Isolation and lipolytic activity of eurycomanone and its epoxy derivative from Eurycoma longifolia.

Authors :: Lahrita L
Hirosawa R
Kato E
Kawabata J
Source :: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2017 Sep 01; Vol. 25 (17), pp. 4829-4834. Date of Electronic Publication: 2017 Jul 19.
Publication Year :: 2017
Abstract: Eurycomanone (1) and 13β,21-epoxyeurycomanone (2) were isolated from Eurycoma longifolia for studies of lipolytic activity. Compound 1 enhanced lipolysis in adipocytes with an EC <subscript>50</subscript> of 14.6μM, while its epoxy derivate, compound 2, had a stronger activity with an EC <subscript>50</subscript> of 8.6μM. Based on molecular mechanistic study using several specific inhibitors to lipolytic signaling pathways, it was found that PKA inhibitor totally diminished the lipolytic activity of 1 and 2. Further immunoblotting analysis confirmed the activation of phosphorylated PKA by both 1 and 2. With the growing need to develop new anti-obesity agents, eurycomanone and its epoxy derivate can be used as promising lead compounds to target lipid catabolism.<br /> (Copyright © 2017 Elsevier Ltd. All rights reserved.)

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