【摘要】 目的:分析二苯乙烯苷在大鼠体内的代谢产物并推测代谢途径。方法:将雄性SD大鼠随机分为血浆组(n=3)、尿液组(n=3)、胆汁组(n=3)和组织组(n=9),各组大鼠均单次灌胃二苯乙烯苷200 mg/kg,分别收集给药后10、30 min和1、1.5、2、4 h的血浆,给药后0～6 h的尿液,给药后0～4 h的胆汁以及给药后30 min和1、2 h(每个时间点3只)的心、肝、脾、肺、肾、胃组织样品,经甲醇沉淀蛋白后,采用超高效液相色谱-四极杆-静电场轨道阱高分辨质谱联用技术和质量亏损过滤技术联合分析、鉴定各样本中的代谢产物,推测代谢途径。结果:从血浆、尿液、胆汁、心、肝、脾、肺、肾、胃样品中分别检出6、7、11、1、5、1、3、4、4个代谢产物,包括Ⅰ相代谢(如水解、加氢、羟化)产物2个、Ⅱ相代谢(如葡萄糖醛酸结合和硫酸化)产物18个,其中葡萄糖醛酸结合产物有12个。结论:二苯乙烯苷在胆汁中的代谢产物种类居多,以Ⅱ相代谢产物二苯乙烯苷的葡萄糖醛酸结合产物为主;代谢途径主要涉及葡萄糖水解、加氢、羟化、葡萄糖醛酸结合、硫酸化反应等。更多还原

【Abstract】 OBJECTIVE:To analyze the metabolites of tetrahydroxystilbene glucoside(THSG) and speculate its metabolism pathway in rats. METHODS:Male SD rats were randomly divided into plasma group(n=3),urine group(n=3),bile group(n=3),and tissue group(n=9). Each group was given single dose of THSG 200 mg/kg intragastrically. Plasma samples 10,30 min and 1,1.5,2,4 h after medication,the unrine 0-6 h after medication,the bile 0-4 h after medication,the tissue of heart,liver,spleen,lung,kidney and stomach 30 min and 1,2 h after medication(3 at each time point) were collected respectively.After precipitated with methanol,the metabolites of samples were analyzed and identified by UHPLC-Q-Exactive Orbitrap MS and mass loss filtration(MDF). Its metabolism pathway was speculated. RESULTS:In the blood,urine,bile,heart,liver,spleen,lung,kidney,stomach samples,6,7,11,1,5,1,3,4,4 metabolites were detected,including two phase Ⅰ (hydrolysis,hydrogenation and hydroxylation) metabolites,18 phase Ⅱ (glucuronic acid binding and sulfation) metabolites. There were 12 glucuronic acid binding products. CONCLUSIONS:Most of the metabolites of THSG are found in bile,mainly glucuronic acid binding products of phase Ⅱ metabolite THSG; main metabolic pathways involve glucose hydrolysis, hydrogenation,hydroxylation,glucuronic acid binding and sulfation.更多还原