ZHAO Li-ping, CHENG Yang-yang, FAN Tian-yun, ZENG Qing-xuan, KONG Wei-jia, SONG Dan-qing, WANG Yan-xiang*. Synthesis and evaluation on triglyceride inhibitory activities of novel indole alkaloidsJ. Acta Pharmaceutica Sinica, 2022,57(2): 433-440. doi: 10.16438/j.0513-4870.2021-1439
Citation: ZHAO Li-ping, CHENG Yang-yang, FAN Tian-yun, ZENG Qing-xuan, KONG Wei-jia, SONG Dan-qing, WANG Yan-xiang*. Synthesis and evaluation on triglyceride inhibitory activities of novel indole alkaloidsJ. Acta Pharmaceutica Sinica, 2022,57(2): 433-440. doi: 10.16438/j.0513-4870.2021-1439

Synthesis and evaluation on triglyceride inhibitory activities of novel indole alkaloids

  • Three tricyclic6,5,7 and six tetracyclic6,5,5,5 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.
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