Molecular property-binding affinity relationship of flavonoids for common rat plasma proteins in vitro

Biochimie. 2011 Feb;93(2):134-40. doi: 10.1016/j.biochi.2010.08.013. Epub 2010 Sep 8.

Abstract

The structural difference of flavonoids strongly affects the binding process with plasma proteins. This work in here mainly concerns about the molecular property-binding affinity relationship of dietary flavonoids for common rat plasma proteins (CRPP). The magnitudes of binding constants between flavonoids and CRPP were within the range of 10(4)-10(5) L/mol and the number of binding sites (n) was determined as 1.02 ± 0.19. These data were much smaller than the affinities between flavonoids and purified bovine and human serum albumins. The hydroxylation on rings A, B and C of flavonoids significantly affected the binding affinity. The glycosylation of dietary flavonoids decreased the binding affinity and the C2=C3 double bond hardly affected it. The galloylated catechins have higher binding affinities for CRPP than non-galloylated catechins. Flavonoids played as a hydrogen bond acceptor when bound to CRPP. The flavonoids with high topological polar surface areas (TPSA) are bound tightly while those with low TPSA are not.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apigenin / chemistry
  • Apigenin / metabolism
  • Blood Proteins / metabolism*
  • Catechin / chemistry
  • Catechin / metabolism
  • Cattle
  • Chromatography, Reverse-Phase
  • Flavonoids / chemistry*
  • Flavonoids / metabolism*
  • Glycosylation
  • Humans
  • Hydroxylation
  • Isomerism
  • Methylation
  • Protein Binding
  • Rats
  • Structure-Activity Relationship
  • Surface Properties

Substances

  • Blood Proteins
  • Flavonoids
  • Apigenin
  • Catechin