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CBMG, a novel derivative of mansonone G suppresses adipocyte differentiation via suppression of PPARγ activity

Title
CBMG, a novel derivative of mansonone G suppresses adipocyte differentiation via suppression of PPARγ activity
Authors
Kim H.K.Hairani R.Jeong H.Jeong M.G.Chavasiri W.Hwang E.S.
Ewha Authors
황은숙
SCOPUS Author ID
황은숙scopus
Issue Date
2017
Journal Title
Chemico-Biological Interactions
ISSN
0009-2797JCR Link
Citation
vol. 273, pp. 160 - 170
Keywords
AdipogenesisC/EBPαCBMGMGPPARγ
Publisher
Elsevier Ireland Ltd
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
Mansorins and mansonones have been isolated from Mansonia gagei heartwoods, a traditional herbal medicine used to treat heart failure, and characterized to have anti-oxidant, anti-bacterial, anti-tumor, and anti-estrogenic activities. However, there is as yet no information on their effects on adipogenesis and lipid storage associated with heart disease. In this study, we investigated the effects of naturally occurring compounds on adipogenic differentiation and sought to develop more potent anti-adipogenic compound. We found that mansonone G (MG) suppressed adipocyte differentiation of 3T3-L1 cells, with a 40% decrease in lipid accumulation at 10 μM. MG derivatives including ether and ester analogues were then synthesized and assayed for their ability to suppress adipogenesis. A novel MG derivative, chlorobenzoyl MG (CBMG) most potently suppressed adipocyte differentiation with the decreased level of aP2 and adiponectin. Interestingly, CBMG treatment decreased the expression of CCAAT enhancer binding protein-α (C/EBPα) and peroxisome proliferator-activated receptor-γ (PPARγ). Further analysis confirmed that CBMG suppressed both the expression and activity of PPARγ, a master regulator of adipogenesis, and subsequently led to decreases in transcription of C/EBPα, aP2, and adiponectin in adipogenesis, thereby attenuating adipocyte differentiation. Our results suggest that a novel MG derivative, CBMG may have beneficial applications in the control of obesity through the suppression of PPARγ-induced adipocyte differentiation and lipid accumulation. © 2017 Elsevier B.V.
DOI
10.1016/j.cbi.2017.06.017
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약학대학 > 약학과 > Journal papers
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