Inhibition of adenosine 3',5'-cyclic monophosphate phosphodiesterase by flavonoids. II.

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Abstract
Thirty-eight flavones obtained from Scutellaria baicalensis and ninety six related flavones were tested for inhibitory activity against adenosine 3'', 5''-cuclic monophosphate phosphodiesterase from beef heart. The most active inhibitor is 8-methoxy-5,7,2''-thrihydroxyflavone from S. baicalenis. Its IC50 value is 0.6 .times. 10-5 M/l). The structure-activity relationships were investigated, a)O-Methylated flavones generally show lower inhibitory activity than the corresponding hydroxyflavones among the flavones having under four substituents. b) O-Methylated flavones generally show higher inhibitory activity than the corresponding hydroxyflavones in the flavones having over five substituents. (c) C-Glycosides are almost all poor inhibtors. (d) O-Glycosides are generally less potent than the corresponding flavones.