| Project/Area Number |
26460162
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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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| Research Field |
Drug development chemistry
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| Research Institution | Osaka Ohtani University |
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Principal Investigator |
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| Project Period (FY) |
2014-04-01 – 2019-03-31
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| Project Status |
Completed (Fiscal Year 2018)
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| Budget Amount *help |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2017: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2016: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2015: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2014: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
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| Keywords | 多剤耐性菌 / 抗生物質 / リューロムチリン / 創薬研究 / 治癒効果 |
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| Outline of Final Research Achievements |
Enlightenment activity for the proper use of antimicrobial agents have been worked, but the problem of resistant bacteria has not been solved, and the risk of life has increased due to the emergence of multi-drug resistant pathogens. Therefore, by deriving from a natural product which has good antibacterial activity and has a unique structure, we have focused to discover and develop novel classes of antibiotics, particularly agents with new mechanisms of action and no cross-resistance to marketed antibacterial agents.
As the result, we have succeeded in finding several compounds that have strong antibacterial activity against Gram-positive pathogens not only susceptible bacteria but also multi-drug resistant bacteria, and show good pharmacokinetics comparable to marketed antibacterial agents in evaluation systems using silkworms. Furthermore, we have succeeded in overcoming the hydrophobic nature of the natural product and in synthesizing of the water-soluble derivatives.
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| Academic Significance and Societal Importance of the Research Achievements |
半世紀以上も前に新規抗生物質として発見されたが、医薬品として開発されていない天然物を医薬品として開発可能な化合物へと誘導することを目的に研究を進めた結果、その特徴的な構造から予想される高い脂溶性を克服し、注射剤として必要な水溶性を持たせること、かつ多剤耐性菌に対して感受性菌と同等の強い抗菌活性を示す化合物を合成することに成功し、新規抗菌薬としての開発の可能性を示すことができた。この新規化合物は既存の抗菌剤とは構造的に大きく異なることから作用機序の差別化を可能とし、高い水溶性を利用した注射剤は、抗菌薬の選択肢数を増やし治療の幅を広げ、適正使用という意味において十分社会に貢献できる。
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