摘要
为了阐明赤芍化学成分没食子酸丙酯在大鼠体内的代谢情况,归属赤芍代谢产物的原型成分来源,该研究首次对没食子酸丙酯进行了动物体内代谢研究。灌胃给予大鼠没食子酸丙酯混悬液,收集尿液和血液,采用液质联用技术检测、鉴定没食子酸丙酯在大鼠体内的代谢产物。通过对比没食子酸丙酯和赤芍代谢产物的液质数据,归属赤芍代谢产物的来源。最终从大鼠含药尿液中鉴定没食子酸丙酯代谢产物33个,从大鼠含药血浆中鉴定没食子酸丙酯代谢产物20个,除去相同的代谢产物,共从大鼠的含药尿液和血浆中鉴定代谢产物37个,其中17个代谢产物和赤芍的代谢产物相同。它们主要为没食子酸丙酯、没食子酸丙二醇酯、没食子酸和焦没食子酸的二相结合产物。37个代谢产物中35个为没食子酸丙酯的新代谢产物,推测22个为新化合物。本研究明确了赤芍的代谢产物中有17个可以来自于没食子酸丙酯,为阐明赤芍代谢产物的来源及没食子酸丙酯在体内的代谢途径奠定基础,并有助于寻找没食子酸丙酯在体内的显效形式。
To make a clear understanding of the in vivo metabolism of propyl gallate in rats and determine the original com- pounds of the metabolites of Paeoniae Radix Rubra （PRR） , the urine and plasma of the rats administrated with propyl gallate were col- lected, and then the HPLC-DAD-ESI-IT-TOF-MS technique was applied to screen and identify the metabolites of propyl gallate from these hio-samples. By comparing the collected LC-MS data, the origin of the metabolites of PRR were confirmed. Finally, 33 metabo- lites of propyl gallate were identified from urine sample, and 20 metabolites of propyl gallate were identified from the plasma sample. In total, 37 metabolites of propyl gallate were identified, and 17 of them were identical to the metabolites of PRR. They are mainly the phase II metabolites of propyl gallate, 3-hydroxypropyl 3,4,5-trihydroxybenzoate, gallic acid and pyrogallol. Phase I reactions （ decar- boxylation, hydroxylation） and phase II reactions （sulfation, glucuronidation and methylation） were observed as the main metabolic pathways of propyl gallate. In this research, the in vivo metabolism of proply gallate was reported for the first time and 37 metabolites were identified, among which 35 were new metabolites of propyl gallate, and 20 were new compounds. The results demonstrated that 17 metabolites of PRR can be formed from propyl gallate. This will enhance our understanding of the metabolism and Effective forms （ the truly active structures） of propyl gallate and PRR.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2013年第22期3970-3976,共7页
China Journal of Chinese Materia Medica
基金
国家自然科学基金重点项目(30830120)
中国博士后科学基金项目(20080430293)
作者简介
梁静，博士，主要从事天然药物的体内代谢研究，E-mail：ljing@bjmu．edu．cn
