Crustecdysone is without estrogenic or antiestrogenic activity in the rat

Prabhu, V. K. K.; Nayar, K. K.

doi:10.1007/bf01924207

Cited by 8 publications

(7 citation statements)

References 7 publications

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“…The effects are similar to those of testosterone-related anabolic steroids, but the negative side effects observed with these compounds are supposedly not associated with ecdysteroids (summarized in Sláma and Lafont, 1995). They also appear not to have androgenic or (anti)oestrogenic effects (Prabhu and Nayar, 1974). However, in a recent double-blind, placebo-controlled trial involving resistance-trained male humans, 30 mg 20E/day did not significantly affect anabolic or catabolic responses to resistance training (Wilborn et al, 2006).…”

Section: Pharmaceutical Applicationsmentioning

confidence: 96%

The Karlson Lecture. Phytoecdysteroids: What use are they?

Dinan

2009

Arch Insect Biochem Physiol

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Phytoecdysteroids are analogues of arthropod steroid hormones found in plants, where they deter predation by non-adapted predators. There is potential to exploit this to develop new strategies for pest control, either by using ecdysteroids as lead molecules for the design of novel pest control agents or by alteration of ecdysteroid levels/profiles in crop plants through plant breeding or genetic modification. However, it is other properties of phytoecdysteroids that have led to a rapid recent increase in scientific and commercial interest in these molecules. They are apparently non-toxic to mammals and a wide range of beneficial pharmacological (adaptogenic, anabolic, anti-diabetic, hepatoprotective, immunoprotective, wound-healing, and perhaps even anti-tumour) activities is claimed for them. In particular, this has led to a large (and unregulated) market for ecdysteroid-containing preparations for body-builders, sportsmen, and pets, among others. Ecdysteroids are also being considered as nutraceutical additives to food products. Further, ecdysteroids are good candidates as elicitors for gene-switch systems to be used in medical gene therapy and research applications. In this article, I review the applications of phytoecdysteroids and assess their future potential.

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Section: Pharmaceutical Applicationsmentioning

confidence: 96%

The Karlson Lecture. Phytoecdysteroids: What use are they?

Dinan

2009

Arch Insect Biochem Physiol

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“…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.…”

Section: Pharmacological Effects Of Ecdysteroids On Vertebratesmentioning

confidence: 99%

Practical uses for ecdysteroids in mammals including humans: and update

Lafont

Dinan

2003

Journal of Insect Science

127

111

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Ecdysteroids are widely used as inducers for gene-switch systems based on insect ecdysteroid receptors and genes of interest placed under the control of ecdysteroid-response elements. We review here these systems, which are currently mainly used in vitro with cultured cells in order to analyse the role of a wide array of genes, but which are expected to represent the basis for future gene therapy strategies. Such developments raise several questions, which are addressed in detail.First, the metabolic fate of ecdysteroids in mammals, including humans, is only poorly known, and the rapid catabolism of ecdysteroids may impede their use as in vivo inducers.A second set of questions arose in fact much earlier with the pioneering “heterophylic” studies of Burdette in the early sixties on the pharmacological effects of ecdysteroids on mammals. These and subsequent studies showed a wide range of effects, most of them being beneficial for the organism (e.g. hypoglycaemic, hypocholesterolaemic, anabolic). These effects are reviewed and critically analysed, and some hypotheses are proposed to explain the putative mechanisms involved.All of these pharmacological effects have led to the development of a wide array of ecdysteroid-containing preparations, which are primarily used for their anabolic and/or “adaptogenic” properties on humans (or horses or dogs). In the same way, increasing numbers of patents have been deposited concerning various beneficial effects of ecdysteroids in many medical or cosmetic domains, which make ecdysteroids very attractive candidates for several practical uses.It may be questioned whether all these pharmacological actions are compatible with the development of ecdysteroid-inducible gene switches for gene therapy, and also if ecdysteroids should be classified among doping substances.20E20-hydroxyecdysone2d20E2-deoxy-20-hydroxyecdysone2dE2-deoxyecdysoneBAHbisacylhydrazineBmEcRBombyx mori EcRCfEcRChoristoneura fumiferana EcRCfUSPChoristoneura fumiferana USPCHOChinese hamster ovaryCMVcytomegalovirusDBDDNA-binding domainDmEcRDrosophila melanogaster EcRAbbEecdysoneEcRecdysteroid receptorEcREecdysteroid response elementEHTeffective half-timeEREoestrogen response elementGRglucocorticoid receptorGREglucocorticoid response elementHEKhuman embryonic kidneyHvEcRHeliothis virescens EcRLBDligand binding domainmurAmuristerone APKAprotein kinase ApolBpolypodine BponAponasterone APPARperoxisome proliferator-activated receptorRARretinoic acid receptorRXRretinoid X receptorTRthyroid receptorUSPultraspiracleVDRvitamin D receptorVEGFvascular endothelial growth factor

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“…This yields more anabolic steroids, but in parallel the androgenic activity also increased as observed for 4-chloro-methyltestosterone (35) or fluoxymesterone (43) relative to methyltestosterone (33) (on the basis of nitrogen retention following oral administration) [86,91].…”

Section: Amentioning

confidence: 99%

“…The possibility of estrogenic or antiestrogenic effects of 20-hydroxyecdysone (6) was investigated by Prabhu & Nayar [35]. In intravaginal doses of 30-500 μg, it was compared with 17 -estradiol dipropionate in adult female rats.…”

Section: Hormonal Activity On Mammalsmentioning

confidence: 99%

Phytoecdysteroids and Anabolic-Androgenic Steroids - Structure and Effects on Humans

Báthori¹,

Tóth²,

Hunyadi³

et al. 2008

CMC

167

168

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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.

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Crustecdysone is without estrogenic or antiestrogenic activity in the rat

Cited by 8 publications

References 7 publications

The Karlson Lecture. Phytoecdysteroids: What use are they?

The Karlson Lecture. Phytoecdysteroids: What use are they?

Practical uses for ecdysteroids in mammals including humans: and update

Phytoecdysteroids and Anabolic-Androgenic Steroids - Structure and Effects on Humans

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