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营钛所介导古白干宫功能.
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 inice uterus, but inhibits uterine excitatory elicited by ergometrine maleate (pA2 = 5.71 ± 0.21), a 5-HT2 receptor agonist. The excitatory effects of 5-HTID, 5-HT2A and 5-HT2c receptor agonists on uterus could be inhibited by brazilein (pA2 = 4.58 ± 0.06, 4.91 ± 0.15, 5.38± 0.15, respectively). The mRNA expression of 5-HT1D and 5-HTzc receptors in mice uterus were decreased by brazilein. CONCLUSION: brazilein blocked 5-HT receptors in mice uterus and might affect the functions mediated by 5-HT receptors.