Hopkins N E, English N, Hughes V, Rowley C W, Wolf C R, Alworth W L
Department of Pharmacology, Tulane University Medical School, New Orleans, Louisiana 70112, USA.
Biochem Biophys Res Commun. 1998 Mar 27;244(3):868-72. doi: 10.1006/bbrc.1998.8170.
CYP102 (Cytochrome P450BM-3) is induced in Bacillus megaterium by barbiturates, peroxisome proliferators, and nonsteroidal anti-inflammatory drugs. We now describe the induction of CYP102 in B. megaterium by 17 beta-estradiol and by 4-sec-butylphenol. These estrogens interact with the repressor protein Bm3R1, causing it to dissociate with the operator of the CYP102 gene and allowing transcription to occur. We have developed a stable transfection of a construct into B. megaterium of a truncated CYP102 gene coupled with the luciferase gene in a promoterless plasmid and have used this construct to test the induction of CYP102 by these estrogens. Estradiol demonstrated a dose-dependent induction of CYP102 which saturated at a 2-fold increase at 150 microM 4 hr post-addition. 4-sec-Butylphenol produced a dose-dependent and time-dependent induction up to 300 microM and 6 hr post-induction.
CYP102（细胞色素P450BM-3）在巨大芽孢杆菌中可被巴比妥类药物、过氧化物酶体增殖剂和非甾体抗炎药诱导。我们现在描述17β-雌二醇和4-仲丁基苯酚对巨大芽孢杆菌中CYP102的诱导作用。这些雌激素与阻遏蛋白Bm3R1相互作用，使其与CYP102基因的操纵子解离，从而允许转录发生。我们已将一个构建体稳定转染到巨大芽孢杆菌中，该构建体是一个截短的CYP102基因与荧光素酶基因连接在一个无启动子的质粒中，并使用这个构建体来测试这些雌激素对CYP102的诱导作用。雌二醇对CYP102表现出剂量依赖性诱导，在添加后4小时，150微摩尔时诱导倍数增加2倍达到饱和。4-仲丁基苯酚在诱导后6小时内，浓度高达300微摩尔时产生剂量依赖性和时间依赖性诱导。
