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首页> 外文期刊>Life sciences >Influence of 5 alpha- and 5 beta-reduced progestins on the contractility of isolated human myometrium at term
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Influence of 5 alpha- and 5 beta-reduced progestins on the contractility of isolated human myometrium at term

机译：5α和5β还原的孕激素对足月分离人子宫肌层收缩力的影响

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摘要

It is very well known that progesterone induces uterine relaxation on myometrium contractile activity. However, little attention has been paid to the effect induced by its metabolites on human uterine contractility. Therefore, we set out to analyze the potential relaxing effect of some 5 alpha- and 5 beta -reduced progesterone derivatives on the spontaneous contractility of myometrium from pregnant women. Samples were obtained by caesarian section at 38-40 weeks of pregnancy. Spontaneous uterine contractions were recorded in vitro in the presence of progesterone, or progestins independently, at different non-cumulative muM concentrations. The progestins elicited an immediate relaxing effect that was concentration-dependent. With the exception of two 5 alpha -reduced progestins (5 alpha and 3 beta ,5 alpha), the remaining progestins used in the present study were more potent than progesterone. The potency order with respect to their IC50 values was: 3 alpha ,5 beta (35 muM) > 5 beta (81 muM) > 3 beta5 beta (156 muM) > 3 alpha ,5 beta (205 muM) > P-4(225 muM) > 5 alpha (19 mM) > 3 beta ,5 alpha (28 mM). When tissues were washed, the contractile activity was recovered. This rapid and reversible relaxing effect was not blocking by antiprogestin RU 486, suggesting that is not through receptor-mediated genomic action. The metabolites from progesterone may also determine the pattern of motility, ensuring the necessary quiescent environment to prevent abortion during gestation. (C) 2001 Elsevier Science Inc. All rights reserved. [References: 39]
机译：众所周知，孕酮在子宫肌层的收缩活动中引起子宫松弛。然而，很少有人关注其代谢产物对人子宫收缩的影响。因此，我们着手分析某些5α和5β还原的孕酮衍生物对孕妇子宫肌层自发收缩力的潜在松弛作用。在妊娠38-40周时通过剖腹产获得样品。在孕酮或孕激素独立存在的情况下，以不同的非累积性muM浓度体外记录自发性子宫收缩。孕激素引起立即放松作用，该作用是浓度依赖性的。除了两种降低5α的孕激素（5α和3β，5α）外，本研究中使用的其余孕激素比孕酮更有效。关于其IC50值的效价顺序为：3 alpha，5 beta（35μM）> 5 beta（81μM）> 3 beta5 beta（156μM）> 3 alpha，5 beta（205 muM）> P-4（ 225μM）> 5 alpha（19 mM）> 3 beta，5 alpha（28 mM）。清洗组织后，收缩活性得以恢复。这种快速和可逆的松弛作用并未被抗孕激素RU 486阻断，表明这不是通过受体介导的基因组作用。孕酮的代谢产物也可能决定运动的方式，从而确保必要的静止环境以防止在妊娠期间流产。 （C）2001 Elsevier Science Inc.保留所有权利。 [参考：39]

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