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  • P-ISSN 2233-4203
  • E-ISSN 2093-8950

Effect of Ginsenoside Rc on the Pharmacokinetics of Mycophenolic Acid, a UGT1A9 Substrate, and its Glucuronide Metabolite in Rats

Mass Spectrometry Letters / Mass Spectrometry Letters, (P)2233-4203; (E)2093-8950
2021, v.12 no.2, pp.53-58
Park So-Young (Kyungpook National University)
Jeon Ji-Hyeon (Kyungpook National University)
Jang Su-Nyeong (Kyungpook National University)
Song Im-Sook (Kyungpook National University)
Liu Kwang-Hyeon (Kyungpook National University)
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Previous in vitro studies have demonstrated that ginsenoside Rc inhibits UGT1A9, but there are no available data to indicate that ginsenoside Rc inhibits UGT1A9 in vivo. The effect of single and repeated intravenous injection of ginsenoside Rc was evaluated on the pharmacokinetics of mycophenolic acid. After injection of ginsenoside Rc (5 mg/kg for one day or 3 mg/kg for five days), 2-mg mycophenolic acid was intravenously injected, and the pharmacokinetics of mycophenolic acid and mycophenolic acid-β-glucuronide were determined. Concentrations of mycophenolic acid and its metabolite from rat plasma were analyzed using a liquid chromatography-triple quadrupole mass spectrometry. Single or repeated pretreatment with ginse-noside Rc had no significant effects on the pharmacokinetics of mycophenolic acid (P > 0.05): The mean difference in maximum plasma concentration (C max ) and area under the concentration-time curve (AUC inf ) were within 0.83- and 0.62-fold, respectively, compared with those in the absence of the ginsenoside Rc. These results indicate that ginsenoside Rc has a negligible effect on the disposition of mycophenolic acid in vivo despite in vitro findings indicating that ginsenoside Rc is a selective UGT1A9 inhibitor. As a result, ginsenoside Rc has little possibility of interacting with drugs that are metabolized by UGT1A9, including mycophenolic acid.

Ginsenoside Rc, herb-drug interaction, mycophenolic acid, UGT1A9, uridine 5’-diphosphoglucuronosyltransferase

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Mass Spectrometry Letters