Näslund B M, Glaumann H, Warner M, Gustafsson J A, Hansson T
Department of Medical Nutrition, Huddinge University Hospital, Sweden.
Mol Pharmacol. 1988 Jan;33(1):31-7.
A quantitative assessment of the levels of cytochromes P-450 b and P-450 c in the brains and pituitary glands of untreated and beta-naphthoflavone (BNF)-pretreated rats was made with polyclonal antibodies raised against hepatic P-450 b and c and the sensitive fluorometric assay of P-450 catalytic activity, namely, the O-deethylation of ethoxycoumarin (ETC). In the microsomal fraction of brains of untreated rats, the rate of formation of 7-hydroxycoumarin from ETC ranged between 0.1 and 20 pmol/min/mg of microsomal protein, which is approximately 0.01-2% of the level of hepatic microsomes of phenobarbital-induced rats. This brain activity was completely inhibited by anti P-450 b antibodies but was unaffected by anti P-450 c antibodies. As with hepatic P-450 b, metyrapone and chloramphenicol (100 microM) were good inhibitors of catalytic activity, whereas alpha-naphthoflavone (1 microM) was a poor inhibitor. No ETC O-deethylase activity was detectable in microsomes prepared from the pituitary glands of untreated rats. Upon pretreatment of rats with BNF, there was induction of ETC O-deethylase activity in the pituitary gland to a level of 3.3 +/- 1.5 pmol/min/mg of microsomal protein, but there was no significant increase in the level of activity in brain microsomes. Despite this, there was evidence of induction of P-450 c in both the brain and pituitary of BNF-pretreated rats since anti P-450 c antibodies inhibited brain activity by 55% and pituitary activity by 84%. The regional distribution of P-450 b and c in the hypothalamic-preoptic area and olfactory bulbs was examined. The level of ETC O-deethylase activity in the hypothalamic-preoptic area was not different from that in the whole brain, but in the olfactory bulbs activity was higher than that in whole brain, with a range of 0.1-52 pmol/min/mg of microsomal protein. The catalytic activity in the whole brain and in the olfactory bulbs was inhibited by anti P-450b but not by anti P-450c antibodies. Neither estradiol, testosterone, dehydrotestosterone, nor 5 alpha-androstane,3 beta,17 beta-diol (100 microM) competitively inhibited ETC O-deethylase activity, indicating that P-450 b is not responsible for the steroid hydroxylations previously reported in the brain. BNS pretreatment of rats did not cause a consistent increase in ETC O-deethylase upon BNF induction. However, there was an induction of P-450 c in the olfactory bulbs since catalytic activity was inhibited with anti P-450c antibodies.(ABSTRACT TRUNCATED AT 400 WORDS)
用针对肝P-450 b和c制备的多克隆抗体以及灵敏的P-450催化活性荧光测定法(即乙氧基香豆素的O-脱乙基化,ETC),对未处理和经β-萘黄酮(BNF)预处理的大鼠的脑和垂体中细胞色素P-450 b和P-450 c的水平进行了定量评估。在未处理大鼠脑的微粒体部分,ETC生成7-羟基香豆素的速率在0.1至20 pmol/分钟/毫克微粒体蛋白之间,这约为苯巴比妥诱导的大鼠肝微粒体水平的0.01%-2%。这种脑活性被抗P-450 b抗体完全抑制,但不受抗P-450 c抗体影响。与肝P-450 b一样,甲吡酮和氯霉素(100 microM)是催化活性的良好抑制剂,而α-萘黄酮(1 microM)是较差的抑制剂。在未处理大鼠垂体制备的微粒体中未检测到ETC O-脱乙基酶活性。用BNF预处理大鼠后,垂体中ETC O-脱乙基酶活性被诱导至3.3±1.5 pmol/分钟/毫克微粒体蛋白水平,但脑微粒体中的活性水平没有显著增加。尽管如此,有证据表明在BNF预处理大鼠的脑和垂体中均诱导了P-450 c,因为抗P-450 c抗体使脑活性抑制了55%,垂体活性抑制了84%。研究了下丘脑-视前区和嗅球中P-450 b和c的区域分布。下丘脑-视前区的ETC O-脱乙基酶活性水平与全脑无异,但嗅球中的活性高于全脑,范围为0.1-52 pmol/分钟/毫克微粒体蛋白。全脑和嗅球中的催化活性被抗P-450b抗体抑制,但不被抗P-450c抗体抑制。雌二醇、睾酮、脱氢睾酮以及5α-雄甾烷-3β,17β-二醇(100 microM)均未竞争性抑制ETC O-脱乙基酶活性,这表明P-450 b与先前报道的脑中类固醇羟化反应无关。大鼠经BNS预处理后,在BNF诱导时并未导致ETC O-脱乙基酶持续增加。然而,嗅球中诱导了P-450 c,因为催化活性被抗P-450c抗体抑制。(摘要截短于400字)