Wang Gui-jun, Yao Yu-sheng, Wang Hong-xin
The First Affiliated Hospital, Liaoning Medical College, China.
Zhongguo Ying Yong Sheng Li Xue Za Zhi. 2010 Feb;26(1):82-5.
To demonstrate the inhibitory effect of kappa-opioid receptor activation by U50488H on hypertrophy induced by NE in cultured neonatal rat cardiac myocytes and compare its effect with that of prazosin and propranolol.
The cellular proliferation was determined with crystal violet staining. The protein content was assayed with Lowry's method. The cardiomyocytes volumes were measured by computer photograph analysis system. The protein synthesis was assayed with [3H]-lencine incorporation method.
(1) NE significantly induced the increase of protein content, [3H]-leucine incorporation and cell size without a concomitant increase in cell number in low serum medium. OThese responses were partially suppressed by prazosin or propranolol alone and completely abolished by both in combination. U50488H significantly inhibited the NE-induced increase of protein content, [3H]-leucine incorporation and cell size. The inhibitory effects of U50488H on NE-induced cardiac hypertrophy were greater than either prazosin or propranolol, but comparable to combination of both.
NE, acting via both alpha1- and beta-adrenergic pathway, stimulates myocyte hypertrophy. Stimulating kappa-opioid receptor significantly inhibits NE-induced cardiac hypertrophy, which may be related with alpha1- and beta1-adrenergic pathway.
证明U50488H激活κ-阿片受体对培养的新生大鼠心肌细胞中去甲肾上腺素（NE）诱导的肥大的抑制作用，并将其与哌唑嗪和普萘洛尔的作用进行比较。
用结晶紫染色法测定细胞增殖。用洛瑞法测定蛋白质含量。通过计算机图像分析系统测量心肌细胞体积。用[3H]-亮氨酸掺入法测定蛋白质合成。
（1）在低血清培养基中，NE显著诱导蛋白质含量、[3H]-亮氨酸掺入量增加以及细胞大小增大，但细胞数量没有相应增加。单独使用哌唑嗪或普萘洛尔可部分抑制这些反应，两者联合使用则可完全消除这些反应。U50488H显著抑制NE诱导的蛋白质含量、[3H]-亮氨酸掺入量增加以及细胞大小增大。U50488H对NE诱导的心肌肥大的抑制作用大于哌唑嗪或普萘洛尔，但与两者联合使用的效果相当。
NE通过α1和β肾上腺素能途径发挥作用，刺激心肌细胞肥大。刺激κ-阿片受体可显著抑制NE诱导的心肌肥大，这可能与α1和β1肾上腺素能途径有关。
