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- Title
Synthesis of Phthalimide Derivatives as Potential PPAR-Ligands.
- Authors
So Hyeon Eom; Sen Liu; Mingzhi Su; Tae Hwan Noh; Jongki Hong; Nam Deuk Kim; Hae Young Chung; Min Hye Yang; Jung, Jee H.
- Abstract
Paecilocin A, a phthalide derivative isolated from the jellyfish-derived fungus Paecilomyces variotii, activates PPAR-(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-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-by establishing crucial H-bonds with key amino acid residues. However, in in vitro assays, PD1 and PD2 consistently displayed significant PPAR-activation in Ac2F and HepG2 cells, and adipogenic activity in 3T3-L1 preadipocytes.
- Subjects
PEROXISOME proliferator-activated receptors; PHTHALIMIDES; TYPE 2 diabetes; ADIPOGENESIS; LIGAND binding (Biochemistry); LABORATORY rats
- Publication
Marine Drugs, 2016, Vol 14, Issue 6, p112
- ISSN
1660-3397
- Publication type
Article
- DOI
10.3390/md14060112