Inhibitory Effects of Garcinia cambogia Extract on CYP2B6 Enzyme Activity

Abstract

This study assessed the inhibitory effects of extract on the cytochrome P450 enzymes 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 extract has significant inhibitory effects on CYP2B6 activity in a concentration-dependent manner. Furthermore, the inhibition was potentiated following preincubation with NADPH, indicating that extract is a time-dependent inhibitor of CYP2B6. Meanwhile, hydroxycitric acid, the major bioactive ingredient of extract, did not exhibit significant inhibition effects on cytochrome P450 enzyme activities. 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 extract with CYP2B6 substrates.

Potential health risks surrounding ingredients of pre-workout and post-workout dietary supplements: a thorough label analysis

“…In several clinical trials, this plant was deemed safe to use in the treatment of obesity. Nonetheless, it has been proven that Garcinia cambogia displays inhibitory effects in CYP2B6 [26]. Despite the relative safety of this ingredient, there have been some disturbing clinical cases that raise suspicion on its use [27].…”

Investigation of Drug-Interaction Potential for Arthritis Dietary Supplements: Chondroitin Sulfate, Glucosamine, and Methylsulfonylmethane

“…For the experimental method, the reference method was used [44]. Briefly, incubation mixtures were composed of 0.5 mg/mL human liver microsomes; varying concentrations of CS in DW (0.1, 0.3, 1, 3, 10, 30, 100, and 200 µM) or MSM in DW (0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1000 µM) or GCS in DMSO (0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1000 µM); a substrate mixture in DMSO (40 µM phenacetin for CYP1A2; 2.5 µM coumarin for CYP2A6; 80 µM bupropion for CYP2B6; 10 µM diclofenac for CYP2C9; 80 µM [±]-mephenytoin for CYP2C19; 5 µM dextromethorphan for CYP2D6; 2.5 µM midazolam and 30 µM testosterone for CYP3A4); and an NADPH generating system (NGS; 0.1 M glucose-6-phosphate, 10 mg/mL β-NADP + , and 1 U/mL glucose-6-phosphate dehydrogenase) in a total volume of 200 µL potassium phosphate buffer (0.1 M, pH 7.4).…”

Awareness on the possible adverse effects of Garcinia cambogia: A scientific approach

“…110 G. cambogia extract has the potency to inhibit CYP2B6 which is a family of CYP450 enzyme in a timely manner, but HCA alone was not able to significantly inhibit CYP2B6. 111 Few contradictory reports were also retrieved, suggesting that G. cambogia is not as effective in weight lowering property as it is claimed to be. 77, [112][113][114][115][116][117][118][119][120] None the less, many herbal based companies are having preparations of G. cambogia that are currently on the global market.…”