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Inhibitory Effects of Garcinia cambogia Extract on CYP2B6 Enzyme Activity.

Authors
  • Yu, Jun Sang1
  • Choi, Min Sun1
  • Park, Jong Suk1
  • Rehman, Shaheed Ur2
  • Nakamura, Katsunori3
  • Yoo, Hye Hyun1
  • 1 Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Republic of Korea. , (North Korea)
  • 2 Department of Pharmacy, COMSATS Institute of Information Technology, Abbottabad, Pakistan. , (Pakistan)
  • 3 Department of Pharmacy, Ryukyu University Hospital, Okinawa, Japan. , (Japan)
Type
Published Article
Journal
Planta Medica
Publisher
Georg Thieme Verlag KG
Publication Date
Jul 01, 2017
Volume
83
Issue
11
Pages
895–900
Identifiers
DOI: 10.1055/s-0043-104934
PMID: 28288493
Source
Medline
License
Unknown

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.

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