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Rosmarinic acid is a novel inhibitor for Hepatitis B virus replication targeting viral epsilon RNA-polymerase interaction
http://hdl.handle.net/10258/00010363
http://hdl.handle.net/10258/0001036340e49562-efd7-4613-958f-e5a6affb932c
名前 / ファイル | ライセンス | アクション |
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PO_13_5_e0197664 (6.3 MB)
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Item type | 学術雑誌論文 / Journal Article.(1) | |||||||||||
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公開日 | 2021-03-09 | |||||||||||
タイトル | ||||||||||||
言語 | en | |||||||||||
タイトル | Rosmarinic acid is a novel inhibitor for Hepatitis B virus replication targeting viral epsilon RNA-polymerase interaction | |||||||||||
言語 | ||||||||||||
言語 | eng | |||||||||||
資源タイプ | ||||||||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||||||||
資源タイプ | journal article | |||||||||||
アクセス権 | ||||||||||||
アクセス権 | open access | |||||||||||
アクセス権URI | http://purl.org/coar/access_right/c_abf2 | |||||||||||
著者 |
TSUKAMOTO, Yuta
× TSUKAMOTO, Yuta× IKEDA, Sotaro× 上井, 幸司
WEKO
911
× 田口, 莉帆× CHAYAMA, Kazuaki× SAKAGUCHI, Takemasa× NARITA, Ryo× YAO, Wan-Ling× TAKEUCHI, Fumihiko× OTAKAKI, Yukie× WATASHI, Koichi× WAKITA, Takaji× KATO, Hiroki× FUJITA, Takashi |
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室蘭工業大学研究者データベースへのリンク | ||||||||||||
上井 幸司(UWAI Koji) | ||||||||||||
http://rdsoran.muroran-it.ac.jp/html/100000240_ja.html | ||||||||||||
抄録 | ||||||||||||
内容記述タイプ | Abstract | |||||||||||
内容記述 | Current therapeutics for hepatitis B virus (HBV) patients such as nucleoside analogs (NAs) are effective; however, new antiviral drugs against HBV are still desired. Since the interaction between the epsilon (c) sequence of HBV pregenomic RNA and viral polymerase (Pot) is a key step in the HBV replication cycle, we aimed to identify small compounds for its inhibition, and established a pull-down assay system for the detection of c-RNA-binding-Pol. Screening showed that 5 out of 3,965 compounds inhibited c-Pol binding, and we identified rosmarinic acid, which exhibited specificity, as a potential antiviral agent. In order to examine the anti-HBV effects of rosmarinic acid, HBV-infected primary human hepatocytes from a humanized mouse liver were treated with rosmarinic acid. The rosmarinic acid treatment decreased HBV components including the amounts of extracellular HBV DNA with negligible cytotoxicity. We also investigated the combined effects of rosmarinic acid and the NA, lamivudine. rosmarinic acid slightly enhanced the anti-HBV activity of lamivudine, suggesting that the HBV replication step targeted by rosmarinic acid is distinct from that of NA. We analyzed an additional 25 rosmarinic acid derivatives, and found that 5 also inhibited c-Pol. Structural comparisons between these derivatives implied that the "two phenolic hydroxyl groups at both ends" and the "caffeic acid-like structure" of rosmarinic acid are critical for the inhibition of c-Pol binding. Collectively, our results demonstrate that rosmarinic acid inhibits HBV replication in HBV-infected cells by specifically targeting c-Pol binding. | |||||||||||
言語 | en | |||||||||||
書誌情報 |
en : PLOS ONE 巻 13, 号 5, 発行日 2018 |
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出版者 | ||||||||||||
言語 | en | |||||||||||
出版者 | PUBLIC LIBRARY SCIENCE | |||||||||||
出版者版へのリンク | ||||||||||||
10.1371/journal.pone.0197664 | ||||||||||||
https://doi.org/10.1371/journal.pone.0197664 | ||||||||||||
DOI | ||||||||||||
関連タイプ | isIdenticalTo | |||||||||||
識別子タイプ | DOI | |||||||||||
関連識別子 | 10.1371/journal.pone.0197664 | |||||||||||
日本十進分類法 | ||||||||||||
主題Scheme | NDC | |||||||||||
主題 | 499 | |||||||||||
ISSN | ||||||||||||
収録物識別子タイプ | EISSN | |||||||||||
収録物識別子 | 1932-6203 | |||||||||||
権利 | ||||||||||||
言語 | en | |||||||||||
権利情報 | https://creativecommons.org/licenses/by/4.0/ | |||||||||||
著者版フラグ | ||||||||||||
出版タイプ | VoR | |||||||||||
出版タイプResource | http://purl.org/coar/version/c_970fb48d4fbd8a85 | |||||||||||
フォーマット | ||||||||||||
内容記述タイプ | Other | |||||||||||
内容記述 | application/pdf |