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Determination of kinetic parameters and structure–activity relationships of ginsenosides as inhibitors of cyclin‐dependent kinase 5/p25 using ultra‐pressure liquid chromatography with triple quadrupole tandem mass spectrometry
Author(s) -
Chen Ning,
Yang Hongmei,
Niu Jun,
Liu Shuying
Publication year - 2013
Publication title -
rapid communications in mass spectrometry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.528
H-Index - 136
eISSN - 1097-0231
pISSN - 0951-4198
DOI - 10.1002/rcm.6537
Subject(s) - chemistry , cyclin dependent kinase 5 , mass spectrometry , tandem mass spectrometry , chromatography , triple quadrupole mass spectrometer , ginsenoside , kinase , in vivo , liquid chromatography–mass spectrometry , protein kinase a , high performance liquid chromatography , selected reaction monitoring , biochemistry , cyclin dependent kinase 2 , ginseng , microbiology and biotechnology , biology , medicine , alternative medicine , pathology
RATIONALE Cyclin‐dependent kinase 5 (cdk5) is a serine/threonine kinase that is reported to play an important role in the pathogenesis of Alzheimer's disease. Ginsenosides have beneficial effects on Alzheimer's disease in both in vivo and in vitro experiments, but the precise mechanisms are not yet entirely clear. METHODS In the present study, an ultrahigh‐pressure liquid chromatography (UPLC) and triple quadrupole mass spectrometry (TQMS) assay was developed to study the activities of cdk5 for the first time. RESULTS The calibration curves showed a good linear behavior over the range 0.04 μM to 10 μM ( y = 0.934 x + 0.045, R 2 = 0.995) with product phosphorylated peptide (PKpTPKKAKKV). The screening results suggested that the inhibition activities of ginsenosides are related to their chemical structures. CONCLUSIONS The developed UPLC/TQMS‐based method for determination of an inhibitor of cdk5/p25 is sensitive and reliable. The effect of ginsenosides on Alzheimer's disease may be involved with the regulation of activities of cdk5/p25. Copyright © 2013 John Wiley & Sons, Ltd.