Absorption, metabolism, and pharmacokinetic profile of xanthohumol in rats as determined via UPLC-MS/MS

IF 1.7 4区医学 Q3 PHARMACOLOGY & PHARMACY

Biopharmaceutics & Drug Disposition Pub Date : 2021-12-16 DOI:10.1002/bdd.2306

Huan-Huan Bai, Tian-Shuang Xia, Yi-Ping Jiang, Wu-Mu Xu, Ping-Cui Xu, Na-Ni Wang, Xiao-Jun Gou, Hai-Liang Xin

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引用次数: 1

Abstract

Xanthohumol, a natural isoflavone from Humulus lupulus L., possesses biological activities. However, the biological fate of xanthohumol in vivo remains unclear. The aim of this study was to investigate the absorption and metabolism of xanthohumol in rats through UPLC-MS/MS. The plasma, urine and fecal samples were collected after oral administration of xanthohumol (25, 50, 100 mg/kg) in SD rats. The contents of xanthohumol and its metabolites were determined by UPLC-MS/MS. A total of 6 metabolites of xanthohumol were identified in rats, including methylated, glucuronidated, acid-catalyzed cyclization and oxidation, indicating xanthohumol underwent phase I and II metabolism. Besides, isoxanthohumol was the major metabolites of xanthohumol. Xanthohumol was rapidly absorbed, metabolized, and eliminated in rats. The pharmacokinetics results showed the T_max of xanthohumol and isoxanthohumol were 3 and 2.33 h, respectively. The AUC_0−t of xanthohumol and isoxanthohumol were 138.83 ± 6.03 and 38.77 ± 4.46 ng/ml·h, respectively. Furthermore, xanthohumol was mainly excreted in the form of prototype through feces and a small amount of xanthohumol was excreted through urine. These results illustrated the absorption, metabolism, and pharmacokinetics process of xanthohumol in rats, and provided a reference for the further rational applications.

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用UPLC-MS/MS测定黄腐酚在大鼠体内的吸收、代谢和药动学特征

黄腐酚是一种从葎草中提取的天然异黄酮，具有一定的生物活性。然而，黄腐酚在体内的生物学命运仍不清楚。本研究采用超高效液相色谱-质谱联用技术研究黄腐酚在大鼠体内的吸收和代谢。分别给药25、50、100 mg/kg黄腐酚后采集SD大鼠血浆、尿液和粪便样本。采用UPLC-MS/MS法测定黄腐酚及其代谢物的含量。黄腐酚在大鼠体内共鉴定出6种代谢产物，包括甲基化、葡萄糖醛酸化、酸催化环化和氧化，表明黄腐酚经历了I期和II期代谢。此外，异黄腐酚是黄腐酚的主要代谢产物。黄腐酚在大鼠体内被迅速吸收、代谢和消除。药动学结果显示，黄腐酚和异黄腐酚的Tmax分别为3 h和2.33 h。黄腐酚和异黄腐酚的AUC0−t分别为138.83±6.03和38.77±4.46 ng/ml·h。黄腐酚主要以原型形式通过粪便排出，少量黄腐酚通过尿液排出。这些结果说明了黄腐酚在大鼠体内的吸收、代谢和药代动力学过程，为其进一步合理应用提供了参考。

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来源期刊

Biopharmaceutics & Drug Disposition 医学-药学

CiteScore

3.60

自引率

0.00%

发文量

审稿时长

6-12 weeks

期刊介绍： Biopharmaceutics & Drug Dispositionpublishes original review articles, short communications, and reports in biopharmaceutics, drug disposition, pharmacokinetics and pharmacodynamics, especially those that have a direct relation to the drug discovery/development and the therapeutic use of drugs. These includes: - animal and human pharmacological studies that focus on therapeutic response. pharmacodynamics, and toxicity related to plasma and tissue concentrations of drugs and their metabolites, - in vitro and in vivo drug absorption, distribution, metabolism, transport, and excretion studies that facilitate investigations related to the use of drugs in man - studies on membrane transport and enzymes, including their regulation and the impact of pharmacogenomics on drug absorption and disposition, - simulation and modeling in drug discovery and development - theoretical treatises - includes themed issues and reviews and exclude manuscripts on - bioavailability studies reporting only on simple PK parameters such as Cmax, tmax and t1/2 without mechanistic interpretation - analytical methods