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α1肾上腺素能刺激和β2肾上腺素能抑制血管平滑肌细胞中的DNA合成。

Alpha 1-adrenergic stimulation and beta 2-adrenergic inhibition of DNA synthesis in vascular smooth muscle cells.

作者信息

Nakaki T, Nakayama M, Yamamoto S, Kato R

机构信息

Department of Pharmacology, Keio University School of Medicine, Tokyo, Japan.

出版信息

Mol Pharmacol. 1990 Jan;37(1):30-6.

PMID:2153907
Abstract

Effects of catecholamines on DNA synthesis in vascular smooth muscle cells (VSMC) were investigated in a chemically defined medium that included insulin, transferrin, and sodium selenite. Smooth muscle-rich preparation was obtained from rat aortic media and VSMC were further purified by cell cloning. A clone that was positive for smooth muscle actin and was negative for the coagulation factor VIII was used in this study. The fetal calf serum-induced proliferation was enhanced by alpha-adrenergic and inhibited by beta-adrenergic stimulation. When cells of low passages were used, dose-response curves for norepinephrine were biphasic; when cells were subconfluent, norepinephrine stimulated DNA synthesis at as low as 1 nM and was apparently ineffective at more than 100 nM. When cells were confluent, the effect of norepinephrine was inhibitory at lower concentrations (less than 1 nM) and stimulatory at relatively higher concentrations. Cells of higher passages exhibited only inhibitory effects of the amine. Stimulatory and inhibitory effects on DNA synthesis were mediated through alpha 1- and beta 2-adrenergic receptors, respectively. Thus, the alpha 1-agonist phenylephrine was more potent than the alpha 2-agonist clonidine in stimulating DNA synthesis. An alpha 1-adrenergic antagonist, prazosin, was more effective than the alpha 2-adrenergic antagonist yohimbine in antagonizing the stimulatory effect of norepinephrine. beta-Adrenergic agonists inhibited DNA synthesis with IC50 values in the nanomolar range; the rank order of potency of agonists was isoproterenol greater than salbutamol greater than or equal to (-)-epinephrine much greater than (-)-norepinephrine, consistent with beta 2-receptor specificity. (+)-Epinephrine or (+)-norepinephrine, the stereoisomers of the catecholamines, were ineffective. The inhibitory effects of norepinephrine were reversed by beta-adrenergic antagonists, with the rank order of potency of pindolol greater than butoxamine greater than atenolol, consistent with beta 2-receptor specificity. The dose-response curves of norepinephrine, therefore, seemed to be determined by a balance between alpha 1-receptor-mediated stimulation and beta 2-receptor-mediated inhibition of DNA synthesis. Minimum time required for exhibiting alpha 1-adrenergic or beta 2-adrenergic effects was between 6 and 15 hr, suggesting that the G0 or G1 phase of the cell cycle might be the site of action. These results show that catecholamines dually modulate DNA synthesis in VSMC through specific adrenergic receptors.

摘要

在一种包含胰岛素、转铁蛋白和亚硒酸钠的化学成分明确的培养基中,研究了儿茶酚胺对血管平滑肌细胞(VSMC)DNA合成的影响。从大鼠主动脉中膜获得富含平滑肌的制剂,并通过细胞克隆进一步纯化VSMC。本研究使用了一种对平滑肌肌动蛋白呈阳性且对凝血因子VIII呈阴性的克隆。胎牛血清诱导的增殖通过α-肾上腺素能增强,而通过β-肾上腺素能刺激受到抑制。当使用低代细胞时,去甲肾上腺素的剂量反应曲线是双相的;当细胞未汇合时,去甲肾上腺素在低至1 nM时即可刺激DNA合成,而在超过100 nM时显然无效。当细胞汇合时,去甲肾上腺素在较低浓度(小于1 nM)时起抑制作用,而在相对较高浓度时起刺激作用。高代细胞仅表现出该胺的抑制作用。对DNA合成的刺激和抑制作用分别通过α1-和β2-肾上腺素能受体介导。因此,α1-激动剂去氧肾上腺素在刺激DNA合成方面比α2-激动剂可乐定更有效。α1-肾上腺素能拮抗剂哌唑嗪在拮抗去甲肾上腺素的刺激作用方面比α2-肾上腺素能拮抗剂育亨宾更有效。β-肾上腺素能激动剂抑制DNA合成,IC50值在纳摩尔范围内;激动剂的效力顺序为异丙肾上腺素大于沙丁胺醇大于或等于(-)-肾上腺素远大于(-)-去甲肾上腺素,这与β2-受体特异性一致。儿茶酚胺的立体异构体(+)-肾上腺素或(+)-去甲肾上腺素无效。去甲肾上腺素的抑制作用可被β-肾上腺素能拮抗剂逆转,其效力顺序为吲哚洛尔大于布托沙明大于阿替洛尔,这与β2-受体特异性一致。因此,去甲肾上腺素的剂量反应曲线似乎由α1-受体介导的刺激和β2-受体介导的DNA合成抑制之间的平衡所决定。表现出α1-肾上腺素能或β2-肾上腺素能作用所需的最短时间在6至15小时之间,这表明细胞周期的G0或G1期可能是作用位点。这些结果表明,儿茶酚胺通过特定的肾上腺素能受体对VSMC中的DNA合成进行双重调节。

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