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Bone-targeting of quinolones conjugated with an acidic oligopeptide
http://hdl.handle.net/2297/14387
http://hdl.handle.net/2297/14387899afffa-7fa8-4a09-8573-c51a4098c234
名前 / ファイル | ライセンス | アクション |
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HO-PR-MIYAMOTO-K-2881.pdf (473.6 kB)
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Item type | 会議発表論文 / Conference Paper(1) | |||||
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公開日 | 2017-10-05 | |||||
タイトル | ||||||
タイトル | Bone-targeting of quinolones conjugated with an acidic oligopeptide | |||||
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_5794 | |||||
資源タイプ | conference paper | |||||
著者 |
Takahashi, Tatsuo
× Takahashi, Tatsuo× Yokogawa, Koichi× Sakura, Naoki× Nomura, Masaaki× Kobayashi, Shinjiro× Miyamoto, Kenichi |
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書誌情報 |
Pharmaceutical Research 巻 25, 号 12, p. 2881-2888, 発行日 2008-12-01 |
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ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 0724-8741 | |||||
NCID | ||||||
収録物識別子タイプ | NCID | |||||
収録物識別子 | AA10632083 | |||||
DOI | ||||||
関連タイプ | isVersionOf | |||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1007/s11095-008-9605-4 | |||||
出版者 | ||||||
出版者 | Springer Science+Business Media B.V. | |||||
抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Purpose. Osteomyelitis is a progressive infectious process resulting in inflammatory destruction and necrosis of bone. The long-term administration of high-dosage antibiotics is required to treat osteomyelitis, owing to the limited distribution of antibiotics within bone. Therefore, targeted delivery of antibiotics to bone promises to improve therapeutic effectiveness. Methods. We synthesized quinolones such as levofloxacin and norfloxacin conjugated to an acidic oligopeptide, which works as a bone-targeting carrier after systemic administration. The therapeutic effectiveness of the conjugated quinolones in osteomyelitis was evaluated using a mouse model of osteomyelitis, created by inoculating Staphylococcus aureus into the tibia of mice. Results. With intravenous injection, the conjugated quinolones selectively distributed to bone, reaching concentrations up to 100-fold those of non-conjugated quinolones. Single intravenous injection of levofloxacin as well as conjugated levofloxacin exhibited antibiotic effects in the osteomyelitis mouse model; conversely, neither conjugated nor non-conjugated norfloxacin was effective. The antibiotic effect of conjugated levofloxacin persisted to at least 6 days after injection, whereas the effect of non-conjugated levofloxacin was temporary. Conclusion. The selective bone delivery of quinolones conjugated with an acidic oligopeptide may be effective in treating osteomyelitis, although the resulting concentration of antibiotic may be insufficient to completely kill S. aureus. © 2008 Springer Science+Business Media, LLC. | |||||
著者版フラグ | ||||||
出版タイプ | AM | |||||
出版タイプResource | http://purl.org/coar/version/c_ab4af688f83e57aa | |||||
関連URI | ||||||
識別子タイプ | DOI | |||||
関連識別子 | http://dx.doi.org/10.1007/s11095-008-9605-4 |