HPLC analysis and blood-brain penetration of 20-hydroxyecdysone diacetonide

Abstract

Summary. Blood-brain penetration of 20-hydroxyecdysone 2,3;20,22-diacetonide (20DA) has been scouted using chromatographic methods. In vivo experiments were performed by treating male Wistar rats intraperitoneally (i.p.) with a dose of 50 mg kg −1 20DA. Control experiment was done by using 20-hydroxyecdysone (20E). Definite brain penetration of 20DA was found by using high-performance liquid chromatography (HPLC), while 20E does not show this type of distribution.

Preparation of novel bioactive semi-synthetic ecdysteroid derivatives

“…Moreover, in a most recent study from our group, 20 was found to have significantly prolonged pharmacokinetics in rats as compared to that of the rapidly eliminating 20E, which suggests an increased metabolic stability [69]. These findings provide further support to the presumption that ecdysteroid dioxolanes should be stable enough to retain their biological activity throughout the metabolic process, and therefore the preparation of novel ecdysteroid dioxolanes deserves further attention.…”

Dietary Phytoecdysteroids

“…However, studies on rats after i.p. injections of ecdysteroids show that although 20E diacetonide will cross the blood-brain barrier, 20E itself does not (Kalász et al 2017).…”