木犀草素及木犀草苷在大鼠体内的代谢研究

In-vivo Studies on Metabolism of Luteolin and Luteoloside in Rats

目的研究木犀草素和木犀草苷在大鼠体内的代谢转化。方法应用UHPLC-Q-TOF-MS方法研究分别灌胃木犀草素、木犀草苷后大鼠血浆、尿和粪中的代谢产物。结果在木犀草素灌胃大鼠的血浆、尿、粪中共检测到25种代谢产物;在木犀草苷灌胃大鼠的血浆、尿、粪中共检测到20种代谢产物,但未检测到其原型。结论木犀草素在大鼠体内的主要代谢途径为氧化、甲基化、葡糖醛酸化和磺酸化;木犀草苷在大鼠体内的主要代谢途径为脱葡萄糖基反应生成木犀草素素后,再氧化、甲基化、葡糖醛酸化和磺酸化。黄酮苷类化合物口服后易被肠道菌群产生的水解酶代谢为苷元吸收入血。

Objective To investigate the metabolite profile of luteolin and luteoloside in rats. Methods Ultra high performance liquid chromatography combined with triple-quadrupole time-of-fly mass spectrometry（UHPLC-QTOF-MS）was used for the separation and analysis of luteolin and luteoloside as well as their metabolites. Results A total of 25 luteolin metabolites were detectable in the rat plasma,urine and feces. A total of 20 luteoloside metabolites were detectable,but the luteoloside was not found. Conclusion The metabolic pathways of luteolin in rats included oxidation, methylation, glucuronidation and sulphonation. And luteoloside in rats was absolutely hydrolyzed into luteolin,and then experienced re-oxidation,methylation,glucuronidation and sulphonation. The flavone glucosides after oral administration were hydrolyzed into aglycone by the hydrolytic enzyme secreted by intestinal bacteria,and then the aglycone can be absorbed into the blood easily.