摘要：

A series of 17 flavonoids and related compounds were tested as inhibitors of bovine lung cyclic AMP- and cyclic GMP-phosphodiesterase, comparatively to 12 reference substances, including antianaphylactic drugs. Most of the chromone-like compounds, including flavonoids disodium cromoglycate, gentiacaulein (a xanthone) and gentiacaulein (an anthraquinone) exhibited a higher potency for the inhibition of cyclic GMP hydrolysis with respect to cyclic AMP hydrolysis. The highest selectivities were observed using pelargonidin chloride and gentiacaulein with potencies similar to that of 1-methyl 3-isobutyl xanthine. Catechins were also highly selective of the cyclic GMP hydrolysis, but showed smaller potencies. These selectivities, however, remained smaller than observed when using 2'deoxy cyclic GMP, cyclic IMP, ICI 74917 and M&B 22948. An opposite selectivity was observed using khellin, a xanthone, papaverine, ZK62711 and Ro-20 1724, which show higher potencies of inhibition of cyclic AMP hydrolysis with respect to cyclic AMP hydrolysis. Altogether, these data suggest that the antianaphylactic properties of chromone-like compounds might be related to the increase of both cyclic AMP and cyclic GMP through the inhibition of phosphodiesterase.

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