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

Parr, Maria Kristina; Zhao, Piwen; Haupt, Oliver; Ngueu, Sandrine Tchoukouegno; Hengevoß, Jonas; Fritzemeier, Karl Heinrich; Marion, P; Schlörer, Nils; Muhn, Peter; Zheng, Wan; Xie, Mingyong; Diel, Patrick

doi:10.1002/mnfr.201300806

Cited by 87 publications

(108 citation statements)

References 32 publications

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“…As further components of the insect meal, which may have contributed to its metabolic effects, ecdysteroids come into question. Ecdysteroids from which 20‐hydroxyecdysone is the quantitatively main in Tenebrio molitor larvae generally control molting (ecdysis) and metamorphosis in insects and have been reported to exert interesting metabolic actions including anti‐obesity and hypoglycemic effects and hypertrophic effects on muscle in mammals . We are not aware of any literature data on ecdysteroid concentrations in Tenebrio molitor larvae meal, but the concentration of 20‐hydroxyecdysone in the hemolymph of Tenebrio molitor larvae was reported to be in the range between 50 and 1500 ng mL –1 depending on the developmental stage of larvae (the peak level is found in larvae of eyestage 12).…”

Section: Discussionmentioning

confidence: 98%

The Antisteatotic and Hypolipidemic Effect of Insect Meal in Obese Zucker Rats is Accompanied by Profound Changes in Hepatic Phospholipid and 1‐Carbon Metabolism

Meyer

Geßner

Wen

et al. 2019

Molecular Nutrition Food Res

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Scope The hypothesis is tested that insect meal, which has a low methionine content, reduces the hepatic phosphatidylcholine (PC):phosphatidylethanolamine (PE) ratio, which is a critical determinant of hepatic lipid synthesis, by decreasing availability of the methionine metabolite S‐adenosylmethionine (SAM). Methods and results Obese rats (n = 24) are randomly divided into two groups (Obese Casein and Obese Insect) of 12 rats each. In addition, lean rats (n = 12) are used as control group (LC). Groups LC and OC receive a control diet with casein as protein source, whereas in the OI group, casein is replaced isonitrogenously by insect meal, which is found to be less digestible (–12% units). Plasma and liver concentrations of lipids and hepatic expression of lipid synthesizing genes are reduced in the OI group compared to the OC group. Plasma and liver concentration of PC and the PC:PE ratio are decreased in the OI group compared to the OC group, while hepatic concentration of SAM and the hepatic SAM:S‐adenosylhomocysteine (SAH) ratio is lower in the OI group than in the OC group. Conclusion The decrease of the hepatic PC:PE ratio is probably a key mechanism explaining the pronounced antisteatotic and hypolipidemic action of insect meal in obese rats.

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Section: Discussionmentioning

confidence: 98%

The Antisteatotic and Hypolipidemic Effect of Insect Meal in Obese Zucker Rats is Accompanied by Profound Changes in Hepatic Phospholipid and 1‐Carbon Metabolism

Meyer

Geßner

Wen

et al. 2019

Molecular Nutrition Food Res

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“…In spite of more than 40 years of research, the mechanism of action of these molecules on mammals/humans has not been elucidated, as only diverging reports are available for the moment. Several data favour an action on membranes through a GPCR receptor (17), whereas other ones suggest the involvement of a nuclear receptor, the estrogen receptor ERβ (18,19).…”

Section: How Do Ecdysteroids Work?mentioning

confidence: 99%

“…There is in fact no direct evidence for the binding of 20E to nuclear estrogen (or androgen) receptors (12,13). The evidence of ERβ involvement in 20E effect is based on the use of specific pharmacological activators or inhibitors of ERs, the former being able to mimic and the latter to inhibit the effects of 20E on target cells such as osteoblasts (20) or myoblasts (19). These studies however do not bring proofs for a direct 20E binding, as ER receptor could be activated indirectly, and even in the absence of ligand, e.g.…”

Section: How Do Ecdysteroids Work?mentioning

confidence: 99%

20-Hydroxyecdysone activates the protective arm of the renin angiotensin system via Mas receptor

Lafont

Raynal

Serova

et al. 2020

Preprint

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20-Hydroxyecdysone (20E) is a steroid hormone that plays a key role in insect development through nuclear ecdysone receptors (EcRs) and at least one membrane GPCR receptor (DopEcR) and displays numerous pharmacological effects in mammals. However, its mechanism of action is still debated, involving either an unidentified GPCR or the estrogen ERβ receptor. The goal of our study was to better understand 20E mechanism of action.A mouse myoblast cell line (C2C12) and the gene expression of myostatin (a negative regulator of muscle growth) was used as a reporter system of anabolic activity. Experiments using protein-bound 20E established the involvement of a membrane receptor. 20E-like effects were also observed with Angiotensin- (1-7), the endogenous ligand of Mas. Additionally, the effect on myostatin gene expression was abolished by Mas receptor knock-down using small interfering RNA (siRNA) or pharmacological inhibitors.17-Estradiol (E2) also inhibited myostatin gene expression, but proteinbound E2 was inactive, and E2 activity was not abolished by angiotensin-(1-7) antagonists. A mechanism involving cooperation between Mas receptor and a membrane-bound palmitoylated estrogen receptor is proposed.The possibility to activate the Mas receptor with a safe steroid molecule is consistent with the pleiotropic pharmacological effects of ecdysteroids in mammals and indeed this mechanism may explain the close similarity between angiotensin-(1-7) and 20E effects. Our findings open a lot of possible therapeutic developments by stimulating the protective arm of the renin-angiotensin-aldosterone system (RAAS) with 20E.

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“…It is essential for moulting and reproduction in many arthropod species, and is also present as an insecticide in some plant species where it disrupts the development of insect pests that would feed upon them . Reports in the older steroid literature have suggested that ecdysteroids may exert a small anabolic effect in several mammal species, although more recent studies offer conflicting reports of their anabolic effects . Nonetheless, 20‐hydroxyecdysone has been found in dietary supplements such as Oxybolin 250 (High‐Tech Pharmaceuticals) and Ecdy‐Bolin (Truly Huge Supplements).…”

Section: ‐Hydroxyecdysone (2β3β14α20β22α25‐hexahydroxy‐5β‐cholmentioning

confidence: 51%

A review of designer anabolic steroids in equine sports

Waller

McLeod

2016

Drug Testing and Analysis

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In recent years, the potential for anabolic steroid abuse in equine sports has increased due to the growing availability of designer steroids. These compounds are readily accessible online in 'dietary' or 'nutritional' supplements and contain steroidal compounds which have never been tested or approved as veterinary agents. They typically have unusual structures or substitution and as a result may pass undetected through current anti-doping screening protocols, making them a significant concern for the integrity of the industry. Despite considerable focus in human sports, until recently there has been limited investigation into these compounds in equine systems. To effectively respond to the threat of designer steroids, a detailed understanding of their metabolism is needed to identify markers and metabolites arising from their misuse. A summary of the literature detailing the metabolism of these compounds in equine systems is presented with an aim to identify metabolites suitable for incorporation into screening protocols by anti-doping laboratories. The future of equine anti-doping research is likely to be guided by the incorporation of alternate testing matrices into routine screening, the improvement of in vitro technologies that can mimic in vivo equine metabolism, and the improvement of instrumentation or analytical methods that allow for the development of untargeted screening, and metabolomics approaches for use in anti-doping screening protocols.

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

Abstract: 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.

Cited by 87 publications

References 32 publications

The Antisteatotic and Hypolipidemic Effect of Insect Meal in Obese Zucker Rats is Accompanied by Profound Changes in Hepatic Phospholipid and 1‐Carbon Metabolism

The Antisteatotic and Hypolipidemic Effect of Insect Meal in Obese Zucker Rats is Accompanied by Profound Changes in Hepatic Phospholipid and 1‐Carbon Metabolism

20-Hydroxyecdysone activates the protective arm of the renin angiotensin system via Mas receptor

A review of designer anabolic steroids in equine sports

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