摘要
目的:探索4-乙基-7-[2-(4-甲基哌嗪基)乙酰胺基]-3,4-二氢-1,4-苯并噁嗪-3-酮的抗血小板聚集机制。方法:采取同一只兔子的心脏动脉血,制备血浆样品,将其分为空白对照组、阳性对照组和实验组。每组进行3次重复实验。在血浆样品中加入胶原Ι诱导剂后加入药品:空白对照组加入0.01%二甲亚砜(DMSO)溶剂;阳性对照组加入阳性对照药物的0.01%DMSO溶液;实验组加入4-乙基-7-[2-(4-甲基哌嗪基)乙酰胺基]-3,4-二氢-1,4-苯并噁嗪-3-酮的0.01%DMSO溶液。通过双抗体一步夹心法酶联免疫吸附试验(Enzyme-linked Immunosorbent Assay, ELISA)检测血小板血栓素B2(TXB2)和五羟色胺(5-HT)的含量变化。结果:阳性对照组和实验组的TXB2含量分别比空白对照组低40%和59%,而5-HT含量分别比空白对照组高19.8%和21.0%,且P<0.05具有统计学意义。结论:4-乙基-7-[2-(4-甲基哌嗪基)乙酰胺基]-3,4-二氢-1,4-苯并噁嗪-3-酮通过抑制血小板TXB2的释放、阻断5-HT与其受体结合来抑制血小板聚集,且抑制血小板TXB2释放的机制作用更显著。
Objective:To investigate the antiplatelet aggregation mechanism of N-(4-ethyl-3-oxo-3,4-dihydro-2 Hbenzo[b][1,4]oxazin-7-yl)-2-(4-methylpiperazin-1-yl) acetamide.Methods:Blood samples were collected from the same rabbit’s heart arteries.Plasma samples were divided into three groups:blank control group,positive control group and experimental group,and three repeated experiments were performed in each group.After adding collagen I inducer and then adding drugs into the plasma samples,blank control group,positive control group and experimental group were treated with 0.01% DMSO solvent,0.01% DMSO solution of positive drug and 0.01% DMSO solution of N-(4-ethyl-3-oxo-3,4-dihydro-2 H-benzo[b][1,4]oxazin-7-yl)-2-(4-methylpiperazin-1-yl) acetamide,respectively.Next,TXB2 and5-HT enzyme-linked immunosorbent assays were performed.The changes of TXB2 and 5-HT contents were determined.Results TXB2 enzyme-linked immunosorbent assays showed that the TXB2 content in the positive control group and experimental group was 40% and 59.0% respectively lower than that in the blank control group,while the 5-HT content in the positive control group and blank control group was 19.8% and 21.0% respectively higher than that in the blank control group.And P<0.05 has statistical significance.Conclusion N-(4-Ethyl-3-oxo-3,4-dihydro-2 H-benzo[b][1,4]oxazin-7-yl)-2-(4-methylpiperazin-1-yl) acetamide inhibits platelet aggregation by inhibiting the release of TXB2 and blocking the binding of 5-HT to its receptors,and N-(4-ethyl-3-oxo-3,4-dihydro-2 H-benzo[b][1,4]oxazin-7-yl)-2-(4-methylpiperazin-1-yl) acetamide has a stronger effect on TXB2 than on 5-HT.
作者
单一桓
邓楠
祁真平
左华
Shan Yihuan;Deng Nan;Qi Zhenping;Zuo Hua(College of Pharmaceutical Sciences,Southwest University,Chongqing 400716,China)
出处
《江苏科技信息》
2020年第20期65-69,共5页
Jiangsu Science and Technology Information
