title: Inhibitory Effects of Garcinia cambogia Extract on CYP2B6 Enzyme Activity.
abstract: This study assessed the inhibitory effects ofGarcinia cambogiaextract on the cytochrome P450 enzymesin vitro. G. cambogiaextract 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 thatG. cambogiaextract has significant inhibitory effects on CYP2B6 activity in a concentration-dependent manner. Furthermore, the inhibition was potentiated following preincubation with NADPH, indicating thatG. cambogiaextract is a time-dependent inhibitor of CYP2B6. Meanwhile, hydroxycitric acid, the major bioactive ingredient ofG. cambogiaextract, did not exhibit significant inhibition effects on cytochrome P450 enzyme activities.G. cambogiaextract 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 containingG. cambogiaextract with CYP2B6 substrates.
authors.affiliation: Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Republic of Korea.
authors.forename: Jun Sang
authors.initials: JS
authors.lastname: Yu
authors.affiliation: Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Republic of Korea.
authors.forename: Min Sun
authors.initials: MS
authors.lastname: Choi
authors.affiliation: Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Republic of Korea.
authors.forename: Jong Suk
authors.initials: JS
authors.lastname: Park
authors.affiliation: Department of Pharmacy, COMSATS Institute of Information Technology, Abbottabad, Pakistan.
authors.forename: Shaheed Ur
authors.initials: SU
authors.lastname: Rehman
authors.affiliation: Department of Pharmacy, Ryukyu University Hospital, Okinawa, Japan.
authors.forename: Katsunori
authors.initials: K
authors.lastname: Nakamura
authors.affiliation: Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan, Republic of Korea.
authors.forename: Hye Hyun
authors.initials: HH
authors.lastname: Yoo
mesh_terms: D065702:Cytochrome P-450 CYP2B6 / Q000378:metabolism; D065686:Cytochrome P-450 CYP2B6 Inhibitors / Q000302:isolation & purification* / Q000494:pharmacology; D029761:Garcinia cambogia / Q000737:chemistry*; D006801:Humans; D066298:In Vitro Techniques; D008862:Microsomes, Liver / Q000187:drug effects* / Q000201:enzymology; D010936:Plant Extracts / Q000494:pharmacology*; D010946:Plants, Medicinal / Q000737:chemistry
chemical_list: D065686:Cytochrome P-450 CYP2B6 Inhibitors; D010936:Plant Extracts; D065702:Cytochrome P-450 CYP2B6