상세 보기
- Ko, Hyejin;
- An, Seungchan;
- Jang, Hongjun;
- Ahn, Sungjin;
- Park, In Guk;
- ... Choi, Won Jun;
- 외 6명
WEB OF SCIENCE
5SCOPUS
5초록
The natural flavonoid macakurzin C (1) exhibited adiponectin biosynthesis-inducing activity during adipogenesis in human bone marrow mesenchymal stem cells and its molecular mechanism was directly associated with a pan-peroxisome proliferator-activat-ed receptor (PPAR) modulator affecting all three PPAR subtypes a, ?, and 6. In this study, increases in adiponectin biosynthesis -inducing activity by macakurzin C derivatives (2-7) were studied. The most potent adiponectin biosynthesis-inducing compound 6, macakurzin C 3,5-dimethylether, was elucidated as a dual PPARa/? modulator. Compound 6 may exhibit the most potent activity because of the antagonistic relationship between PPAR6 and PPAR?. Docking studies revealed that the O-methylation of macakurzin C to generate compound 6 significantly disrupted PPAR6 binding. Compound 6 has therapeutic potential in hypoadi-ponectinemia-related metabolic diseases.
키워드
- 제목
- Macakurzin C Derivatives as a Novel Pharmacophore for Pan-Peroxisome Proliferator-Activated Receptor Modulator
- 저자
- Ko, Hyejin; An, Seungchan; Jang, Hongjun; Ahn, Sungjin; Park, In Guk; Hwang, Seok Young; Gong, Junpyo; Oh, Soyeon; Kwak, Soo Yeon; Choi, Won Jun; Kim, Hyoungsu; Noh, Minsoo
- 발행일
- 2023-05
- 유형
- Article
- 권
- 31
- 호
- 3
- 페이지
- 312 ~ 318