20-Hydroxyecdysone bioavailability and pharmacokinetics in Gerbillus tarabuli, a gerbil model for metabolic syndrome studies
Abstract
Phytoecdysteroids are active natural compounds that have demonstrated many beneficial pharmacological effects on mammals, including Humans. 20-Hydroxyecdysone (20E) is the major phytoecdysteroid present in plants, and gerbils are particularly good responders to the addition of 20E to their diet. We have examined the oral bioavailability of 20E in the desert gerbil, Gerbillus tarabuli. 20E (5 and 50 mg.kg-1 body weight) was administered to gerbils by intra-peritoneal injection and oral gavage, respectively. Plasma samples were collected over 8 h and analyzed by HPLC-MS/MS to determine the 20E concentrations. The calculated oral bioavailability of 20E is approx. 12%, with a half-life of 30.6 and 33 min after per os administration or intra-peritoneal injection, respectively. This bioavailabilitty is much higher than that observed in laboratory rodents (ca. 1%). It is proposed that this unexpectedly high oral bioavailability of 20E in gerbils contributes to its high efficacy in this animal.
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Single oral administration of 50 mg 20E/kg body weight in gerbil revealed 12% bioavailability, about 10-fold higher than after similar administration in rats and humans (1-2%).
“The single administration of 50 mg 20E/kg bw. by oral gavage in gerbil revealed 12% bioavailability of 20E, about 10-fold higher than after a similar administration in rats and humans (1–2%).”
From Molecular Targets of 20-Hydroxyecdysone in Mammals, Mechanism of Action: Is It a Calorie Restriction Mimetic and Anti-Aging Compound? (2025) · cites this paper as [71]
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Zádor, E. (2025) · Cells · doi:10.3390/cells14060431 · Cited by 9 · see citing works
“Considering the high efficacy in gerbil, the prevalence of 20E in blood plasma has been studied after per os or i.p. administrations [71].”
- Authors
- Bellahreche, Z., & Dahmani, Y.
- Affiliations
- University of Sciences and Technology Houari Boumediene (DZ)
- Corresponding author
- Bellahreche, Zineb
- ORCID
- Bellahreche, Zineb
- Venue
- Steroids
- Publisher
- Elsevier BV
- Published
- 2023-10
- Volume
- 198
- Pages
- 109262
- ISSN
- 0039-128X (ISSN-L)
- OpenAlex
- W4381743433
- Cited by
- 4
- References
- 10
- Citations by year
- 2026: 1 · 2025: 2 · 2024: 1
- FWCI
- 0.36
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- Locations
- Steroids (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 › Steroid Chemistry and Biochemistry
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Keywords
- 20-hydroxyecdysone, phytoecdysteroids, oral bioavailability, pharmacokinetics, desert gerbil, metabolic syndrome, plasma half-life, animal models
- MeSH terms
- Animals, Biological Availability, Ecdysterone, Gerbillinae, Metabolic Syndrome, Tandem Mass Spectrometry
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