCM数据库获取并分析DZQE的主要活性成分及其作用靶点,通过GeneCards和DisGeNET数据库收集下尿路症状的作用靶点,通过Cytoscape软件构建中药-活性成分-作用靶点网络,通过DAVID 6.8数据库对相关靶点进行基因本体(GO)分析和信号通路富集分析(KEGG),预测DZQE抑制下尿路症状的可能作用靶点和通路。结果 DZQE可以明显降低大鼠膀胱漏尿点压(DLPP)和最大排尿压(MVP);增加大鼠膀胱逼尿肌肌条本底水平肌条张力,但抑制KCL诱导的肌条收缩,呈现双向调节效应。经筛选得到DZQE的102个化合物进行靶点预测,其中有28个直接或间接与下尿路症状有关,进一步分析表明DZQE可主要通过调节肾上腺信号通路、钙离子信号通路、雌激素信号通路等发挥调节作用。结论 DZQE可以抑制下尿路症状,可能与调节细胞内信号转导抑制平滑肌收缩通路有关。     

参茸益精片对急性高原缺氧脑损伤的保护作用研究

目的观察参茸益精片对急性高原缺氧脑损伤的保护作用,并探讨其分子机制。方法将SD大鼠随机分为空白对照组(对照组)、高原急性缺氧模型组(模型组)和参茸益精片治疗组(治疗组),每组6只。建立急性高原缺氧脑损伤大鼠动物模型,治疗组灌胃参茸益精片。观察大鼠脑组织SOD活性和MDA水平的变化,Western blot和RT-PCR检测胆碱乙酰转移酶(Choline acetyltransferase,ChAT)和蛋白激酶C(Protein kinase C,PKC)表达水平的变化。结果与对照组比较,模型组大鼠脑组织SOD活性显著降低(P<0.01),MDA水平显著增加(P<0.01);治疗组大鼠脑组织SOD活性显著增加(P<0.01),MDA水平显著降低(P<0.01)。模型组大鼠脑组织ChAT和PKC表达水平显著降低(P<0.05),治疗组ChAT和PKC表达水平显著升高(P<0.05)。结论参茸益精片可以保护急性高原缺氧引起的脑损伤,可能与其调节ChAT和PKC的表达水平有关。     

银杏叶提取物对大鼠糖尿病性白内障防治作用的研究

目的探讨银杏叶提取物(extract of ginkgo biloba,GBE)对大鼠糖尿病性白内障(diabetic cataract,DC)的防治作用及可能机制。方法 60只♂SD大鼠随机分为正常对照组、DC模型组、GBE低、中、高剂量组和苄达赖氨酸组。给药12周后,裂隙灯观察大鼠晶状体变化并对其混浊度进行分级;可见光分光光度法测定晶状体中过氧化氢酶(cata-lase,CAT)、谷胱甘肽(glutathione,GSH)和总超氧化物歧化酶(total superoxide dismutase,T-SOD)水平;ELISA法测定糖基化终末产物(advanced glycosylation end products,AGEs)含量;Western blot法测定醛糖还原酶(aldose reductase,AR)相对表达水平。结果 DC组大鼠晶状体明显混浊;GBE中高剂量组较DC组大鼠晶状体混浊程度减轻。DC组大鼠与NS组相比,晶状体中CAT、T-SOD活性降低,GSH含量减少(P<0.01);中高剂量GBE可提高CAT、T-SOD活性及GSH含量(P<0.05或P<0.01)。与NS组相比,DC组大鼠晶状体中的AGEs含量及AR表达明显升高(P<0.01);中高剂量GBE治疗后,AGEs含量与AR表达明显下调(P<0.01)。结论 GBE可能通过增强抗氧化能力、抑制AGEs产生及AR表达,从而减轻大鼠晶状体混浊度,对DC的防治具有积极作用。     

荞麦花总黄酮对体内外蛋白质非酶糖基化的抑制作用

目的　探讨荞麦花总黄酮 (TFBF)对体内外蛋白质非酶糖基化终产物 (AGEs)形成的影响。方法　用链脲佐菌素建立大鼠糖尿病模型 ,以不同剂量 (0 1,0 2 ,0 4g·kg-1·d-1)TFBF口服治疗 12wk ,检测血糖、血浆及肾组织果糖胺和AGEs的含量。同时将不同浓度TFBF与葡萄糖和牛血清白蛋白孵育 ,于 4、8、12wk取出 ,用荧光光度法测定糖基化终产物的自发荧光值。结果　TFBF能明显降低糖尿病大鼠血糖含量 (P <0 0 1) ,抑制肾脏果糖胺和肾脏AGEs的形成 (P <0 0 1) ,并呈明显的剂量依赖性。TFBF对体外蛋白质非酶糖基化终产物的生成也有明显的抑制作用 ,孵育时间越长 ,TFBF剂量越大 ,其抑制作用越明显。结论　TFBF对体内外蛋白质非酶糖基化终产物 (AGEs)的形成具有明显的抑制作用。     

基于网络药理学研究三草降压汤抗糖尿病合并高血压的分子机制

目的采用网络药理学方法研究三草降压汤抗糖尿病合并高血压的活性成分、潜在作用靶点和信号通路,探讨其抗糖尿病合并高血压的“多成分 -多靶点 -多通路”分子机制。方法基于中药系统药理学数据库和分析平台( TCMSP)和毒性与基因比较数据库( CTD)及中国知网筛选三草降压汤相关的成分及作用靶点,利用 CTD、药物靶标数据库( TTD)、生物信息学和化学信息学数据库( DrugBank)和遗传药理数据库( PharmGKB)检索糖尿病合并高血压相关靶点;采用 Cytoscape 3.7插件获得三草降压汤活性成分和糖尿病合并高血压的共同作用靶点。通过 String在线分析平台获得共同作用靶点的“蛋白质 ?蛋白质”相互作用关系( PPI)网络图,最后通过 DAVID的 GO富集分析和 KEGG通路富集分析研究共同作用靶点。结果筛选出三草降压汤的 22个活性成分, 72个关键靶点, 21条显著信号通路。三草降压汤抗糖尿病合并高血压的主要活性成分是槲皮素、山柰酚、木樨草素等,潜在作用靶点和信号通路分别为肿瘤抑制蛋白( TP53)、肿瘤坏死因子( TNF)、白细胞介素 ?6(IL?6)等靶点和 Toll样受体信号通路、丝裂原活化蛋白激酶( MAPK)信号通路、脂肪因子信号通路等,涉及细胞增殖、凋亡、炎症反应等生物学过程。结论三草降压汤抗糖尿病合并高血压的主要分子机制是固醇类、黄酮类和萜类化合物通过影响丝裂原活化蛋白激酶信号通路、脂肪因子信号通路中的相关靶点如 TP53、TNF、IL?6等发挥药效。     

野菊花提取物对糖尿病肾病大鼠的影响及作用机制

目的 观察野菊花提取物对糖尿病肾病大鼠的影响及作用机制。方法 将48只SD大鼠,♀,随机分为正常对照组、模型对照组和野菊花低、中、高剂量组和阳性药依帕司他组(n=8)。除正常对照组外,其余各组大鼠腹腔注射链脲佐菌素35 mg·kg^-1,成功造模后野菊花组分别给予1,2,4 g·kg^-1野菊花提取物,依帕司他组给予10 mg·kg^-1依帕司他,连续灌胃8周后,检测大鼠血糖、体质量、肾脏脏体比、24 h尿白蛋白量、肾组织超氧化歧化酶(SOD)、过氧化氢酶(CAT)的活性及丙二醛(MDA)的含量;HE染色检测肾脏病理改变,ELISA法检测醛糖还原酶(AR)活性并测定其基因表达。结果 与正常对照组相比,模型对照组上述指标除CAT外均有显著改变;与模型对照组相比,野菊花能明显降低大鼠血糖水平、AR活性及其基因表达,明显减少24 h尿白蛋白,升高肾组织SOD、CAT活性,显著降低MDA含量。结论 野菊花提取物对大鼠糖尿病肾病有一定治疗作用,在调节血糖的同时,可能通过提高机体抗氧化能力、减少肾脏AR活性与基因表达以抑制多元醇通路的激活发挥其肾功能的保护作用。     

正交试验优选滁菊总黄酮的提取工艺

目的优选滁菊总黄酮的最佳提取工艺。方法以滁菊总黄酮含量为考察指标,采用正交试验法,对提取过程中乙醇浓度、加醇量、提取时间和提取次数四个影响因素进行研究。结果影响滁菊总黄酮提取的显著因素是加醇量和乙醇浓度。结论以总黄酮含量为考察指标的滁菊最佳提取工艺为用12倍75%乙醇提取2次,每次1 h。     

白背三七总黄酮含量季节性变化规律研究

目的:研究白背三七总黄酮含量的季节性变化规律,为适时采收药材提供依据。方法:对1年12个月采收的白背三七中的总黄酮进行了提取,以芦丁为对照品,用紫外分光光度法测定其含量。结果:白背三七地上部分中的总黄酮含量12月～次年4月较低,5～11月较高。结论:可以根据白背三七的生长周期和总黄酮变化规律,对白背三七进行适时扦插采收,提高白背三七产量。     

凉粉草中总黄酮的提取工艺研究

目的:研究凉粉草中总黄酮的最佳提取工艺。方法:以乙醇为提取剂,芦丁为对照品,NaNO2-Al(N0)3-Na0H显色体系进行显色,测定波长510nm,采用分光光度法测定仙人草中的总黄酮含量。实验设计以单因素实验为重点,考察了温度,浸提时间,浸提次数,和溶媒倍量对总黄酮提取率的影响。结果:总黄酮最佳提取条件为:乙醇浓度50%,提取温度100℃,溶媒倍量12倍,提取次数2次,每次1.0h。结论:凉粉草总黄酮的提取率稳定,RSD为0.52%,总黄酮含量平均值为28.55%。该方法简便,重现性好。     

Influence of flavonoid extracts from celery on oxidative stress induced by dichlorvos in rats

The present work was to investigate the effects of flavonoid extracts from celery on oxidative stress induced by dichlorvos (DIC) in male Wistar rats maintained on a normal diet. The rats were given DIC through intragastric administration by the dose of 7.2 mg/kg·body weight (bw)/day and additionally added 5% flavonoid extracts to the diet for 4 weeks continuously. The activities of superoxide dismutase (SOD), glutathione peroxidase (GPx), catalase (CAT), glutathione-S-transferase (GST) and the content of malondialdehyde (MDA) in livers of rats were measured at the end of the experiment. Under the influence of DIC, there were significant decrease in the activities of SOD, CAT and GST and significant increase in GPx activity and MDA content. The results also showed that the activities of SOD, GST and CAT in the DIC-treated group declined significantly when compared with the flavonoid extracts group and the DIC + flavonoid extracts group, respectively. With regard to GPx activity and MDA content, significant increase were showed in the DIC-treated group in comparison to those in the flavonoid extracts group and the DIC + flavonoid extracts group, respectively. The observations presented lead us to conclude the harmful effects of DIC during the exposure and the protective role of flavonoids in minimizing these effects.     

The use of information theory and numerical taxonomy methods for evaluating the quality of thin-layer chromatographic separations of flavonoid constituents of Matricariae flos

A methanol extract of Matricariae flos was analysed with regard to the flavonoid composition. Rational selection of a restricted set from eight chromatographic systems tested for the separation of these compounds is discussed. Series of mathematical techniques for the evaluation of solvents and solvent combinations in thin-layer chromatography of flavonoid constituents have been explored. The chromatographic systems are classified according to their mutual resemblance by numerical taxonomy techniques. The selection criterion in the groups, obtained by numerical taxonomy classification, is the information content or the discriminating power. The most suitable mobile phases for TLC separation of flavonoid constituents of Matricariae flos are: ethylacetate-methanol-water (75:15:0 v/v), ethylacetate-formic acid-water (80:10:10 v/v) and ethylacetate-formic acid-acetic acid-water (100:11:11:27 v/v).     

玉郎伞化学成分对自发性高血压大鼠血压的影响

目的:研究从玉郎伞块根分离得到的黄酮、皂苷和多糖对大鼠血压的影响,筛选出降压活性成分。方法:用BL-420生物信号分析系统测定麻醉大鼠颈动脉压和用ALC-NIBP无创尾动脉压测量分析系测定清醒大鼠尾动脉压,观察玉郎伞黄酮、皂苷和多糖对自发性高血压大鼠(SHR)和W istar大鼠血压的影响。结果:静脉注射玉郎伞黄酮和皂苷均能明显降低SHR s和正常W istar大鼠的血压,灌胃给药也能明显降低SHR s的血压,而且降压作用较持久。结论:玉郎伞黄酮和皂苷是玉郎伞中主要的降压活性成分,对正常SHR s和W istar大鼠均有明显的降压作用。     

Effects of the Flavonoid Pilloin Isolated from Marrubium cylleneum on Mitogen-Induced Lymphocyte Transformation

Flavonoids are known to exhibit a wide range of biological functions. In the present study, the possible immunomodulatory and cytotoxic effects of pilloin, a flavone extracted from the Greek endemic herb Marrubium cylleneum were investigated by using the in vitro lymphocyte transformation and the cytotoxicity assays, respectively. Apigenin was used as the control flavonoid. Pilloin exerted a cytotoxic action targeted at the transformed lymphoblasts. On the other hand, the glycosylated flavonoid chrysoeriol-7- O -ß-D-(3?- E-p -coumaroyl)-glucopyranoside was inactive, providing further evidence that glycosylation may eliminate the effects of aglycones.     

Simultaneous reversed-phase high-performance liquid chromatographic method for the determination of diosmin,hesperidin and naringin in different citrus fruit juices and pharmaceutical formulations

Diosmin, hesperidin and naringin are flavonoid glycosides that occur naturally in citrus fruits. They exert a variety of pharmacological properties such as anti-inflammatory, antioxidant and free radical scavenging and antiulcer effects and also inhibit selected cytochrome P-450 enzymes resulting in drug interactions. A reversed-phase high-performance liquid chromatographic method has been developed for the simultaneous determination of diosmin, hesperidin and naringin in different citrus fruit juices and pharmaceutical preparations. Diosmin, hesperidin, naringin and the internal standard rhoifolin were separated using tetrahydrofuran/water/acetic acid (21:77:2, v/v/v) as the mobile phase at 34 degrees C, using a C8 reversed-phase column. The method was linear in the 0.25-20.0 microg/ml concentration range for all three flavonoid glycosides (r>0.999). The method has been successfully applied to the determination of all three flavonoid glycosides in several samples of different citrus fruit juices sold in Greece and for the determination of diosmin and hesperidin in pharmaceutical preparations.     

Phenolic content and anti-hyperglycemic activity of pecan cultivars from Egypt

Context: Pecans are commonly used nuts with important health benefits such as anti-hyperglycemic and anti-hyperlipidemic effects.

Objective: A comparative investigation of the antihyperglycemic and total phenolic content of the leaves and shells of four pecan cultivars growing in Egypt was carried out. The selected cultivars (cv.) were Carya illinoinensis Wangneh. K. Koch. cv. Wichita, cv. WesternSchely, cv. Cherokee, and cv. Sioux family Juglandaceae.

Materials and methods: Total phenolic and flavonoid contents of the leaves and shells of pecan cultivars were carried out using Folin–Ciocalteu’s and aluminum chloride assays, respectively. Moreover, HPLC profiling of phenolic and flavonoid contents was carried out using RP-HPLC-UV. In addition, in vivo anti-hyperglycemic activity of the ethanolic extracts (125?mg/kg bw, p.o.) of C. illinoinensis cultivars was carried out using streptozotocin (STZ)-induced diabetes in Sprague–Dawley rats for 4 weeks.

Results and discussion: Phenolic contents were higher in shells than leaves in all studied cultivars, while flavonoids were higher in leaves. Leaves and shells of cv. Sioux showed the highest phenolics (251.7?µg gallic acid equivalent (GAE)/g), and flavonoid contents (103.27?µg rutin equivalent (RE)/g and 210.67?µg quercetin equivalent (QE)/g), respectively. The HPLC profiling of C. illinoinensis cultivars resulted in the identification of eight flavonoids (five of these compounds are identified for the first time from pecan), and 15 phenolic acids (six are identified for the first time from pecan). Leaves of cv. Sioux revealed the most potent decrease in blood glucose and glycated hemoglobin (HbA_1c%) (194.9?mg/dl and 6.52%, respectively), among other tested cultivars. Moreover, leaves of cv. Sioux significantly elevated serum total antioxidant capacity (TAC) and reduced glutathione (GSH) (0.33?mMol/l and 30.68?mg/dl, respectively), and significantly suppressed the markers of both lipid peroxidation (malondialdehyde, MDA) and protein oxidation (protein carbonyl, PC) (14.25?µmol/ml and 3.18?nmol/mg protein, respectively).

Conclusion: Different pecan cultivars showed significant variation in its phenolic and flavonoid contents and consequently their antioxidant and anti-hyperglycemic effects.     

红花檵木叶黄酮类化学成分的分离与鉴定

目的:研究红花檵木叶中的黄酮类化学成分。方法:采用D101大孔树脂分离富集红花檵木叶乙醇提取物中的黄酮类成分,应用硅胶柱、Sephadex LH-20凝胶柱和RP-ODS柱色谱分离化合物,并通过核磁共振光谱、紫外光谱和电喷雾质谱等谱学手段鉴定化合物结构。结果:从红花檵木叶乙醇提取物中分离鉴定了5个黄酮类化合物,分别为山柰酚、槲皮素、杨梅素、杨梅素-3-O-α-L-鼠李糖苷、异槲皮苷。所有黄酮类化合物均为首次从该植物中分离得到。结论:本试验结果可为红花檵木的进一步开发利用提供科学依据。