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Hokkaido University Collection of Scholarly and Academic Papers >
Graduate School of Health Sciences / Faculty of Health Sciences >
Peer-reviewed Journal Articles, etc >
Food-Derived beta-Carboline Alkaloids Ameliorate Lipid Droplet Accumulation in Human Hepatocytes
| Title: | Food-Derived beta-Carboline Alkaloids Ameliorate Lipid Droplet Accumulation in Human Hepatocytes |
| Authors: | Dibwe, Dya Fita Browse this author | | Oba, Saki Browse this author | | Takeishi, Nire Browse this author | | Sakurai, Toshihiro Browse this author | | Tsukui, Takayuki Browse this author →KAKEN DB | | Chiba, Hitoshi Browse this author →KAKEN DB | | Hui, Shu-Ping Browse this author →KAKEN DB |
| Keywords: | functional foods | | Crassostrea gigas | | beta-carboline alkaloids | | bioactive compounds | | lipid droplet accumulation inhibition | | lipidomics | | neutral lipids | | triacylglycerols |
| Issue Date: | 5-May-2022 |
| Publisher: | MDPI |
| Journal Title: | Pharmaceuticals |
| Volume: | 15 |
| Issue: | 5 |
| Start Page: | 578 |
| Publisher DOI: | 10.3390/ph15050578 |
| PMID: | 35631404 |
| Abstract: | 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. |
| Type: | article |
| URI: | http://hdl.handle.net/2115/86094 |
| Appears in Collections: | 保健科学院・保健科学研究院 (Graduate School of Health Sciences / Faculty of Health Sciences) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)
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