论文部分内容阅读
目的 采用LTD4 放射受体结合实验方法 ,在分析LTD4 受体的有关特征的基础上 ,观察比较二苯乙烯低聚体 (Gn 3)对LTD4 受体的拮抗作用。方法 以豚鼠肺膜为实验材料 ,采用3 H LTD4 为放射配体 ,以FPL55712 作阳性对照药物 ,Gn 3为实验药物 ,进行药物竞争结合实验。采用离体器官生物检测法鉴定Gn 3对LTD4 受体的拮抗作用。结果 3 H LTD4 与其相应受体呈现单一结合位点 ,其Kd 和Bmax值分别为 19.9× 10 -11mol·L-1和 2 32 .9fmol·mg-1蛋白。Gn 3可明显取代3 H LTD4 与其受体结合 ,IC50 值为 5 .71× 10 -7mol·L-1,Ki值为 2 .5 4× 10 -7mol·L-1。生物学鉴定法证实Gn 3可抑制LTD4 引起的生物学效应。结论 豚鼠肺膜LTD4 受体为单一结合位点受体 ,Gn 3为高活性的LTD4 受体拮抗剂。
OBJECTIVE To investigate the antagonistic effect of stilbene oligomer (Gn 3) on LTD4 receptor by the LTD4 radioreceptor binding assay based on the analysis of the related features of LTD4 receptor. Methods Guinea pig lung membrane was used as experimental material, 3 H LTD4 was used as radioligand, FPL55712 was used as positive control and Gn 3 was used as experimental drug. Drug competition and binding experiments were carried out. The antagonistic effect of Gn 3 on LTD4 receptor was identified by the method of ex vivo organism detection. Results 3 H LTD4 showed a single binding site with its corresponding receptor, and its Kd and Bmax values were 19.9 × 10 -11 mol·L-1 and 2 · 32 · 9 fmol · mg-1, respectively. Gn 3 could obviously replace the binding of 3 H LTD4 to its receptor with an IC50 value of 5.71 × 10 -7 mol·L -1 and a Ki value of 2.54 × 10 -7 mol·L -1. Biological assays confirm that Gn 3 inhibits the biological effects induced by LTD4. Conclusion The LTD4 receptor of guinea pig lung membrane is a single binding site receptor, and Gn 3 is a highly active LTD4 receptor antagonist.