Food-Derived beta-Carboline Alkaloids Ameliorate Lipid Droplet Accumulation in Human Hepatocytes

Dibwe, Dya Fita; Oba, Saki; Takeishi, Nire; Sakurai, Toshihiro; Tsukui, Takayuki; Chiba, Hitoshi; Hui, Shu-Ping

Food-Derived beta-Carboline Alkaloids Ameliorate Lipid Droplet Accumulation in Human Hepatocytes

Dibwe, Dya Fita; Oba, Saki; Takeishi, Nire et al.

Pharmaceuticals, 2022, 15(5), 578

Permalink : https://hdl.handle.net/2115/86094

このアイテムのアクセス数:381件（2026-10-07 10:17 集計）

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https://doi.org/10.3390/ph15050578			323

論文情報

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アクセス権	open access
URI	https://hdl.handle.net/2115/86094
タイトル	Food-Derived beta-Carboline Alkaloids Ameliorate Lipid Droplet Accumulation in Human Hepatocytes
著者	Dibwe, Dya Fita ; Oba, Saki ; Takeishi, Nire ; Sakurai, Toshihiro ; Tsukui, Takayuki ; Chiba, Hitoshi ; Hui, Shu-Ping
著者名 Dibwe, Dya Fita
著者名 Oba, Saki
著者名 Takeishi, Nire
著者名 Sakurai, Toshihiro
e-Rad_Researcher 70610591 著者名 Tsukui, Takayuki
e-Rad_Researcher 70197622 著者名 Chiba, Hitoshi
e-Rad_Researcher 90337030 著者名 Hui, Shu-Ping
言語	英語
キーワード	functional foods
	Crassostrea gigas
	beta-carboline alkaloids
	bioactive compounds
	lipid droplet accumulation inhibition
	lipidomics
	neutral lipids
	triacylglycerols
発行日	2022-05-05
出版者	MDPI
収録物名	Pharmaceuticals
巻(号)	15(5)
ページ	578
抄録	Lipid droplet accumulation (LDA) in hepatocytes is the initial stage of nonalcoholic fatty liver disease (NAFLD). In the search for natural compounds for the prevention of NAFLD, a series of beta-carboline alkaloid derivatives, inspired by flazin and its derivative, newly identified in Crassostrea gigas Thunberg. extracts, were examined for LDA inhibition (LDAI) activity in oleic acid-loaded hepatocytes (HepG2). Eight compounds with a piperidine or pyridine C-ring were chemically synthesized (1-8). Among them, compounds 2 and 4 (flazin) with a carboxy group at C-3 and furfuryl alcohol moiety at C-1 showed low cytotoxicity and they exhibited significant LDAI activity. Compound 2 with piperidine C-ring was identified for the first time in C. gigas extract, and ameliorated the lipid accumulation with the LDAI value of 25.4%. Active compounds 2 and 4 significantly inhibited triacylglycerol species accumulation in cells. These compounds upregulated ATGL and downregulated SREBP1, FASN, and SCD1 genes, suggesting that they activated lipolysis and suppressed lipogenesis, respectively. These results suggest that beta-carboline alkaloids, especially compounds 2 and 4, might be potentially useful for preventing NAFLD.
資源タイプ	学術雑誌論文
出版タイプ	Version of Record
EISSN	1424-8247
関連情報	PMID 35631404
関連情報 (isIdenticalTo)	出版社版DOI https://doi.org/10.3390/ph15050578