2015
DOI: 10.1002/dta.1863
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Cytochrome P450 2D6 and 3A4 enzyme inhibition by amine stimulants in dietary supplements

Abstract: A number of dietary supplements used for weight loss and athletic performance enhancement have been recently shown to contain a variety of stimulants, for which there is a lack of pharmacological and toxicological information. One concern for these emerging compounds is their potential to inhibit metabolic enzymes in the liver such as cytochromes P450 (CYP), which can lead to unexpected interactions among dietary supplements, drugs, and other xenobiotics. In this study, inhibition of human recombinant CYP2D6 a… Show more

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Cited by 9 publications
(10 citation statements)
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“…Pharmacokinetic interactions among OEP-NF ingredients must also be taken into consideration. From that perspective, it is worth noting that aegeline, higenamine, yohimbine, and coclaurine are all CYP3A4 substrates and yohimbine, higenamine, and coclaurine are also CYP2D6 substrates, with the latter two also being CYP2D6 inhibitors (Le Corre et al, 2004; Liu and Santillo, 2016; Manda et al, 2016). Moreover, CYP2D6 is highly polymorphic and individuals exhibiting a CYP2D6 “poor metabolizer” phenotype may be more susceptible to the effects of OEP-NF (Ingelman-Sundberg, 2005).…”
Section: Discussionmentioning
confidence: 99%
“…Pharmacokinetic interactions among OEP-NF ingredients must also be taken into consideration. From that perspective, it is worth noting that aegeline, higenamine, yohimbine, and coclaurine are all CYP3A4 substrates and yohimbine, higenamine, and coclaurine are also CYP2D6 substrates, with the latter two also being CYP2D6 inhibitors (Le Corre et al, 2004; Liu and Santillo, 2016; Manda et al, 2016). Moreover, CYP2D6 is highly polymorphic and individuals exhibiting a CYP2D6 “poor metabolizer” phenotype may be more susceptible to the effects of OEP-NF (Ingelman-Sundberg, 2005).…”
Section: Discussionmentioning
confidence: 99%
“…Santillo (2014) reported that AEPEA inhibits human monoamine-oxidase type A (MAO-A) in vitro in a competitive and reversible manner similar to amphetamine, whereas DEPEA has much weaker effects in this regard. Liu and Santillo (2016) reported that DEPEA inhibits activity of the hepatic cytochrome P-450 enzyme, CYP2D6, which could alter the effects of other drugs taken in combination with DEPEA. Due to the paucity of information about the pharmacology of -ethyl PEA analogs, we sought to study the effects of AEPEA and its amine-substituted analogs, N-methyl--ethylphenethylamine (MEPEA) and DEPEA, as compared to the effects of amphetamine (see Figure 1 for chemical structures).…”
Section: Downloaded Frommentioning
confidence: 99%
“…The top priority of the FDA’s Office of Dietary Supplement Programs (ODSP) is to protect public health, which requires coordination of many different avenues including, but not limited to, reviewing premarket safety notifications surrounding new dietary ingredients (NDIs), conducting dietary supplement and ingredient-specific research, and monitoring reported adverse events and case studies. Some recent research is looking at the possibility of linking in vitro and in vivo results to specific human health endpoints such as cardiotoxicity and hepatotoxicity (Liu and Flynn, 2015; Liu and Santillo, 2016). The ODSP faces many challenges in regulating botanical dietary supplements due to the inherent complexity and variability of botanical-sourced ingredients, with the added challenge of intentional adulteration of supplements, a complex supply chain, a lack of a single standard that can be used to verify the integrity of each botanical sample, and failure of manufacturers to submit NDI notifications to the FDA.…”
Section: Regulation Of Botanical Dietary Supplementsmentioning
confidence: 99%