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猪囊胚中雌激素-2/4-羟化酶的特性:甾体和非甾体药物的抑制作用

Characteristics of estrogen-2/4-hydroxylase in pig blastocysts: inhibition by steroidal and nonsteroidal agents.

作者信息

Chakraborty C, Davis D L, Dey S K

机构信息

Department of Obstetrics and Gynecology, University of Kansas Medical Center, Kansas City 66103.

出版信息

J Steroid Biochem. 1988 Aug;31(2):231-5. doi: 10.1016/0022-4731(88)90060-x.

DOI:10.1016/0022-4731(88)90060-x
PMID:2841540
Abstract

The inhibitory potencies of steroidal and non-steroidal estrogens, catechol-estrogens, methoxyestrogen, haloestrogens, cholesterol and its side-chain-cleaved products, and inhibitors of steroid aromatase against the activity of estradiol-2/4-hydroxylase (E-2/4-H) in pig blastocysts were studied. All tested compounds, except cholesterol and 4-hydroxyandrostenedione, inhibited E-2/4-H in vitro. The fluctuation of E-2/4-H activity in pig blastocysts on different days of pregnancy may be due to the modulation of enzyme activity by steroids in the uterine lumen. Although alpha-naphthoflavone and aminoglutethimide did not affect E-2/4-H activity in vitro, inhibition by CO (95% CO + 5% O2), SKF-525A, piperonyl butoxide, and antibody to cytochrome P-450 reductase provides evidence for the involvement of cytochrome P-450 in E-2/4-H activity in pig blastocysts.

摘要

研究了甾体和非甾体雌激素、儿茶酚雌激素、甲氧基雌激素、卤代雌激素、胆固醇及其侧链裂解产物以及甾体芳香化酶抑制剂对猪胚泡中雌二醇-2/4-羟化酶(E-2/4-H)活性的抑制效力。除胆固醇和4-羟基雄烯二酮外,所有测试化合物均在体外抑制E-2/4-H。妊娠不同天数猪胚泡中E-2/4-H活性的波动可能是由于子宫腔内类固醇对酶活性的调节所致。尽管α-萘黄酮和氨鲁米特在体外不影响E-2/4-H活性,但一氧化碳(95%CO + 5%O2)、SKF-525A、胡椒基丁醚和细胞色素P-450还原酶抗体的抑制作用为细胞色素P-450参与猪胚泡中E-2/4-H活性提供了证据。

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1
Characteristics of estrogen-2/4-hydroxylase in pig blastocysts: inhibition by steroidal and nonsteroidal agents.猪囊胚中雌激素-2/4-羟化酶的特性:甾体和非甾体药物的抑制作用
J Steroid Biochem. 1988 Aug;31(2):231-5. doi: 10.1016/0022-4731(88)90060-x.
2
Catechol estrogen formation by pig blastocysts during the preimplantation period: biochemical characterization of estrogen-2/4-hydroxylase and correlation with aromatase activity.猪胚泡植入前期儿茶酚雌激素的形成:雌激素-2/4-羟化酶的生化特性及其与芳香化酶活性的相关性
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Estradiol-15 alpha-hydroxylation: a new avenue of estrogen metabolism in peri-implantation pig blastocysts.雌二醇-15α-羟基化:着床前猪囊胚雌激素代谢的新途径。
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Characteristics of estrogen-2/4-hydroxylase of porcine ovarian follicles: influence of steroidal and non-steroidal agents on the activity of the enzyme in vitro.猪卵巢卵泡雌激素-2/4-羟化酶的特性:甾体和非甾体药物对该酶体外活性的影响。
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Effect of aromatase inhibitors on estrogen 2-hydroxylase in rat liver.芳香化酶抑制剂对大鼠肝脏中雌激素2-羟化酶的影响。
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Catechol estrogen formation in the mouse uterus and its role in implantation.小鼠子宫中儿茶酚雌激素的形成及其在着床中的作用。
Mol Cell Endocrinol. 1990 Feb 12;69(1):25-32. doi: 10.1016/0303-7207(90)90085-m.
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Inhibition of estrogen 2-hydroxylase.雌激素2-羟化酶的抑制作用。
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Preimplantation mouse blastocysts fail to express CYP genes required for estrogen biosynthesis.植入前的小鼠囊胚无法表达雌激素生物合成所需的CYP基因。
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Kinetic studies of inhibition of estradiol 2- and 16 alpha-hydroxylases in rat liver microsomes with various cytochrome P-450 inhibitors.用各种细胞色素P-450抑制剂对大鼠肝微粒体中雌二醇2-羟化酶和16α-羟化酶抑制作用的动力学研究。
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