大鼠肝微粒体CYP2B1的活性和P450含量的变化  

Changes of the CYP2B1 activity and the cytochome P450 content in rat liver microsomes

作　　者：严敏芬[1] 郝福荣[1] 许立明[1] 童顺高[1] 季华钧[1] 沈芝芬[1] 金一尊[1] 

机构地区：[1]复旦大学放射医学研究所,上海200032

出　　处：《复旦学报（医学版）》2006年第4期513-516,共4页Fudan University Journal of Medical Sciences

摘　　要：目的研究3种诱导[地塞米松(Dexamethasone,DEX)、苯巴比妥钠(Phenobarbital sodium,PB)、β-奈黄酮(-βnaphthoflavone,-βNF)]和丝裂霉素C(Mitomycin,MMC)对雄性SD大鼠细胞色素P450含量、CYP2B1活性的影响,以及普罗地芬(Proadifen,SKF525A)对不同活性CYP2B1的抑制作用。方法连续3d给大鼠腹腔注射各种诱导剂和MMC,另设空白对照和溶剂对照,处理结束后制备肝微粒体,测P450含量和CYP2B1活性;取各诱导组微粒体,用1.25mmol/L SKF525A处理,测CYP2B1活性。结果PB作用后使P450含量上升(P<0.05),CYP2B1活性明显增大(P<0.01);DEX、β-NF、MMC作用后,P450含量、CYP2B1活性变化无统计意义(P>0.05),但与空白对照组相比,-βNF组的CYP2B1活性增加显著(P<0.05);用SKF525A处理不同组别的微粒体后,CYP2B1活性均下降(P<0.05或P<0.01)。结论在体内一定条件下,PB能够诱导P450含量、CYP2B1活性,而DEX、β-NF、MMC对它们的作用不显著;1.25mmol/L的SKF525A在体外能够抑制不同水平的CYP2B1活性。Purpose To study the changes of the cytochrome P450 content and the CYP2B1 activity in male SD rats by inducers（DEX, PB or β-NF） or MMC in vivo and the inhibitive effect of the CYP2B1 activity by SKF525A in vitro. Methods The rats were treated with one of inducers or MMC respectively for 3 days. Biological measurements of the experimental groups were compared to blank group and solvent control group. The hepatic microsomes from induced rats were treated by 1.25 mmol/L SKF525A,and CYP2B1 activity was determined. Results In vivo,PB injected to rats intraperitoneally increased the content of cytochrome P450（P〈0.05） and the activity of CYP2B1（P〈0.01）. For the goup injected with DEX, β-NF, MMC, no significant changes were found in the P450 content and the CYP2B1 activity（P〉0.05）,whearas the CYP2B1 activity increased compared with the blank group by β-NF（P〈0.05） ; In vitro,SKF525A decreased the activity of CYP2B1 in different groups. Conclusions In vivo,PB induced the P450 content and CYP2B1 activity,but DEX,β-NF or MMC showed no significant effect; SKF525A of 1.25 mmol/L could inhibit the CYP2B1 activity in vitro.

关 键 词：细胞色素P450 CYP281 丝裂霉素C 苯巴比妥钠 地塞米松 β-奈黄酮 普罗地芬 

分 类 号：R730[医药卫生—肿瘤]