中国药房2017，Vol.28Issue(10)：1310-1315,6.DOI:10.6039/j.issn.1001-0408.2017.10.04
哈巴苷在大鼠体内代谢产物的鉴定与分析
Identification and Analysis of Harpagide Metabolites in Rats in vivo
摘要
Abstract
OBJECTIVE:To study the metabolites,distribution,metabolic type and the possible activity of harpagide which is the active component from Scrophularia ningpoensis in rats in vivo. METHODS:4 SD rats were divided into blank group (ul-tra-pure water) and administration group (harpagide reference solution),2 in each group,ig,160 mg/kg,twice a day,for 3 d. Urine and feces were collected every 12 h before administration and the first administration;sample blood 8 mL was taken after 0.5,1 h of last administration;heart,liver,spleen,lung,kidney,stomach and small intestine were taken. The blood,urine,fe-ces and other tissue solutions were prepared,HPLC-MS was conducted to detect and identify the harpagide metabolites in rats in vi-vo and presume metabolic pathways,and PharmMapper software was used to predict metabolites activity. RESULTS:12 harpagide metabolites were identified in rats in vivo,the form of prototypes and metabolites were distributed in heart,liver,spleen,lung, kidney,stomach and small intestine. The metabolic type mainly included hydrolysis,dehydration,reduction,methylation,sul-fation,glucuronic acid binding,grade A coumaric acid binding,etc. The 12 compounds may have activities in the treatment of epi-lepsy,amyotrophic lateral sclerosis,diabetes,stroke,etc. CONCLUSIONS:Harpagide may be effective in the form of prototypes and metabolites. The study has provided basis for attributing the origins of metabolite,studying the effective form of S. ningpoensis clarifying its pharmacological mechanism and processing mechanism.关键词
玄参/哈巴苷/液质联用/代谢产物/代谢途径/活性Key words
Scrophularia ningpoensis/Harpagide/LC-MS/Metabolite/Metabolic pathway/Activity分类
医药卫生引用本文复制引用
刘震,徐风,王静哲,刘广学,尚明英,蔡少青..哈巴苷在大鼠体内代谢产物的鉴定与分析[J].中国药房,2017,28(10):1310-1315,6.基金项目
国家自然科学基金资助项目(No.81274074) （No.81274074）
