Practical uses for ecdysteroids in mammals including humans: and update

Lafont, R.; Dinan, L.

doi:10.1093/jis/3.1.7

Cited by 196Hormonal and reproductive studiesSteroid Chemistry and BiochemistryEstrogen and related hormone effects

Practical uses for ecdysteroids in mammals including humans: and update

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Lafont, R., Dinan, L.·2003·Journal of Insect Science

DOI 10.1093/jis/3.1.7PMC PMC524647

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Abstract

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.

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Phytoecdysteroids have been shown to stimulate growth in several animal species, including mice, rats, sheep, pigs, and quail.
“Indeed, phytoecdysteroids have been shown to stimulate growth in several animal species, including mice [4, 15], rats, sheep, pigs, and quail [16].”
From Acute and chronic effects of Rhaponticum carthamoides and Rhodiola rosea extracts supplementation coupled to resistance exercise on muscle protein synthesis and mechanical power in rats (2020) · cites this paper as [16]
Ecdysterone possesses a variety of beneficial pharmacological effects on humans, including anabolic and adaptogenic ones.
“However, ecdysterone possesses a variety of beneficial pharmacological effects on humans, including anabolic and adaptogenic ones (Báthori et al., 2008).”
From An Arthropod Hormone, Ecdysterone, Inhibits the Growth of Breast Cancer Cells via Different Mechanisms (2020) · cites this paper as Lafont and Dinan, 2003
Phytoecdysteroids possess a wide range of potentially therapeutic properties for humans, including anabolic, adaptogenic, hepatoprotective, spasmolytic and anti-inflammatory activity.
“Phytoecdysteroids are acknowledged today to possess a wide range of potentially therapeutic properties for humans, including anabolic [10], adaptogenic [11], hepatoprotective [12], spasmolytic [13] and anti-inflammatory activity [14].”
From Ecdysteroid Content and Therapeutic Activity in Elicited Spinach Accessions (2020) · cites this paper as [11]

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Tumor suppressor protein VHL is induced at high cell density and mediates contact inhibition of cell growth
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p27Kip1‐mediated controlled proliferation technology increases constitutive sICAM production in CHO‐DUKX adapted for growth in suspension and serum‐free media
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A Chimeric Ecdysone Receptor Facilitates Methoxyfenozide-Dependent Restoration of Male Fertility in ms45 Maize
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Ecdysteroids in Spinacia oleracea and Chenopodium bonus-henricus
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Stimulation of Protein Synthesis in Mouse Liver by Insect-Moulting Steroids
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“…effects of ecdysteroids on vertebrates The pharmacological actions of ecdysteroids on vertebrates have been reviewed in several previous articles (Burdette, 1962, 1972; Ogawa et al., 1974; Syrov, 1984, 1994; Sláma and Lafont, 1995; Xu et al., 1997; Syrov, 2000; Kholodova, 2001; Báthori, 2002).”
Background
Nongenomic effects of ecdysteroids
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Developmental Genetics
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Immunomodulating effects of the hydrolysis products of formosanin C and beta-ecdysone from Paris formosana Hayata.
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Evaluation of the tetracycline‐ and ecdysone‐inducible systems for expression of neurotransmitter receptors in mammalian cells
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Protection against chemotherapy-induced cytotoxicity by cyclin-dependent kinase inhibitors (CKI) in CKI-responsive cells compared with CKI-unresponsive cells
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Electrophysiological responses of gustatory sensilla of Mamestra brassicae (Lepidoptera, Noctuidae) larvae to three ecdysteroids: ecdysone, 20-hydroxyecdysone and ponasterone A
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Molecular cloning and expression of Tenebrio molitor ultraspiracle during metamorphosis and in vivo induction of its phosphorylation by 20‐hydroxyecdysone
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Involvement of the Fungal Nuclear Migration Gene nudC Human Homolog in Cell Proliferation and Mitotic Spindle Formation
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Stimulatory Effect of Insect-Metamorphosing Steroids from Achyranthes and Cyathula on Protein Synthesis in Mouse Liver
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[The action of methandrostenolone and ecdysterone on the physical endurance of animals and on protein metabolism in the skeletal muscles].
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Alterations in Rat Lipid Metabolism Following Ecdysterone Treatment
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Study of excretion of ecdysterone in human urine
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Pharmacology of Ecdysones in Vertebrates
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Self-citation
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Ecdysone-controlled expression of transgenes
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V642I APP-Inducible Neuronal Cells: A Model System for Investigating Alzheimer's Disorders
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Cloning and characterization of CcEcR
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Reconstruction of Ligand-Dependent Transactivation of Choristoneura fumiferana Ecdysone Receptor in Yeast
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Koudela K Tenora J Bajer J Mathova A Sláma K 1995 Stimulation of growth and development in Japanese quails after oral administration of ecdysteroid-containing diet European Journal of Entomology 92 349 354
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Wu X Lin S Yang Y Feng S 1998b Effects of ecdysterone on human umbilical vein endothelial cells injuried by tumor necrosis factor Chinese Journal of Pathophysiology 14 58 62
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Effects and applications of arthropod steroid hormones (ecdysteroids) in mammals
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Phytoecdysteroids increase protein synthesis in skeletal muscle cells.
Gorelick-Feldman, J., MacLean, D., Ilic, N., Poulev, A., Lila, M. A., Cheng, D., & Raskin, I. (2008) · Journal of Agricultural and Food Chemistry · doi:10.1021/jf073059z · Cited by 166 · see citing works
Ecdysteroids as non-conventional anabolic agent: performance enhancement by ecdysterone supplementation in humans
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Quinoa Extract Enriched in 20‐Hydroxyecdysone Protects Mice From Diet‐Induced Obesity and Modulates Adipokines Expression
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Ecdysteroids: Production in plant in vitro cultures
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“…other effects that have been reported include nephroprotective and hepatoprotective activities, increase in bile secretion and restoration of normal glomerular filtration rate (Lafont and Dinan 2003; Dinan and Lafont 2006; Báthori and Pongracz 2005; Festucci-Buselli et al. 2008; Graf et al. 2014).”
BackgroundInfluential
Phytoecdysteroids: Diversity, biosynthesis and distribution
Dinan, L., Harmatha, J., Volodin, V., & Lafont, R. (2009) · Ecdysone: Structures and Functions · doi:10.1007/978-1-4020-9112-4_1 · Cited by 77 · see citing works
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Additional minor ecdysteroid components of Leuzea carthamoides
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Hu, J., Luo, C. X., Chu, W. H., Shan, Y. A., Qian, Z.-M., Zhu, G., Yu, Y. B., & Feng, H. (2012) · PLoS ONE · doi:10.1371/journal.pone.0050764 · Cited by 67 · see citing works
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Kapur, P., Wuttke, W., Jarry, H., & Seidlova-Wuttke, D. (2010) · Phytomedicine · doi:10.1016/j.phymed.2010.01.005 · Cited by 66 · see citing works
Ecdysteroids in Spinach (Spinacia oleracea L.): Biosynthesis, Transport and Regulation of Levels
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Ecdysteroid-containing food supplements from Cyanotis arachnoidea on the European market: Evidence for spinach product counterfeiting
Hunyadi, A., Herke, I., Lengyel, K., Báthori, M., Kele, Z., Simon, A., Tóth, G., & Szendrei, K. (2016) · Scientific Reports · doi:10.1038/srep37322 · Cited by 59 · see citing works
Plant ecdysteroids: plant sterols with intriguing distributions, biological effects and relations to plant hormones
Tarkowská, D., & Strnad, M. (2016) · Planta · doi:10.1007/s00425-016-2561-z · Cited by 56 · see citing works
Comparison between the Biological Active Compounds in Plants with Adaptogenic Properties (Rhaponticum carthamoides, Lepidium meyenii, Eleutherococcus senticosus and Panax ginseng)
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Ecdysteroids
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Effects of the combination of high-intensity interval training and Ecdysterone on learning and memory abilities, antioxidant enzyme activities, and neuronal population in an Amyloid-beta-induced rat model of Alzheimer’s disease
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Continuous infusion of 20-hydroxyecdysone increased mass of triceps brachii in C57BL/6 mice
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Backstabbing P-gp: Side-Chain Cleaved Ecdysteroid 2,3-Dioxolanes Hyper-Sensitize MDR Cancer Cells to Doxorubicin without Efflux Inhibition
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Effects of plant hormones and 20-hydroxyecdysone on tomato (Lycopersicum esculentum) seed germination and seedlings growth
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An Arthropod Hormone, Ecdysterone, Inhibits the Growth of Breast Cancer Cells via Different Mechanisms
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Proapoptotic and proautophagic activity of 20-hydroxyecdysone in breast cancer cells in vitro
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“Indeed, phytoecdysteroids have been shown to stimulate growth in several animal species, including mice [4, 15], rats, sheep, pigs, and quail [16].”
Background
Protective effects of 20‐hydroxyecdysone on CoCl2‐induced cell injury in PC12 cells
Hu, J., Zhao, T. Z., Chu, W. H., Luo, C. X., Tang, W. H., Yi, L., & Feng, H. (2010) · Journal of Cellular Biochemistry · doi:10.1002/jcb.22877 · Cited by 26 · see citing works
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Ecdysteroid derivatives that reverse P-glycoprotein-mediated drug resistance
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Ecdysteroid Content and Therapeutic Activity in Elicited Spinach Accessions
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Self-citation
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Effects ofLeuzea carthamoideson Human Breast Adenocarcinoma MCF-7 Cells Determined by Gene Expression Profiling and Functional Assays
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Low-polarity phytoecdysteroids from the juice of Serratula coronata L. (Asteraceae)
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Self-citation
Urinary Elimination of Ecdysterone and its Metabolites following a Single-Dose Administration in Humans
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Background
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Authors: Lafont, R., & Dinan, L.
Affiliations: Université Pierre-et-Marie-Curie (FR)
University of Exeter (GB)
ORCID: Lafont, R.
Dinan, L.
Venue: Journal of Insect Science
Publisher: Oxford University Press (OUP)
Published: 2003
Volume: 3
Issue: 1
Pages: 7-7
ISSN: 1536-2442 (ISSN-L)
DOI: 10.1093/jis/3.1.7
PMC: PMC524647
OpenAlex: W2058365346
Cited by: 196
References: 284
Citations by year: 2026: 4 · 2025: 5 · 2024: 5 · 2023: 4 · 2022: 6 · 2021: 20 · 2020: 13 · 2019: 9 · 2018: 9 · 2017: 9 · 2016: 13 · 2015: 8 · 2014: 11 · 2013: 5 · 2012: 15
FWCI: 0.64
Type: journal article
Language: en
Open access: gold
doi.org
Locations: Journal of Insect Science (publishedVersion)
PubMed Central (publishedVersion, other-oa)
PubMed (publishedVersion)
Topics: Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Hormonal and reproductive studies
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Steroid Chemistry and Biochemistry
Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
Keywords: ecdysteroids, ecdysteroid receptor, gene therapy, hypoglycemic effect, hypocholesterolaemic effect, anabolic effects, adaptogenic properties, doping substances, patents
MeSH terms: Animals, Gene Expression Regulation, Humans, Plants, Molecular Structure, Ecdysteroids

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Practical uses for ecdysteroids in mammals including humans: and update

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