Metabolic Profiling of 5‐Methoxypinocembroside and Pharmacokinetics Study of Its Major Metabolite Alpinetin in Rat Plasma by UHPLC–MS
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<sub>max</sub>) of 70.7 ± 44.4 ng/mL, with a peak time (T<sub>max</sub>) of 0.4 ± 0.5 h. The area under the concentration-time curve from zero to the last measurable concentration (AUC<sub>0 - t</sub>) 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.
Authors
- Zhipeng Deng (ORCID: https://orcid.org/0009-0008-7550-2861)
- Qingping Xiong (ORCID: https://orcid.org/0000-0001-5242-4970)
- Xinyi Zhu (ORCID: https://orcid.org/0000-0002-7361-8958)
- Yue Jiang (ORCID: https://orcid.org/0009-0009-7952-6833)
- Miao Hou
Institutions
- Shandong University of Traditional Chinese Medicine (CN)
- Huaiyin Institute of Technology (CN)
Publication Details
- Journal
- Biomedical Chromatography
- Published
- 2025-08-25
- DOI
- https://doi.org/10.1002/bmc.70200
- Primary Topic
- Drug-Induced Hepatotoxicity and Protection
- Type
- article
- Field-Weighted Citation Impact
- 0.00