The detection of a synthetic Interleukin-1 receptor antagonist peptide in a seized product from a racing stable.
Abstract: A synthetic Interleukin-1 receptor antagonist peptide with the sequence Acetyl-Phe-Glu-Trp-Thr-Pro-Gly-Tyr-Trp-Gln-Pro-Tyr-Ala-Leu-Pro-Leu-OH has been identified in a vial seized during a stable inspection. The use of peptide-based Interleukin-1 receptor antagonists as anti-inflammatory agents has not been previously reported, making this peptide the first in a new class of sports doping peptides. The peptide has been characterized by high-resolution mass spectrometry and a detection method developed based on solid-phase extraction and liquid chromatography - triple quadrupole mass spectrometry. Using in vitro and in vivo models to study the properties of the peptide after administration, the peptide was shown to be highly unstable in plasma and was not detected in urine after administration in a rat. The poor stability of the peptide makes detection challenging but also suggests that it has limited effectiveness as an anti-inflammatory drug. Copyright © 2015 John Wiley & Sons, Ltd.
Copyright © 2015 John Wiley & Sons, Ltd.
Publication Date: 2015-09-11 PubMed ID: 26360925DOI: 10.1002/dta.1869Google Scholar: Lookup
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Summary
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This research article focuses on the discovery of a synthetic peptide, which acts as an Interleukin-1 receptor antagonist in a product seized from a racing stable. Its usage has not been reported prior to this, marking this as a new class of doping substances in sports. The paper outlines the use of various techniques to both identify and establish the properties of this peptide, highlighting some difficulties in detection and doubts about its effectiveness as an anti-inflammatory agent.
Identification of the Synthetic Peptide
- The compound found in the material confiscated during a racing stable’s inspection is a synthetic peptide, which acts as an antagonist to the Interleukin-1 receptor. This antagonist is made up of a specific chain of amino acids.
- The blocking of the Interleukin-1 receptor inhibits the inflammatory response, which would be beneficial in a sporting context, where managing inflammation is a significant concern.
- This is the first-ever report on the use of a peptide-based Interleukin-1 receptor antagonist, thus designating this substance as a new class in sports doping agents.
Characterizing the Peptide
- The research team utilized high-resolution mass spectrometry to characterize the peptide, a technique that allows for the accurate measurement of the molecular weight of the compound, and thereby identifies its structure.
Developing a Detection Method
- The detection method itself was based on the process of solid-phase extraction, which helps in isolating the substances from a complex mixture, followed by liquid chromatography and triple quadrupole mass spectrometry. This detailed approach helps in identifying and separating the peptide from other compounds.
Studying the Peptide Properties
- Through the use of in vitro (test-tube) and in vivo (living organism) models, the team studied the properties of the peptide after being administered to the subjects.
- The synthetic peptide had shown high instability when present in plasma, raising questions regarding its durability.
- The team further shared that the peptide could not be detected in urine after being administered to rats, adding an additional challenge for detection in tests.
Efficacy as an Anti-Inflammatory Drug
- Finally, due to the peptide’s low stability in plasma, the authors suggest that its efficacy as an anti-inflammatory drug may be limited. This casts doubt on whether this newly discovered doping agent would be effective at all in a sporting context.
Cite This Article
APA
Levina V, Timms M, Vine J, Steel R.
(2015).
The detection of a synthetic Interleukin-1 receptor antagonist peptide in a seized product from a racing stable.
Drug Test Anal, 8(9), 957-965.
https://doi.org/10.1002/dta.1869 Publication
Researcher Affiliations
- Biological Research Unit, Racing Analytical Services Ltd, 400 Epsom Road, Flemington, Victoria, Australia, 3031.
- Biological Research Unit, Racing Analytical Services Ltd, 400 Epsom Road, Flemington, Victoria, Australia, 3031.
- Biological Research Unit, Racing Analytical Services Ltd, 400 Epsom Road, Flemington, Victoria, Australia, 3031.
- Biological Research Unit, Racing Analytical Services Ltd, 400 Epsom Road, Flemington, Victoria, Australia, 3031.
MeSH Terms
- Amino Acid Sequence
- Animals
- Anti-Inflammatory Agents / administration & dosage
- Anti-Inflammatory Agents / analysis
- Anti-Inflammatory Agents / blood
- Anti-Inflammatory Agents / urine
- Chromatography, Liquid
- Doping in Sports
- Drug Stability
- Horses
- Interleukin 1 Receptor Antagonist Protein / administration & dosage
- Interleukin 1 Receptor Antagonist Protein / analysis
- Interleukin 1 Receptor Antagonist Protein / blood
- Interleukin 1 Receptor Antagonist Protein / urine
- Peptides / administration & dosage
- Peptides / analysis
- Peptides / blood
- Peptides / urine
- Rats
- Receptors, Interleukin-1 / antagonists & inhibitors
- Substance Abuse Detection
- Tandem Mass Spectrometry
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