CAJ | 학술논문

目的：考察双黄连粉针及其7种主要活性成分对大鼠肝微粒中细胞色素 P450酶(CYP)1A、CYP2D 和CYP3A 酶的体外抑制作用。方法将 CYP1A、CYP2D 和 CYP3A 的探针底物(非那西丁、右美沙芬、咪达唑仑)分别与双黄连粉针及其7种活性成分(黄芩苷、连翘苷、连翘酯苷 A、芦丁、绿原酸、咖啡酸、木樨草苷)在大鼠肝微粒中进行孵育反应，采用高效液相色谱(HPLC)法同时测定3种探针底物的含量，评价底物的代谢率是否被抑制。结果与空白对照组比较，双黄连粉针和黄芩苷对 CYP2D 和 CYP3A 有抑制作用，对 CYP1A 无影响；其他活性成分对三种酶无影响。结论双黄连粉针在与 CYP2D 和 CYP3A 底物合用时可能产生相互作用，黄芩苷可能是这种作用的主要效应物质。
목적：고찰쌍황련분침급기7충주요활성성분대대서간미립중세포색소 P450매(CYP)1A、CYP2D 화CYP3A 매적체외억제작용。방법장 CYP1A、CYP2D 화 CYP3A 적탐침저물(비나서정、우미사분、미체서륜)분별여쌍황련분침급기7충활성성분(황금감、련교감、련교지감 A、호정、록원산、가배산、목서초감)재대서간미립중진행부육반응，채용고효액상색보(HPLC)법동시측정3충탐침저물적함량，평개저물적대사솔시부피억제。결과여공백대조조비교，쌍황련분침화황금감대 CYP2D 화 CYP3A 유억제작용，대 CYP1A 무영향；기타활성성분대삼충매무영향。결론쌍황련분침재여 CYP2D 화 CYP3A 저물합용시가능산생상호작용，황금감가능시저충작용적주요효응물질。
Objective To evaluate the inhibition effects of shuanghuanglian injection powder and its active components on the activities of CYP1A,CYP 2D and CYP 3A in rats liver microsomes. Methods Three probe substrates including phenacetin for CYP1A,dextromethorphan for CYP2D and midazolam for CYP3A were incubated with shuanghuanglian injection powder and the active components (baicalin,phillyrin,forsythiaside A,lutin,chlorogenic acid,coffeic acid and lutiolin) in rat liver microsomes. Contents of three probe substrates were simultaneously determined by HPLC to evaluate the metabolic rates. Results Shuanghuanglian injection powder and baicalin inhibited the activities of CYP2D and CYP 3A, but didn 't affect CYP1A. The other active components showed no effect on CYP1A,CYP2D and CYP3A. Conclusion Drug-drug interactions may occur when combining shuanghuanglian powder injection with CYP2D and CYP 3A substrates and baicalin may be the effector substance responsible for the interactions.