Structure-based hybridization of the bioactive natural products rhizonin A and ternatin leading to a selective fat-accumulation inhibitor against 3T3-L1 adipocytes.
Based on the structural similarity between the naturally occurring cyclic heptapeptides rhizonin A and ternatin, two novel analogues were designed. The synthetic analogues were assessed with regard to their fat-accumulation inhibitory effect against 3T3-L1 adipocytes, and this led to the discovery of a potent and selective fat-accumulation inhibitor compared to the parent compound rhizonin A.
Shimokawa
Kenichiro
K
Department of Chemistry, Graduate School of Science, Nagoya University, Furo-cho, Chikusa, Nagoya 464-8602, Japan.
Yamada
Kaoru
K
Uemura
Daisuke
D
D041721:3T3-L1 Cells; D017667:Adipocytes / Q000166:cytology* / Q000378:metabolism; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D005419:Flavonoids / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D051379:Mice; D008954:Models, Biological; D008956:Models, Chemical; D008968:Molecular Conformation; D009693:Nucleic Acid Hybridization; D010455:Peptides / Q000737:chemistry; D010456:Peptides, Cyclic / Q000737:chemistry*
D005419:Flavonoids; D010455:Peptides; D010456:Peptides, Cyclic; C051080:ternatin (flavonoid); C040695:rhizonin A