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 A2s (PLA2s) activity. The synthetic C–C biflavones (a–f) showed rather different inhibitory activity against various PLA2s. Most synthetic C–C biflavonoids exhibited potent and broad inhibitory activity against various sPLA2s and cPLA2 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 sPLA2 X. None of the natural and synthetic biflavonoids tested showed inhibitory activity against sPLA2 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 PLA2.

Several C–C biflavones (a–f) were synthesized and evaluated for their inhibitory activity against phospholipase A2s (PLA2s) activity. The synthetic C–C biflavones showed rather different inhibitory activity against various sPLA2s. Most synthetic C–C biflavonoids exhibited potent and broad inhibitory activity against various PLA2s 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 sPLA2 X. None of the natural and synthetic biflavonoids tested showed inhibitory activity against sPLA2 IB.Figure optionsDownload as PowerPoint slide