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 Chemjournal_title
Bioorganic & medicinal chemistryauthors
Lahrita L,Hirosawa R,Kato E,Kawabata Jdoi
10.1016/j.bmc.2017.07.032subject
Has Abstractpub_date
2017-09-01 00:00:00pages
4829-4834issue
17eissn
0968-0896issn
1464-3391pii
S0968-0896(17)31348-2journal_volume
25pub_type
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