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Synthesis and anti-SARS-CoV-2 activity and mechanism research of lycorine derivatives
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Yu-heng MEI, Jia-yu LI, Dan-qing SONG, Zong-gen PENG, Ying-hong LI*
Acta Pharmaceutica Sinica | 2024, 59(2) : 395 - 403
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Acta Pharmaceutica Sinica | 2024, 59(2): 395-403
• Original Articles •
Synthesis and anti-SARS-CoV-2 activity and mechanism research of lycorine derivatives
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Yu-heng MEI, Jia-yu LI, Dan-qing SONG, Zong-gen PENG, Ying-hong LI*
Affiliations
  • Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2024-02-12 doi: 10.16438/j.0513-4870.2023-1121
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We designed and synthesized eighteen lycorine derivatives with five different structural types, and evaluated their antiviral activities on a HCoV-OC43-infected H460 cell model. Structure-activity relationships suggested that the introduction of appropriate substituents on the 6N atom of lycorine was beneficial to activity. Compound 6a gave a good activity with the half effective concentration (EC50) and selectivity index (SI) values of 2.36 μmol·L-1 and 16.52, respectively. Surface plasmon resonance (SPR) result indicated that 6a might target the non-structural protein 12 (NSP12) subunit in RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2 with the dissociation constant (KD) value of 1.36 μmol·L-1. Molecular docking indicated that 6a might act on nidovirus RdRp-associated nucleotidyltransferase (NiRAN) catalytic center of NSP12, distinct from the mechanism of nucleoside-like drugs such as remdesivir. This study provides scientific data for the development of lycorine derivatives into a new class of anti-SARS-CoV-2 small molecule inhibitors.

lycorine derivative  /  SARS-CoV-2  /  RNA-dependent RNA polymerase (RdRp)  /  nidovirus RdRp-associated nucleotidyltransferase (NiRAN)  /  antivirus
Yu-heng MEI, Jia-yu LI, Dan-qing SONG, Zong-gen PENG, Ying-hong LI. Synthesis and anti-SARS-CoV-2 activity and mechanism research of lycorine derivatives[J]. Acta Pharmaceutica Sinica, 2024 , 59 (2) : 395 -403 . DOI: 10.16438/j.0513-4870.2023-1121
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doi: 10.16438/j.0513-4870.2023-1121
  • Receive Date：2023-09-28
  • Online Date：2025-11-28
  • Published：2024-02-12
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  • Received：2023-09-28
  • Revised：2023-11-07
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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
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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