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REVIEW
Effects and applications of arthropod steroid hormones (ecdysteroids)
in mammals
Laurence Dinan and ReneŽ Lafont
1
Department of Biological Sciences, University of Exeter, Exeter, Devon EX4 4PS, UK
1
Laboratoire ProteŽines: Biochimie Structurale et Fonctionnelle, UniversiteŽ Pierre et Marie Curie, 7 Quai St. Bernard, F-75252 Paris 05, France
(Requests for offprints should be addressed to L Dinan who is now at 30 Hederman Close, Silverton, Nr. Exeter, Devon EX5 4HW, UK;
Email: laurie@dinan.wanadoo.co.uk)
Abstract
Zooecdysteroids (arthropod steroid hormones) regulate the
development of arthropods and probably many other
invertebrates. Phytoecdysteroids are analogues occurring in
a wide range of plant species, where they contribute to the
deterrence of phytophagous invertebrates. The purpose of
this short review is to summarise findings on the occurrence,
metabolism and pharmacological effects of ecdysteroids in
mammalian systems and to draw attention to their potential
applications, particularly in gene-switch technology, where
ecdysteroid analogues (steroidal and non-steroidal) can be
used as effective and potent elicitors.
Journal of Endocrinology (2006) 191, 1­8
Introduction
Ecdysteroids are the steroid hormones of arthropods, where
they regulate moulting, metamorphosis, reproduction and
diapause (
). They probably fulfil similar roles in
many other invertebrate phyla, but these have not been so
extensively investigated (Lafont 1997). Ecdysteroids are also
present in 5­6% of plant species (
), generally at
far higher concentrations than those typically found in
arthropods, where they are regarded as contributing to the
deterrence of invertebrate predators (
). The archetypal ecdysteroid in both arthropods and
plants is 20-hydroxyecdysone (20E;
), since it is the most
commonly occurring and the most abundant, but a very wide
range of structural analogues has been elucidated, especially
from plant sources (
). The first ecdysteroid
(ecdysone;
) was isolated in 1954 (
) and its structure was unambiguously identified only in
1965 (
), with the result that research on
ecdysteroids has generally lagged far behind that on the
various classes of vertebrate steroid hormones, in spite of the
fact that development in more than 90% of all animal species
is dependent upon ecdysteroids. However, since the early
reports of the occurrence of ecdysteroids in insects and plants,
researchers have posed questions about the occurrence (from
the diet), metabolism and possible effects of ecdysteroids in
mammals. In the intervening period, a substantial body of
evidence relevant to these questions has been obtained,
suggesting that ecdysteroids may have significantly positive
pharmacological properties. This is consistent with the use of
several ecdysteroid-containing plant species in traditional
medicines. The ready availability of large amounts of 20E
from certain plant sources has led to a boom in recent years in
its inclusion in many commercial anabolic preparations for
body-builders and sportsmen. Further, since ecdysteroids are
not endogenous products of mammalian metabolism and are
non-toxic to mammals, they are also finding application as
elicitors of novel gene-switch systems. With the intention of
bringing this area to a wider audience of endocrinologists, we
shall summarise the most significant findings. Also, we shall
focus on the developments in this area since our previous
review (
), but the reader is referred to
that review for a more extensive treatment of the relevant
literature and the concepts.
Occurrence of ecdysteroids in mammals
Ecdysteroids are not regarded as products of mammalian
metabolism. However, they can be detected in mammalian
tissues and fluids as a consequence of dietary intake of
ecdysteroid-containing plants (or insects in certain population
groups) or infection by invertebrate parasites. Most crop plant
species do not contain phytoecdysteroids, although both
spinach (Spinacia oleracea) and quinoa (Chenopodium quinoa)
do contain significant levels, especially in the seeds and
1
Journal of Endocrinology (2006) 191, 1­8
DOI: 10.1677/joe.1.06900
0022­0795/06/0191­001 q 2006 Society for Endocrinology Printed in Great Britain
Online version via http://www.endocrinology-journals.org


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