Jiao Qishu, Xu Lulu, Jiang Lijuan, Jiang Yanyan, Zhang Jiayu, Liu Bin
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing, China.
Beijing Research Institution of Chinese Medicine, Beijing University of Chinese Medicine, Beijing, China.
Xenobiotica. 2020 Nov;50(11):1311-1322. doi: 10.1080/00498254.2019.1567956. Epub 2020 Aug 12.
Hesperidin (HPD) and hesperetin (HPT), as a kind of flavonone compounds, are abundant in fruits with various pharmacological effects. HPD and HPT are not always consistent in some biological activities, even if they have the same skeletal structure. The aim of this study was to screen and identify HPT and HPD metabolites in rats using UHPLC-LTQ-Orbitrap MS , compare the possible metabolism and provide the research basis for further understanding the similarities and differences in pharmacodynamics and pharmacokinetics of HPT and HPD. A total of 17 and 52 metabolites were identified in rats after oral administration of HPT or HPD, respectively. Three of HPT and HPD metabolites, glucuronidation, sulfation and diglucuronidation of HPT, were the same and could be the active components for the same pharmacodynamic action of them. We could find prototype in the urine sample of HPD group, but no prototypes in any samples of HPT group. There were hardly any general phase I metabolites of HPT, while 33 phase I metabolites of HPD could be identified. These data suggested that the poorer bioavailability of HPD compared with HPT.
橙皮苷（HPD）和橙皮素（HPT）作为一种黄酮酮类化合物，在水果中含量丰富，具有多种药理作用。尽管HPD和HPT具有相同的骨架结构，但它们在某些生物活性方面并不总是一致的。本研究旨在利用超高效液相色谱-线性离子阱-轨道阱质谱（UHPLC-LTQ-Orbitrap MS）筛选和鉴定大鼠体内的HPT和HPD代谢产物，比较其可能的代谢情况，并为进一步了解HPT和HPD在药效学和药代动力学方面的异同提供研究依据。口服HPT或HPD后，分别在大鼠体内鉴定出17种和52种代谢产物。HPT和HPD的三种代谢产物，即HPT的葡萄糖醛酸化、硫酸化和二葡萄糖醛酸化，是相同的，可能是它们相同药效学作用的活性成分。在HPD组的尿液样本中可以发现原型，但在HPT组的任何样本中均未发现原型。HPT几乎没有任何I相代谢产物，而HPD可鉴定出33种I相代谢产物。这些数据表明，与HPT相比，HPD的生物利用度较差。
