Inhibitory effect of synthetic C-C biflavones on various phospholipase A(2)s activity

Bioorg Med Chem. 2007 Nov 15;15(22):7138-43. doi: 10.1016/j.bmc.2007.07.054. Epub 2007 Aug 22.

Abstract

Several prototypes of C-C biflavones (a-f) were synthesized and evaluated their inhibitory activity against phospholipase A(2)s (PLA(2)s) activity. The synthetic C-C biflavones (a-f) showed rather different inhibitory activity against various PLA(2)s. Most synthetic C-C biflavonoids exhibited potent and broad inhibitory activity against various sPLA(2)s and cPLA(2) tested regardless of their structural array. In particular, of natural and synthetic biflavonoids tested, the synthetic C-C biflavonoid (d) only showed inhibitory activity against sPLA(2) X. None of the natural and synthetic biflavonoids tested showed inhibitory activity against sPLA(2) IB. Further chemical modification of these basic structures will be carried out in order to investigate the synthetic C-C biflavones which possess more selective inhibitory activity against isozymes of PLA(2).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Enzyme Activation / drug effects
  • Flavones / chemical synthesis*
  • Flavones / chemistry
  • Flavones / pharmacology*
  • Isoenzymes / antagonists & inhibitors*
  • Molecular Structure
  • Phospholipase A2 Inhibitors*
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Flavones
  • Isoenzymes
  • Phospholipase A2 Inhibitors