LC‐MS Behavior of Girard’s Reagent T Derivatives of Oxosteroid Intact Phase II Metabolites for Doping Control Purposes

2021 ◽  
Author(s):  
P. Kiousi ◽  
A. G. Fragkaki ◽  
N. Kioukia‐Fougia ◽  
Y. S. Angelis
2012 ◽  
Vol 40 (8) ◽  
pp. 1566-1574 ◽  
Author(s):  
Yung-Ping Lee ◽  
Feng-Lin Hsu ◽  
Jaw-Jou Kang ◽  
Chien-Kuang Chen ◽  
Shoei-Sheng Lee

Xenobiotica ◽  
2011 ◽  
Vol 42 (3) ◽  
pp. 285-293 ◽  
Author(s):  
Cyrille Marvalin ◽  
Mireille Denoux ◽  
Serge Pérard ◽  
Sébastien Roy ◽  
Robert Azerad

2010 ◽  
Vol 7 (1) ◽  
pp. 111 ◽  
Author(s):  
Manjula Sunkara ◽  
Martha J. M. Wells

Environmental context. Excretion of pharmaceuticals and their metabolites by humans and animals, flushing unused pharmaceuticals and inadequate water treatment result in the occurrence of these chemicals as pollutants in wastewater, surface water and drinking water. In this research, the pharmaceutical agent acetaminophen (paracetamol, Tylenol) and its glucuronide and sulfate metabolites were examined as a model system for monitoring wastewater influent and effluent. The true risk to ecosystems and humans from the occurrence of pharmaceuticals in our water supply can only be estimated if accurate concentrations of parent pharmaceutical chemicals as well as their metabolites are measured. Abstract. An analytical method was developed to separately determine acetaminophen and its Phase II metabolites, acetaminophen glucuronide and acetaminophen sulfate, from wastewater in a single extract. The method developed will serve as a model for screening for the presence of other non-steroidal pharmaceutical compounds and their Phase II metabolites in wastewater. Acetaminophen glucuronide was not present in the wastewater influent tested to verify the analytical protocol, whereas concentrations of acetaminophen and acetaminophen sulfate in the influent were reproducible over time. A Phase I metabolite, p-aminophenol, was also determined to occur in the wastewater influent. Concentrations of the analytes-of-interest, detected in effluent samples collected after secondary treatment, but before UV treatment, were highly variable and were undetectable after UV treatment before release to surface water.


Pharmacology ◽  
1981 ◽  
Vol 23 (3) ◽  
pp. 149-155 ◽  
Author(s):  
Herbert J. Kramer ◽  
M. Rörig ◽  
KD. Völger

2017 ◽  
Vol 1061-1062 ◽  
pp. 72-78 ◽  
Author(s):  
Claire Grignon ◽  
Antoine Dupuis ◽  
Marion Albouy-Llaty ◽  
Maxime Condylis ◽  
Laurence Barrier ◽  
...  

Author(s):  
Aneta Bobowska ◽  
Sebastian Granica ◽  
Agnieszka Filipek ◽  
Matthias F. Melzig ◽  
Thomas Moeslinger ◽  
...  

Abstract Purpose Ellagitannins are high molecular weight polyphenols present in high quantities in various food products. They are metabolized by human and animal gut microbiota to postbiotic metabolites-urolithins, bioavailable molecules of a low molecular weight. Following absorption in the gut, urolithins rapidly undergo phase II metabolism. Thus, to fully evaluate the mechanisms of their biological activity, the in vitro studies should be conducted for their phase II conjugates, mainly glucuronides. The aim of the study was to comparatively determine the influence of urolithin A, iso-urolithin A, and urolithin B together with their respective glucuronides on processes associated with the inflammatory response. Methods The urolithins obtained by chemical synthesis or isolation from microbiota cultures were tested with their respective glucuronides isolated from human urine towards modulation of inflammatory response in THP-1-derived macrophages, RAW 264.7 macrophages, PBMCs-derived macrophages, and primary neutrophils. Results Urolithin A was confirmed to be the most active metabolite in terms of LPS-induced inflammatory response inhibition (TNF-α attenuation, IL-10 induction). The observed strong induction of ERK1/2 phosphorylation has been postulated as the mechanism of its action. None of the tested glucuronide conjugates was active in terms of pro-inflammatory TNF-α inhibition and anti-inflammatory IL-10 and TGF-β1 induction. Conclusion Comparative studies of the most abundant urolithins and their phase II conjugates conducted on human and murine immune cells unambiguously confirmed urolithin A to be the most active metabolite in terms of inhibition of the inflammatory response. Phase II metabolism was shown to result in the loss of urolithins’ pharmacological properties.


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