albumin - publications

Predict more albumin - ligand interactions now!


1. Biomed Chromatogr. 2012 Jan 25. doi: 10.1002/bmc.2704. [Epub ahead of print]

Electrokinetic chromatographic estimation of the enantioselective binding of
nomifensine to human serum albumin and total plasma proteins.

Asensi-Bernardi L, Martín-Biosca Y, Sagrado S, Medina-Hernández MJ.

Departamento de Química Analítica, Facultad de Farmacia, Universidad de Valencia,
Burjassot, Valencia, Spain.

This report is the first evidence of enantioselective binding of nomifensine to
human serum albumin (HSA) and plasma proteins. The overall process with HSA
included: (i) consistent experimental design along two independent sessions; (ii)
incubation of nomifensine-HSA designed mixtures; (iii) ultrafiltration for
separating the unbound enantiomers fraction; (iv) electrokinetic chromatography
(EKC) using heptakis-2,3,6-tri-O-methyl-β-cyclodextrin as chiral selector to
provide experimental data for enantiomers (first, E1, and second, E2, eluted
ones); and (v) a recent direct equation allowing univariate tests and robust
statistics to provide consistent parameters and uncertainty. A significant
enantioselectivity to HSA (2.7 ± 0.1) was encountered, related to a 1:1
stoichiometry and log affinity constants of 3.24 ± 0.10 and 3.67 ± 0.08 for E1
and E2, respectively. The protein binding (PB) estimated at physiological
concentration levels was 40 ± 5 and 63 ± 4% for E1 and E2, respectively. The use
of synthetic human sera allowed in vitro estimation of the total plasma PB for
the racemate (61 ± 5%; coincident with in vivo values), and its enantiomers
(58 ± 7 and 64 ± 4% for E1 and E2, respectively). Comparison allowed the relative
importance of HSA respect to other plasma proteins for binding nomifensine to be
established. Copyright © 2012 John Wiley & Sons, Ltd.

Copyright © 2012 John Wiley & Sons, Ltd.

PMID: 22275209 [PubMed - as supplied by publisher]