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Planta Med 2017; 83(11): 895-900
DOI: 10.1055/s-0043-104934
Pharmacokinetic Investigations
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Inhibitory Effects of Garcinia cambogia Extract on CYP2B6 Enzyme Activity

Jun Sang Yu   *
1   Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Republic of Korea
,
Min Sun Choi   *
1   Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Republic of Korea
,
Jong Suk Park
1   Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Republic of Korea
,
Shaheed Ur Rehman
2   Department of Pharmacy, COMSATS Institute of Information Technology, Abbottabad, Pakistan
,
Katsunori Nakamura
3   Department of Pharmacy, Ryukyu University Hospital, Okinawa, Japan
,
Hye Hyun Yoo
1   Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Republic of Korea
› Author Affiliations
Further Information

Publication History

received 29 September 2016
revised 09 February 2017

accepted 22 February 2017

Publication Date:
13 March 2017 (online)

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Abstract

This study assessed the inhibitory effects of Garcinia cambogia extract on the cytochrome P450 enzymes in vitro. G. cambogia extract was incubated with cytochrome P450 isozyme-specific substrates in human liver microsomes and recombinant CYP2B6 isozyme, and the formation of the marker metabolites was measured to investigate the inhibitory potential on cytochrome P450 enzyme activities. The results showed that G. cambogia extract has significant inhibitory effects on CYP2B6 activity in a concentration-dependent manner. Furthermore, the inhibition was potentiated following preincubation with NADPH, indicating that G. cambogia extract is a time-dependent inhibitor of CYP2B6. Meanwhile, hydroxycitric acid, the major bioactive ingredient of G. cambogia extract, did not exhibit significant inhibition effects on cytochrome P450 enzyme activities. G. cambogia extract could modulate the pharmacokinetics of CYP2B6 substrate drugs and lead to interactions with those drugs. Therefore, caution may be required with respect to concomitant intake of dietary supplements containing G. cambogia extract with CYP2B6 substrates.

Key words

Garcinia cambogia - Clusiaceae - CYP - drug metabolism - drug interaction

* Jun Sang Yu and Min Sun Choi contributed equally to this work.


Supporting information

The representative LC-MS/MS chromatograms for the CYP isozyme-specific metabolites are available as Supporting Information.

 

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