The Karlson Lecture. Phytoecdysteroids: what use are they?
Abstract
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. © 2009 Wiley Periodicals, Inc.
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Phytoecdysteroids have beneficial effects on mammals, including anabolic, adaptogenic, antidiabetic, hypolipidemic, and hepatoprotective effects.
“They are known for their numerous beneficial effects on mammals, which include as anabolic, adaptogenic, antidiabetic, hypolipidemic, and hepatoprotective effects150, 151, 152, 153.”
From The Phytochemical, Biological, and Medicinal Attributes of Phytoecdysteroids: An Updated Review (2021) · cites this paper as [151]
20-HE improves dermal thickness and promotes wound-healing in vivo.
“20-HE has been shown to improve dermal thickness151,158 and promote wound-healing in vivo13,150.”
From The Phytochemical, Biological, and Medicinal Attributes of Phytoecdysteroids: An Updated Review (2021) · cites this paper as [151]
Taxons used in traditional medicines such as Leuzea carthamoides, Ajuga turkestanica, and several Pfaffia species have abundant ECs in their roots.
“The taxons that are used in traditional medicines such as Leuzea carthamoides, Ajuga turkestanica, and several Pfaffia species have abundant ECs in their roots.”
From Phytoecdysteroids: Distribution, Structural Diversity, Biosynthesis, Activity, and Crosstalk with Phytohormones (2022) · cites this paper as [32]
Cyanotis vaga and Cyanotis arachnoidea belong to monocot species, and several species of ferns that belong to Polypodium are rich sources of ECs.
“Cyanotis vaga and Cyanotis arachnoidea belong to monocot species, and several species of ferns that belong to Polypodium are rich sources of ECs [7,8,30,31,32,33,34,35].”
From Phytoecdysteroids: Distribution, Structural Diversity, Biosynthesis, Activity, and Crosstalk with Phytohormones (2022) · cites this paper as [32]
Steroid ring structure shows variation that is not significant; substantial variations are found in the number, positioning, and orientation of hydroxyl groups and conjugating groups.
“Steroid ring structure shows variation, which is not significant; substantial variations are found in the number, positioning, and orientation of hydroxyl groups and conjugating groups.”
From Phytoecdysteroids: Distribution, Structural Diversity, Biosynthesis, Activity, and Crosstalk with Phytohormones (2022) · cites this paper as [32]
Several structural modifications are present in different plant families, probably due to different uses of metabolites.
“Several structural modifications are present in different plant families, probably due to different uses of metabolites [4,8,15,32].”
From Phytoecdysteroids: Distribution, Structural Diversity, Biosynthesis, Activity, and Crosstalk with Phytohormones (2022) · cites this paper as [32]
In some cases, the oxo group may be located at different carbon positions, such as C-2, C-12, C-17, C-20, or C-22, along with the required C-6 position.
“In some cases, the oxo group may be located at different carbon positions, such as C-2, C-12, C-17, C-20, or C-22, along with the required C-6 position.”
From Phytoecdysteroids: Distribution, Structural Diversity, Biosynthesis, Activity, and Crosstalk with Phytohormones (2022) · cites this paper as [32]
Ecdysteroids are a,b-unsaturated 6-ketosteroids that occur in a wide range of plant species and are analogs of the insect molting hormone ecdysone.
“Ecdysteroids are a,b-unsaturated 6-ketosteroids that occur in a wide range of plant species; as analogs of the insect molting hormone ecdysone, these compounds possess several biological functions in the flora and the fauna [11,12].”
From Nitrogen-containing ecdysteroid derivatives vs. multi-drug resistance in cancer: Preparation and antitumor activity of oximes, oxime ethers and a lactam (2018) · cites this paper as [12]
PE and FG are under rigorous investigation for their anti-diabetic, weight reducing, cardioprotective, and anticarcinogenic properties.
“while PE and FG are under rigorous investigation for their anti-diabetic, weight reducing, cardioprotective, and anticarcinogenic properties.10, 11, 22, 24”
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“Previous reviews on the bioactivities of phytoecdysteroids highlight their growth-promoting, antidiabetic, immunomodulatory, hepatoprotective, neuroprotective, hypocholesterolemic, wound healing, antidepressive, and antioxidant activities (Lafont and Dinan 2003; Dinan and Lafont 2006; Dinan 2009).”
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“Extracts of plants containing phytoecdysteroids have been used as stress reducers, muscle builders, and adaptogens (Dinan, 2009).”
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Quinoa: From Farm to Traditional Healing, Food Application, and Phytopharmacology
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20-Hydroxyecdysone activates the protective arm of the RAAS via the MAS receptor
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Ecdysteroids in Plants and their Pharmacological Effects in Vertebrates and Humans
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Ajuga remota Benth.: From ethnopharmacology to phytomedical perspective in the treatment of malaria
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Ecdysteroids: Isolation, Chemical Transformations, and Biological Activity
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“The adaptogenic action of ecdysteroids manifested in insects on contact with toxic agents ranging from methanol to chemical insecticides (Dinan, 2009) is associated with the reaction of a set of genes including those encoding ecdysone receptor components (Planelló et al.”
BackgroundTargeting the administration of ecdysterone in doping control samples
Parr, M. K., Ambrosio, G., Wuest, B., Mazzarino, M., de la Torre, X., Sibilia, F., Joseph, J. F., Diel, P., & Botrè, F. (2020) · Forensic Toxicology · doi:10.1007/s11419-019-00504-y · Cited by 38 · see citing works
“Growth promoting and anabolic effects in various animal species including humans have been reported [1-18].”
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Moult induction methods in soft‐shell crab production
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“These bioactivities have thoroughly been reviewed (Dinan, 2009; Laekeman and Vlietinck, 2013), including their most frequently referred non-hormonal, anabolic and adaptogenic, “whole-body strengthening” effect (Bathori et al., 2008) that have led to a worldwide consumption of ecdysteroid-containing…”
BackgroundEcdysteroid signalling in insects—From biosynthesis to gene expression regulation
Yamanaka, N. (2021) · Advances in insect physiology · doi:10.1016/bs.aiip.2021.03.002 · Cited by 32 · see citing works
The minor ecdysteroids from <i>Ajuga turkestanica</i>
Guibout, L., Mamadalieva, N., Balducci, C., Girault, J., & Lafont, R. (2015) · Phytochemical Analysis · doi:10.1002/pca.2563 · Cited by 30 · see citing works
“Most of these effects are probably related to the presence of ecdysteroids (Dinan, 2009).”
Hunyadi, A., Csábi, J., Martins, A., Molnár, J., Balázs, A., & Tóth, G. (2017) · Molecules · doi:10.3390/molecules22020199 · Cited by 31 · see citing works
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“On the other hand, a number of beneficial metabolic effects are attributed to them [4–6], which has encouraged the production and worldwide marketing of many food supplements, mainly containing the isolated ecdysteroid compound 20E [6].”
Background24-Epibrassinolide and 20-hydroxyecdysone affect photosynthesis differently in maize and spinach
Rothová, O., Hola, D., Kočová, M., Tůmová, L., Hnilička, F., Hniličková, H., Kamlar, M., & Macek, T. (2014) · Steroids · doi:10.1016/j.steroids.2014.04.006 · Cited by 29 · see citing works
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Assessing herbal products with health claims
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“The same holds true for their proposed “adaptogenic” effects (Dinan, 2009) and their effects on adipose tissue (Foucault et al., 2011), as well as for other suggested hypocholesterolemic, anti-inflammatory, woundhealing, and anti-osteoporotic effects (Lafont and Dinan, 2003).”
BackgroundPatel, U., Girme, A., Patel, K. G., Ghule, C., Hingorani, L., & Gandhi, T. R. (2021) · Journal of Planar Chromatography – Modern TLC · doi:10.1007/s00764-021-00115-7 · Cited by 23 · see citing works
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“Most of the ecdysteroid action in insects is mediated via nuclear receptors and only some by membrane-bound receptors.(2)”
BackgroundInfluentialSide-chain cleaved phytoecdysteroid metabolites as activators of protein kinase B
Issaadi, H. M., Csábi, J., Hsieh, T., Gáti, T., Tóth, G., & Hunyadi, A. (2018) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2018.10.049 · Cited by 21 · see citing works
Structure–Activity Relationships of Ecdysteroids and Non-Steroidal Ecdysone Agonists
Dinan, L. N., Nakagawa, Y., & Hormann, R. E. (2012) · Advances in insect physiology · doi:10.1016/b978-0-12-391500-9.00003-6 · Cited by 20 · see citing works
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“Since the isolation and identification of the first phytoecdysteroids in the mid-1960s, 487 natural analogues have become listed in the online database of herbal ecdysteroids (last update: August, 2015) [11], and the range of biochemical permutations detected so far suggests that probably > 1,000 analogues could exist…”
Phytoecdysteroids: Phytochemistry and Pharmacological Activity
Laekeman, G., & Vlietinck, A. J. (2013) · Springer eBooks · doi:10.1007/978-3-642-22144-6_173 · Cited by 17 · see citing works
Ambrosio, G., Yuliandra, T., Wuest, B., Mazzarino, M., Torre, X. D. L., Botrè, F., Diel, P., Isenmann, E., & Parr, M. K. (2021) · doi:10.20944/preprints202105.0106.v1 · Cited by 16 · see citing works
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“Literature suggest that they stimulate protein synthesis in animals and humans, and have adaptogenic, antimutagenic, hypocholesterolemic, immunostimulating, nutritive and tonic properties (Lafont and Dinan 2003; Dinan and Lafont 2006; Dinan 2009).”
Major Constituents and Cytotoxic Effects of Ajuga chamaecistus ssp. tomentella
Sadati, N., Jenett‐Siems, K., Siems, K., Ardekania, M. R. S., Hadjiakhoondi, A., Akbarzadeh, T., Ostad, S. N., & Khanavi, M. (2012) · Zeitschrift für Naturforschung C · doi:10.1515/znc-2012-5-606 · Cited by 21 · see citing works
“…et al., 2010), antidiabetic and hypoglycemic (Hamden et al., 2008; Kutepova et al., 2001), hepatoprotective, immunoprotective, wound-healing (Dinan, 2009), antioxidant, and free radical scavenging effects (Cai et al., 2002), and perhaps even antitumour effects (Akbay et al., 2002).”
Backgroundβ-Ecdysone Augments Peak Bone Mass in Mice of Both Sexes
Dai, W., Zhang, H., Zhong, Z. A., Jiang, L., Chen, H., Lay, Y.-A. E., Kot, A., Ritchie, R. O., Lane, N. E., & Yao, W. (2015) · Clinical Orthopaedics & Related Research · doi:10.1007/s11999-015-4246-5 · Cited by 15 · see citing works
“A number of plants produce ecdysteroids that protect them from herbivores [14, 15].”
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Rapid, laser-induced conversion of 20-hydroxyecdysone – A follow-up study on the products obtained
Lai, W.-C., Dankó, B., Csábi, J., Kele, Z., Chang, F., Pascu, M., Gáti, T., Simon, A., Amaral, L., Tóth, G., et al. (2014) · Steroids · doi:10.1016/j.steroids.2014.07.016 · Cited by 14 · see citing works
“Interestingly, ecdysteroids can also exert various rather beneficial effects in vertebrates: a general strengthening, somewhat ‘‘Ginseng-like’’ activity has been attributed to them, which includes a non-hormonal anabolic action and a series of further metabolic effects usually referred to as adaptogenic [2,3].”
Csábi, J., Martins, A., Sinka, I., Csorba, A., Molnár, J., Zupkó, I., Tóth, G., Tillekeratne, L. M. V., & Hunyadi, A. (2016) · MedChemComm · doi:10.1039/c6md00431h · Cited by 13 · see citing works
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“For example, it was useful in fighting diabetes [5, 6], and preventing the body from infections and cancers [7, 8].”
BackgroundTóth, G., Herke, I., Gáti, T., Vágvölgyi, M., Berkecz, R., Parfenova, L. V., Ueno, M., Yokoi, T., Nakagawa, Y., & Hunyadi, A. (2021) · Journal of Natural Products · doi:10.1021/acs.jnatprod.0c01274 · Cited by 12 · see citing works
Urinary Excretion of Ecdysterone and Its Metabolites Following Spinach Consumption
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“Ecdysteroids 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 are claimed for them [6].”
BackgroundHo, R., Teai, T., Meybeck, A., & Raharivelomanana, P. (2015) · Natural Product Communications · doi:10.1177/1934578x1501000110 · Cited by 12 · see citing works
“grossum frond and rhizome extracts contain, as their main bioactive components, phytoecdysteroids such as 20-hydroxyecdysone, known to have many interesting biological activities and considered to be adaptogenic compounds [1].”
Background20-Hydroxyecdysone activates the protective arm of the renin angiotensin system via Mas receptor
Lafont, R., Raynal, S., Serova, M., Didry-Barca, B., Guibout, L., Latil, M., Dilda, P. J., Dioh, W., & Veillet, S. (2020) · doi:10.1101/2020.04.08.032607 · Cited by 11 · see citing works
“Ecdysteroids are a large family of steroids initially discovered in arthropods (zooecdysteroids) and later in plants (phytoecdysteroids) (9).”
BackgroundEcdysteroids as defensive chemicals
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Self-citationNawrot, J., Gornowicz‐Porowska, J., & Nowak, G. (2020) · Molecules · doi:10.3390/molecules25225329 · Cited by 11 · see citing works
“development of new pharmaceutical products [9].”
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Phytoecdysteroid and Clerodane Content in Three Wild <i>Ajuga</i> Species in Israel
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Ecdysone Elicits Chronic Renal Impairment via Mineralocorticoid-Like Pathogenic Activities
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A MONOGRAPHIC REVISION OF THE GENUS PODOCARPUS (PODOCARPACEAE): I. HISTORICAL REVIEW
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“This group of secondary compounds exhibits a wide range of biological activities in mammals and adaptogenic, anabolic (72), hypoglycemic (73), hepatoprotective, immunoprotective, wound-healing (72), and free radical scavenging effects (74).”
Background1H and 13C NMR assignments of new ecdysteroids from Callisia fragrans
Hằng, Đ. T. T., Hằng, N. T. M., Anh, H. L. T., Nhiệm, N. X., Hue, C. T., Binh, P. T., Đạt, N. T., Nam, N. H., Yến, P. H., Minh, C. V., et al. (2015) · Magnetic Resonance in Chemistry · doi:10.1002/mrc.4214 · Cited by 9 · see citing works
20-hydroxyecdysone accumulation and regulation in Ajuga lobata D. Don suspension culture
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“Also, phytosterols (campesterol) detected by GC-MS in quinoa extract decrease cholesterol levels by competing for cholesterol intestinal absorption and by decreasing atherogenic lipoprotein production in the liver (Dinan 2009).”
BackgroundKaratt, T. K., Sathiq, M. A., Laya, S., Ajeebsanu, M. M., Kal, A. K. K., Subhahar, M. B., & Perwad, Z. (2023) · Rapid Communications in Mass Spectrometry · doi:10.1002/rcm.9611 · Cited by 6 · see citing works
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“These compounds possess steroid-like effect and are recognized as safe [32, 33].”
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Vedasree, N., Peddanna, K., Rajasekhar, A., Parthasarathi, C., Munirajeswari, P., Sireesha, Y., & Chippada, A. R. (2021) · Journal of Ethnopharmacology · doi:10.1016/j.jep.2021.114856 · Cited by 6 · see citing works
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“…Entomology © 2012 The Royal Entomological Society 241 hypothesis currently accepted as explaining the function of phytoecdysteroids in plants points towards an allelochemical effect, which protects plants against attack by non-adapted invertebrate herbivores (Dinan, 2009; Dinan et al., 2009).”
BackgroundLafont, R., & Dinan, L. N. (2024) · Advances in experimental medicine and biology · doi:10.1007/5584_2024_823 · Cited by 4 · see citing works
Self-citationOn gonads and gadflies: the estrus angle
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“A likely function of ecdysteroids in plants is to defend against insect and nematode infestation, through unbridled activation of ecdysteroid receptor (EcR) signaling (i.e. endocrine disruption) in the invader (Dinan 2009).”
BackgroundTayeb, B. A., Njangiru, I. K., & Minorics, R. (2024) · Neuroprotection/Neuroprotection (Chichester, England. Print) · doi:10.1002/nep3.37 · Cited by 3 · see citing works
“These bioactivities have been extensively reviewed, 21,22 including their well ‐ known nonhormonal, anabolic, and adaptogenic effects on the entire body, known as “ whole ‐ body strengthening.”
New ring‐rearranged metabolite of 20‐hydroxyecdysone obtained by base‐catalyzed auto‐oxidation
Gáti, T., Simon, A., Hunyadi, A., Csábi, J., Kele, Z., & Tóth, G. (2015) · Magnetic Resonance in Chemistry · doi:10.1002/mrc.4389 · Cited by 3 · see citing works
Small organic ligands for the ecdysone receptor – agrochemicals, gene switches, and beyond
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Lamardi, S. N. S., Jahantab, S., Ziarati, P., Khanavi, M., & Shams‐Ardekani, M. R. (2016) · DOAJ (DOAJ: Directory of Open Access Journals)
Preparation of novel bioactive semi-synthetic ecdysteroid derivatives
Csábi, J. (2017) · doi:10.14232/phd.3986
“Though ecdysteroids are also present in certain fungi and algae, their most important source is considered to be plants, where their concentration can reach as much as 1,000-fold higher than that typically found in arthropods [4, 5, 6].”
BackgroundInfluentialSreejit, C. M. (2019) · International Journal for Research in Applied Science and Engineering Technology · doi:10.22214/ijraset.2019.4207
“Further, ECs are good candidates as elicitors for geneswitch systems to be used in medical gene therapy and research applications [4].”
BackgroundPreparation of bioactive oxidized ecdysteroid derivatives
Issaadi, H. M. (2019) · doi:10.14232/phd.10913
Quinoa grains (Chenopodium quinoa Willd.) - a source of protein and biologically active substances
Zorin, S. N., Petrov, N. A., Bokov, D. O., & Bessonov, V. V. (2021) · Research Journal of Pharmacy and Technology · doi:10.52711/0974-360x.2021.01005 · Cited by 1 · see citing works
Kellogg, J. J., Schmidt, B. M., Graf, B. L., Jofré‐Jimenez, C., Aguayo‐Cumplido, H., Calfío, C., Rojo, L. E., Cubillos‐Roble, K., Troncoso‐Fonseca, A., & Delatorre-Herrera, J. (2017) · Wiley eBooks · doi:10.1002/9781118961933.ch5
Local plants as sources of the phytoecdysteroid, 20-hydroxyecdysone
Obra, E. P. (2023) · International Journal of Biosciences (IJB) · doi:10.12692/ijb/23.3.132-140
- Authors
- Dinan, L.
- Affiliations
- Centre National de la Recherche Scientifique (FR)
- Corresponding author
- Dinan, Laurence
- ORCID
- Dinan, Laurence
- Venue
- Archives of Insect Biochemistry and Physiology
- Publisher
- Wiley
- Published
- 2009-09-21
- Volume
- 72
- Issue
- 3
- Pages
- 126-141
- ISSN
- 0739-4462 (ISSN-L)
- 1520-6327
- OpenAlex
- W2048668276
- Cited by
- 106
- References
- 83
- Citations by year
- 2026: 4 · 2025: 2 · 2024: 4 · 2023: 8 · 2022: 5 · 2021: 14 · 2020: 6 · 2019: 7 · 2018: 5 · 2017: 9 · 2016: 8 · 2015: 12 · 2014: 6 · 2013: 5 · 2012: 6
- FWCI
- 0.28
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Archives of Insect Biochemistry and Physiology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Phytochemical Studies and Bioactivities
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Plant biochemistry and biosynthesis
- Life Sciences › Agricultural and Biological Sciences › Insect Science › Insect-Plant Interactions and Control
- Keywords
- phytoecdysteroids, ecdysteroids, plant hormones, pest control, crop breeding, genetic modification, adaptogenic activity, anabolic activity, antidiabetic activity, hepatoprotection, wound healing, antitumour activity, nutraceuticals, gene therapy
- MeSH terms
- Animals, Arthropods, Pharmaceutical Preparations, Gene Expression Regulation, Humans, Insecticides, Pest Control, Biological, Plant Extracts, Plants, Ecdysteroids
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