Synthesis and evaluation on triglyceride inhibitory activities of novel indole alkaloids
10.16438/j.0513-4870.2021-1439
- VernacularTitle:全新结构吲哚类生物碱的合成及降甘油三酯活性研究
- Author:
Li-ping ZHAO
;
Yang-yang CHENG
;
Tian-yun FAN
;
Qing-xuan ZENG
;
Wei-jia KONG
;
Dan-qing SONG
;
Yan-xiang WANG
- Publication Type:Research Article
- Keywords:
indole alkaloid;
synthesis;
anti-triglyceride activity;
AMPK
- From:
Acta Pharmaceutica Sinica
2022;57(2):433-440
- CountryChina
- Language:Chinese
-
Abstract:
Three tricyclic [6,5,7] and six tetracyclic [6,5,5,5] novel indole alkaloids were synthesized and evaluated on triglyceride inhibitory activities for the first time. Among them, compound 4c showed the most potent activity with IC50 value of 6.35 μmol·L-1. Meanwhile, compound 4c also exhibited a good safety profile at the cellular level. Preliminary mechanism study indicated that 4c might increase intracellular lipid metabolism by activating AMPK. These results provide a novel family of lead compounds for the discovery of anti-NAFLD candidates.
