In vitro glycosidation potential towards olomoucine-type cyclin-dependent kinase inhibitors in rodent and primate microsomes

Title:

In vitro glycosidation potential towards olomoucine-type cyclin-dependent kinase inhibitors in rodent and primate microsomes

Creator:

Kateřina Červenková, Marie Belejová, Chmela, Z., Rypka, M., Riegrová, D., Michnová, K., Michalíková, K., Šúrová, I., Brejcha, A., Hanuš, J., Bohuslav Černý, Fuksová, K., Libor Havlíček, and Veselý, J.

Identifier:

https://cdk.lib.cas.cz/client/handle/uuid:64c0b337-abb6-44a5-8f48-3e82ae963b69
uuid:64c0b337-abb6-44a5-8f48-3e82ae963b69
issn:0862-8408

Subject:

Fyziologie člověka a srovnávací fyziologie, fyziologie, myši, opice, mice, monkeys, physiology, CDK inhibitors, glycosidation, rat, human, 14, and 612

Type:

article, články, model:article, and TEXT

Format:

print, bez média, and svazek

Description:

Interspecies differences in glycosidation potential in mammalian tissues represent a factor contributing to ambiguity when endobiotic and/or xenobiotic metabolic pathways are extrapolated from animals to man. Using the TLC/autoradiographic technique, we conducted an in vitro investigation involving mouse, rat, monkey, as well as human liver and kidney microsomes to evaluate their glycoconjugation potential towards 3H-labeled, purine-derived selective inhibitors of cyclin-dependent kinases such as olomoucine, bohemine, roscovitine, 6-(2-hydroxybenzyl)amino-2-(1-hydroxymethyl-2-methylpropyl)amino-9-isopropylpurine (compound A-4), and 6-(3-hydroxybenzyl)amino-2-[(1(R/S)-hydroxymethyl)propyl]amino-9-isopropylpurine (compound A-5) as aglycones. Principally, this study confirmed the aliphatic hydroxyl group of olomoucine-type inhibitors as a relatively suitable target for glucuronide, glucoside, xyloside, galactoside, and/or N-acetylaminoglucoside conjugation. Of the tissues examined, only the mouse microsomes were able to perform glucosidation and galactosidation reactions with the aglycones. On the other hand, monkey microsomes were superior to the mouse microsomes in a variety of glucuronide conjugates produced with compounds A-4 and A-5., K. Červenková, M. Belejová, Z. Chmela, M. Rypka, D. Riegrová, K. Michnová, K. Michalíková, I. Šúrová, A. Brejcha, J. Hanuš, B. Černý, K. Fuksová, L. Havlíček, J. Veselý., and Obsahuje bibliografii

Language:

English

Rights:

http://creativecommons.org/licenses/by-nc-sa/4.0/
policy:public

Source:

Physiological research | 2003 Volume:52 | Number:4

Harvested from:

CDK

Metadata only:

false