Chakraborty C, Davis D L, Dey S K
Department of Obstetrics and Gynecology, University of Kansas Medical Center, Kansas City 66103.
J Steroid Biochem. 1988 Aug;31(2):231-5. doi: 10.1016/0022-4731(88)90060-x.
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.
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。