Ecdysteroid agonists

Elbrecht et al. [167] reported that the iridoid glucoside 8-0-acetylharpagide (8-7), isolated from Ajuga reptans, possessed ecdysteroid agonist activity. Unfortunately, A. reptans is also a rich source of phytoecdysteroids and it is now clear that 8-0-acetylharpagide, per se, possesses no agonistic activity [168],... 

Researchers at FMC Corp. (Princeton, NJ, U.S.A.) reported that 4-phenylamino-l,2,3,4-tetrahydroquinolines also act as ecdysteroid agonists [169],... 

As part of an extensive survey of natural products to detect those showing ecdysteroid agonist or antagonist activities in the Bn bioassay [170], it was found that the diterpene maocrystal E (8-8) showed agonist activity (EC50 = 5 x 10 6M). 

Dinan L. reported that three resveratrol trimers, suffruticosols A (100), B (101), C (102), and one monomer cis resveratrol from Paeonia suffruticosa are active as ecdysteroids (antagonists (EDso) 10-50 pM vs. 5xlO 8pM of 20-hydroxyecdyson), but inactive as agonists in the Drosophila melanogaster BII cell bioassay for ecdysteroids agonists/ antagonists [75]. 

Dinan, L., Hormann, R.E., 2005, Ecdysteroid agonists and antagonists in Comprehensive Insect Molecular Science, Vol. 3, Gilbert, L.L, latrou, K., Gill, S.S. (Eds) Elsevier Pergamon, New York, 198-236. 

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