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Title of Journal: Amino Acids

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Abbravation: Amino Acids

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Springer Vienna

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DOI

10.1002/lt.21290

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ISSN

1438-2199

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LC/MS evaluation of metabolism and membrane transp

Authors: Dongyu Gu Ying Ma Gang Niu Yongjun Yan Lixin Lang Haji Akber Aisaand Haokao Gao Dale O Kiesewetter Xiaoyuan Chen
Publish Date: 2010/07/30
Volume: 40, Issue: 2, Pages: 669-675
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Abstract

Two bombsin peptides GRPR agonist AcaQWAVGHLMNH2 and antagonist fQWAVGHLNHEthyl were evaluated We employed the highly sensitive Waters QTof Premier MS coupled with a UPLC system to identify the metabolites produced by rat hepatocytes or PC3 human prostate cancer cells and we utilized the AB/MDS 4000 QTrap LC/MS/MS system with highly sensitive quantitative and qualitative performance to quantitatively analyze the internalization of GRPR agonist and antagonist in PC3 cells The major metabolites of both GRPR agonist and antagonist were the result of peptide bond hydrolysis between W and A which was demonstrated by observation of the Nterminal fragment m/z 446 AcaQWOH for agonist and m/z 480 fQWOH for antagonist Both peptides were also hydrolyzed between A and V which formed peaks m/z 517 AcaQWAOH and m/z 555 VGHLMNH2 for the agonist and m/z 551 fQWAOH and m/z 452 VGHLNHEthyl for the antagonist The peptide agonist also formed a unique metabolite that resulted from hydrolysis of the Cterminal amide The antagonist showed significantly slower metabolism as compared to the agonist in both rat hepatocytes and PC3 cells The antagonist also showed significantly lower PC3 cell internalization rate than that of the agonist In conclusion the metabolism profiles of both GRPR agonist and antagonist peptides were identified by LC/MS The antagonist peptide was more stable than the agonist peptide in rat hepatocyte incubation One major factor could be the hydrolysisresistant Cterminal LNHEthyl group compared with the unsubstituted amide of the agonist Another factor could be different amino acid sequences of the agonist and antagonist that may also influence the enzymatic hydrolysis The antagonist ligand is potentially more useful for receptortargeted imaging due primarily to its higher metabolic stability

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