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Metabolism study of hesperetin and hesperidin in rats by UHPLC-LTQ-Orbitrap MS n.
Xenobiotica ( IF 1.8 ) Pub Date : 2020-08-12 , DOI: 10.1080/00498254.2019.1567956
Qishu Jiao 1 , Lulu Xu 1 , Lijuan Jiang 1 , Yanyan Jiang 1 , Jiayu Zhang 2 , Bin Liu 1
Affiliation  

  1. Hesperidin (HPD) and hesperetin (HPT), as a kind of flavonone compounds, are abundant in citrus fruits with various pharmacological effects. HPD and HPT are not always consistent in some biological activities, even if they have the same skeletal structure.

  2. The aim of this study was to screen and identify HPT and HPD metabolites in rats using UHPLC-LTQ-Orbitrap MS n , compare the possible metabolism and provide the research basis for further understanding the similarities and differences in pharmacodynamics and pharmacokinetics of HPT and HPD.

  3. A total of 17 and 52 metabolites were identified in rats after oral administration of HPT or HPD, respectively.

  4. 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.

  5. 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.



中文翻译:

UHPLC-LTQ-Orbitrap MS n对大鼠中橙皮苷和橙皮苷的代谢研究。

  1. 橙皮素(HPD)和橙皮素(HPT)作为一种黄酮类化合物,在柑橘类水果中含量丰富,具有多种药理作用。HPD和HPT在某些生物学活动中并不总是一致的,即使它们具有相同的骨骼结构。

  2. 这项研究的目的是使用UHPLC-LTQ-Orbitrap MS n筛选和鉴定大鼠中的HPT和HPD代谢物,比较可能的代谢,并为进一步了解HPT和HPD的药效学和药代动力学的异同提供研究依据。

  3. 口服HPT或HPD后,在大鼠中总共鉴定出17种和52种代谢物。

  4. HPT和HPD代谢物中的三种,即HPT的葡糖醛酸化,硫酸化和葡糖醛酸化,是相同的,并且可能是它们具有相同药效作用的活性成分。

  5. 我们可以在HPD组的尿液样本中找到原型,但在HPT组的任何样本中都找不到原型。几乎没有HPT的一般I期代谢产物,而可以鉴定出33种HPD I期代谢产物。这些数据表明,与HPT相比,HPD的生物利用度较差。

更新日期:2020-09-15
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