Xin Wenkuan, Li Ning, Cheng Qiuping, Fernandes Vitor S, Petkov Georgi V
Department of Drug Discovery and Biomedical Sciences, South Carolina College of Pharmacy, University of South Carolina, Columbia, South Carolina; and.
Department of Drug Discovery and Biomedical Sciences, South Carolina College of Pharmacy, University of South Carolina, Columbia, South Carolina; and Department of Urology, Fourth Hospital of China Medical University, Shenyang, China.
Am J Physiol Cell Physiol. 2014 Dec 15;307(12):C1142-50. doi: 10.1152/ajpcell.00167.2014. Epub 2014 Oct 15.
The elevation of protein kinase A (PKA) activity activates the large-conductance voltage- and Ca(2+)-activated K(+) (BK) channels in urinary bladder smooth muscle (UBSM) cells and consequently attenuates spontaneous phasic contractions of UBSM. However, the role of constitutive PKA activity in UBSM function has not been studied. Here, we tested the hypothesis that constitutive PKA activity is essential for controlling the excitability and contractility of UBSM. We used patch clamp electrophysiology, line-scanning confocal and ratiometric fluorescence microscopy on freshly isolated guinea pig UBSM cells, and isometric tension recordings on freshly isolated UBSM strips. Pharmacological inhibition of the constitutive PKA activity with H-89 or PKI 14-22 significantly reduced the frequency and amplitude of spontaneous transient BK channel currents (TBKCs) in UBSM cells. Confocal and ratiometric fluorescence microscopy studies revealed that inhibition of constitutive PKA activity with H-89 reduced the frequency and amplitude of the localized Ca(2+) sparks but increased global Ca(2+) levels and the magnitude of Ca(2+) oscillations in UBSM cells. H-89 abolished the spontaneous transient membrane hyperpolarizations and depolarized the membrane potential in UBSM cells. Inhibition of PKA with H-89 or KT-5720 also increased the amplitude and muscle force of UBSM spontaneous phasic contractions. This study reveals the novel concept that constitutive PKA activity is essential for controlling localized Ca(2+) signals generated by intracellular Ca(2+) stores and cytosolic Ca(2+) levels. Furthermore, constitutive PKA activity is critical for mediating the spontaneous TBKCs in UBSM cells, where it plays a key role in regulating spontaneous phasic contractions in UBSM.
蛋白激酶A(PKA)活性的升高可激活膀胱平滑肌(UBSM)细胞中的大电导电压和Ca(2 +)激活的K(+)(BK)通道,从而减弱UBSM的自发性相性收缩。然而,组成型PKA活性在UBSM功能中的作用尚未得到研究。在此,我们测试了这样一个假设,即组成型PKA活性对于控制UBSM的兴奋性和收缩性至关重要。我们对新鲜分离的豚鼠UBSM细胞进行了膜片钳电生理学、线扫描共聚焦和比率荧光显微镜检查,并对新鲜分离的UBSM条带进行了等长张力记录。用H - 89或PKI 14 - 22对组成型PKA活性进行药理抑制,可显著降低UBSM细胞中自发性瞬时BK通道电流(TBKCs)的频率和幅度。共聚焦和比率荧光显微镜研究表明,用H - 89抑制组成型PKA活性可降低局部Ca(2 +)火花的频率和幅度,但会增加UBSM细胞中的整体Ca(2 +)水平和Ca(2 +)振荡的幅度。H - 89消除了UBSM细胞中的自发性瞬时膜超极化,并使膜电位去极化。用H - 89或KT - 5720抑制PKA也会增加UBSM自发性相性收缩的幅度和肌肉力量。这项研究揭示了一个新的概念,即组成型PKA活性对于控制细胞内Ca(2 +)储存产生的局部Ca(2 +)信号和胞质Ca(2 +)水平至关重要。此外,组成型PKA活性对于介导UBSM细胞中的自发性TBKCs至关重要,它在调节UBSM的自发性相性收缩中起关键作用。