Donowitz M, Cohen M E, Gould M, Sharp G W
Department of Medicine, Tufts University School of Medicine, Boston, Massachusetts.
J Clin Invest. 1989 Jun;83(6):1953-62. doi: 10.1172/JCI114104.
Calcium/calmodulin is involved in the regulation of basal rabbit ileal active Na and Cl absorption, but the mechanism by which elevated intracellular Ca2+ affects Na and Cl transport is unknown. To investigate the roles of the Ca2+/calmodulin and protein kinase C systems in ileal NaCl transport, two drugs, the isoquinolenesulfonamide, H-7, and the naphthalenesulfonamide, W13, were used in concentrations that conferred specificity in the antagonism of protein kinase C (60 microM H-7) and Ca2+/calmodulin (45 microM W13), respectively, as determined using phosphorylation assays in ileal villus cells. W13 but not H-7 stimulated basal active NaCl absorption. H-7 inhibited changes in Na and Cl absorption caused by maximal concentrations of Ca2+ ionophore A23187 and carbachol and serotonin, secretagogues that act by increasing cytosol Ca2+, while W13 had no effect. In contrast, neither H-7 nor W13 altered the change in NaCl transport caused by the cyclic nucleotides 8-Br-cAMP and 8-Br-cGMP. These data suggest that: (a) basal rabbit ileal NaCl absorption is regulated by the Ca2+/calmodulin complex and not by protein kinase C; (b) the effect of elevating intracellular Ca2+ to decrease NaCl absorption is mediated via protein kinase C but not by Ca2+/calmodulin; (c) the effects of protein kinase C are not overlapping or synergistic with those of Ca2+/calmodulin on either basal absorption or on the effects of increased Ca2+; and (d) neither Ca2+/calmodulin nor protein kinase C are involved in the effects of cAMP and cGMP on ileal active NaCl transport.
钙/钙调蛋白参与基础状态下兔回肠对钠和氯的主动吸收调节,但细胞内钙离子升高影响钠和氯转运的机制尚不清楚。为了研究钙/钙调蛋白和蛋白激酶C系统在回肠氯化钠转运中的作用,使用了两种药物,异喹啉磺酰胺H-7和萘磺酰胺W13,其浓度分别对蛋白激酶C(60μM H-7)和钙/钙调蛋白(45μM W13)具有特异性拮抗作用,这是通过回肠绒毛细胞的磷酸化测定确定的。W13而非H-7刺激基础状态下的主动氯化钠吸收。H-7抑制由最大浓度的钙离子载体A23187、卡巴胆碱和5-羟色胺(通过增加胞质溶胶钙离子起作用的促分泌剂)引起的钠和氯吸收变化,而W13没有作用。相反,H-7和W13均未改变由环核苷酸8-溴-cAMP和8-溴-cGMP引起的氯化钠转运变化。这些数据表明:(a)基础状态下兔回肠氯化钠吸收受钙/钙调蛋白复合物调节而非蛋白激酶C调节;(b)细胞内钙离子升高导致氯化钠吸收减少的作用是通过蛋白激酶C介导的,而非钙/钙调蛋白;(c)蛋白激酶C的作用与钙/钙调蛋白在基础吸收或钙离子增加的作用方面既不重叠也不协同;(d)钙/钙调蛋白和蛋白激酶C均不参与cAMP和cGMP对回肠主动氯化钠转运的作用。