Amiloride blocks cell-free protein synthesis at levels attained inside cultured rat hepatocytes.
Amiloride blocks cell-free protein synthesis at levels attained inside cultured rat hepatocytes.
复制标题
阿米洛利可阻断培养大鼠肝细胞内达到的无细胞蛋白质合成水平。
DOI：
10.1016/0006-291x(82)90891-9
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发表时间：
1982
影响因子：
3.1
通讯作者：
Skelly,H
中科院分区：
文献类型：
--
作者：
Leffert,HL;Koch,KS;Fehlmann,M;Heiser,W;Lad,PJ;Skelly,H
阿米洛利是一种被动Na+内流抑制剂，可降低无细胞兔网织红细胞裂解物中[35 S]met摄取到蛋白质中的初始速率和平台水平（ID 50 ≤ 0.4 mM）。分离的肝细胞通过饱和的Na+依赖性过程摄取阿米洛利（Km = 0.02 mM; Vmax = 1.43 nmol/106 cells/min）。在培养的肝细胞单层中发生类似的温度依赖性摄取。在化学成分确定的培养基中，在生长再起始条件下，阿米洛利降低细胞蛋白质和白蛋白合成的总体速率（ID 50分别为0.4和0.028 mM）。阿米洛利浓度（0.02 mM），最大限度地抑制肝细胞DNA合成的重新启动的一半达到，在30分钟内，细胞水平（约0.14 mM），阻止网织红细胞裂解物蛋白质合成的25%。这些发现复杂的解释，从许多真核系统的研究，有丝分裂原激活的膜Na+流入和DNA合成的重新启动之间的因果关系。
Amiloride, a passive Na+influx inhibitor, lowers initial rates and plateau levels of [35S]met uptake into proteins in cell-free rabbit reticulocyte lysates (ID50∽0.4 mM). Isolated hepatocytes take up amiloride through a saturable (Km∽0.02 mM; Vmax∽1.43 nmol/ 106cells/min) Na+-dependent process. Similar temperature dependent uptake occurs in cultured hepatocyte monolayers. In chemically defined media, under growth reinitiation conditions, amiloride lowers overall rates of cellular protein and albumin synthesis (ID50∽0.4 and ∽0.028 mM, respectively). Amiloride concentrations (0.02 mM) that half-maximally inhibit reinitiation of hepatocyte DNA synthesis reach, within 30 min, cellular levels (∽0.14 mM) that block reticulocyte lysate protein synthesis by 25%. These findings complicate interpretations, from studies in many eukaryotic systems, of cause and effect between mitogen-activated membrane Na+influxes and the reinitiation of DNA synthesis.