CAJ | 학술논문

研究大黄苷元对大鼠体内药物代谢酶 CYP2A6、CYP3A4活性的影响，以预测大黄与临床常用药物的相互作用．大鼠分组，分别灌胃不同质量浓度大黄苷元、质量分数0.5％羧甲基纤维素钠（CMC-Na）、苯巴比妥钠（PB）、地塞米松（DEX）、β-奈黄酮（β-NF）和酮康唑（KET），取各给药组给药后24 h 的肝微粒体（RLM）与 CYP2A6、CYP3A4的探针底物香豆素、睾酮进行体外温孵，通过高效液相色谱法分别测定各底物的代谢产物7-羟基香豆素、6β-羟基睾酮的生成量，考察大黄苷元对 CYP2A6、CYP3A4活性的影响．大黄苷元高、中、低剂量给药组代谢产物7-羟基香豆素的生成量高于空白给药组和 KET 给药组，均有统计学意义（P ＜0.05）、（P ＜0.01），大黄苷元高剂量给药组代谢产物6β-羟基睾酮的生成量高于空白给药组和 KET 给药组，均有统计学意义（P ＜0.05）、（P ＜0.01）．随着大黄苷元给药剂量的增加，7-羟基香豆素、6β-羟基睾酮的生成量均随之增加．大黄苷元对 CYP2A6、CYP3A4均有诱导作用，并且随着大黄苷元剂量的增加，其对 CYP2A6、CYP3A4诱导作用均增强．
연구대황감원대대서체내약물대사매 CYP2A6、CYP3A4활성적영향，이예측대황여림상상용약물적상호작용．대서분조，분별관위불동질량농도대황감원、질량분수0.5％최갑기섬유소납（CMC-Na）、분파비타납（PB）、지새미송（DEX）、β-내황동（β-NF）화동강서（KET），취각급약조급약후24 h 적간미립체（RLM）여 CYP2A6、CYP3A4적탐침저물향두소、고동진행체외온부，통과고효액상색보법분별측정각저물적대사산물7-간기향두소、6β-간기고동적생성량，고찰대황감원대 CYP2A6、CYP3A4활성적영향．대황감원고、중、저제량급약조대사산물7-간기향두소적생성량고우공백급약조화 KET 급약조，균유통계학의의（P ＜0.05）、（P ＜0.01），대황감원고제량급약조대사산물6β-간기고동적생성량고우공백급약조화 KET 급약조，균유통계학의의（P ＜0.05）、（P ＜0.01）．수착대황감원급약제량적증가，7-간기향두소、6β-간기고동적생성량균수지증가．대황감원대 CYP2A6、CYP3A4균유유도작용，병차수착대황감원제량적증가，기대 CYP2A6、CYP3A4유도작용균증강．
To evaluate the anthraquinones from Radix et Rhizoma Rhei impact on CYP3A4 and CYP2A6 activity in rats and to forecast the drug-drug interaction with it.SD rats were randomly grouped, Giving 0.5% sodium carboxymethyl cellulose(CMC-Na)、phenobarbital phenobarbital sodium(PB)、dex-amethasone(DEX)、beta-naphthoflavone(β-NF)、ketocon-azole (KET)and different dosages of Rhubarb aglycone respectively to them.Blending and incubating each dose group liver microsome of 24 after treat-ment with the probe of CYP2A6、CYP3A4.Meanwhile,the production of the two probe were detected by HPLC.The metabolites of Rhubarb aglycone high,medium and low dosage groups were higher than the blank group and KET group,both had statistical significance(P <0.05)、(P <0.01 ),the metabolites generation of rhubarb aglycone high dosage groups was higher than the blank and KET group,both had statistical significance(P <0.05)、(P <0.01),Along with the increasing dosage of rhubarb aglycone,the production of 7-hydroxycoumarin,6β-hydroy testosterone were increased.Both CYP2A6 and CYP3A4 can be induced by rhubarb aglycone,With the increase dosage of rhubarb,its induced function were en-hanced.