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Tolcapone derivative PCDNA inhibits Aβ42 fibrillogenesis and reduces its cytotoxicity
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Bei-bei CHEN1, Lu-ying JIANG1, Fang-yan GUO2, Li-li QU1, Wen-qian WANG1, Cheng-hua JIN2, *, Fu-feng LIU1, *
Acta Pharmaceutica Sinica | 2021, 56(4) : 1063 - 1069
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Acta Pharmaceutica Sinica | 2021, 56(4): 1063-1069
• Original Articles •
Tolcapone derivative PCDNA inhibits Aβ42 fibrillogenesis and reduces its cytotoxicity
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Bei-bei CHEN1, Lu-ying JIANG1, Fang-yan GUO2, Li-li QU1, Wen-qian WANG1, Cheng-hua JIN2, *, Fu-feng LIU1, *
Affiliations
  • 1. College of Biotechnology, Tianjin University of Science and Technology, Tianjin 300457, China
  • 2. College of Pharmacy, Yanbian University, Yanji 133002, China
Published: 2021-04-12 doi: 10.16438/j.0513-4870.2020-1853
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Abnormal aggregation of amyloid-β protein (Aβ) in brain plays a vital role in the occurrence of Alzheimer's disease (AD). Hence, inhibiting Aβ aggregation is one major tactic for therapy of AD. Previous studies have found that tolcapone can inhibit Aβ42 aggregation and reduce the cytotoxicity induced by Aβ42 aggregates, but clinical studies have found that tolcapone has strong liver toxicity. To reduce the liver toxicity of tolcapone, its side chain structure was modified to obtain its derivative phenethyl (E)-2-cyano-3-(3, 4 dihydroxy-5-nitrobenzene)-acrylate (PCDNA). Thioflavin T (ThT) and atomic force microscopy (AFM) assays were used to explore the inhibitory effect of PCDNA on Aβ42 fibrillogenesis. The cytotoxicity assays were used to explore the inhibitory effect of PCDNA against the cytotoxicity induced by Aβ42 aggregates. In addition, the depolymerization effect of PCDNA on mature Aβ42 fibrils was also explored. Finally, molecular docking was used to explore the interaction between PCDNA and Aβ42 pentamer. These results lay the foundation for the study of the structural analogues of tolcapone as Aβ inhibitors.

Alzheimer's disease  /  amyloid-β protein  /  inhibitor  /  tolcapone derivative  /  fibrillogenesis  /  molecular docking
Bei-bei CHEN, Lu-ying JIANG, Fang-yan GUO, Li-li QU, Wen-qian WANG, Cheng-hua JIN, Fu-feng LIU. Tolcapone derivative PCDNA inhibits Aβ42 fibrillogenesis and reduces its cytotoxicity[J]. Acta Pharmaceutica Sinica, 2021 , 56 (4) : 1063 -1069 . DOI: 10.16438/j.0513-4870.2020-1853
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Article Info
doi: 10.16438/j.0513-4870.2020-1853
  • Receive Date：2020-12-03
  • Online Date：2025-12-18
  • Published：2021-04-12
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  • Received：2020-12-03
  • Revised：2021-01-21
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    1. College of Biotechnology, Tianjin University of Science and Technology, Tianjin 300457, China
    2. College of Pharmacy, Yanbian University, Yanji 133002, China
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多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
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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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