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首页> 外文期刊>The Journal of Steroid Biochemistry and Molecular Biology >Structure-effect relationship in the induction of mitotic phase-specific abnormality of centrosome integrity and multipolar spindles by steroidal estrogens and their derivatives in cultured mammalian cells.
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Structure-effect relationship in the induction of mitotic phase-specific abnormality of centrosome integrity and multipolar spindles by steroidal estrogens and their derivatives in cultured mammalian cells.

机译：甾体雌激素及其衍生物在哺乳动物细胞中诱导中心体完整性和多极纺锤体有丝分裂期特异性异常的结构效应关系。

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摘要

In order to determine the structure-effect relationship in the induction of centrosome disintegrity (abnormality of gamma-tubulin signals) and multipolar spindles in a cultured fibroblast cell line V79 by steroidal estrogens, the activities of various estrogens and their derivatives were investigated. Induction of centrosome disintegrity by estrogens was specific in cells in the mitotic phase and was not observed in interphase cells. The centrosome disintegrity induced 24 h after exposure to estrogens was accompanied by the appearance of multinucleated cells, but the microtubule network was organized. The rank order of potency of estrogens in inducing mitotic phase-specific centrosome disintegrity and multipolar spindles was as follows: 2-methoxyestradiol>dihydroequilin 3-methyl ether=equilin 3-methyl ether>17alpha-estradiol>17beta-estradiol 3-methyl ether=17beta-estradiol>dihydroequilin>estrone 3-methyl ether. Equilin and estrone were not effective in causing centrosome disintegrity. These results suggest that the 17-hydroxyl group, irrespective of whether it is the sterically alpha or beta form, is necessary for estradiol and dihydroequilin to cause centrosome disintegrity and that O-methylation at the C-3 position was effective for equilin and dihydroequilin in enhancing the centrosome abnormality. 2-Methoxyestradiol was the most potent inducer of the centrosome disintegrity among the tested compounds and caused the induction of multiple signals of gamma-tubulin, including more than five signals.
机译：为了确定甾体雌激素在培养的成纤维细胞系V79中诱导中心体不完整性（γ-微管蛋白信号异常）和多极纺锤体的结构效应关系，研究了各种雌激素及其衍生物的活性。雌激素引起的中心体完整性的破坏在有丝分裂期的细胞中是特异性的，而在间期细胞中未观察到。暴露于雌激素后24 h诱导的中心体不完整性伴随着多核细胞的出现，但微管网络是有组织的。雌激素在诱导有丝分裂期特异性中心体不完整性和多极纺锤体中的效力等级顺序如下：2-甲氧基雌二醇>二氢表鬼鸟苷3-甲基醚=蛇毒蛋白3-甲基醚>17α-雌二醇>17β-雌二醇3-甲基醚= 17β-雌二醇>二氢安息香>雌酮3-甲基醚。 Equilin和雌酮不能有效地引起中心体不完整。这些结果表明，无论是立体α还是β形式的17-羟基基团，对于雌二醇和二氢equilin引起中心体不完整性都是必需的，并且C-3位的O-甲基化对于雌马酚和二氢equilin有效。增强中心体异常。 2-甲氧基雌二醇是被测化合物中中心体不完整的最强诱导剂，并引起多种γ-微管蛋白信号的诱导，包括五个以上的信号。

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