Inhibitory effect of synthetic C–C biflavones on various phospholipase A2s activity

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 .