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

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 EC50 of 14.6μM, while its epoxy derivate, compound 2, had a stronger activity with an EC50 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.

journal_name

Bioorg Med Chem

authors

Lahrita L,Hirosawa R,Kato E,Kawabata J

doi

10.1016/j.bmc.2017.07.032

subject

Has Abstract

pub_date

2017-09-01 00:00:00

pages

4829-4834

issue

17

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(17)31348-2

journal_volume

25

pub_type

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