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10.1021/acs.jnatprod.0c01136

http://scihub22266oqcxt.onion/10.1021/acs.jnatprod.0c01136
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33560122!ä!33560122

suck abstract from ncbi


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pmid33560122      J+Nat+Prod 2021 ; 84 (2): 436-443
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  • Axial Chiral Binaphthoquinone and Perylenequinones from the Stromata of Hypocrella bambusae Are SARS-CoV-2 Entry Inhibitors #MMPMID33560122
  • Li YT; Yang C; Wu Y; Lv JJ; Feng X; Tian X; Zhou Z; Pan X; Liu S; Tian LW
  • J Nat Prod 2021[Feb]; 84 (2): 436-443 PMID33560122show ga
  • 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 pseudotyped SARS-CoV-2 infection in 293T-ACE2 cells with IC(50) values of 0.17, 0.038, and 0.12 muM. Compounds 4 and 5 were also active against live SARS-CoV-2 infection with EC(50) values of 0.22 and 0.21 muM, 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.
  • |Hypocreales/*chemistry[MESH]
  • |Naphthoquinones/chemistry/*pharmacology[MESH]
  • |Perylene/*analogs & derivatives/chemistry/pharmacology[MESH]
  • |Quinones/chemistry/*pharmacology[MESH]
  • |SARS-CoV-2/*drug effects/physiology[MESH]


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