2. Academic Validation
  3. Active Ingredients of Reduning Injections Maintain High Potency against SARS-CoV-2 Variants

Active Ingredients of Reduning Injections Maintain High Potency against SARS-CoV-2 Variants

  • Chin J Integr Med. 2022 Nov 14;1-8. doi: 10.1007/s11655-022-3686-5.
Zhen Xiao 1 2,  Huan Xu 3,  Ze-Yang Qu 1 2,  Xin-Yuan Ma 4,  Bo-Xuan Huang 2 5,  Meng-Si Sun 3,  Bu-Qing Wang 6,  Guan-Yu Wang 7 8 9 10
Affiliations

Affiliations

  • 1 Department of Biology, School of Life Sciences, Southern University of Science and Technology, Shenzhen, Guangdong, 518055, China.
  • 2 Guangdong Provincial Key Laboratory of Computational Science and Material Design, Shenzhen, Guangdong Province, 518055, China.
  • 3 Institute of Chemical Biology, Shenzhen Bay Laboratories, Shenzhen, Guangdong Province, 518132, China.
  • 4 State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, 100191, China.
  • 5 Institute for Advanced Study, Shenzhen University, Shenzhen, Guangdong Province, 518052, China.
  • 6 Key Laboratory of Carbohydrate Chemistry and Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi, Jiangsu Province, 214122, China.
  • 7 Department of Biology, School of Life Sciences, Southern University of Science and Technology, Shenzhen, Guangdong, 518055, China. [email protected].
  • 8 Guangdong Provincial Key Laboratory of Computational Science and Material Design, Shenzhen, Guangdong Province, 518055, China. [email protected].
  • 9 School of Medicine Life and Health Sciences, Chinese University of Hong Kong, Shenzhen, Guangdong Province, 518172, China. [email protected].
  • 10 Center for Endocrinology and Metabolic Diseases, Second Affiliated Hospital, The Chinese University of Hong Kong, Shenzhen, Guangdong Province, 518172, China. [email protected].
PMID: 36374439 DOI: 10.1007/s11655-022-3686-5
Abstract

Objective: To investigate the anti-coronavirus potential and the corresponding mechanisms of the two ingredients of Reduning Injection: quercetin and luteolin.

Methods: A pseudovirus system was designed to test the efficacy of quercetin and luteolin to inhibit SARS-CoV-2 Infection and the corresponding cellular toxicity. Luteolin was tested for its activities against the pseudoviruses of SARS-CoV-2 and its variants. Virtual screening was performed to predict the binding sites by Autodock Vina 1.1.230 and PyMol. To validate docking results, surface plasmon resonance (SPR) was used to measure the binding affinity of the compounds with various proteins of the coronaviruses. Quercetin and luteolin were further tested for their inhibitory effects on other coronaviruses by indirect immunofluorescence assay on rhabdomyosarcoma cells infected with HCoV-OC43.

Results: The inhibition of SARS-CoV-2 pseudovirus by luteolin and quercetin were strongly dose-dependent, with concentration for 50% of maximal effect (EC50) of 8.817 and 52.98 µmol/L, respectively. Their cytotoxicity to BHK21-hACE2 were 177.6 and 405.1 µmol/L, respectively. In addition, luetolin significantly blocked the entry of 4 pseudoviruses of SARS-CoV-2 variants, with EC50 lower than 7 µmol/L. Virtual screening and SPR confirmed that luteolin binds to the S-proteins and quercetin binds to the active center of the 3CLpro, PLpro, and helicase proteins. Quercetin and luteolin showed over 99% inhibition against HCoV-OC43.

Conclusions: The mechanisms were revealed of quercetin and luteolin inhibiting the Infection of SARS-CoV-2 and its variants. Reduning Injection is a promising drug for COVID-19.

Keywords

Chinese medicine; Reduning injection; SARS-CoV-2; luteolin; quercetin.

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