选择性5-羟色氨受体抑制剂——巴西苏木红素(英文) Brazilein,a Selective 5-HT Receptors Antagonist in Mouse Uterus
中国天然药物 , Chinese Journal of Natural Medicines, 编辑部邮箱 , 2011年05期 【作者】 王秀坤; 雷帆; 柴玉爽; 王玉刚; 詹宏磊; 邢东明; 游学甫; 李慧颖; 杜力军;
【Author】 WANG Xiu-Kun 1,2,LEI Fan 1,CHAI Yu-Shuang 1,WANG Yu-Gang 1,ZHAN Hong-Lei 1,XING Dong-Ming 1,YOU Xue-Fu 2,LI Hui-Ying 1,DU Li-Jun 1 1Protein Science Laboratory of the Ministry of Education,Laboratory of Pharmaceutical Sciences,School of Life Sciences and School of Medicine,Tsinghua University,Beijing 100084,China;2Institute of Medicinal Biotechnology,Peking Union Medical College and Chinese Academy of Medical Sciences,Beijing 100050,China
【机构】 清华大学生命科学学院医学院药物药理研究室; 中国医学科学院北京协和医学院医药生物技术研究所药理室;
【摘要】 目的:子宫平滑肌内存在多种5-HT受体,5-HT通过作用于5-HT受体实现其对子宫收缩活性的影响。本研究探讨巴西苏木红素对5-HT受体的作用及其特点。方法:小鼠分离子宫平滑肌条,采用受体拮抗实验和real time PCR方法,对巴西苏木红素的5-HT受体的抑制作用进行研究。结果:巴西苏木红素虽然对正常子宫平滑肌的收缩幅度和频率无影响,但能明显抑制5-HT2受体激动剂马来酸麦角新碱的收缩活性,其pA2为5.71±0.21。而5-HT亚型的选择性激动剂舒马普坦(5-HT1D)、AL34662(5-HT2A)、MCPP(5-HT2C)的收缩子宫活性同样能够被巴西苏木红素抑制,pA2分别为4.58±0.06;4.91±0.15;5.38±0.15。巴西苏木红素明显抑制了5-HT受体1D和2C亚型mRNA的表达。结论:巴西苏木红素能够阻滞小鼠子宫5-HT受体,并通过可能影响5-HT受体所介导的子宫功能。 更多还原
【Abstract】 AIM:To prove brazilein’s effect on 5-HT receptor and to understand the characteristics of the action.METHODS:In this work,the blocking effect of brazilein on 5-HT receptor subtypes was investigated in isolated uterine strips using pharmacological(selective agonists) and molecular biological(real time PCR) approaches.RESULTS:brazilein does not affect the contractions of normal mice uterus,but inhibits uterine excitatory elicited by ergometrine maleate(pA2 = 5.71 ± 0.21),a 5-HT2 receptor agonist.T... 更多还原 【关键词】 巴西苏木红素; 5-HT受体; 子宫; 小鼠; 【Key words】 Brazilein; 5-HT receptor; Uterus; Mouse; 【基金】 supported by the National S&T Major Special Project for New Drug R&D of China (Nos. 2009ZX09103-301, 2009ZX09502-021 and 2011ZX09101-002-11);the National Natural Science Foundation of China (Nos. 30973896,30801523 and 81073092);the Scientific Foundation for China Postdoctoral fellows (No. 20080440418);the Special Foundation for Laboratory of Tsinghua University (No. LF 20103579)~~【分类号】R93
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