Bueb J L, Da Silva A, Mousli M, Landry Y
Laboratoire de Neuroimmunopharmacologie, Université Louis Pasteur-Strasbourg I, Illkirch, France.
Biochem J. 1992 Mar 1;282 ( Pt 2)(Pt 2):545-50. doi: 10.1042/bj2820545.
The natural polyamines spermine and spermidine, the biosynthetic precursor putrescine and their analogues cadaverine and tyramine stimulate the GTPase activity of purified GTP-binding proteins (Go/Gi) from calf brain reconstituted into phospholipid vesicles. The order of potency was spermine greater than spermidine greater than putrescine = cadaverine greater than tyramine. The physiological relevance of this observation was assessed, showing the same order of potency of polyamines in the stimulation of peritoneal and tracheal rat mast cells. The activation of rat mast cells by polyamines was inhibited by benzalkonium chloride or by a 2 h pretreatment of the cells with pertussis toxin. The increase in inositol phosphates evoked by polyamines was also inhibited by pertussis toxin. Therefore we propose that intracellular polyamines might control the basal level of second messengers and modulate extracellular signals transduced through G-protein-coupled receptors.
天然多胺精胺和亚精胺、生物合成前体腐胺及其类似物尸胺和酪胺，可刺激重构于磷脂囊泡中的小牛脑纯化GTP结合蛋白（Go/Gi）的GTP酶活性。效力顺序为精胺＞亚精胺＞腐胺 = 尸胺＞酪胺。评估了这一观察结果的生理相关性，结果表明多胺在刺激大鼠腹膜和气管肥大细胞时具有相同的效力顺序。多胺对大鼠肥大细胞的激活受到苯扎氯铵或用百日咳毒素对细胞进行2小时预处理的抑制。多胺引起的肌醇磷酸增加也受到百日咳毒素的抑制。因此，我们提出细胞内多胺可能控制第二信使的基础水平，并调节通过G蛋白偶联受体转导的细胞外信号。
