Metabolic Profiling of 5-Methoxypinocembroside and Pharmacokinetics Study of Its Major Metabolite Alpinetin in Rat Plasma by UHPLC–MS

IF 1.7 4区医学 Q4 BIOCHEMICAL RESEARCH METHODS

Biomedical Chromatography Pub Date : 2025-08-25 DOI:10.1002/bmc.70200

Yue Jiang, Qingping Xiong, Xinyi Zhu, Miao Hou, Zhipeng Deng

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Abstract

5-Methoxypinocembroside (5-MP), a key bioactive compound isolated from Penthrum chinense Pursh (PCP), has demonstrated a specific pharmacological effect against hepatic steatosis. However, its metabolism and pharmacokinetics remain unexplored. In this study, rats were administered 5-MP intragastrically at a dose of 25 mg/kg, and blood samples were collected and processed for analysis. Ultra-high-performance liquid chromatography–mass spectrometry (UHPLC–MS) was employed to identify plasma metabolites of 5-MP, and its pharmacokinetics in rats were further evaluated. A total of 20 metabolites were characterized, including those formed via demethylation, sulfation, and deglycosylation. Among these, the aglycone alpinetin (ALP) was identified as the predominant metabolite of 5-MP. The pharmacokinetic analysis of ALP revealed a maximum plasma concentration (C_max) of 70.7 ± 44.4 ng/mL, with a peak time (T_max) of 0.4 ± 0.5 h. The area under the concentration–time curve from zero to the last measurable concentration (AUC_0 − t) was 266.7 ± 146.2 μg/L·h. This study is the first to elucidate the metabolic profile of 5-MP in rats and to characterize the pharmacokinetics of ALP as its primary metabolite.

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用UHPLC-MS研究5-甲氧基葡萄皂苷在大鼠血浆中的代谢特征及其主要代谢物高松素的药动学

5- methoxypinoembroside （5-MP）是从五香草（PCP）中分离得到的一种重要的生物活性化合物，对肝脏脂肪变性具有特殊的药理作用。然而，其代谢和药代动力学仍未被研究。在本研究中，大鼠以25 mg/kg的剂量灌胃5-MP，并采集血样进行分析。采用超高效液相色谱-质谱法（UHPLC-MS）鉴定5-MP的血浆代谢产物，并进一步评价其在大鼠体内的药代动力学。总共鉴定了20种代谢物，包括通过去甲基化、磺化和去糖基化形成的代谢物。其中，糖苷高松素（ALP）被确定为5-MP的主要代谢物。药代动力学分析显示ALP的最大血药浓度（Cmax）为70.7±44.4 ng/mL，峰值时间（Tmax）为0.4±0.5 h。从0到最后可测浓度（AUC0−t），浓度-时间曲线下面积为266.7±146.2 μg/L·h。本研究首次阐明了5-MP在大鼠体内的代谢特征，并描述了ALP作为其主要代谢物的药代动力学特征。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Biomedical Chromatography 生物-分析化学

CiteScore

3.60

自引率

5.60%

发文量

268

审稿时长

2.3 months

期刊介绍： Biomedical Chromatography is devoted to the publication of original papers on the applications of chromatography and allied techniques in the biological and medical sciences. Research papers and review articles cover the methods and techniques relevant to the separation, identification and determination of substances in biochemistry, biotechnology, molecular biology, cell biology, clinical chemistry, pharmacology and related disciplines. These include the analysis of body fluids, cells and tissues, purification of biologically important compounds, pharmaco-kinetics and sequencing methods using HPLC, GC, HPLC-MS, TLC, paper chromatography, affinity chromatography, gel filtration, electrophoresis and related techniques.