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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.
• 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.
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.
According to our results 20E may provide an alternative for substitution of anabolic–androgenic steroids in therapeutic treatments against muscle atrophy.
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.
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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.
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.
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..
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.
All tested substances taken orally for three weeks diminished fat content under conditions of daily aerobic-anaerobic training. Ekdisten (ecdysten) and Prime Plus (combination of ekdisten and pure protein) elevated the muscle mass.
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.
Ecdysteroids and physical performance20E is claimed to have tonic properties (Abubakirov et al., 1988). Indeed it stimulates muscle growth, provided that protein supply is adequate. Such anabolic effects result in increased physical performance without training (Chermnykh et al., 1988). This was for instance demonstrated using the forced swimming test with rats: animals given ecdysteroids for one week were able to swim for significantly longer times (Azizov and Seifulla, 1998). These effects are similar to those of anabolic steroids. 20E is also able to increase muscle ATP content in vitamin D-deprived rats (Kholodova et al., 1997).
Ecdysteroids and growth (Table 2)The anabolic effects of several phytoecdysteroids (20E, cyasterone, turkesterone, viticosterone E – see structures on Ecdybase) on mice or rats were reported long ago (see e.g. Okui et al., 1968; Syrov and Kurmukov, 1975a&b; 1976a–c, Syrov et al., 1978, 1981a; Stopka et al., 1999). Growth-promoting effects have also been more recently reported for pigs (Kratky et al., 1997) and Japanese quails (Koudela et al., 1995; Sláma et al., 1996). In many instances however, these effects are not spectacular when considering the growth (weight) curves as they are observed during certain phases of growth or for one sex only and, in many cases, adequate statistical analyses are lacking. Nevertheless, even small effects (i.e. <5 % increase) on growth could be of economical interest for nutritionists, but their firm establishment requires the use of large numbers of animals, which is hardly feasible with large mammals. The addition of E to sheep food increases body growth rate and also wool growth (Purser and Baker, 1994). Surprisingly, these effects were obtained with minute amounts of ecdysone (0.02 µg/kg per day!), and were more evident when animals were fed on a poor quality diet, which indicates that E improves food utilization. In this case, it has been suggested that the effect results from the toxicity of E towards rumen protozoa, but this has not been fully established. In fact, through a stimulation of protein synthesis (and/or a reduction of protein catabolism), ecdysteroids would increase the lean body mass. In pigs, doses of 0.2–0.4 mg/kg/day resulted in better nitrogen retention and a body weight increase of 112–116% relative to controls, while food consumption was lowered by 11–17% (Kratky et al., 1997). Other experiments used diets supplemented with ecdysteroid-containing plants (e.g. Rhaponticum carthamoides) and reported similar growth-promoting effects on pigs over a 30-day period (Selepcova et al., 1993b). In quails, 20E in the diet promoted increased growth (115% of controls), but this was associated with a decreased index of food conversion (Sláma et al., 1996). From these data, it appears difficult to draw general conclusions.
Ecdysteroids and protein synthesisStimulatory effects of ecdysone on protein synthesis were reported as early as 1963 (Burdette and Coda, 1963), and the discovery of phytoecdysteroids made these molecules available in large amounts for pharmacological assays. It was rapidly shown that ecdysteroids were able to stimulate protein synthesis in mouse liver (Okui et al., 1968; Otaka et al., 1968, 1969a&b). In fact, it was shown that 20E stimulates the incorporation of [14C]leucine in a cell-free translation system (rat liver polysomes), i.e. it increases the efficiency of the translational machinery (Syrov et al., 1978). Such conclusions have been confirmed and extended to other tissues, especially heart and muscles (Syrov et al., 1975a; Aizikov et al., 1978; Khimiko et al., 2000). Recent structure-activity studies (Syrov et al., 2001) as measured by a stimulation of [14C] aminoacid incorporation into proteins showed that among the compounds tested turkesterone was the most active, followed by cyasterone and 20E.
Ecdysteroids and glucose metabolismIt was shown early on (Table 3) that 20E given per os to rats reduces hyperglycaemia induced either by glucagon or by alloxan treatment (Matsuda et al., 1970; Uchiyama and Ogawa, 1970; Yoshida et al., 1971, Uchiyama and Yoshida, 1974). In fact, 20E stimulates the incorporation of glucose into glycogen and protein in mouse liver (Yoshida et al., 1971) and more generally it enhances glucose utilization by tissues (Syrov et al., 1997a). The mechanism involved seems to be an increase of tissue sensitivity to insulin (Kosovsky et al., 1989) and preparations containing phytoecdysteroids have been proposed as oral antidiabetics (Takahashi and Nishimoto, 1992; Yang et al., 2001). Depending on the extent of hyperglycaemia, phytoecdysteroid effects may be more or less pronounced that those of manilil, a widely used pharmacological molecule (Kutepova et al., 2001).
Ecdysteroids and lipid metabolismEcdysteroids display hypocholesterolaemic effects (Lupien et al., 1969; Mironova et al., 1982; Syrov et al., 1983), through a reduction of cholesterol biosynthesis and an increase of its catabolism (Uchiyama and Yoshida, 1974). 20E (5 mg/kg per os) stimulates the conversion of cholesterol into bile acids in rats (Syrov et al., 1986b), and such an effect is reminiscent of some oxysterols (Schroepfer, 2000). In connection with these effects, ecdysteroids may also have antiatherosclerotic actions (Matsuda et al., 1974; Syrov et al., 1983). Intraperitoneally injected 20E (0.5 mg/kg in rats) also enhances [14C]acetate incorporation into liver triglycerides and reduces triglyceride lipase activity (Catalán et al., 1985).
Ecdysteroids are not toxic to vertebrates: ecdysteroids have a very low toxicity (LD50 > 6g/kg), they are not hypertensive and, in spite of their anabolic action, they would have neither androgenic nor oestrogenic (or antioestrogenic) effects; they induce no virilisation and they do not induce significant changes in castrated animals (e.g. Prabhu and Nayar, 1974). All together this suggests that ecdysteroids are attractive compounds for a wide array of uses, which have been proposed, and of course it would be of particular interest to understand more precisely their mode(s) of action in mammals.
