本文選題：阿司匹林　切入點：血小板聚集　出處：《世界臨床藥物》2016年02期

【摘要】：目的探究腺苷二磷酸(ADP)監(jiān)測阿司匹林抗血小板聚集的作用及相關的信號轉導通路,為抗血小板聚集藥物的篩選提供指導。方法 SD大鼠灌胃給藥(0.5%CMC-Na,5 ml/kg;阿司匹林20、50和100 mg/kg;普拉格雷25 mg/kg),均為一日1次,共4 d。最后一次給藥后1 h,大鼠經(jīng)水合氯醛麻醉,腹主動脈采血,低速離心,收集上層液(富血小板血漿)。應用不同濃度(0、0.1、0.3、1和10μmol/L)的ADP對阿司匹林抗血小板聚集的作用進行監(jiān)測。利用富血小板血漿進行蛋白質(zhì)印跡試驗,觀察相關蛋白激酶的激活情況。結果不同劑量阿司匹林對ADP誘導血小板聚集的抑制率隨著ADP濃度的增加(0~10μmol/L)呈先升高后降低的趨勢,這種現(xiàn)象與阿司匹林劑量無關。在ADP濃度為0.3μmol/L時,阿司匹林低(20 mg/kg)、中(50 mg/kg)及高劑量(100 mg/kg)組的血小板聚集抑制率均為同組中最高(與陰性對照組比較,P0.01)。而在ADP濃度為10μmol/L時,阿司匹林的血小板聚集抑制率均小于10%,對應普拉格雷組(25 mg/kg)的血小板聚集抑制率為(76.72±7.83)%;蛋白質(zhì)印跡試驗結果表明,不同劑量阿司匹林均可引起ERK2顯著磷酸化,且ERK2磷酸化程度隨阿司匹林劑量的增加有減弱趨勢。結論低劑量ADP(0.3μmol/L)用于監(jiān)測阿司匹林的抗血小板聚集作用更為可靠。
[Abstract]:Objective to investigate the role of Aspirin in antiplatelet aggregation and its signal transduction pathway in order to provide guidance for the screening of antiplatelet aggregation drugs.Methods Sprague-Dawley rats were given 0.5 ml / kg CMC-NaOH, 50 mg / kg aspirin and 100 mg / kg aspirin, and 25 mg / kg Pragray once a day for 4 days.One hour after the last administration, rats were anesthetized by chloral hydrate, blood was collected from abdominal aorta, centrifuged at low speed, and the supernatant (platelet-rich plasma) was collected.The antiplatelet effect of aspirin on platelet aggregation was monitored by ADP with different concentrations of 0.1 渭 mol / L and 10 渭 mol / L of Aspirin.The activation of protein kinase was observed by Western blotting assay with platelet rich plasma.Results the inhibitory rate of different doses of aspirin on platelet aggregation induced by ADP was increased first and then decreased with the increase of ADP concentration, which was independent of the dose of aspirin.When the concentration of ADP was 0.3 渭 mol/L, the inhibition rate of platelet aggregation was the highest in the group of 20 mg / kg Aspirin, 50 mg / kg Aspirin and 100 mg / kg of high dose of Aspirin (compared with the negative control group (P 0.01).When the concentration of ADP was 10 渭 mol/L, the inhibition rate of platelet aggregation of aspirin was less than 10. The inhibition rate of platelet aggregation was 76.72 鹵7.83% in the Pragray group (25 mg / kg). The results of Western blot showed that different doses of aspirin could induce the phosphorylation of ERK2.The degree of phosphorylation of ERK2 decreased with the increase of aspirin dosage.Conclusion low dose ADP(0.3 渭 mol / L is more reliable for monitoring the antiplatelet aggregation of aspirin.
【作者單位】： 中國醫(yī)藥工業(yè)研究總院上海醫(yī)藥工業(yè)研究院創(chuàng)新藥物與制藥工藝國家重點實驗室;
【基金】：上海市浦江人才計劃(編號:13PJ1433100) 留學人員科技活動項目資助 上海市生物物質(zhì)成藥性評價專業(yè)技術服務平臺(編號:15DZ2291700)
【分類號】：R965

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