𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Plant natural products as insect steroid receptor agonists and antagonists

✍ Scribed by Dinan, Laurence; Savchenko, Tamara; Whiting, Pensri; Sarker, Satyajit D

Book ID
101215286
Publisher
John Wiley and Sons
Year
1999
Tongue
English
Weight
119 KB
Volume
55
Category
Article
ISSN
1526-498X

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✦ Synopsis

Findings to date on plant secondary compounds which possess ecdysteroid-like or antiecdysteroid activities in an efficient and eþ ective bioassay based on an ecdysteroid-responsive insect cell-line are summarised. Several novel antagonists have been identiüed, among which the cucurbitacins are the best characterised and have been shown to compete with ecdysteroids for the ligand binding site of the insect steroid hormone receptor. Certain withanolides, limonoids and resveratrol derivatives also antagonise 20-hydroxyecdysone action. Additionally, several new phytoecdysteroids have been isolated and identiüed. In common with all other ecdysteriods, these possess agonistic activity in the bioassay. Extensive SAR studies based on the potencies of a large number of puriüed B II ecdysteroids have been performed and molecular (CoMFA) modelling used to characterise ecdysteroid binding to the ligand binding site of the receptor complex.

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