The Pharmacokinetics, Bioavailability, and Excretion Studies of α-Cyperone in Rats by UHPLC-QQQ-MS/MS
2025
Ye Shang | Yameng Zhu | Kaili Zhang | Zijing Zhang | Huining Geng | Xueyu Liu | Wenwen Li | Lu Chen | Caixia Li | Yang Liu | Huizi Ouyang | Jun He
&alpha:-Cyperone (C15H22O), a critical bioactive sesquiterpene, serves as a representative chemical compound of Cyperi Rhizoma&mdash:a classical functional food. To investigate the pharmacokinetic characteristics of &alpha:-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 &alpha:-cyperone, which suggested extensive first-pass metabolism. This study provided crucial insight into explaining the in vivo process and promoting the further development of &alpha:-cyperone.
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