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Synthesis and evaluation on triglyceride inhibitory activities of novel indole alkaloids
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Li-ping ZHAO, Yang-yang CHENG, Tian-yun FAN, Qing-xuan ZENG, Wei-jia KONG, Dan-qing SONG, Yan-xiang WANG*
Acta Pharmaceutica Sinica | 2022, 57(2) : 433 - 440
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Acta Pharmaceutica Sinica | 2022, 57(2): 433-440
Original Articles
Synthesis and evaluation on triglyceride inhibitory activities of novel indole alkaloids
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Li-ping ZHAO, Yang-yang CHENG, Tian-yun FAN, Qing-xuan ZENG, Wei-jia KONG, Dan-qing SONG, Yan-xiang WANG*
Affiliations
  • Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2022-02-12 doi: 10.16438/j.0513-4870.2021-1439
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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.

indole alkaloid  /  synthesis  /  anti-triglyceride activity  /  AMPK
Li-ping ZHAO, Yang-yang CHENG, Tian-yun FAN, Qing-xuan ZENG, Wei-jia KONG, Dan-qing SONG, Yan-xiang WANG. Synthesis and evaluation on triglyceride inhibitory activities of novel indole alkaloids[J]. Acta Pharmaceutica Sinica, 2022 , 57 (2) : 433 -440 . DOI: 10.16438/j.0513-4870.2021-1439
Year 2022 volume 57 Issue 2
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Article Info
doi: 10.16438/j.0513-4870.2021-1439
  • Receive Date:2021-10-05
  • Online Date:2025-12-22
  • Published:2022-02-12
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  • Received:2021-10-05
  • Revised:2021-11-09
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    Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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