The stimulant higenamine in weight loss and sports supplements

Cohen, Pieter A.; Travis, John C.; Keizers, Peter H. J.; Boyer, F; Venhuis, Bastiaan J.

doi:10.1080/15563650.2018.1497171

Cited by 45 publications

(40 citation statements)

References 23 publications

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“…Higenamine is the racemic form of norcoclaurine, present in several plant species (Ahmad et al 2016). Interestingly, higenamine is a natural component of numerous traditional botanical remedies, dietary supplements or nutrients and is listed as an ingredient recommended for weight control and sports supplements (Cohen et al 2019), thus making its consumption to result in violation of anti-doping regulations. In fact, due to its presumed on β2-receptors actions, higenamine is prohibited in sport at all times, being included, among β2-agonists, in the list of prohibited substances of the World Anti-Doping Agency (Grucza et al 2017).…”

Section: Higenaminementioning

confidence: 99%

Not Just from Ethanol. Tetrahydroisoquinolinic (TIQ) Derivatives: from Neurotoxicity to Neuroprotection

2019

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Your article is protected by copyright and all rights are held exclusively by Springer Science+Business Media, LLC, part of Springer Nature. This e-offprint is for personal use only and shall not be self-archived in electronic repositories. If you wish to selfarchive your article, please use the accepted manuscript version for posting on your own website. You may further deposit the accepted manuscript version in any repository, provided it is only made publicly available 12 months after official publication or later and provided acknowledgement is given to the original source of publication and a link is inserted to the published article on Springer's website. The link must be accompanied by the following text: "The final publication is available at link.springer.com". AbstractThe 1,2,3,4-tetrahydroisoquinolines (TIQs) are compounds frequently described as alkaloids that can be found in the human body fluids and/or tissues including the brain. In most circumstances, TIQs may be originated as a consequence of reactions, known as Pictet-Spengler condensations, between biogenic amines and electrophilic carbonyl compounds, including ethanol's main metabolite, acetaldehyde. Several TIQs may also be synthesized enzymatically whilst others may be formed in the body as by-products of other compounds including TIQs themselves. The biological actions of TIQs appear critically dependent on their metabolism, and nowadays, among TIQs, 1-methyl-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline (salsolinol), N-methyl-1methyl-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline (N-methyl-(R)-salsolinol), 1-[(3,4-dihydroxyphenyl)methyl]-1,2,3,4tetrahydroisoquinoline-6,7-diol (norlaudanosoline or tetrahydropapaveroline or THP) and 1-benzyl-1,2,3,4tetrahydroisoquinoline (1BnTIQ) are considered as those endowed with the most potent neurotoxic actions. However, it remains to be established whether a continuous exposure to TIQs or to their metabolites might carry toxicological consequences in the short-or long-term period. Remarkably, recent findings suggest that some TIQs such as (1-[(4-hydroxyphenyl)methyl]-1,2,3,4tetrahydroisoquinoline-6,7-diol) (higenamine) and 1-methyl-1,2,3,4-tetrahydroisoquinoline (1-MeTIQ) as well as N-methyltetrahydroisoquinoline (N-methyl-TIQ) exert unique neuroprotective and neurorestorative actions. The present review article provides an overview on these aspects of TIQs and summarizes those that presently appear the most significant highlights on this puzzling topic.

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Section: Higenaminementioning

confidence: 99%

Not Just from Ethanol. Tetrahydroisoquinolinic (TIQ) Derivatives: from Neurotoxicity to Neuroprotection

2019

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“…Plumula nelumbinis is considered to exhibit many biological effects such as anti‐inflammation, anti‐oxidation, and anti‐hypertension. A growing number of medicinal products and nutritional supplements are observed to contain plumula nelumbinis extracts and can be purchased easily . Therefore, an evaluation of the risk of an adverse analytical finding due to higenamine in doping control caused by plumula nelumbinis products is necessary.…”

Section: Introductionmentioning

confidence: 99%

“…A growing number of medicinal products and nutritional supplements are observed to contain plumula nelumbinis extracts and can be purchased easily. [5][6][7][8][9][10][11][12] Therefore, an evaluation of the risk of an adverse analytical finding due to higenamine in doping control caused by plumula nelumbinis products is necessary.…”

Section: Introductionmentioning

confidence: 99%

The risk of higenamine adverse analytical findings following oral administration of plumula nelumbinis capsules

Yan

Wang

et al. 2019

Drug Testing and Analysis

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Higenamine is a β2‐agonist that has been included in the Prohibited List of the World Anti‐Doping Agency (WADA) since 2017. Meanwhile, it exists in plumula nelumbinis, a part of the lotus seed, and is commonly used as an ingredient in cuisines, herbal medicines, and nutritional supplements in China and other countries in East Asia. Therefore, an evaluation of the risk of an adverse analytical finding (AAF) of higenamine caused by plumula nelumbinis products is necessary in doping control. In this study, 14 volunteers took plumula nelumbinis capsules orally (0.34 g/caplet, 6 caplets/day, 7 days), and another 11 volunteers ingested higenamine tablets (three 5 mg tablets/day for 7 days). Urine samples were collected over a period of 14 days. All urine samples were subjected to quantitative dilute‐and‐shoot analysis using liquid chromatography–tandem mass spectrometry (LC–MS/MS). The analytical results showed that urinary higenamine concentrations exceeded the WADA reporting limit (10 ng/mL) during the drug period in most sample groups. The maximum higenamine concentration observed in the plumula nelumbinis capsule group was 500 ng/mL. Based on confidence interval theory, appropriate data were used to establish mathematical models. The models reflected that the higenamine concentration in urine can exceed the WADA reporting limit with a high probability after taking plumula nelumbinis capsules. In conclusion, oral administration of plumula nelumbinis capsules showed a high risk of an AAF due to higenamine.

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“…Higenamine (Figure ) is one of the substances commonly occurring in dietary supplements even though it is prohibited in sport at all times and included in S3 group (β2‐agonist) of the WADA 2019 Prohibited List . Higenamine (also known as norcoclaurine) is an alkaloid found in many plants including: Nelumbo nucifera , Nandina domestica , Aconitum carmichaelii ( Aconitum napellus ), Asarum heterotropides, and Galium divaricatu .…”

Section: Introductionmentioning

confidence: 99%

The use of a valid and straightforward method for the identification of higenamine in dietary supplements in view of anti‐doping rule violation cases

Grucza

Kowalczyk

Wicka³

et al. 2019

Drug Testing and Analysis

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The stimulant higenamine in weight loss and sports supplements

Abstract: Dosages of up to 62 ± 6.0 mg per serving of the stimulant higenamine were found in dietary supplements sold in the United States.

Cited by 45 publications

References 23 publications

Not Just from Ethanol. Tetrahydroisoquinolinic (TIQ) Derivatives: from Neurotoxicity to Neuroprotection

Not Just from Ethanol. Tetrahydroisoquinolinic (TIQ) Derivatives: from Neurotoxicity to Neuroprotection

The risk of higenamine adverse analytical findings following oral administration of plumula nelumbinis capsules

The use of a valid and straightforward method for the identification of higenamine in dietary supplements in view of anti‐doping rule violation cases

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