【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。更多还原

【Abstract】 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.更多还原