Phytoecdysteroids: Distribution, Structural Diversity, Biosynthesis, Activity, and Crosstalk with Phytohormones

Abstract

Phytoecdysteroids (PEs) are naturally occurring polyhydroxylated compounds with a structure similar to that of insect molting hormone and the plant hormone brassinosteroids. PEs have a four-ringed skeleton composed of 27, 28, 29, or 30 carbon atoms (derived from plant sterols). The carbon skeleton of ecdysteroid is known as cyclopentanoperhydrophenanthrene and has a β-sidechain on C-17. Plants produce PEs via the mevalonate pathway with the help of the precursor acetyl-CoA. PEs are found in algae, fungi, ferns, gymnosperms, and angiosperms; more than 500 different PEs are found in over 100 terrestrial plants. 20-hydroxyecdysone is the most common PE. PEs exhibit versatile biological roles in plants, invertebrates, and mammals. These compounds contribute to mitigating biotic and abiotic stresses. In plants, PEs play a potent role in enhancing tolerance against insects and nematodes via their allelochemical activity, which increases plant biological and metabolic responses. PEs promote enzymatic and non-enzymatic antioxidant defense systems, which decrease reactive oxygen species in the form of superoxide radicals and hydroxyl radicals and reduce malondialdehyde content. PEs also induce protein biosynthesis and modulate carbohydrate and lipid synthesis. In humans, PEs display biological, pharmacological, and medicinal properties, such as anti-diabetic, antioxidant, anti-microbial, hepatoprotective, hypoglycemic, anti-cancer, anti-inflammatory, antidepressant, and tissue differentiation activity.

Prumnopitys Andina Fruit Extract Activates Liver X Receptors after In Vitro Digestion

“…Phytoecdysteroids can affect metabolic pathways in mammals, such as protein synthesis, lipid and carbohydrate metabolism, acting as hepatoprotective, immunostimulants, and hypoglycemic agents. [11,12] The anabolic properties of phytoecdysteroids in mammals have supported the idea that these compounds might have effects in the endocrine system. [9] However, studies show contradictory results on the binding of 20E and ecdysone to some mammalian nuclear receptors.…”

“…[ 11 ] However, the molecular mechanisms explaining the bioactivity of phytoecdysteroids have not been well characterized. [ 6,12 ]…”

“…[11] However, the molecular mechanisms explaining the bioactivity of phytoecdysteroids have not been well characterized. [6,12] The pharmacokinetics of phytoecdysteroids have been studied in vivo, [13] and we still know little regarding the absorption and transport of phytoecdysteroids through the epithelial barrier and their interactions with nuclear receptors. We therefore aimed to fill these gaps by performing simulated in vitro digestion experiments, transepithelial transport studies with Caco-2 cells and reporter gene assays with digested 20E.…”

Ecdysteroids from the Korean Endemic Species Ajuga spectabilis with Activities against Glucocorticoid Receptors and 11β-Hydroxysteroid Dehydrogenase Type 1

“…The genus Ajuga belongs to the Lamiaceae family and consists of more than 300 species that produce diverse secondary metabolites. In particular, Ajuga species are known as rich sources of ecdysteroids . Ecdysteroids are characteristically polyhydroxylated and generally possess a 14α-hydroxy-7-en-6-one chromophoric moiety.…”

Phytochemical Screening and Pesticidal Efficacy of Phytoecdysteroid Fraction of a Fern Pityrogramma Calomelanos (L.) Link Against Spodoptera Litura (Fabricius.)

“…Phytoecdysteroids (PEs) are a class of chemicals synthesized by plants for defense against phytophagous insects and causes severe adverse effects including weight loss, moulting disruption and mortality. Approximately 6% of all plant species synthesis phytoecdysteroids and it have been detected in 27 families of pteridophyta (Arif et al, 2022). Phytoecdysteroids found in more than 50% of fern families such as Pteridaceae, Polypodiaceae and Blechneaceae (Savchenko et al, 2022).…”