Galbraith R A, Jellinck P H
Biochem Biophys Res Commun. 1987 May 29;145(1):376-83. doi: 10.1016/0006-291x(87)91332-5.
A single injection of cobalt-protoporphyrin (CoPP), which produces a marked and sustained decline in hepatic cytochrome P450 content, reduced the ability of male rat liver microsomes to form catechol estrogens to about 30% of control values within 1 day, as measured by the release of 3H2O from [2-3H]estradiol. Two days after treatment, the apparent Km of estrogen 2-hydroxylase for estradiol was increased, but other inhibitors of cytochrome P450 function (SKF-525A or piperonyl butoxide) failed to affect the enzyme. Inhibition by CoPP was also demonstrated by measuring the conversion of [4-14C]estradiol to its 2-hydroxylated derivative visualized by autoradiography after chromatographic separation. These findings point to yet another site in the multifaceted action of cobalt protoporphyrin.
单次注射钴原卟啉（CoPP）可使肝细胞色素P450含量显著且持续下降，雄性大鼠肝微粒体将雌二醇转化为儿茶酚雌激素的能力在1天内降至对照值的约30%，这是通过[2-³H]雌二醇释放³H₂O来测定的。处理两天后，雌激素2-羟化酶对雌二醇的表观Km增加，但其他细胞色素P450功能抑制剂（SKF-525A或胡椒基丁醚）未能影响该酶。通过色谱分离后放射自显影观察[4-¹⁴C]雌二醇向其2-羟基化衍生物的转化，也证实了CoPP的抑制作用。这些发现指出了钴原卟啉多方面作用中的另一个位点。
