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Discovery of a novel SARS-CoV-2 main protease inhibitor by a simple and optimized colorimetric screening assay
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Gan-gan YAN1, Hao-hao YAN1, Zhi-cheng LIU1, Hai-yan QI1, Xiao-li LIU1, Xiao-ping LIU1, Jing ZHANG2, *, Yun-yu CHEN1, *
Acta Pharmaceutica Sinica | 2022, 57(10) : 3019 - 3026
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Acta Pharmaceutica Sinica | 2022, 57(10): 3019-3026
• Special Reports Ⅰ: New Targets, New Strategies for Drug Discovery and Advances in Antiviral Drug Research •
Discovery of a novel SARS-CoV-2 main protease inhibitor by a simple and optimized colorimetric screening assay
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Gan-gan YAN1, Hao-hao YAN1, Zhi-cheng LIU1, Hai-yan QI1, Xiao-li LIU1, Xiao-ping LIU1, Jing ZHANG2, *, Yun-yu CHEN1, *
Affiliations
  • 1. Institute for Drug Screening and Evaluation, Wannan Medical College, Wuhu 241002, China
  • 2. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2022-10-12 doi: 10.16438/j.0513-4870.2022-0365
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For rapid discovery of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro) inhibitors from a natural product library, a novel colorimetric screening assay was developed. According to the colorimetric principle, the synthetic peptide TSAVLQ-para-nitroanilide (pNA) was used as the Mpro hydrolysis substrate. Subsequently, the working concentration of pNA substrate, Mpro working concentration, hydrolysis time and DMSO tolerance were optimized for the development of a simple and robust colorimetric screening assay. Through these systematic optimizations, we selected 0.4 μmol·L-1 Mpro and 100 μmol·L-1 pNA substrate as the optimal working concentrations in this colorimetric screening assay, and a high Z' factor of 0.9 was achieved. Using this screening assay, natural product ginkgolic acid C13:0 (GA13:0) was identified as a novel competitive Mpro inhibitor in vitro. Taken together, we have successfully developed a simple and optimized colorimetric screening assay, which will be vital for the discovery of novel SARS-CoV-2 Mpro inhibitors.

SARS-CoV-2  /  main protease inhibitor  /  colorimetric screening assay  /  fluorescence resonance energy transfer  /  fluorescence polarization  /  ginkgolic acid C13:0
Gan-gan YAN, Hao-hao YAN, Zhi-cheng LIU, Hai-yan QI, Xiao-li LIU, Xiao-ping LIU, Jing ZHANG, Yun-yu CHEN. Discovery of a novel SARS-CoV-2 main protease inhibitor by a simple and optimized colorimetric screening assay[J]. Acta Pharmaceutica Sinica, 2022 , 57 (10) : 3019 -3026 . DOI: 10.16438/j.0513-4870.2022-0365
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Year 2022 volume 57 Issue 10
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Article Info
doi: 10.16438/j.0513-4870.2022-0365
  • Receive Date：2022-03-28
  • Online Date：2025-12-24
  • Published：2022-10-12
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History
  • Received：2022-03-28
  • Revised：2022-05-01
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Affiliations
    1. Institute for Drug Screening and Evaluation, Wannan Medical College, Wuhu 241002, China
    2. 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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