Total synthesis and dual PPARα/γ agonist effects of Amorphastilbol and its synthetic derivatives
- Total synthesis and dual PPARα/γ agonist effects of Amorphastilbol and its synthetic derivatives
- 김태정; 이우정; 정규혁; 송중호; 박순혜; 최필주; 김수남; 이석준; 함정엽
- Natural product; Amorphastilbol; Type 2 diabetes; Dual PPARα/γ agonists; Suzuki-Miyaura cross-coupling
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 22, NO 12, 4122-4126
- Amorphastilbol (APH-1), isolated from a Robinia pseudoacacia var. umbraculifer seed extract, is a biologically
interesting natural trans-stilbene compound with dual peroxisome proliferator-activated receptor
(PPAR) α/γ agonist activity. After total synthesis of APH-1 and its derivatives by Pd-catalyzed Suzuki–
Miyaura cross-coupling of a common (E)-styryl bromide intermediate and various aromatic trifluoroborate
compounds, we biologically evaluated APH-2–APH-12 for PPAR agonist activity. APH-4 and APH-11
were effective PPARα/γ transcriptional activators, compared with APH-1. Therefore, we suggest that
APH-4 and APH-11 are novel dual PPARα/γ agonists and are potentially useful for treating type 2 diabetes
by enhancing glucose and lipid metabolism.
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