Browse > Article
http://dx.doi.org/10.17480/psk.2015.59.2.49

In vitro Assessment of Cytochrome P450 Inhibition by Red Ginseng Ginsenosides  

Ryu, Chang Seon (College of Pharmacy, Chungnam National University)
Shin, Jang Hyun (Bomoon High School)
Shin, Byoung Chan (Bomoon High School)
Sim, Jae Han (Bomoon High School)
Yang, Hyeon Dong (Bomoon High School)
Lee, Sung Woo (Bomoon High School)
Kim, Bong-Hee (College of Pharmacy, Chungnam National University)
Publication Information
YAKHAK HOEJI / v.59, no.2, 2015 , pp. 49-54 More about this Journal
Abstract
In the present study we evaluated comparative herb-drug interaction potential of red ginseng total powder, ginsenoside Rg1, and Rb1 by inhibition of CYP isoforms including CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4 using pooled human liver microsomes (HLMs). As measured by liquid chromatography-electrospray ionization tandem mass spectrometry, red ginseng total powder inhibited significantly activities of CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and testosterone 6-beta hydroxylation by CYP3A4, but the $IC_{50}$ values were higher than $556{\mu}g/ml$. Activities of CYP2B6, CYP2C9, CYP2D6 and CYP3A4 were inhibited by ginsenoside Rb1. Also, activities of CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, CYP2D6 and testosterone 6-beta hydroxylation by CYP3A4 were inhibited by ginsenoside Rg1. The $IC_{50}$ values of ginsenoside Rb1 and Rg1 were higher than $200{\mu}g/ml$. Based on $IC_{50}$ values against CYP isoforms, ginsenosides-drug interactions by CYP inhibition may be very low in clinical situations.
Keywords
cytochrome P450; red ginseng; ginsenoside; drug-drug interaction;
Citations & Related Records
Times Cited By KSCI : 1  (Citation Analysis)
연도 인용수 순위
1 U.S. Food and drug administration: Draft FDA guidance for industry, drug interaction studies - study design, data analysis, implications for dosing, and labeling recommendations (2012).
2 Lee, K. S. and Kim, S. K. : Direct and metabolism-dependent cytochrome P450 inhibition assays for evaluating drug-drug interactions. J. Appl. Toxicol. 33, 100 (2013).   DOI
3 Liu, Y., Zhang, J. W., Li, W., Ma, H., Sun, J., Deng, M. C. and Yang, L. : Ginsenoside metabolites, rather than naturally occurring ginsenosides, lead to inhibition of human cytochrome P450 enzymes. Toxicol. Sci. 91, 356 (2006).   DOI
4 Chang, T. K., Chen, J. and Benetton, S. A. : In vitro effect of standardized ginseng extracts and individual ginsenosides on the catalytic activity of human CYP1A1, CYP1A2, and CYP1B1. Drug. Metab. Dispos. 30, 378 (2002).   DOI
5 Wang, C. Z., Kim, K. E., Du, G. J., Qi, L. W., Wen, X. D., Li, P., Bauer, B. A., Bissonnette, M. B., Musch, M. W., Chang, E. B. and Yuan C. S. : Ultra-performance liquid chromatography and time-of-flight mass spectrometry analysis of ginsenoside metabolites in human plasma. Am. J. Chin. Med. 39, 1161 (2011).   DOI
6 Feng, L., Wang, L., Hu, C. and Jiang, X. : Pharmacokinetics, tissue distribution, metabolism, and excretion of ginsenoside Rg1 in rats. Arch. Pharm. Res. 33, 1975 (2010).   DOI
7 식품의약품안전처, 건강기능식품의 기준 및 규격 고시, 2014 2014 available online:http://www.foodnara.go.kr/hfoodi/industry/ main/sub.jsp?Mode=view&boardID=s_0503_bbs&num= 407&tpage=1&keyfield=&key=&bCate= [Accessed 31 March 2015].
8 통계청 : 장래인구추계: 2010-2060. 2011 available online: http:// kostat.go.kr/smart/news/file_dn.jsp?aSeq=252623&ord=13 [Accessed 31 March 2015].
9 한국보건사회연구원, 2011년 노인실태조사, 2011 (2011) available online: http://www.prism.go.kr/homepage/researchCommon/ downloadResearchAttachFile.do;jsessionid=23737876FD5A92C DD57CE1F71558724F.node02?work_key=001&file_type=CPR &seq_no=001&pdf_conv_yn=N&research_id=1351000- 201100144 [Accessed 31 March 2015].
10 소비자안전센터, 고령자 건강기능식품 실태조사 결과 (2010).
11 식품의약품안정처, 2011년 건강기능식품 생산실적 분석결과 (2012).
12 Guengerich, F. P. : Role of cytochrome P450 enzymes in drug_drug interactions. Adv. Pharmacol. 43, 7 (1997).   DOI
13 Henderson, G. L., Harkey, M. R., Gershwin, M. E., Hackman, R. M., Stern, J. S. and Stresser, D. M. : Effects of ginseng components on c-DNA-expressed cytochrome P450 enzyme catalytic activity. Life Sci. 65, 209 (1999).