tetano
Editor, Senior Moderator
Biomed Pharmacother
. 2022 Mar 9;149:112802.
doi: 10.1016/j.biopha.2022.112802. Online ahead of print.
Potential inhibitor for blocking binding between ACE2 and SARS-CoV-2 spike protein with mutations
Ming-Shao Tsai[SUP] 1 [/SUP], Wei-Tai Shih[SUP] 2 [/SUP], Yao-Hsu Yang[SUP] 3 [/SUP], Yu-Shih Lin[SUP] 4 [/SUP], Geng-He Chang[SUP] 5 [/SUP], Cheng-Ming Hsu[SUP] 1 [/SUP], Reming-Albert Yeh[SUP] 6 [/SUP], Li-Hsin Shu[SUP] 2 [/SUP], Yu-Ching Cheng[SUP] 7 [/SUP], Hung-Te Liu[SUP] 2 [/SUP], Yu-Huei Wu[SUP] 8 [/SUP], Yu-Heng Wu[SUP] 9 [/SUP], Rou-Chen Shen[SUP] 6 [/SUP], Ching-Yuan Wu[SUP] 10 [/SUP]
Affiliations
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).
Keywords: (+)-Catechin (Pubchem CID: 9064); COVID-19; GB-1; Glycyrrhizic acid; Glycyrrhizic acid (Pubchem CID: 14982); SARS-CoV-2; Spike protein.
. 2022 Mar 9;149:112802.
doi: 10.1016/j.biopha.2022.112802. Online ahead of print.
Potential inhibitor for blocking binding between ACE2 and SARS-CoV-2 spike protein with mutations
Ming-Shao Tsai[SUP] 1 [/SUP], Wei-Tai Shih[SUP] 2 [/SUP], Yao-Hsu Yang[SUP] 3 [/SUP], Yu-Shih Lin[SUP] 4 [/SUP], Geng-He Chang[SUP] 5 [/SUP], Cheng-Ming Hsu[SUP] 1 [/SUP], Reming-Albert Yeh[SUP] 6 [/SUP], Li-Hsin Shu[SUP] 2 [/SUP], Yu-Ching Cheng[SUP] 7 [/SUP], Hung-Te Liu[SUP] 2 [/SUP], Yu-Huei Wu[SUP] 8 [/SUP], Yu-Heng Wu[SUP] 9 [/SUP], Rou-Chen Shen[SUP] 6 [/SUP], Ching-Yuan Wu[SUP] 10 [/SUP]
Affiliations
- PMID: 35279013
- DOI: 10.1016/j.biopha.2022.112802
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).
Keywords: (+)-Catechin (Pubchem CID: 9064); COVID-19; GB-1; Glycyrrhizic acid; Glycyrrhizic acid (Pubchem CID: 14982); SARS-CoV-2; Spike protein.