Journal
JOURNAL OF NATURAL PRODUCTS
Volume 84, Issue 2, Pages 436-443Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.0c01136
Keywords
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Funding
- National Natural Science Foundation of China [81703381]
- Natural Science Foundation of Guangdong Province [2020A1515011027]
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A new axial chiral binaphtoquinone and a new perylenequinone were isolated from the stromata of Hypocrella bambusae and showed inhibitory activity against SARS-CoV-2 infection. These compounds were found to potentially bind with the receptor-binding domain of SARS-CoV-2 S protein, indicating their potential as entry inhibitors for the virus.
A new axial chiral binaphtoquinone, hypocrellone (1), and a new perylenequinone, hypomycin F (2), were isolated from the stromata of Hypocrella bambusae, together with five known compounds, 3-7. The structures of 1 and 2 were assigned by spectroscopic and HRESIMS data analyses. The axial chirality of 1 was determined by electronic circular dichroism data analysis, and the absolute configurations of 2 and 3 were determined by X-ray crystallography. The axial chirality of 7 was determined by UV-induced photooxidation from 4. Compounds 1, 4, and 5 showed inhibitory activity against pseudo typed SARS-CoV-2 infection in 293T-ACE2 cells with IC50 values of 0.17, 0.038, and 0.12 mu M. Compounds 4 and 5 were also active against live SARS-CoV-2 infection with EC50 values of 0.22 and 0.21 mu M, respectively. Further cell-cell fusion assays, surface plasmon resonance assays, and molecular docking studies revealed that 4 and 5 could bind with the receptor-binding domain of SARS-CoV-2 S protein to prevent its interaction with human angiotensin-converting enzyme II receptor. Our results revealed that 4 and 5 are potential SARS-CoV-2 entry inhibitors.
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