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Synthesis, cholinesterase inhibition and hepatotoxicity of tacrine-phenol-bifendate hybrids
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Chen HONG1, Yong-mei ZHAO2, *, Hui-yan GUO3, Wen LUO3, *
Acta Pharmaceutica Sinica | 2022, 57(9) : 2759 - 2766
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Acta Pharmaceutica Sinica | 2022, 57(9): 2759-2766
• Original Articles •
Synthesis, cholinesterase inhibition and hepatotoxicity of tacrine-phenol-bifendate hybrids
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Chen HONG1, Yong-mei ZHAO2, *, Hui-yan GUO3, Wen LUO3, *
Affiliations
  • 1. Huaihe Hospital, Henan University, Kaifeng 475004, China
  • 2. Pharmaceutical Engineering Department, Henan Vocational College of Applied Technology, Kaifeng 475004, China
  • 3. Key Laboratory of Natural Medicine and Immuno-Engineering, Henan University, Kaifeng 475004, China
Published: 2022-09-12 doi: 10.16438/j.0513-4870.2022-0437
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A series of tacrine-phenol-bifendate hybrids (7a-7e, 8a-8e) were designed, synthesized and evaluated as inhibitors of cholinesterases (ChEs) with low hepatotoxicity. All the compounds had potent ChEs inhibitory activity with half-inhibitory concentration (IC50) values at the nanomolar range. Compound 8d exhibited the strongest inhibition to acetylcholinesterase (AChE) with an IC50 value of 156.39 nmol·L-1 and compound 7b showed the most potent inhibition for butyrylcholinesterase with IC50 value of 16.33 nmol·L-1. Kinetic and molecular modeling studies showed that 8d targeted both the catalytic active site and the peripheral anionic site of AChE. In addition, these compounds showed low toxicity to hepatocytes, and compound 8d did not increase the level of reactive oxygen species in HepG2 cells.

tacrine  /  cholinesterase  /  hepatotoxicity  /  Alzheimer's disease
Chen HONG, Yong-mei ZHAO, Hui-yan GUO, Wen LUO. Synthesis, cholinesterase inhibition and hepatotoxicity of tacrine-phenol-bifendate hybrids[J]. Acta Pharmaceutica Sinica, 2022 , 57 (9) : 2759 -2766 . DOI: 10.16438/j.0513-4870.2022-0437
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Article Info
doi: 10.16438/j.0513-4870.2022-0437
  • Receive Date：2022-04-18
  • Online Date：2025-12-24
  • Published：2022-09-12
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History
  • Received：2022-04-18
  • Revised：2022-05-13
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Affiliations
    1. Huaihe Hospital, Henan University, Kaifeng 475004, China
    2. Pharmaceutical Engineering Department, Henan Vocational College of Applied Technology, Kaifeng 475004, China
    3. Key Laboratory of Natural Medicine and Immuno-Engineering, Henan University, Kaifeng 475004, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
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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