Phytoecdysteroids Increase Protein Synthesis in Skeletal Muscle Cells
* Abstract
* HTMLFull Text HTML
* PDFHi-Res PDF[1013 KB]
* PDFPDF w/ Links[229 KB]
Jonathan Gorelick-Feldman*†, David MacLean§, Nebojsa Ilic†, Alexander Poulev†, Mary Ann Lila#, Diana Cheng# and Ilya Raskin†
Biotech Center, Cook College, Rutgers University, 59 Dudley Road, New Brunswick, New Jersey 08901;Hallett Center for Diabetes and Endocrinology, Brown Medical School, Providence, Rhode Island 02912; and Department of Natural Resources and Environmental Sciences, University ofIllinois, Urbana, Illinois 61801
J. Agric. Food Chem., 2008, 56 (10), pp 3532–3537
DOI: 10.1021/jf073059z
Publication Date (Web): April 30, 2008
Copyright © 2008 American Chemical Society
Phytoecdysteroids, which are structurally similar or identical to insect molting hormones, produce a range of effects in mammals, including increasing growth and physical performance. To study the mechanism of action of phytoecdysteroids in mammalian tissue, an in vitro cellular assay of protein synthesis was developed. In C2C12 murine myotubes and human primary myotubes, phytoecdysteroids increased protein synthesis by up to 20%. In vivo, ecdysteroids increased rat grip strength. Ecdysteroid-containing plant extracts produced similar results. The effect was inhibited by a phosphoinositide kinase-3 inhibitor, which suggests a PI3K-mediated mechanism.
Phytoecdysteroids - From Isolation to Their Effects on Humans
Authors: Maria Bathori1; Zita Pongracz1
Source: Current Medicinal Chemistry, Volume 12, Number 2, January 2005 , pp. 153-172(20)
Publisher: Bentham Science Publishers
* < previous article
* |
* next article >
* |
* view table of contents
Key:
Free Content - Free Content
New Content - New Content
Subscribed Content - Subscribed Content
Free Trial Content - Free Trial Content
Click here to find out more!
Abstract:
An overview is given on both well-known and recently discovered phytoecdyteroids including a sophisticated isolation scheme and notable physiological and pharmacological effects of ecdysteroids on vertebrates. The isolation of pure ecdysteroids has been improved by the use of low-pressure reversed-phase chromatography. An optimized combination of preliminary purification and chromatographic separations results in pure ecdysteroids. Structural elucidation has been done using spectroscopic methods, however, the final proof of the steric structure is rendered using x-ray crystallography.
Ecdysteroid containing preparations show a boom and both OTC products and numerous preparation techniques can be found using the Internet. This paper will give a review on the kaleidoscope of pharmacological effects attributed to the ecdysteroids, such as:
• An increase of protein synthesis (for body-building, AIDS, patients with neoplasm disease, etc.), and other body functions;
• Antidepressant effect; • Shielding the body from stress, and improve the physical and sexual performance; • Prevention from infections and certain diseases. A list of recent offers of ecdysteroid-containing products will also be given. The perspective use of ecdysteroids is promising in genetics. Steroid regulation of programmed cell death during development and differentiation has recently come to the limelight. Murine model of human diseases and its influencing with ecdysteroids are detailed.
Phytoecdysteroids and Anabolic-Androgenic Steroids - Structure and Effects on Humans
Authors: Bathori, Maria1; Toth, Noemi1; Hunyadi, Attila1; Marki, Arpad1; Zador, Erno1
Source: Current Medicinal Chemistry, Volume 15, Number 1, January 2008 , pp. 75-91(17)
Publisher: Bentham Science Publishers
* < previous article
* |
* next article >
* |
* view table of contents
Key:
Free Content - Free Content
New Content - New Content
Subscribed Content - Subscribed Content
Free Trial Content - Free Trial Content
Click here to find out more!
Abstract:
Phytoecdysteroids are structural analogs of the insect molting hormone ecdysone. Plants comprise rich sources of ecdysteroids in high concentration and with broad structural diversity. Ecdysteroids have a number of proven beneficial effects on mammals but the hormonal effects of ecdysteroids have been proven only in arthropods. Their structures are somewhat similar to those of the vertebrate steroid hormones but there are several structural differences between the two steroid groups. Despite of these essential structural differences, ecdysteroids exert numerous effects in vertebrates that are similar to those of vertebrate hormonal steroids, and they may serve as effective anabolic, hepatoprotective, immunoprotective, antioxidant and hypoglycemic agents.
Ecdysteroids do not bind to the cytosolic steroid receptors, instead, they are likely to influence signal transduction pathways, like the anabolic steroids, possibly via membrane bound receptors.
The application of phytoecdysteroids is a promising alternative to the use of anabolic-androgenic steroids because of the apparent lack of adverse effects. The prospective use of phytoecdysteroids may extend to treatments of pathological conditions where anabolic steroids are routinely applied. One of the most cited aspects of phytoecdysteroid application (on the Internet) is the increase of muscle size. However in this field too stringent research is needed as an adequate cytological explanation is not yet available for the anabolic.
This paper reports on the most important structural differences between androgenic hormones, their synthetic analogs and ecdysteroids. The anabolic/hormonal effects and the possible mechanisms of action of these compounds are also discussed as concerns the skeletal muscle.
20-Hydroxyecdysone increases fiber size in a muscle-specific fashion in rat
Phytomedicine, Volume 15, Issue 9, Pages 691-698
N. Tóth, A. Szabó, P. Kacsala, J. Héger, E. Zádor
You can get the full-text article here... ...if you are:
* healthcare practitioner
* interested in pay-per-view article purchase
* visitor or subscriber to the website
* student or faculty member
* researcher or librarian
* visitor or subscriber to the journal website
Learn which websites I use (cookies required)
Update your website selections
Abstract
20-Hydroxyecdysone (20E) is an ecdysteroid hormone that regulates moulting in insects. Interestingly, 20E is also found most abundantly in plant species and has anabolic effects in vertebrates, i.e. increasing muscle size without androgen influence. The effect of 20E on slow and fast fiber types of skeletal muscle has not been reported yet. Here we present that 20E affects the size (cross-sectional area, CSA) of the different fiber types in a muscle-specific manner. The effect on fiber size was modified by the distance from the site of the treatment and the presence of a regenerating soleus muscle in the animal. Besides the fiber size, 20E also increased the myonuclear number in the fibers of normal and regenerating muscles, suggesting the activation of satellite cells. According to our results 20E may provide an alternative for substitution of anabolic–androgenic steroids in therapeutic treatments against muscle atrophy.
Beneficial effects of β-Ecdysone on the joint, epiphyseal cartilage tissue and trabecular bone in ovariectomized rats
Phytomedicine, Volume 17, Issue 5, Pages 350-355
P. Kapur, W. Wuttke, H. Jarry, D. Seidlova-Wuttke
You can get the full-text article here... ...if you are:
* healthcare practitioner
* interested in pay-per-view article purchase
* visitor or subscriber to the website
* student or faculty member
* researcher or librarian
* visitor or subscriber to the journal website
Learn which websites I use (cookies required)
Update your website selections
Abstract
Ecdysteroids are steroids found in invertebrates and plants. In mammals they have protein anabolic effects. We have recently published antiosteoporotic effects of Tinospora cordifolia (TC) extract and the search for the possible active ingredients yielded the presence of β-Ecdysone (Ecd). Therefore, we investigated the effects of pure Ecd in ovariectomized rats on morphological changes in joint, epiphyseal cartilage and trabecular tissue. Following ovariectomy rats were fed for 1 month with Ecd containing food at a dose of 52.8mg/day/animal. Positive and negative control animals received 17-β Estradiol (E2, 132μg/day/animal) and soy free (sf) food respectively. At sacrifice, specimens consisting of upper tibiae-lower femurs and knee joint were harvested and processed for histomorphometry. The parameters measured included thickness of the joint cartilage, thickness of the whole epiphyseal growth plate and its three zones. Furthermore, the percentage of trabecular bone in the metaphysis region of tibiae was quantified. Ecd and E2 induced a significant increase in the thickness of joint cartilage. The whole epiphyseal growth plate and its proliferative and hypertrophic zones were also increased by Ecd whereas E2 reduced their size. The percentage of trabecular area in the metaphysis of tibia was significantly increased in Ecd and E2 treated animals. Results provide a plausible explanation for the antiosteoporotic effects of TC. Hence, TC as well as other Ecd producing plants or pure Ecd may be of value in the prevention and treatment of osteoporosis and osteoarthritis which is of increasing importance due to aging and obesity among individuals.
Effects and applications of arthropod steroid hormones (ecdysteroids) in mammals
Laurence Dinan and René Lafont1
Department of Biological Sciences, University of Exeter, Exeter, Devon EX4 4PS, UK
1 Laboratoire Protéines: Biochimie Structurale et Fonctionnelle, Université Pierre et Marie Curie, 7 Quai St. Bernard, F-75252 Paris 05, France
(Requests for offprints should be addressed to L Dinan who is now at 30 Hederman Close, Silverton, Nr. Exeter, Devon EX5 4HW, UK; Email:
laurie@dinan.wanadoo.co.uk)
Zooecdysteroids (arthropod steroid hormones) regulate the development of arthropods and probably many other invertebrates. Phytoecdysteroids are analogues occurring in a wide range of plant species, where they contribute to the deterrence of phytophagous invertebrates. The purpose of this short review is to summarise findings on the occurrence, metabolism and pharmacological effects of ecdysteroids in mammalian systems and to draw attention to their potential applications, particularly in gene-switch technology, where ecdysteroid analogues (steroidal and non-steroidal) can be used as effective and potent elicitors.
[Effect of vitamin D3 and 20-hydroxyecdysone on the content of ATP, creatine phosphate, carnosine and Ca2+ in skeletal muscles]
[Article in Russian]
Kholodova IuD, Tugaĭ VA, Zimina VP.
A.V. Palladin Institute of Biochemistry, National Academy of Sciences of Ukraine, Kyiv.
The effect of vitamin D3, 20-hydroxyecdysone and extract from Serratula coronata containing 20-hydroxyecdysone on the level of basic metabolites in the skeletal muscles of rats has been studied. It was shown that development of D-hypovitaminosis is accompanied by the decrease in content of ATP, creatine phosphate, carnosine, and by the increase of Ca2+ content. Against the background of D-hypovitaminosis the 20-hydroxyecdysone and the extract from Serratula coronata which contains 20-hydroxyecdysone promote the increase of the amount of these metabolites up to the control of one and normalize Ca2+ content in them.
[Effect of vitamin D3 and 20-hydroxyecdysone on the content of ATP, creatine phosphate, carnosine and Ca2+ in skeletal muscles]
[Article in Russian]
Kholodova IuD, Tugaĭ VA, Zimina VP.
A.V. Palladin Institute of Biochemistry, National Academy of Sciences of Ukraine, Kyiv.
The effect of vitamin D3, 20-hydroxyecdysone and extract from Serratula coronata containing 20-hydroxyecdysone on the level of basic metabolites in the skeletal muscles of rats has been studied. It was shown that development of D-hypovitaminosis is accompanied by the decrease in content of ATP, creatine phosphate, carnosine, and by the increase of Ca2+ content. Against the background of D-hypovitaminosis the 20-hydroxyecdysone and the extract from Serratula coronata which contains 20-hydroxyecdysone promote the increase of the amount of these metabolites up to the control of one and normalize Ca2+ content in them.
Effects of Methoxyisoflavone, Ecdysterone, and Sulfo-Polysaccharide Supplementation on Training Adaptations in Resistance-Trained Males
Colin D Wilborn,1 Lemuel W Taylor,2 Bill I Campbell,3 Chad Kerksick,4 Chris J Rasmussen,3 Michael Greenwood,3 and Richard B Kreidercorresponding author3
1Human Performance Lab, University of Mary Hardin Baylor, Belton, TX
2Exercise Physiology Lab, University of West Florida, Pensacola, FL
3Exercise and Sport Nutrition Laboratory, Baylor University, Waco, TX
4Applied Biochemistry and Molecular Physiology Laboratory, University of Oklahoma, Norman, OK
corresponding authorCorresponding author.
Richard B Kreider:
richard_kreider@baylor.eduReceived September 8, 2006; Accepted November 16, 2006.
* Other Sections▼
o Abstract
o Introduction
o Methodology
o Results
o Discussion
o References
Abstract
Purpose
Methoxyisoflavone (M), 20-hydroxyecdysone (E), and sulfo-polysaccharide (CSP3) have been marketed to athletes as dietary supplements that can increase strength and muscle mass during resistance-training. However, little is known about their potential ergogenic value. The purpose of this study was to determine whether these supplements affect training adaptations and/or markers of muscle anabolism/catabolism in resistance-trained athletes.
Methods
Forty-five resistance-trained males (20.5 ± 3 yrs; 179 ± 7 cm, 84 ± 16 kg, 17.3 ± 9% body fat) were matched according to FFM and randomly assigned to ingest in a double blind manner supplements containing either a placebo (P); 800 mg/day of M; 200 mg of E; or, 1,000 mg/day of CSP3 for 8-weeks during training. At 0, 4, and 8-weeks, subjects donated fasting blood samples and completed comprehensive muscular strength, muscular endurance, anaerobic capacity, and body composition analysis. Data were analyzed by repeated measures ANOVA.
Results
No significant differences (p > 0.05) were observed in training adaptations among groups in the variables FFM, percent body fat, bench press 1 RM, leg press 1 RM or sprint peak power. Anabolic/catabolic analysis revealed no significant differences among groups in active testosterone (AT), free testosterone (FT), cortisol, the AT to cortisol ratio, urea nitrogen, creatinine, the blood urea nitrogen to creatinine ratio. In addition, no significant differences were seen from pre to post supplementation and/or training in AT, FT, or cortisol.
Conclusion
Results indicate that M, E, and CSP3 supplementation do not affect body composition or training adaptations nor do they influence the anabolic/catabolic hormone status or general markers of catabolism in resistance-trained males.
Human urinary excretion profiles after exposure to ecdysterone. (2008)
* Bolduc, Timothy Michael.
Abstract
20-hydroxyecdysone (20E) is the active component of several nutritional supplements, which are becoming popular alternatives to anabolic-androgenic steroids for enhancement of athletic performance. Supplements containing 20E are promoted to increase muscle growth and decrease fat mass, with limited side effects. Limited data regarding the quantitative excretion of 20E in human urine are available. The purpose of this study was to investigate the excretion of 20E after single-day (SD) and multiple-day (MD) administration, and to determine if alterations to the urinary endogenous steroid profiles occur. Male and female subjects received both SD and MD 20E. Urine was collected for up to 7 days after the final administration. A liquid chromatography-quadrupole-time-offlight mass spectrometry (LC-Q-TOF) method was developed and validated for the detection and quantitation of 20E and its metabolite, 2-deoxy-20-hydroxyecydsone (2d), in human urine, following solid phase extraction. The nutritional supplement was also analyzed to determine the presence of banned substances of abuse. The urine concentrations of unconjugated 20E and 2d were 5,313.9 ± 1,092.4 |j,g/day and 70.2 ± 18.6 |Lig/day, respectively, 0-24 h after dosing in the SD protocol. In the MD protocol, the concentrations of 20E and 2d ranged from 3,269.4 ± 976.8 to 5,471.3 ± 2,093.1 ng/day, and 43.7 ± 23.8 to 76.8 ± 30.8 ng/day, respectively, during the 5 days of dosing. The urine 20E concentrations returned to baseline by 48 h for both protocols. Urine 2d concentrations remained detectable up to 168 h for both protocols, for several subjects. No differences in urine concentrations were found between the hydrolyzed and nonhydrolyzed urine. An additional metabolite, with an identical m/z and similar retention time to 2d was detected in all patient samples. This metabolite's peak intensity ranged from approximately 7 to 11 fold greater than that for 2d. No changes were found in the total daily urinary excretion of the endogenous steroids, testosterone, epitestosterone, androsterone, and etiocholanolone. These data demonstrate that 20E and 2d, as well as an unidentified metabolite, are excreted in human urine for up to 48 h after administration. These data also indicate that consumption of a 20E-containing supplement does not alter endogenous urinary steroid profiles.. Master of Science;. USADA Grant 2409166 and the SMRTL research fund.
0-Hydroxyecdysone decreases weight and hyperglycemia in a diet-induced obesity mice model
Pablo Kizelsztein,1 Dmitry Govorko,1 Slavko Komarnytsky,1 Alysa Evans,1 Zhong Wang,2 William T. Cefalu,2 and Ilya Raskin1
1Biotech Center, Rutgers University, New Brunswick, New Jersey; and 2Pennington Biomedical Research Center, Baton Rouge, Louisiana
Submitted 17 September 2008 ; accepted in final form 30 December 2008
The steroid hormone 20-hydroxyecdysone (20HE) is an essential signaling molecule that modulates molting response in insects and may function as a putative anabolic factor in vertebrate animals, although no mammalian 20HE receptor has been identified. Here we show that in H4IIE cell culture, 20HE treatment decreased expression of phosphoenolpyruvate carboxykinase (PEPCK) and glucose-6-phosphatase (G6Pase), reduced glucose production, and induced Akt2 phosphorylation sensitive to the phosphoinositide-3 kinase pathway-specific inhibitor LY-294002. Daily oral administration of 20HE (10 mg/kg for 13 wk) ameliorated obesity and insulin resistance in C57BL/6J mice fed a high-fat diet and produced a significant decrease of body weight gain and body fat mass compared with nontreated animals as demonstrated by dual-energy X-ray absorptiometry analysis. In addition, plasma insulin levels and glucose tolerance were significantly lowered by 20HE treatment. These changes were accompanied by the reduced hepatic expression of PEPCK and G6Pase and increased adiponectin production by visceral fat tissue. These studies demonstrate the anti-obesity and anti-diabetic effects of 20HE and begin to elucidate its putative cellular targets both in vitro and in vivo.
[A comparative study of the anabolic action of ecdysten, leveton and Prime Plus, preparations of plant origin]
[Article in Russian]
Gadzhieva RM, Portugalov SN, Paniushkin VV, Kondrat'eva II.
A new class of anabolic substances includes different saponins, originated from Leuzea rhaponticum sp. The effect of these substances on the human body was studied by caliperometric measurements of body folds. All tested substances taken orally for three weeks diminished fat content under conditions of daily aerobic-anaerobic training. Ekdisten and Prime Plus (combination of ekdisten and pure protein) elevated the muscle mass. The same effect of leventon was less pronounced. We showed that all substances studied elevated the magnitude of "total work", estimated per 1 kg of body weight. Ekdisten and Prime Plus again appeared to be most efficient. The prospects of using the saponins in sport medicine are discussed.
Metabolic effects of 20-OH-Ecdysone in ovariectomized rats
Purchase the full-text article
References and further reading may be available for this article. To view references and further reading you must purchase this article.
Dana Seidlova-Wuttkea, Caroline Ehrhardta and Wolfgang WuttkeCorresponding Author Contact Information, a, E-mail The Corresponding Author
a Department of Endocrinology, University Medical Center Göttingen, Georg-August-Universität, Robert-Koch-Strasse, 40, D-37099 Göttingen, Germany
Received 13 July 2009;
revised 11 January 2010;
accepted 15 January 2010.
Available online 25 January 2010.
Abstract
Postmenopausal women develop often obesity which may be prevented by 20-OH-Ecdysone (Ecd). This was investigated in ovariectomized (ovx) rats. They were orally treated with 3 doses of Ecd (18, 56 or 116 mg/day/animal). Positive controls received 159 μg estradiol (E2). Quantitative computer tomography at the level of the abdomen and the metaphysis of the tibia allowed estimation of surface, fat depots and muscles. The highest dose of Ecd resulted in serum concentrations of 0.4 × 10−6 M. Serum E2 concentrations in the positive controls were 73.3 ± 24.41 pg/ml. E2 but not Ecd stimulated uterine weights. Under Ecd ovx animals gained less fat but had more muscle mass. Serum TSH, T4 and T3 levels remained unaffected while E2 treatment increases T4 but decreases T3 levels. Ecd at the lowest dose lowered serum LDL and did not result in increased serum triglycerides, an effect seen in the E2 treated rats. At the Ecd highest dose serum HDL was higher than in the controls.
In conclusion Ecd has beneficial effects on fat and muscle tissue and may be able to prevent the metabolic syndrome and sarcopenia by a non-estrogenic mechanism.
