Ecdysteroids: A novel class of anabolic agents?

被引:69
作者
Parr, M. K. [1 ]
Botre, F. [2 ]
Nass, A. [1 ]
Hengevoss, J. [3 ]
Diel, P. [3 ]
Wolber, G. [1 ]
机构
[1] Free Univ Berlin, Inst Pharmaceut & Med Chem, Dept Biol Chem Pharm, D-14195 Berlin, Germany
[2] Federaz Med Sport Italiana, Lab Antidoping, Rome, Italy
[3] German Sport Univ Cologne, Inst Cardiovasc Res & Sports Med, Dept Cellular & Mol Sports Med, Cologne, Germany
关键词
ecdysteroids; doping in sport; anabolic effect; estrogen receptor beta; beta-ecdysone; muscle hypertrophy; SKELETAL-MUSCLE CELLS; LIGAND-BINDING DOMAIN; PROTEIN-SYNTHESIS; INSECT HORMONES; 20-HYDROXYECDYSONE; PHYTOECDYSTEROIDS;
D O I
10.5604/20831862.1144420
中图分类号
G8 [体育];
学科分类号
04 ; 0403 ;
摘要
Increasing numbers of dietary supplements with ecdysteroids are marketed as "natural anabolic agents". Results of recent studies suggested that their anabolic effect is mediated by estrogen receptor (ER) binding. Within this study the anabolic potency of ecdysterone was compared to well characterized anabolic substances. Effects on the fiber sizes of the soleus muscle in rats as well the diameter of C2C12 derived myotubes were used as biological readouts. Ecdysterone exhibited a strong hypertrophic effect on the fiber size of rat soleus muscle that was found even stronger compared to the test compounds metandienone (dianabol), estradienedione (trenbolox), and SARM S 1, all administered in the same dose (5 mg/kg body weight, for 21 days). In C2C12 myotubes ecdysterone (1 mu M) induced a significant increase of the diameter comparable to dihydrotestosterone (1 mu M) and IGF 1 (1.3 nM). Molecular docking experiments supported the ER beta mediated action of ecdysterone. To clarify its status in sports, ecdysterone should be considered to be included in the class "S1.2 Other Anabolic Agents" of the list of prohibited substances of the World Anti-Doping Agency.
引用
收藏
页码:169 / 173
页数:5
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