The Pharmacokinetics, Bioavailability, and Excretion Studies of α-Cyperone in Rats by UHPLC-QQQ-MS/MS
<i>α</i>-Cyperone (C<sub>15</sub>H<sub>22</sub>O), a critical bioactive sesquiterpene, serves as a representative chemical compound of <i>Cyperi Rhizoma</i>-a classical functional food. To investigate the pharmacokinetic characteristics of α-cyperone, a quantified method was developed in plasma, bile, urine, and feces by ultra-high-performance liquid chromatography tandem triple quadrupole mass spectrometry (UHPLC-QQQ-MS/MS). After being validated, the developed method was applied in a plasma pharmacokinetic study as well as biliary, urinary, and fecal excretion kinetics studies. It revealed poor absolute bioavailability (F = 1.36%) and rare excretion (total cumulative excretion = 0.022%) of α-cyperone, which suggested extensive first-pass metabolism. This study provided crucial insight into explaining the in vivo process and promoting the further development of α-cyperone.
Authors
- Yameng Zhu (ORCID: https://orcid.org/0000-0002-8735-165X)
- Jun He (ORCID: https://orcid.org/0000-0002-3781-9234)
- Ye Shang (ORCID: https://orcid.org/0000-0002-4250-128X)
- Xueyu Liu (ORCID: https://orcid.org/0000-0001-5745-4722)
- Wenwen Li (ORCID: https://orcid.org/0000-0001-7698-2846)
- Yang Liu (ORCID: https://orcid.org/0000-0001-5908-4278)
- Caixia Li (ORCID: https://orcid.org/0000-0003-0382-6169)
- Kaili Zhang (ORCID: https://orcid.org/0000-0002-5150-2372)
- Huizi Ouyang (ORCID: https://orcid.org/0000-0001-7742-124X)
- Zijing Zhang (ORCID: https://orcid.org/0000-0002-3990-1442)
- Lu Chen (ORCID: https://orcid.org/0009-0004-7877-8274)
- Haoran Geng (ORCID: https://orcid.org/0000-0001-5115-4446)
Institutions
- Tianjin University of Traditional Chinese Medicine (CN)
Publication Details
- Journal
- Molecules
- Published
- 2025-09-26
- DOI
- https://doi.org/10.3390/molecules30193899
- Citations
- 1
- Primary Topic
- Pharmacological Effects of Natural Compounds
- Type
- article
- Field-Weighted Citation Impact
- 1.56
Funders
- National Natural Science Foundation of China
- Tianjin University