Anti-adipogenic activity of a new cyclic diarylheptanoid isolated from Alnus japonica on 3T3-L1 cells via modulation of PPAR纬, C/EBP伪 and SREBP1c signaling

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• 作者：Sang Hyun Sung^a ; Mina Lee^a ; ^b ; ^{minalee@sunchon.ac.kr" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Alnus japonica ; Betulaceae ; Diarylheptanoids ; Adipogenesis ; Adipocyte differentiation ; Obesity ; 3T3-L1 cells
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2015
• 出版时间：15 October 2015
• 年：2015
• 卷：25
• 期：20
• 页码：4648-4651
• 全文大小：596 K

文摘

Total methanolic extract of Alnus japonica fruits exhibited significant anti-adipogenic activities in 3T3-L1 cells. A new cyclic diarylheptanoid (1) along with ten known compounds (2–11) were isolated by activity-guided fractionation. Compound 1, determined to be 4-hydroxy-alnus-3,5-dione, showed the most potent anti-adipogenic effect. Compound 1 significantly down-regulated expression of peroxisome proliferator-activated receptor 纬 (PPAR纬), CCAAT/enhancer binding protein 伪 (C/EBP伪), and sterol regulatory element binding protein 1 (SREBP1c) in 3T3-L1 cells, as determined by quantitative real-time PCR and Western blot analysis. Furthermore, compound 1 suppressed mRNA expression of C/EBP尾 and C/EBP未 during the early stage of adipogenesis as well as stearoyl coenzyme A desaturase 1 (SCD-1) and fatty acid synthase (FAS), target genes of SREBP1c. Upon investigating the mechanism of natural products, we propose that cyclic diarylheptanoid (1), the most potent constituent of A. japonica, can be a potent therapeutic agent against obesity through anti-adipogenesis via down-regulation of PPAR纬, C/EBP伪, and SREBP1c signaling.