• P-ISSN2233-4203
  • E-ISSN2093-8950

Article Detail

Home > Article Detail
  • P-ISSN 2233-4203
  • E-ISSN 2093-8950

Inhibitory Effects of 12 Ginsenosides on the Activities of Seven Cytochromes P450 in Human Liver Microsomes

Mass Spectrometry Letters, (P)2233-4203; (E)2093-8950
2016, v.7 no.4, pp.106-110
https://doi.org/10.5478/MSL.2016.7.4.106
Jo Jung Jae (Kyungpook National University)
Shrestha Riya (Kyungpook National University)
Lee Sangkyu (Kyungpook National University)
  • Downloaded
  • Viewed

Abstract

Ginseng, a traditional herbal drug, has been used in Eastern Asia for more than 2000 years. Various ginsenosides, which are the major bioactive components of ginseng products, have been shown to exert numerous beneficial effects on the human body when co-administered with drugs. However, this may give rise to ginsenoside-drug interactions, which is an important research consideration. In this study, acassette assay was performed the inhibitory effects of 12 ginsenosides on seven cytochrome P450 (CYP) isoforms in human liver microsomes (HLMs) using LC-MS/MS to predict the herb-drug interaction. After incubation of the 12 ginsenosides with seven cocktail CYP probes, the generated specific metabolites were quantified by LC-MS/MS to determine their activities. Ginsenoside Rb1 and F2 showed strong selective inhibitory effect on CYP2C9-catalyzed diclofenac 4′-hydroxylation and CYP2B6-catalyzed bupropion hydroxylation, respectively. Ginsenosides Rd showed weak inhibitory effect on the activities of CYP2B6, 2C9, 2C19, 2D6, 3A4, and compound K, while ginsenoside Rg3 showed weak inhibitory effects on CYP2B6. Other ginsenosides, Rc, Rf, Rg1, Rh1, Rf, and Re did not show significant inhibitory effects on the activities of the seven CYPs in HLM. Owing to the poor absorption of ginsenosides after oral administration in vivo, ginsenosides may not have significant side effects caused by interaction with other drugs.

keywords
cytochrome P450 ginsenoside F2 drug-drug interaction LC-MS/MS multiple reaction monitoring


Reference

1

Ahmed, T.. (2016). . Brain Res. Bull, 125, 30-.

2

Chang, T. K.. (2002). . Drug Metab. Dispos, 30, 378-.

3

Chen, X. J.. (2016). . Evid-Based Compl. Alt, , 5738694-.

4

Cheng, Y.. (2005). . Acta. Pharmacol. Sin, 26, 143-.

5

Ha, K. C.. (2012). . BMC Complem. Altern. M, 12, 10-.

6

Han, M.. (2006). . Acta. Pharmacol. Sin, 27, 499-.

7

He, N.. (2006). . Clin. Exp. Pharmacol. P, 33, 813-.

8

Henderson, G. L.. (1999). . Life Sci, 65, PL209-.

9

이상명. (2015). Characterization of Korean Red Ginseng (Panax ginseng Meyer): History, preparation method, and chemical composition. Journal of Ginseng Research, 39(4), 384-391.

10

Li, X.. (2007). . Biomed. Chromatogr, 21, 735-.

11

Li, X.. (2007). . Biol. Pharm. Bull, 30, 847-.

12

Liao, B.. (2002). . Exp. Neurol, 173, 224-.

13

Liu, Y.. (2006). . Planta Med, 72, 126-.

14

Mao, Q.. (2014). . Phytomedicine, 21, 515-.

15

Park, S. H.. (2016). . Biochem. Bioph. Res. Co, 478, 1713-.

16

Sengupta, S.. (2004). . Circulation, 110, 1219-.

17

Sim, J.. (2015). . Food Chem. Toxicol, 81, 171-.

18

Siraj, F. M.. (2015). . J. Enzym. Inhib. Med. Ch, 30, 9-.

19

Smith, I.. (2014). . Nutr. Rev, 72, 319-.

20

Wang, W.. (2007). . J. Chromatogr. B, 852, 8-.

21

Xie, H. T.. (2005). . J. Chromatogr. B, 818, 167-.

22

Yun, T. K.. (2001). . J. Korean Med. Sci, 16, S19-.

23

Zhang, X.. (2007). . J. Chromatogr. B, 858, 65-.

Submission Date
2016-12-09
Revised Date
2016-12-14
Accepted Date
2016-12-14
상단으로 이동

Mass Spectrometry Letters