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1、第23卷第1期广 东 药 学 院 学 报Vol.23No.1
2007年2月JOURNALOFGUANGDONGCOLLEGEOFPHARMACYFeb.2007雷诺嗪对大鼠肝微粒体蛋白质及细胞色素P450的影响叶亚琳,张贞良,曹 洋,金 星(解放军第421医院药剂科,广东广州510318)摘要:目的研究雷诺嗪对大鼠肝重、肝微粒体蛋白质及细胞色素P450含量的影响。方法将大鼠分成空白对照组和雷诺嗪组各8只,雷诺嗪组连续给予雷诺嗪为50mg·kg-1·d-1,连续灌胃给药7d后,测定大鼠的肝重、肝微粒体蛋白质及细胞色素P450含量,氨基比林2N2脱甲基酶、红霉素脱甲基转
2、移酶和72乙氧基232异吩噁唑酮脱烃酶的活性。结果雷诺嗪灌胃7d后,大鼠肝重、肝微粒体蛋白含量与对照组比较差异无显著性;雷诺嗪组肝微粒体细胞色素P450含量与对照组比较明显减少(P<
0.01)。雷诺嗪对大鼠肝微粒体中红霉素脱甲基酶和72乙氧基232异吩噁唑酮脱烃酶的活性基本无影响,对氨基比林2N2脱甲基酶有明显的抑制作用(P<0.05)。结论雷诺嗪可能引起肝药酶对某些药物代谢的改变。关键词:雷诺嗪;肝重;肝微粒体蛋白质;细胞色素P450;大鼠中图分类号:R965 文献标识码:A 文章编号:1006-8783(2007)02-0053-03EffectsofRanol
3、azineOnliverWeight,ContentofMicrosomalProtein,andCytochromeP450ofRatsYEYa2lin,ZHANGZhen2liang,CAOYang,JINXing(No.421HospitalofPLA,Guangzhou,Guangdong510318,China)Abstract:ObjectiveTostudytheeffectsofranolazineonliverweight,contentsofmicrosomalproteinandcytochromeP450,the
activitiesofami
4、nopyrine2N2demethylase,erythromycin2N2demethylaseandcoumarin72hydroxylationofrats.MethodsRatsweredividedintotwogroups.Oneiscontrolgroup,anotherisdosagegroup.Afteradministeredwithanoraldoseofranolazine50mg·kg-1oncedailyfor7days,thelivermicrosomesofratswasdistilledbydifferentvelocitycentr
5、ifugation.AUVmethodwasusedtodetectcontentofcytochromeP450inlivermicrosomes,andtheactivitiesofsomeCYP450ofratswerestudiedbyspectrophotometer.ResultsThestudyshowedthatliverweightandcontentofcytochromeP450inhepaticmicrosomesofratsdecreasedsignificantly,differencesbetweendosegroupandcontrol
6、groupwerestatisticallysignificant(P<0.01).Theactivitiesofranolazinecanalsosignificantlysuppress
theactivityofaminopyrine2N2demethylase(P<0.05),butcannotsuppresstheactivityoferythromycin2N2demethylaseandcoumarin72hydroxylationsignificantly.ConclusionEffectsofranolazineonliverweightandcyt
7、ochromeP450ofratscouldresultinalterationofmetabolismofsomedrugsaffectedbyliverdrugmetabolicenzymeactivity.Keywords:ranolazine;contentofmicrosomalprotein;cytochromeP450 雷诺嗪(ranolazine)是由美国CVTherapeutics分别占P450总量的13%、4%、0.4%、20%、1～[3]。其中,CYP2E1不仅参与药物的公司最新开发研制的部分脂肪酸氧化(pFOX)抑制2%、7
