城西大学機関リポジトリJURAInhibition of furin-like enzymatic activities and SARS-CoV-2 infection by osthole and phenolic compounds with aryl side chains

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Inhibition of furin-like enzymatic activities and SARS-CoV-2 infection by osthole and phenolic compounds with aryl side chains

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ID	JOS-j.biopha.2023.115940
著者：名前	騎馬, 由佳/谷川, 尚/林, 豪士/鎌内, 等/關, 大志/鈴木, 龍一郎/北村, 雅史
著者：別形式	Kiba, Yuka / Tanikawa, Takashi / Hayashi, Tsuyoshi / Kamauchi, Hitoshi / Seki,Taishi / Suzuki, Ryuichiro / Kitamura , Masashi
著者：カナ	キバ, ユカ/タニカワ, タカシ/ハヤシ, ツヨシ/カマウチ, ヒトシ/セキ, タイシ/スズキ, リュウイチロウ/キタムラ, マサシ
著者：所属	城西大学薬学部薬学科 / 城西大学薬学部薬学科 / 国立感染症研究所ウイルス第二部 / 城西大学薬学部薬科学科 / 城西大学薬学部薬学科 / 城西大学薬学部薬科学科 / 城西大学薬学部薬学科
著者：所属(別形式）	Josai University, Faculty of Pharmacy and Pharmaceutical Sciences, School of Pharmacy / Josai University, Faculty of Pharmacy and Pharmaceutical Sciences, School of Pharmacy / National Institute of Infectious Diseases, Department of Virology II / Josai University, Faculty of Pharmacy and Pharmaceutical Sciences, Department of Pharmaceutical Sciences / Josai University, Faculty of Pharmacy and Pharmaceutical Sciences, School of Pharmacy / Josai University, Faculty of Pharmacy and Pharmaceutical Sciences, Department of Pharmaceutical Sciences / Josai University, Faculty of Pharmacy and Pharmaceutical Sciences, School of Pharmacy
著者版フラグ	publisher
出版地	Amsterdam
出版者	Elsevier
冊子ISSN	07533322
掲載誌名	Biomedicine & Pharmacotherapy
巻	169
刊行年月	2023-12
開始ページ	1
終了ページ	6
コンテンツ作成日	2023-09-11
コンテンツ修正日	2023-11-21
コンテンツ登録日	2023-12-25
識別番号：DOI	info:doi/10.1016/j.biopha.2023.115940
識別番号：DOI（リンク）	https://doi.org/10.1016/j.biopha.2023.115940
PubMed番号	38007936
抄録	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.
キーワード	Coumarin/Furin/Osthole/SARS-CoV-2.
注記	Article number: 115940 (2023) Published by Elsevier Masson SAS. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).
言語	eng
資源タイプ	text
ジャンル	01学術雑誌論文 / Journal Article
フォーマット	application/pdf
権利	Copyright © 2023 The Author(s).
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このアイテムを表示する：URI	https://libir.josai.ac.jp/il/meta_pub/G0000284repository_JOS-j.biopha.2023.115940

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