Harden T K, Hawkins P T, Stephens L, Boyer J L, Downes C P
Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill 27514.
Biochem J. 1988 Jun 1;252(2):583-93. doi: 10.1042/bj2520583.
Phosphatidylinositol (PtdIns), phosphatidylinositol 4-phosphate (PtdIns4P) and phosphatidylinositol 4,5-bisphosphate [PtdIns(4,5)P2] of turkey erythrocytes were labelled by using either [32P]Pi or [3H]inositol. Although there was little basal release of inositol phosphates from membranes purified from labelled cells, in the presence of guanosine 5'-[gamma-thio]triphosphate (GTP[S]) the rate of accumulation of inositol bis-, tris- and tetrakis-phosphate (InsP2, InsP3 and InsP4) was increased 20-50-fold. The enhanced rate of accumulation of 3H-labelled inositol phosphates was linear for up to 20 min; owing to decreases in 32P specific radioactivity of phosphoinositides during incubation of membranes with unlabelled ATP, the accumulation of 32P-labelled inositol phosphates was linear for only 5 min. In the absence of ATP and a nucleotide-regenerating system, no InsP4 was formed, and the overall inositol phosphate response to GTP[S] was decreased. Analyses of phosphoinositides during incubation with ATP indicated that interconversions of PtdIns to PtdIns4P and PtdIns4P to PtdIns(4,5)P2 occurred to maintain PtdIns(4,5)P2 concentrations; GTP[S]-induced inositol phosphate formation was accompanied by a corresponding decrease in 32P- and 3H-labelled PtdIns, PtdIns4P and PtdIns(4,5)P2. In the absence of ATP, only GTP[S]-induced decreases in PtdIns(4,5)P2 occurred. Since inositol monophosphate was not formed under any condition, PtdIns is not a substrate for the phospholipase C. The production of InsP2 was decreased markedly, but not blocked, under conditions where Ins(1,4,5)P3 5-phosphomonoesterase activity in the preparation was inhibited. Thus the predominant substrate of the GTP[S]-activated phospholipase C of turkey erythrocyte membranes is PtdIns(4,5)P2. Ins(1,4,5)P3 was the major product of this reaction; only a small amount of Ins(1:2-cyclic, 4,5)P3 was released. The effects of ATP on inositol phosphate formation apparently involve the contributions of two phenomena. First, the P2-receptor agonist 2-methylthioadenosine triphosphate (2MeSATP) greatly increased inositol phosphate formation and decreased [3H]PtdIns4P and [3H]PtdIns(4,5)P2 in the presence of a low (0.1 microM) concentration of GTP[S]. ATP over the concentration range 0-100 microM produced effects in the presence of 0.1 microM-GTP[S] essentially identical with those observed with 2MeSATP, suggesting that the effects of low concentrations of ATP are also explained by a stimulation of P2-receptors. Higher concentrations of ATP also increase inositol phosphate formation, apparently by supporting the synthesis of substrate phospholipids.(ABSTRACT TRUNCATED AT 400 WORDS)
利用[32P]Pi或[3H]肌醇标记火鸡红细胞中的磷脂酰肌醇(PtdIns)、磷脂酰肌醇4-磷酸(PtdIns4P)和磷脂酰肌醇4,5-二磷酸[PtdIns(4,5)P2]。尽管从标记细胞中纯化的膜中肌醇磷酸的基础释放量很少,但在鸟苷5'-[γ-硫代]三磷酸(GTP[S])存在下,肌醇二磷酸、三磷酸和四磷酸(InsP2、InsP3和InsP4)的积累速率增加了20至50倍。3H标记的肌醇磷酸积累速率在长达20分钟内呈线性;由于在膜与未标记ATP孵育期间磷酸肌醇的32P比放射性降低,32P标记的肌醇磷酸积累仅在5分钟内呈线性。在没有ATP和核苷酸再生系统的情况下,不形成InsP4,并且对GTP[S]的总体肌醇磷酸反应降低。在与ATP孵育期间对磷酸肌醇的分析表明,发生了PtdIns向PtdIns4P以及PtdIns4P向PtdIns(4,5)P2的相互转化以维持PtdIns(4,5)P2浓度;GTP[S]诱导的肌醇磷酸形成伴随着32P和3H标记的PtdIns、PtdIns4P和PtdIns(4,5)P2相应减少。在没有ATP的情况下,仅发生GTP[S]诱导的PtdIns(4,5)P2减少。由于在任何条件下都不形成肌醇单磷酸,PtdIns不是磷脂酶C的底物。在制剂中Ins(1,4,5)P3 5-磷酸单酯酶活性受到抑制的条件下,InsP2的产生明显减少但未被阻断。因此,火鸡红细胞膜中GTP[S]激活的磷脂酶C的主要底物是PtdIns(4,5)P2。Ins(1,4,5)P3是该反应的主要产物;仅释放少量Ins(1:2-环,4,5)P3。ATP对肌醇磷酸形成的影响显然涉及两种现象的作用。首先,P2受体激动剂2-甲硫基三磷酸腺苷(2MeSATP)在低(0.1 microM)浓度的GTP[S]存在下极大地增加了肌醇磷酸形成并降低了[3H]PtdIns4P和[3H]PtdIns(4,5)P2。在0至100 microM浓度范围内的ATP在0.1 microM - GTP[S]存在下产生的效应与用2MeSATP观察到的效应基本相同,表明低浓度ATP的效应也可以通过刺激P2受体来解释。较高浓度的ATP也增加肌醇磷酸形成,显然是通过支持底物磷脂的合成。(摘要截断于400字)