Biological activity of natural and synthetic ecdysteroids in the BII bioassay.

The potencies of 19 ecdysteroids are compared in the BII bioassay, which reflects the affinity of binding to the ligand binding site of the Drosophila melanogaster ecdysteroid receptor. The compounds tested represent either natural products isolated from plants (phytoecdysteroids) or fungi (mycoecdysteroids) or synthetic analogues based on insect metabolites (zooecdysteroids). None of the tested compounds showed any antagonistic activity, but all possessed quantifiable agonistic activity. All the mycoecdysteroids were less potent than the major insect ecdysteroid, 20-hydroxyecdysone (20E). Also, conjugation of 20E with a glucose moiety results, as expected, in considerable reduction in biological activity, but the remaining activity is dependent on the position of conjugation. The implications of these findings for the structure/activity relationship of ecdysteroids are discussed.