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Potential inhibitor for blocking binding between ACE2 and SARS-CoV-2 spike protein with mutations - 20/04/22

Doi : 10.1016/j.biopha.2022.112802 
Ming-Shao Tsai a, b, Wei-Tai Shih c, Yao-Hsu Yang c, d, Yu-Shih Lin e, Geng-He Chang a, b, f, Cheng-Ming Hsu a, b, Reming-Albert Yeh a, Li-Hsin Shu c, Yu-Ching Cheng a, c, Hung-Te Liu c, Yu-Huei Wu g, Yu-Heng Wu h, Rou-Chen Shen a, Ching-Yuan Wu c, d, i,
a Department of Otolaryngology, Chang Gung Memorial Hospital, Chiayi, Taiwan 
b Faculty of Medicine, College of Medicine, Chang Gung University, Tao-Yuan, Taiwan 
c Department of Chinese Medicine, Chiayi Chang Gung Memorial Hospital, Chiayi, Taiwan 
d School of Chinese Medicine, College of Medicine, Chang Gung University, Tao-Yuan, Taiwan 
e Department of Pharmacy, Chiayi Chang Gung Memorial Hospital, Chiayi, Taiwan 
f Health Information and Epidemiology Laboratory, Chang Gung Memorial Hospital, Chiayi, Taiwan 
g Department of Biomedical Sciences, Chang Gung University, Tao-Yuan, Taiwan 
h Department of Electrical Engineering, National Sun Yat-Sen University, Kaohsiung, Taiwan 
i Research Center for Chinese Herbal Medicine, College of Human Ecology, Chang Gung University of Science and Technology, Taoyuan, Taiwan 

Correspondence to: Department of Traditional Chinese Medicine, Chang Gung Memorial Hospital, Chiayi Branch, Putzu, Taiwan.Department of Traditional Chinese Medicine, Chang Gung Memorial Hospital, Chiayi BranchPutzuTaiwan

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Abstract

At the time of writing, more than 440 million confirmed coronavirus disease 2019 (COVID-19) cases and more than 5.97 million COVID-19 deaths worldwide have been reported by the World Health Organization since the start of the outbreak of the pandemic in Wuhan, China. During the COVID-19 pandemic, many variants of SARS-CoV-2 have arisen because of high mutation rates. N501Y, E484K, K417N, K417T, L452R and T478K in the receptor binding domain (RBD) region may increase the infectivity in several variants of SARS-CoV-2. In this study, we discovered that GB-1, developed from Chiehyuan herbal formula which obtained from Tian Shang Sheng Mu of Chiayi Puzi Peitian Temple, can inhibit the binding between ACE2 and RBD with Wuhan type, K417N-E484K-N501Y and L452R-T478K mutation. In addition, GB-1 inhibited the binding between ACE2 and RBD with a single mutation (E484K or N501Y), except the K417N mutation. In the compositions of GB-1, glycyrrhizic acid can inhibit the binding between ACE2 and RBD with Wuhan type, except K417N-E484K-N501Y mutation. Our results suggest that GB-1 could be a potential candidate for the prophylaxis of different variants of SARS-CoV-2 infection because of its inhibition of binding between ACE2 and RBD with different mutations (L452R-T478K, K417N-E484K-N501Y, N501Y or E484K).

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Graphical Abstract




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Highlights

GB-1 can inhibit the binding between ACE2 and RBD with Wuhan type, K417N-E484K-N501Y and L452R-T478K mutation.
GB-1 inhibited the binding between ACE2 and RBD with a single mutation (E484K or N501Y), except the K417N mutation.
Glycyrrhizic acid can inhibit the binding between ACE2 and RBD with Wuhan type, except K417N-E484K-N501Y mutation.
GB-1 could be a potential candidate for the prophylaxis of different variants of SARS-CoV-2 infection because of its inhibition of binding between ACE2 and RBD with different mutations.

El texto completo de este artículo está disponible en PDF.

Chemical compounds studied in this article : Glycyrrhizic acid (Pubchem CID: 14982), (+)-Catechin (Pubchem CID: 9064)

Abbreviations : ACE2, SARS-CoV-2, COVID-19, RBD

Keywords : SARS-CoV-2, Spike protein, GB-1, Glycyrrhizic acid, COVID-19


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© 2022  The Authors. Publicado por Elsevier Masson SAS. Todos los derechos reservados.
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Vol 149

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