Gillzan K M, Stewart A G
Bernard O'Brien Institute of Microsurgery, St Vincent's Hospital, Fitzroy, Victoria, Australia.
Pulm Pharmacol Ther. 1997;10(2):71-9. doi: 10.1006/pupt.1997.0077.
Opening of calcium-dependent K+ channels by beta 2-adrenoceptor agonists has been shown to contribute to their smooth muscle relaxant activity. In this study, the influence of K+ channel activity on human cultured airway smooth muscle proliferation and on its inhibition by salbutamol have been examined. Studies of 86Rb+ efflux from the airway smooth muscle cell cultures confirmed that both cromakalim, an activator of ATP-dependent K+ channels and salbutamol increased K+ channel activity in cultured airway smooth muscle. The efflux of 86Rb+ was significantly attenuated by non-specific K+ channel blockade. Potassium channel blockers had only small and variable effects on [3H]-thymidine incorporation in unstimulated cells and those stimulated with fetal calf serum (FCS) and no effect on FCS-induced increases in cell number. Potassium channel openers also had no substantial inhibitory effects on DNA synthesis or proliferation in cells stimulated with other mitogens including thrombin. Blockade of K+ channels had no consistent effects on the inhibition of DNA synthesis and cell proliferation caused by salbutamol (0.3 nM-10 microM). The inhibition of DNA synthesis caused by 8 bromoadenosine 3'5' cyclic monophosphate (1 microM-1 mM) or 8 bromoguanosine 3'5' cyclic monophosphate (1 microM-1 mM) was also unaffected by K+ channel blockade. These results indicate that changes in K+ channel activity have no detectable influence on DNA synthesis and proliferation of human cultured airway smooth muscle cells or on the antiproliferative effects of beta 2-agonists.
β2肾上腺素能受体激动剂可使钙依赖性钾通道开放,这已被证明有助于其平滑肌舒张活性。在本研究中,已检测了钾通道活性对人培养气道平滑肌增殖及其受沙丁胺醇抑制的影响。对气道平滑肌细胞培养物中86Rb+外流的研究证实,ATP依赖性钾通道激活剂克罗卡林和沙丁胺醇均可增加培养气道平滑肌中的钾通道活性。非特异性钾通道阻断可显著减弱86Rb+的外流。钾通道阻滞剂对未刺激细胞以及用胎牛血清(FCS)刺激的细胞中[3H] - 胸腺嘧啶核苷掺入仅有微小且多变的影响,对FCS诱导的细胞数量增加无影响。钾通道开放剂对用包括凝血酶在内的其他促有丝分裂原刺激的细胞中的DNA合成或增殖也无实质性抑制作用。钾通道阻断对沙丁胺醇(0.3 nM - 10 μM)引起的DNA合成和细胞增殖抑制无一致影响。8 - 溴腺苷3',5'-环磷酸(1 μM - 1 mM)或8 - 溴鸟苷3',5'-环磷酸(1 μM - 1 mM)引起的DNA合成抑制也不受钾通道阻断的影响。这些结果表明,钾通道活性的变化对人培养气道平滑肌细胞的DNA合成和增殖或β2激动剂的抗增殖作用无明显影响。