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

Lahrita, Lucy; Hirosawa, Ryota; Kato, Eisuke; Kawabata, Jun

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

Lahrita, Lucy; Hirosawa, Ryota; Kato, Eisuke et al.

Bioorganic and Medicinal Chemistry, 2017, 25(17), 4829-4834

Permalink : https://hdl.handle.net/2115/75320

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アクセス権	open access
URI	https://hdl.handle.net/2115/75320
タイトル	Isolation and lipolytic activity of eurycomanone and its epoxy derivative from Eurycoma longifolia
著者	Lahrita, Lucy ; Hirosawa, Ryota ; Kato, Eisuke ; Kawabata, Jun
著者名 Lahrita, Lucy
著者名 Hirosawa, Ryota
e-Rad_Researcher 40466446 著者名 Kato, Eisuke
e-Rad_Researcher 60142197 著者名 Kawabata, Jun
言語	英語
キーワード	3T3-L1 adipocytes
	Eurycoma longifolia
	Lipolysis
	Obesity
	Quassinoid
発行日	2017-09-01
出版者	Elsevier
収録物名	Bioorganic and Medicinal Chemistry
巻(号)	25(17)
ページ	4829-4834
抄録	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.
資源タイプ	学術雑誌論文
出版タイプ	Accepted Manuscript
権利情報	Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International
権利情報	© 2017, Elsevier. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/
PISSN	0968-0896
EISSN	1464-3391
NCID	AA10938083
関連情報	PMID 28760530
関連情報 (isVersionOf)	出版社版DOI https://doi.org/10.1016/j.bmc.2017.07.032