Estrogen receptor beta is involved in skeletal muscle hypertrophy induced by the phytoecdysteroid ecdysterone.

Abstract

SCOPE:

The phytoectysteroid ecdysterone (Ecdy) was reported to stimulate protein synthesis and enhance physical performance. The aim of this study was to investigate underlying molecular mechanisms particularly the role of ER beta (ERβ).

RESULTS:

In male rats, Ecdy treatment increased muscle fiber size, serum IGF-1 increased, and corticosteron and 17β-estradiol (E2) decreased. In differentiated C2C12 myoblastoma cells, treatment with Ecdy, dihydrotestosterone, IGF-1 but also E2 results in hypertrophy. Hypertrophy induced by E2 and Ecdy could be antagonized with an antiestrogen but not by an antiandrogen. In HEK293 cells transfected with ER alpha (ERα) or ERβ, Ecdy treatment transactivated a reporter gene. To elucidate the role of ERβ in Ecdy-mediated muscle hypertrophy, C2C12 myotubes were treated with ERα (ALPHA) and ERβ (BETA) selective ligands. Ecdy and BETA treatment but not ALPHA induced hypertrophy. The effect of Ecdy, E2, and BETA could be antagonized by an ERβ-selective antagonist (ANTIBETA). In summary, our results indicate that ERβ is involved in the mediation of the anabolic activity of the Ecdy.

CONCLUSION:

These findings provide new therapeutic perspectives for the treatment of muscle injuries, sarcopenia, and cachectic disease, but also imply that such a substance could be abused for doping purposes.

• Authors: Maria Kristina Parr, Piwen Zhao, Oliver Haupt, Sandrine Tchoukouegno Ngueu, Jonas Hengevoss, Karl Heinrich Fritzemeier, Marion Piechotta, Nils Schlörer, Peter Muhn, Wen-Ya Zheng, Ming-Yong Xie, Patrick Diel
• Journal: Molecular nutrition & food research (Mol Nutr Food Res) Vol. 58 Issue 9 Pg. 1861-72 (Sep 2014) ISSN: 1613-4133 [Electronic] Germany
• PMID: 24974955 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Chemical References

• Anabolic Agents
• Estrogen Receptor beta
• Estradiol
• Ecdysterone
• Dexamethasone

Topics

• Anabolic Agents (adverse effects)
• Animals
• Cell Line (drug effects)
• Dexamethasone (pharmacology)
• Ecdysterone (adverse effects, chemistry, metabolism)
• Estradiol (pharmacology)
• Estrogen Receptor beta (antagonists & inhibitors, genetics, metabolism)
• HEK293 Cells (drug effects)
• Humans
• Hypertrophy (chemically induced, pathology)
• Male
• Muscle Fibers, Skeletal (drug effects)
• Muscle, Skeletal (drug effects, metabolism, pathology)
• Rats, Wistar