Two dimensional separation schemes for investigation of the interaction of an anticancer ruthenium(III) compound with plasma proteins

Author(s)
Michael Sulyok, Stephan Hann, Christian Hartinger, Bernhard Keppler, Gerhard Stingeder, Gunda Köllensperger
Abstract

On-line 2-dimensional size exclusion/anion exchange chromatography was coupled to inductively coupled mass spectrometry with dynamic reaction cell technology (SEC-IC-ICP-MS) in order to characterize the interaction of the ruthenium-based anticancer drug KP1019 with human plasma proteins in vitro and, for the first time, in vivo. In SEC-ICP-MS studies the drug was found to bind exclusively to the protein fraction of 60-80 kDa in human plasma samples (clinical study/phase 1). The respective size fraction was collected and subsequently analyzed by reversed phase chromatography coupled to electrospray mass spectrometry (LC-ESI-MS) confirming the presence of the two well known transporter proteins, i.e. human serum albumin (HSA) and transferrin (Tf). Hence, for in vivo investigation of KP1019 interaction with HSA and Tf a fully automated SEC-IC-ICP-MS approach was applied. The stoichiometry of the KP1019 protein binding was determined through the molar Ru/S ratio. Human apo-Tf standards incubated with different stoichiometric equivalents of KP 1019 were used for species-specific and species-unspecific calibration of the molar Ru/S ratio. Competitive in vitro incubation of KP1019 to both HSA and Tf for ca. 10 h showed that

Organisation(s)
Department of Inorganic Chemistry
External organisation(s)
University of Natural Resources and Life Sciences
Journal
Journal of Analytical Atomic Spectrometry
Volume
20
Pages
856-863
No. of pages
8
ISSN
0267-9477
Publication date
2005
Peer reviewed
Yes
Austrian Fields of Science 2012
1040 Chemistry
Portal url
https://ucrisportal.univie.ac.at/en/publications/f8666166-8051-4020-998e-2c110598be1d