Yang K X, Black J L
Department of Pharmacology, University of Sydney, NSW, Australia.
Eur J Pharmacol. 1995 Mar 14;275(3):283-9. doi: 10.1016/0014-2999(94)00785-6.
The involvement of protein kinase C in the contraction of airway smooth muscle has been investigated in human isolated bronchus. Phorbol 12,13-dibutyrate (PDB) (10 microM) produced aw biphasic response--relaxation followed by contraction. The protein kinase C inhibitor, staurosporine (0.1 microM) reduced the contractile response to PDB from 89 +/- 2.9% to 53 +/- 4.5% of the response to 1 mM acetylcholine (P < 0.05, n = 6) but increased the relaxation response from 12 +/- 6.1% to 29 +/- 5% (P < 0.05, n = 6). Staurosporine also reduced the maximal contractile response to a single dose of histamine (10 microM) from 121 +/- 13% to 91 +/- 10% (P < 0.05, n = 4) and the sustained phase tension from 94 +/- 4% to 85 +/- 5% at 30 min (P < 0.05, n = 4). However, GF 109203X, a more selective inhibitor of protein kinase C at 0.1 microM, 1 microM and 10 microM had no effect on the maximal contractile response and reduced only the sustained phase of the contraction to histamine. These results suggest that protein kinase C plays a role in maintenance of contraction in human airway smooth muscle.
在人离体支气管中，对蛋白激酶C参与气道平滑肌收缩的情况进行了研究。佛波醇12,13 - 二丁酸酯（PDB）（10微摩尔）产生双相反应——先是舒张，随后是收缩。蛋白激酶C抑制剂星形孢菌素（0.1微摩尔）使对PDB的收缩反应从对1毫摩尔乙酰胆碱反应的89±2.9%降至53±4.5%（P<0.05，n = 6），但使舒张反应从12±6.1%增至29±5%（P<0.05，n = 6）。星形孢菌素还使对单剂量组胺（10微摩尔）的最大收缩反应从121±13%降至91±10%（P<0.05，n = 4），并使30分钟时的持续相张力从94±4%降至85±5%（P<0.05，n = 4）。然而，GF 109203X作为一种更具选择性的蛋白激酶C抑制剂，在浓度为0.1微摩尔、1微摩尔和10微摩尔时，对最大收缩反应无影响，仅降低了对组胺收缩的持续相。这些结果表明，蛋白激酶C在人气道平滑肌收缩的维持中发挥作用。
