論文 - 詳細
| RRC ID | 27715 |
|---|---|
| 著者 | Shoji M, Takahashi E, Hatakeyama D, Iwai Y, Morita Y, Shirayama R, Echigo N, Kido H, Nakamura S, Mashino T, Okutani T, Kuzuhara T. |
| タイトル | Anti-influenza activity of c60 fullerene derivatives. |
| ジャーナル | PLoS One |
| Abstract |
The H1N1 influenza A virus, which originated in swine, caused a global pandemic in 2009, and the highly pathogenic H5N1 avian influenza virus has also caused epidemics in Southeast Asia in recent years. Thus, the threat from influenza A remains a serious global health issue, and novel drugs that target these viruses are highly desirable. Influenza A RNA polymerase consists of the PA, PB1, and PB2 subunits, and the N-terminal domain of the PA subunit demonstrates endonuclease activity. Fullerene (C60) is a unique carbon molecule that forms a sphere. To identify potential new anti-influenza compounds, we screened 12 fullerene derivatives using an in vitro PA endonuclease inhibition assay. We identified 8 fullerene derivatives that inhibited the endonuclease activity of the PA N-terminal domain or full-length PA protein in vitro. We also performed in silico docking simulation analysis of the C60 fullerene and PA endonuclease, which suggested that fullerenes can bind to the active pocket of PA endonuclease. In a cell culture system, we found that several fullerene derivatives inhibit influenza A viral infection and the expression of influenza A nucleoprotein and nonstructural protein 1. These results indicate that fullerene derivatives are possible candidates for the development of novel anti-influenza drugs. |
| 巻・号 | 8(6) |
| ページ | e66337 |
| 公開日 | 2013-1-1 |
| DOI | 10.1371/journal.pone.0066337 |
| PII | PONE-D-13-01705 |
| PMID | 23785493 |
| PMC | PMC3681905 |
| MeSH | Animals Antiviral Agents / chemistry Antiviral Agents / pharmacology* Antiviral Agents / toxicity Cell Line Dogs Enzyme Activation / drug effects Fullerenes / chemistry Fullerenes / pharmacology* Fullerenes / toxicity Influenza A Virus, H1N1 Subtype / drug effects Influenza A Virus, H1N1 Subtype / physiology Influenza A Virus, H3N2 Subtype / drug effects Influenza A Virus, H3N2 Subtype / physiology Influenza A virus / drug effects* Influenza A virus / physiology Molecular Conformation Molecular Docking Simulation RNA-Dependent RNA Polymerase / antagonists & inhibitors Viral Proteins / antagonists & inhibitors Viral Proteins / genetics Viral Proteins / metabolism |
| IF | 2.74 |
| 引用数 | 38 |
| WOS 分野 | VIROLOGY |
| オルトメトリクス指標 |
オルトメトリクス指標項目
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| 最多言及媒体 | X(Twitter) |
| 各媒体での言及数の合計 | 31 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| 遺伝子材料 | pBMSA-PA (RDB01971) |