- 著者
-
下川 賢一郎
岩瀬 賢明
三輪 亮佳
池田 麻理子
大野 修
山田 薫
宮本 憲二
上村 大輔
- 出版者
- 天然有機化合物討論会
- 雑誌
- 天然有機化合物討論会講演要旨集
- 巻号頁・発行日
- no.50, pp.487-492, 2008-09-01
(-)-Ternatin (1) is a highly N-methylated cyclic heptapeptide that was isolated from the mushroom Coriolus versicolor during our continuing search for potential anti-obesity agents from natural resources such as mushrooms. In our previous presentation (2006), we reported the isolation, structure elucidation and synthesis of 1, which potently inhibited fat accumulation against 3T3-L1 murine adipocytes. To clarify the detailed mode of action of (-)-ternatin (1) with regard to fat-accumulation inhibition in adipocytes, we started bioorganic studies of 1 and its analogues. We achieved the solution-phase synthesis of 1 and then evaluated its in vivo biological activity. Treatment with 1 at 5mg/kg/day was found to suppress the increase in body weight and fat accumulation in diet-induced obese mice. Due to the course, a structure-activity relationship (SAR) study of 1 was first investigated aimed at the recognition of the importance of side chain functionalities as well as a suitable site for advanced functionalization in its structure, e.g., biotinylation and introduction of a fluorescent unit.