Anti-adipogenic activity of a new cyclic diarylheptanoid isolated from Alnus japonica on 3T3-L1 cells via modulation of PPARγ, C/EBPα and SREBP1c signaling. Issue 20 (15th October 2015)

• Record Type: Journal Article
• Authors: Sung, Sang Hyun; Lee, Mina
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 20(2015)
• Page Start: 4648
• Page End: 4651
• Publication Date: 2015-10-15
• Subjects: Alnus japonica -- Betulaceae -- Diarylheptanoids -- Adipogenesis -- Adipocyte differentiation -- Obesity -- 3T3-L1 cells; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.08.032
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: 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. Compound1, determined to be 4-hydroxy-alnus-3, 5-dione, showed the most potent anti-adipogenic effect. Compound1 significantly down-regulated expression of peroxisome proliferator-activated receptor γ (PPARγ), CCAAT/enhancer binding protein α (C/EBPα), and sterol regulatory element binding protein 1 (SREBP1c) in 3T3-L1 cells, as determined by quantitative real-time PCR and Western blot analysis. Furthermore, compound1 suppressed mRNA expression of C/EBPβ and C/EBPδ 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 PPARγ, C/EBPα, and SREBP1c signaling.