白三烯C_4(LTC_4)放射受体结合方法的建立及二苯乙烯低聚体和LTC_4受体结合特性  

STUDIES ON THE CHARACTERISTICS OF LTC_4 RECEPTOR WITH RADIO LIGAND BINDING ASSAY AND THE EFFECT OF STILBENE POLYMER(Gn_3)

作　　者：侯艳宁[1,2] 朱秀媛[1] 程桂芳[1] 

机构地区：[1]中国医学科学院,中国协和医科大学药物研究所,石家庄市050082 [2]白求恩国际和平医院,北京100050

出　　处：《药学学报》2000年第2期81-84,共4页Acta Pharmaceutica Sinica

摘　　要：目的:建立LTC4放射受体结合实验方法,并比较二苯乙烯低聚体(Gn3)和LTC4受体的结合特性。方法:以豚鼠肺膜为实验材料,采用3HLTC4为放射配体,以FPL55712作阳性对照药物,Gn3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Gn3对LTC4受体的拮抗作用。结果:3HLTC4与其相应受体呈现单一结合位点,Gn3可明显取代3HLTC4与其受体结合。生物学检定法证实Gn3可抑制LTC4引起的生物学效应。结论:豚鼠肺膜LTC4受体为单一结合位点受体,Gn3为高活性的LTC4受体拮抗剂。AIM: To set up a radio ligand binding assay of LTC 4 for studying the effect of Gn 3(a stilbene polymer isolated from Gnetum parvifolium ) on the LTC 4 receptor.METHODS: Guinea pig lung membrane was used as experimental materials, 3H LTC 4 as radio ligand, FPL 55712 as positive control drug and Gn 3 as test drug. Bioassay in vitro was used to determine the biological function of Gn 3. RESULTS: The binding of 3H LTC 4 to its receptor was shown to be specific, saturable and reversible. The Ki and Bmax values were 2 7× 10 -10 mol·L -1 and 3 55×10 -13 mol·mg -1 protein, respectively, at 30℃. Gn 3 was found to inhibit 3H LTC 4 in competing for LTC 4 receptor. The IC 50 and Ki values were 6 39×10 -7 mol·L -1 and 3 32×10 -7 mol·L -1 respectively. Gn 3 was also found to be a LTC 4 receptor antagonist by bioassay in vitro . CONCLUSION: The binding of 3H LTC 4 on guinea pig lung membrane showed a single binding site. Gn 3 is an effective LTC 4 receptor antagonist.

关 键 词：白三烯C4 放射受体结合 二苯乙烯低聚体 

分 类 号：R962[医药卫生—药理学]