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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >Nongenomic inhibition of coronary constriction by 17beta-estradiol, 2-hydroxyestradiol, and 2-methoxyestradiol.
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Nongenomic inhibition of coronary constriction by 17beta-estradiol, 2-hydroxyestradiol, and 2-methoxyestradiol.

机译：17β-雌二醇，2-羟基雌二醇和2-甲氧基雌二醇对冠状动脉收缩的非基因组抑制。

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摘要

The cardioprotective effects of 17beta-estradiol (E2) in women are hypothesized to be partially mediated by the E2 metabolites 2-hydroxyestradiol (2-HOE) and 2-methoxyestradiol (2-MeOH). Therefore, the purpose of our study was to determine the acute effects of E2, 2-HOE, and 2-MeOH on inhibition of coronary arterial constriction. Right coronary arteries obtained from breeding sows were cut into 4 mm rings and suspended in organ baths. Incubation of the rings with E2, 2-HOE, and 2-MeOH (10 micromol/L) for 60 min attenuated a subsequent KCl-induced contraction by approximately 50%. The protein synthesis inhibitor cycloheximide and the estrogen receptor antagonists ICI 182780 and tamoxifen did not affect the attenuation. Moreover, E2, 2-HOE, and 2-MeOH antagonized the contraction induced by the vasospasm agonist endothelin-1 (0.1 micromol/L) by approximately 36%. When the L-type Ca2+ channel blocker nifedipine was added at the conclusion of the experiment, no additional contractile attenuation was present. Our results suggest that E2, 2-HOE, and 2-MeOH demonstrate a similar nongenomic inhibition of agonist-induced extracellular Ca2+-dependent contractions.
机译：据推测17β-雌二醇（E2）对女性的心脏保护作用部分是由E2代谢物2-羟基雌二醇（2-HOE）和2-甲氧基雌二醇（2-MeOH）介导的。因此，我们的研究目的是确定E2、2-HOE和2-MeOH对抑制冠状动脉收缩的急性作用。从种母猪获得的右冠状动脉被切成4毫米的环，并悬浮在器官浴中。将环与E2、2-HOE和2-MeOH（10 micromol / L）孵育60分钟，可使随后的KCl诱导的收缩减弱约50％。蛋白质合成抑制剂环己酰亚胺和雌激素受体拮抗剂ICI 182780和他莫昔芬不影响衰减。此外，E2、2-HOE和2-MeOH拮抗血管痉挛激动剂内皮素-1（0.1 micromol / L）诱导的收缩约36％。在实验结束时添加L型Ca2 +通道阻滞剂硝苯地平时，不存在额外的收缩衰减。我们的结果表明，E2、2-HOE和2-MeOH表现出对激动剂诱导的细胞外Ca2 +依赖性收缩的类似非基因组抑制作用。

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