Effect of a Dietary Supplement Containing Raspberry Ketone on CYP3A Activity in Healthy Women

T. Aomori, J. Qi, Y. Okada, Katsunori Nakamura, H. Hiraoka, T. Araki, Tomonori Nakamura, R. Horiuchi, Koujirou Yamamoto
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Abstract

Objective: Raspberry ketone (RK) is available as a supplement with effect on weight gain suppression. Recent studies have found that various herbal products can affect the activities of drug metabolizing enzymes and drug efflux proteins, and provoke clinically relevant drug-drug interactions. Capsaicin, a molecule having a similar chemical structure to RK, is another well-known cytochrome P450 (CYP) inhibitor. On the other hand, it is totally unclear whether RK has any effect on human CYP activities. In this study, we evaluated the effect of orally administered RK on CYP3A activity by measuring 6beta-hydroxycortisol/cortisol ratio in urine samples. Methods: This clinical study was conducted with approval by the Institutional Review Board at Gunma University Hospital. A total of 7 healthy women aged between 20 and 35 years were included and all of them provided written informed consent. Urine samples were collected from all subjects on the morning of day 5 (± 1 day) of menstrual cycle. In the subsequent RK phase, subjects took 3 tablets (16.7 mg/tab) of RK 3 times daily for 7 days, followed by urine sampling on the morning of day 8. In the control phase, the second morning urine sampling was performed 8 days after the first sampling. Urine 6 beta-hydroxycortisol and cortisol concentrations were measured by HPLC UV method and the 6 beta-hydroxycortisol to cortisol ratio was compared between the two phases. Results: The mean basal and assessment ratios in the RK phase were 7.49 ± 4.76 and 9.20 ± 8.05, respectively, while the corresponding ratios in the control phase were 5.36 ± 3.17 and 5.19 ± 4.61, showing no significant difference in either phase. Conclusion: RK does not affect CYP3A activity.
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含覆盆子酮膳食补充剂对健康女性CYP3A活性的影响
目的:树莓酮(RK)作为一种具有抑制体重增加作用的补充剂。最近的研究发现,各种草药产品可以影响药物代谢酶和药物外排蛋白的活性,并引起临床相关的药物-药物相互作用。辣椒素是另一种众所周知的细胞色素P450 (CYP)抑制剂,与RK具有相似的化学结构。另一方面,RK是否对人类CYP活性有影响尚不清楚。在这项研究中,我们通过测量尿液样本中的6 -羟基皮质醇/皮质醇比值来评估口服RK对CYP3A活性的影响。方法:本临床研究经群马大学附属医院机构审查委员会批准进行。共有7名年龄在20至35岁之间的健康妇女被纳入研究,她们都提供了书面知情同意。所有受试者于月经周期第5天(±1天)上午采集尿样。在随后的RK阶段,受试者每天服用3次RK 3片(16.7 mg/片),连续7天,然后在第8天早上进行尿液采样。在对照阶段,第一次尿样8天后进行第二次晨尿取样。采用高效液相色谱-紫外分光光度法测定尿液中6 -羟基皮质醇和皮质醇的浓度,比较两相间6 -羟基皮质醇与皮质醇的比值。结果:RK期的平均基础比和评估比分别为7.49±4.76和9.20±8.05,对照期的平均基础比和评估比分别为5.36±3.17和5.19±4.61,两期差异均无统计学意义。结论:RK不影响CYP3A活性。
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