Hatt J F, Hanson P J
Pharmaceutical Sciences Institute, Aston University, Birmingham, United Kingdom.
Am J Physiol. 1989 Jan;256(1 Pt 1):G129-38. doi: 10.1152/ajpgi.1989.256.1.G129.
Sites at which the calcium-sensitive phospholipid-dependent protein kinase, protein kinase C, may influence acid secretion have been investigated in rat isolated parietal cells. In both crude and enriched preparations of parietal cells incubated in a medium containing 100 mM K+, the activators of protein kinase C, 12-O-tetradecanoylphorbol 13-acetate (TPA) and 1-oleoyl-2-acetyl-glycerol (OAG), produced a dose-dependent stimulation [half-maximally effective concentration (EC50) values of 1 nM and 70 microM, respectively] of aminopyrine accumulation, an index of the sequestration of acid in the cell. In a medium containing 4.5 mM K+, and with no added secretagogues, TPA and OAG did not affect aminopyrine accumulation. Histamine-stimulated aminopyrine accumulation was inhibited by TPA [half-maximally effective inhibitory concentration (IC50) of 2.9 nM]. TPA reduced the histamine-stimulation of the adenosine 3',5'-cyclic monophosphate (cAMP) content of parietal cells (47% inhibition at 100 nM TPA) but also inhibited aminopyrine accumulation at or distal to cAMP-dependent protein kinase. Activators of protein kinase C can produce multiple effects on secretory activity in the rat parietal cell.
在大鼠离体壁细胞中,对钙敏感的磷脂依赖性蛋白激酶即蛋白激酶C可能影响胃酸分泌的位点进行了研究。在含有100 mM钾离子的培养基中孵育的壁细胞粗提物和富集提取物中,蛋白激酶C的激活剂,12 - O - 十四烷酰佛波醇13 - 乙酸酯(TPA)和1 - 油酰 - 2 - 乙酰甘油(OAG),对氨基比林蓄积产生了剂量依赖性刺激作用[半数最大效应浓度(EC50)值分别为1 nM和70 microM],氨基比林蓄积是细胞内酸隔离的一个指标。在含有4.5 mM钾离子且未添加促分泌剂的培养基中,TPA和OAG不影响氨基比林蓄积。组胺刺激的氨基比林蓄积受到TPA抑制[半数最大效应抑制浓度(IC50)为2.9 nM]。TPA降低了组胺对壁细胞腺苷3',5'-环磷酸(cAMP)含量的刺激作用(在100 nM TPA时抑制47%),但也在cAMP依赖性蛋白激酶处或其下游抑制了氨基比林蓄积。蛋白激酶C激活剂可对大鼠壁细胞的分泌活性产生多种影响。