Abstract
The coronavirus disease 2019 (COVID-19) pandemic is caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Despite the development of vaccines, the emergence of SARS-CoV-2 variants and the absence of effective therapeutics demand the continual investigation of COVID-19. Natural products containing active ingredients may be good therapeutic candidates. Here, we investigated the effectiveness of geraniin, the main ingredient in medical plants Elaeocarpus sylvestris var. ellipticus and Nephelium lappaceum, for treating COVID-19. The SARS-CoV-2 spike protein binds to the human angiotensin-converting enzyme 2 (hACE2) receptor to initiate virus entry into cells; viral entry may be an important target of COVID-19 therapeutics. Geraniin was found to effectively block the binding between the SARS-CoV-2 spike protein and hACE2 receptor in competitive enzyme-linked immunosorbent assay, suggesting that geraniin might inhibit the entry of SARS-CoV-2 into human epithelial cells. Geraniin also demonstrated a high affinity to both proteins despite a relatively lower equilibrium dissociation constant (KD) for the spike protein (0.63 μM) than hACE2 receptor (1.12 μM), according to biolayer interferometry-based analysis. In silico analysis indicated geraniin’s interaction with the residues functionally important in the binding between the two proteins. Thus, geraniin is a promising therapeutic agent for COVID-19 by blocking SARS-CoV-2’s entry into human cells.
Highlights
Introduction published maps and institutional affilThe coronavirus disease 2019 (COVID-19) pandemic, caused by an outbreak of a novel virus named severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in December 2019, seriously threatens human health globally
We investigated the potential of geraniin in inhibiting the entry of SARS-CoV-2 into cells by evaluating the interaction between the spike protein receptor-binding domain (RBD) and the human angiotensin-converting enzyme 2 (hACE2) receptor in the presence of geraniin using competitive ELISA (Figure 1)
In the plate coated with spike protein RBD, the antibody dramatically blocked the binding between spike protein RBD and the hACE2 receptor with the IC50 value of 0.106 μg/mL
Summary
The coronavirus disease 2019 (COVID-19) pandemic, caused by an outbreak of a novel virus named severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in December 2019, seriously threatens human health globally. 79% and 51.8% identity with SARS-CoV and Middle East respiratory syndrome coronavirus (MERS-CoV), respectively, and causes respiratory infections in humans [1]. SARS-CoV2 is more infectious, with a reproductive rate (R0 ) of 2.5 (range 1.8–3.6) than the H1N1 influenza A virus, SARS-CoV (2.0–3.0), MERS-CoV (0.9), and H1N1/09 virus (1.5) [2,3]. The high infectivity and fast mutation of SARS-CoV-2 have made the control of COVID-19 incredibly difficult. After SARS-CoV-2’s spike protein binds to the human angiotensin-converting enzyme 2 (hACE2) receptor on the surface of a host epithelial cell, it is primed, or cleaved, by transmembrane serine protease 2 (TMPRSS2) before the virus enters the cells.
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