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Media type:
E-Article
Title:
Synthesis of Phthalimide Derivatives as Potential PPAR-γ Ligands
Contributor:
Eom, So;
Liu, Sen;
Su, Mingzhi;
Noh, Tae;
Hong, Jongki;
Kim, Nam;
Chung, Hae;
Yang, Min;
Jung, Jee
Published:
MDPI AG, 2016
Published in:
Marine Drugs, 14 (2016) 6, Seite 112
Language:
English
DOI:
10.3390/md14060112
ISSN:
1660-3397
Origination:
Footnote:
Description:
Paecilocin A, a phthalide derivative isolated from the jellyfish-derived fungus Paecilomyces variotii, activates PPAR-γ (Peroxisome proliferator-activated receptor gamma) in rat liver Ac2F cells. Based on a SAR (Structure-activity relationships) study and in silico analysis of paecilocin A-mimetic derivatives, additional N-substituted phthalimide derivatives were synthesized and evaluated for PPAR-γ agonistic activity in both murine liver Ac2F cells and in human liver HepG2 cells by luciferase assay, and for adipogenic activity in 3T3-L1 cells. Docking simulation indicated PD6 was likely to bind most strongly to the ligand binding domain of PPAR-γ by establishing crucial H-bonds with key amino acid residues. However, in in vitro assays, PD1 and PD2 consistently displayed significant PPAR-γ activation in Ac2F and HepG2 cells, and adipogenic activity in 3T3-L1 preadipocytes.