Ginkgetin, a biflavone from Ginkgo biloba leaves, prevents adipogenesis through STAT5-mediated PPARγ and C/EBPα regulation.

Pharmacol Res 2019 01 22;139:325-336. Epub 2018 Nov 22.

Biotherapeutics Translational Research Center, Korea Research Institute of Bioscience and Biotechnology, Daejeon, 34141, Republic of Korea; Department of Biomolecular Science, University of Science & Technology (UST), Daejeon, Republic of Korea. Electronic address:

Adipogenesis involved in hypertrophy and hyperplasia of adipocytes is responsible for expanding the mass of adipose tissues in obese individuals. Peroxisome proliferator-activated receptor γ (PPARγ) and CCAAT/enhancer-binding protein α (C/EBPα) are two principal transcription factors induced by delicate signaling pathways, including signal transducer and activator of transcription 5 (STAT5), in adipogenesis. Here, we demonstrated a novel role of ginkgetin, a biflavone from Ginkgo biloba leaves, as a STAT5 inhibitor that blocks the differentiation of preadipocytes into adipocytes. During the differentiation of 3T3-L1 cells, ginkgetin treatment during the first 2 days markedly inhibited the formation of lipid-bearing adipocytes. PPARγ and C/EBPα expression was decreased in 3T3-L1 cells during adipogenesis following ginkgetin treatment, whereas no change was observed in C/EBPβ or C/EBPδ expression. Inhibition of PPARγ and C/EBPα expression by ginkgetin occurred through the prevention of STAT5 activation during the initiation phase of adipogenesis. In addition, ginkgetin-mediated the inhibition of adipogenesis was recapitulated in the differentiation of primary preadipocytes. Lastly, we confirmed the inhibitory effects of ginkgetin on the hypertrophy of white adipose tissues from high-fat diet-fed mice. These results indicate that ginkgetin is a potential anti-adipogenesis and anti-obesity drug.

Download full-text PDF

Source
https://linkinghub.elsevier.com/retrieve/pii/S10436618183073
Publisher Site
http://dx.doi.org/10.1016/j.phrs.2018.11.027DOI Listing
January 2019

Publication Analysis

Top Keywords

pparγ c/ebpα
12
ginkgetin biflavone
8
biloba leaves
8
c/ebpα expression
8
3t3-l1 cells
8
ginkgo biloba
8
ginkgetin treatment
8
biflavone ginkgo
8
adipose tissues
8
ginkgetin
7
adipogenesis
6
expression inhibition
4
activator transcription
4
novel role
4
transducer activator
4
transcription stat5
4
stat5 adipogenesis
4
demonstrated novel
4
adipogenesis demonstrated
4
expression ginkgetin
4

Similar Publications