Reference - Detail
| RRC ID | 77786 |
|---|---|
| Author | Kiba Y, Tanikawa T, Hayashi T, Kamauchi H, Seki T, Suzuki R, Kitamura M. |
| Title | Inhibition of furin-like enzymatic activities and SARS-CoV-2 infection by osthole and phenolic compounds with aryl side chains. |
| Journal | Biomed Pharmacother |
| Abstract |
Coronavirus disease 2019 (COVID-19), caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), spread as a pandemic and caused damage to people's lives and countries' economies. The spike (S) protein of SARS-CoV-2 contains a cleavage motif, Arg-X-X-Arg, for furin and furin-like enzymes at the boundary of the S1/S2 subunits. Given that cleavage plays a crucial role in S protein activation and viral entry, the cleavage motif was selected as the target. Our previous fluorogenic substrate study showed that osthole, a coumarin compound, inhibits furin-like enzyme activity. In this study, we examined the potential activities of 15 compounds with a structure-activity relationship with osthole, and evaluated their protective ability against SARS-CoV-2 infection. Of the 15 compounds tested, compounds C1 and C2 exhibited the inhibitory effects of osthole against furin-like enzymatic activity; however, little or no inhibitory effects against furin activity were observed. We further examined the inhibition of SARS-CoV-2 activity by compounds C1 and C2 using a Vero E6 cell line that expresses the transmembrane protease serine 2 (TMPRSS2). Compounds C1, C2, and osthole effectively inhibited SARS-CoV-2 infection. Therefore, osthole and its derivatives can potentially be used as therapeutic agents against SARS-CoV-2. |
| Volume | 169 |
| Pages | 115940 |
| Published | 2023-12-31 |
| DOI | 10.1016/j.biopha.2023.115940 |
| PII | S0753-3322(23)01738-9 |
| PMID | 38007936 |
| MeSH | COVID-19* Coumarins / pharmacology Furin* Humans SARS-CoV-2 / metabolism |
| IF | 4.545 |
| Altmetric score |
オルトメトリクス指標項目
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| The most frequently cited source | X(Twitter) |
| Total number of mentions | 3 |
| Altmetric score changes over past 6months | 0.0 |
| Resource | |
| Human and Animal Cells | CACO-2(RCB0988) |