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影响糖皮质激素在心肌组织中非特异性结合的因素。

Factors influencing nonspecific binding of glucocorticoids in myocardial tissue.

作者信息

Beardsley A C, Okuda M, Lefer A M

出版信息

Proc Soc Exp Biol Med. 1976 Mar;151(3):457-61. doi: 10.3181/00379727-151-29234.

DOI:10.3181/00379727-151-29234
PMID:3798
Abstract

Myocardial slices from the left ventricle of cat hearts were incubated in Krebs-Henseleit buffer containing 10 mM glucose which were gassed with 95% O2 and 5% CO2. Tritiated dexamethasone (DEXA 0.171 MM) or methylprednisolone (MP 0.805 mM) was added under varying conditions of temperature, pH, and in the presence of various metabolic inhibitors. Glucocorticoid uptake by myocardial tissue was found to be temperature-dependent, plateauting after 60 min of incubation at 0.21 mumole of DEXA/g of tissue and 0.95 mumole of MP/g of tissue at 37 degrees. Steroid uptake was retarded about 50% at 0 degrees. Increasing the concentration of either steroid resulted in a linear increase in the uptake of that steroid. Incubation in the presence of metabolic or SH-inhibitors produced no significant changes in glucocorticoid uptake. Optimal glucocorticoid uptake occurred between pH 7.3-7.4. Thus, myocardial cells appear to be able to take up large quantities of glucocorticoids, but the uptake process does not appear to be energy-dependent.

摘要

取自猫心脏左心室的心肌切片在含有10 mM葡萄糖的Krebs-Henseleit缓冲液中孵育,该缓冲液用95% O₂和5% CO₂ 进行通气。在不同的温度、pH条件下以及存在各种代谢抑制剂的情况下,加入氚标记的地塞米松(DEXA 0.171 mM)或甲泼尼龙(MP 0.805 mM)。发现心肌组织对糖皮质激素的摄取是温度依赖性的,在37℃孵育60分钟后达到平台期,此时地塞米松的摄取量为0.21微摩尔/克组织,甲泼尼龙的摄取量为0.95微摩尔/克组织。在0℃时,类固醇的摄取约延迟50%。增加任何一种类固醇的浓度都会导致该类固醇摄取量呈线性增加。在存在代谢抑制剂或SH抑制剂的情况下孵育,糖皮质激素的摄取没有显著变化。最佳糖皮质激素摄取发生在pH 7.3 - 7.4之间。因此,心肌细胞似乎能够摄取大量的糖皮质激素,但摄取过程似乎不是能量依赖性的。

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Factors influencing nonspecific binding of glucocorticoids in myocardial tissue.影响糖皮质激素在心肌组织中非特异性结合的因素。
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引用本文的文献

1
Mechanism of the beneficial effect of dexamethasone on myocardial cell integrity in acure myocardial ischemia.地塞米松对急性心肌缺血中心肌细胞完整性有益作用的机制
Basic Res Cardiol. 1980 Mar-Apr;75(2):328-39. doi: 10.1007/BF01907581.
2
Morphometric observations on the rat heart after high-dose treatment with cortisol.
Virchows Arch A Pathol Anat Histol. 1980;385(2):169-80. doi: 10.1007/BF00427402.