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首页> 外文期刊>Bioorganic and medicinal chemistry >Isolation and lipolytic activity of eurycomanone and its epoxy derivative from Eurycoma longifolia
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Isolation and lipolytic activity of eurycomanone and its epoxy derivative from Eurycoma longifolia

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

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Graphical abstract Display Omitted Highlights ? Eurycomanone ( 1 ) and 13β,21-epoxyeurycomanone ( 2 ), isolated from Eurycoma longifolia , exert lipolytic activity. ? EC 50 values for compound 1 and 2 are 14.6 μM and 8.6 μM, respectively. ? PKA inhibitor totally diminished the lipolytic activity of 1 and 2 . ? Immunoblotting analysis confirmed the activation of phosphorylated PKA by 1 and 2 . ? Eurycomanone and its epoxy derivate can be used as promising lead compounds to target lipid catabolism. 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 50 of 14.6 μM, while its epoxy derivate, compound 2 , had a stronger activity with an EC 50 of 8.6 μM. 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. >

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