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1、第23卷第1期廣 東 藥 學(xué) 院 學(xué) 報(bào)Vol.23No.1
2007年2月JOURNALOFGUANGDONGCOLLEGEOFPHARMACYFeb.2007雷諾嗪對(duì)大鼠肝微粒體蛋白質(zhì)及細(xì)胞色素P450的影響葉亞琳,張貞良,曹 洋,金 星(解放軍第421醫(yī)院藥劑科,廣東廣州510318)摘要:目的研究雷諾嗪對(duì)大鼠肝重、肝微粒體蛋白質(zhì)及細(xì)胞色素P450含量的影響。方法將大鼠分成空白對(duì)照組和雷諾嗪組各8只,雷諾嗪組連續(xù)給予雷諾嗪為50mg·kg-1·d-1,連續(xù)灌胃給藥7d后,測(cè)定大鼠的肝重、肝微粒體蛋白質(zhì)及細(xì)胞色素P450含量,氨基比林2N2脫甲基酶、紅霉素脫甲基轉(zhuǎn)
2、移酶和72乙氧基232異吩噁唑酮脫烴酶的活性。結(jié)果雷諾嗪灌胃7d后,大鼠肝重、肝微粒體蛋白含量與對(duì)照組比較差異無(wú)顯著性;雷諾嗪組肝微粒體細(xì)胞色素P450含量與對(duì)照組比較明顯減少(P<
0.01)。雷諾嗪對(duì)大鼠肝微粒體中紅霉素脫甲基酶和72乙氧基232異吩噁唑酮脫烴酶的活性基本無(wú)影響,對(duì)氨基比林2N2脫甲基酶有明顯的抑制作用(P<0.05)。結(jié)論雷諾嗪可能引起肝藥酶對(duì)某些藥物代謝的改變。關(guān)鍵詞:雷諾嗪;肝重;肝微粒體蛋白質(zhì);細(xì)胞色素P450;大鼠中圖分類(lèi)號(hào):R965 文獻(xiàn)標(biāo)識(shí)碼:A 文章編號(hào):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 雷諾嗪(ranolazine)是由美國(guó)CVTherapeutics分別占P450總量的13%、4%、0.4%、20%、1～[3]。其中,CYP2E1不僅參與藥物的公司最新開(kāi)發(fā)研制的部分脂肪酸氧化(pFOX)抑制2%、7
