2024 Fiscal Year Final Research Report
Quantitative structure-activity relationship analysis of anti-inflammatory drugs with activate Nrf2
| Project/Area Number |
22K06572
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Review Section |
Basic Section 47020:Pharmaceutical analytical chemistry and physicochemistry-related
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| Research Institution | Shujitsu University |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
田坂 祐一 就実大学, 薬学部, 准教授 (00574758)
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| Project Period (FY) |
2022-04-01 – 2025-03-31
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| Keywords | 非ステロイド系抗炎症薬 / Nrf2－ARE経路 / 酸化ストレス / 構造活性相関 |
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| Outline of Final Research Achievements |
In this study, we focused on the fact that nonsteroidal anti-inflammatory drugs (non-steroidal drugs that relieve fever and pain) have antioxidant effects, and discovered a compound from existing drugs that effectively activates the Nrf2-ARE pathway (a mechanism that protects cells from stress) in HEK-293 cell lines (cells made from human kidneys and often used in experiments). In addition, by analyzing the structure-activity relationship of this compound (changing the structure of the drug to examine differences in effectiveness), we identified the key structure that contributes to the activation of the Nrf2-ARE pathway and the induction of HO-1 (a type of enzyme that works in ecological defense).
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| Free Research Field |
創薬化学
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| Academic Significance and Societal Importance of the Research Achievements |
本研究では、NSAIDs（熱や痛みを和らげる、ステロイドではない薬）の抗酸化活性（体の中の有害な物質を取り除いて細胞を守る力）に注目し、生体における酸化ストレス（体の中で発生する有害な物質が細胞を傷つける状態）に対して防御作用を示す新しいタイプのNSAIDの創製を目指して研究を実施した。具体的には、既存のNSAIDsの中からHEK-293細胞（ヒトの腎臓から作られた、実験によく使用される細胞）に対する抗酸化作用が強いNSAIDを発見し、化学構造の観点から薬理活性に関与する鍵構造を同定した。本研究で得られた成果は、医薬品開発に直結する点においても社会的貢献性が極めて高いと考えられる。
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