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Updated: Feb 2, 2026

Assaying Protein Kinase Activity with Radiolabeled ATP
Published on: May 26, 2017
Side-chain cleaved phytoecdysteroid metabolites as activators of protein kinase B
Halima Meriem Issaadi1, József Csábi1, Tusty-Jiuan Hsieh2
1Institute of Pharmacognosy, Interdisciplinary Excellence Center, University of Szeged, Eötvös str. 6, 6720 Szeged, Hungary.
Abstract:
Phytoecdysteroids exert their non-hormonal anabolic and adaptogenic effects in mammals, including humans, through a partially revealed mechanism of action involving the activation of protein kinase B (Akt). We have recently found that poststerone, a side-chain cleaved in vivo metabolite of 20-hydroxyecdysone, exerts potent anabolic activity in rats. Here we report the semi-synthetic preparation of a series of side-chain cleaved ecdysteroids and their activity on the Akt phosphorylation in murine skeletal muscle cells. Twelve C-21 ecdysteroids including 8 new compounds were obtained through the oxidative side-chain cleavage of various phytoecdysteroids, or through the base-catalyzed autoxidation of poststerone. The complete 1H and 13C NMR spectroscopic assignments of the new compounds are presented. Among the tested compounds, 9 could activate Akt stronger than poststerone revealing that side-chain cleaved derivatives of phytoecdysteroids other than 20-hydroxyecdysone are valuable bioactive metabolites. Thus, our results suggest that the expectable in vivo formation of such compounds should contribute to the bioactivity of herbal preparations containing ecdysteroid mixtures.
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