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Synthesis and evaluation of N-cycloberberine derivatives as a novel class of anti-SARS-CoV-2 pseudovirus agents
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Tian-yun FAN1, Jia-jing WU2, Ying-hong LI1, Wei-jin HUANG2, Xi-xi GUO1, Li-ping ZHAO1, Yan-xiang WANG1, You-chun WANG2, Dan-qing SONG1, *
Acta Pharmaceutica Sinica | 2021, 56(6) : 1663 - 1669
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Acta Pharmaceutica Sinica | 2021, 56(6): 1663-1669
• Original Articles •
Synthesis and evaluation of N-cycloberberine derivatives as a novel class of anti-SARS-CoV-2 pseudovirus agents
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Tian-yun FAN1, Jia-jing WU2, Ying-hong LI1, Wei-jin HUANG2, Xi-xi GUO1, Li-ping ZHAO1, Yan-xiang WANG1, You-chun WANG2, Dan-qing SONG1, *
Affiliations
  • 1. Beijing Key Laboratory of Antimicrobial Agents, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
  • 2. National Institute for Food and Drug Control, Beijing 102629, China
Published: 2021-06-12 doi: 10.16438/j.0513-4870.2021-0203
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There is no specific drug against COVID-19, but berberine (BBR) has moderate anti-SARS-CoV-2 pseudovirus activity. Taking BBR as the lead, 18 novel N-cycloberberine derivatives were synthesized and evaluated for their anti-SARS-CoV-2 pseudovirus activities in vitro. Structure-activity relationship analysis revealed that introducing an appropriate heterocyclic group at position 9 might be beneficial for potency. Among the tested compounds, compound 3m showed the most potent activity against SARS-CoV-2, with EC50 value of 1.61 μmol·L-1 and SI value of 22.2, much better than that of BBR. Additional experiment indicated that 3m had inhibitory activity on multiple processes in viral invasion, including adsorption and membrane fusion, suggesting a multi-target synergistic mechanism of action. These results provide a novel family of lead compounds for the discovery of anti-SARS-CoV-2 candidates.

N-cycloberberine  /  SARS-CoV-2  /  structure-activity relationship  /  time-of-addition
Tian-yun FAN, Jia-jing WU, Ying-hong LI, Wei-jin HUANG, Xi-xi GUO, Li-ping ZHAO, Yan-xiang WANG, You-chun WANG, Dan-qing SONG. Synthesis and evaluation of N-cycloberberine derivatives as a novel class of anti-SARS-CoV-2 pseudovirus agents[J]. Acta Pharmaceutica Sinica, 2021 , 56 (6) : 1663 -1669 . DOI: 10.16438/j.0513-4870.2021-0203
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Year 2021 volume 56 Issue 6
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Article Info
doi: 10.16438/j.0513-4870.2021-0203
  • Receive Date：2021-02-05
  • Online Date：2025-12-18
  • Published：2021-06-12
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History
  • Received：2021-02-05
  • Revised：2021-03-10
Funding
Affiliations
    1. Beijing Key Laboratory of Antimicrobial Agents, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
    2. National Institute for Food and Drug Control, Beijing 102629, 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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