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銅および亜鉛キレート形成によるACE阻害剤エナラプリラトの脂溶性増加(発表論文抄録(2013))
https://fukuyama-u.repo.nii.ac.jp/records/8735
https://fukuyama-u.repo.nii.ac.jp/records/8735bb54851c-59b1-47a4-ab1a-cee58e6491ec
| 名前 / ファイル | ライセンス | アクション |
|---|---|---|
藤岡晴人(発表論文抄録(2013)) (134.4 kB)
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Copyright (c) 2014 by Fukuyama University
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| Item type | 紀要論文 / Departmental Bulletin Paper(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2017-12-18 | |||||
| タイトル | ||||||
| タイトル | 銅および亜鉛キレート形成によるACE阻害剤エナラプリラトの脂溶性増加(発表論文抄録(2013)) | |||||
| タイトル | ||||||
| タイトル | Increase in Lipophilicity of Enalaprilat by Complexation with Copper(II) or Zinc(II) Ions | |||||
| 言語 | en | |||||
| 言語 | ||||||
| 言語 | jpn | |||||
| キーワード | ||||||
| 言語 | en | |||||
| 主題Scheme | Other | |||||
| 主題 | angiotensin-converting enzyme inhibitor | |||||
| キーワード | ||||||
| 言語 | en | |||||
| 主題Scheme | Other | |||||
| 主題 | enalaprilat | |||||
| キーワード | ||||||
| 言語 | en | |||||
| 主題Scheme | Other | |||||
| 主題 | metal-ligand interaction | |||||
| キーワード | ||||||
| 言語 | en | |||||
| 主題Scheme | Other | |||||
| 主題 | metal deficiency | |||||
| 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 | departmental bulletin paper | |||||
| 著者 |
藤岡, 晴人
× 藤岡, 晴人× 稗田, 雄三× 倉本, 康弘× 小西, 華那世× 木下(菊田), 恵美子× 木下, 英司× 小池, 透 |
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| 著者別名 | ||||||
| 識別子Scheme | WEKO | |||||
| 識別子 | 45631 | |||||
| 姓名 | Fujioka, Haruto | |||||
| 著者別名 | ||||||
| 識別子Scheme | WEKO | |||||
| 識別子 | 45632 | |||||
| 姓名 | Hieda, Yuhzo | |||||
| 著者別名 | ||||||
| 識別子Scheme | WEKO | |||||
| 識別子 | 45633 | |||||
| 姓名 | Kuramoto, Yasuhiro | |||||
| 著者別名 | ||||||
| 識別子Scheme | WEKO | |||||
| 識別子 | 45634 | |||||
| 姓名 | Konishi, Kanayo | |||||
| 著者別名 | ||||||
| 識別子Scheme | WEKO | |||||
| 識別子 | 45635 | |||||
| 姓名 | Kinoshita-Kikuta, Emiko | |||||
| 著者別名 | ||||||
| 識別子Scheme | WEKO | |||||
| 識別子 | 45636 | |||||
| 姓名 | Kinoshita, Eiji | |||||
| 著者別名 | ||||||
| 識別子Scheme | WEKO | |||||
| 識別子 | 45637 | |||||
| 姓名 | Koike, Tohru | |||||
| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Enalaprilat (H<sub>2</sub>L), which is the active metabolite of the pro-drug enalapril, is an angiotensin-converting enzyme inhibitor. Some side effects such as neurodegeneration and taste disorder can be related to copper or zinc deficiency, which would be caused by the metal complex formation of dianionic elalaprilat (L<sup>2−</sup>). For a better understanding of this phenomenon, we investigated the solution species of enalaprilat in the presence of copper(II) or zinc(II) ions by pH titration analysis with <i>I</i>=0.10 <small>M</small> (NaCl) at 25℃. The 1:1 complex formation constants (<i>K</i><sub>ML</sub>=[ML]/[M<sup>2+</sup>][L<sup>2−</sup>] <small>M</small><sup>−1</sup>) of 10<sup>7.4</sup> for CuL and 10<sup>4.4</sup> for ZnL complexes were evaluated, indicating the presence of those complexes at a physiological pH. Furthermore, partition experiments with a two-phase system of 1-butanol/water at 25℃ disclosed that copper(II) and zinc(II) complexes of enalaprilat were partially extracted into the organic layer. In the absence of those metal ions, enalaprilat was not soluble in the 1-butanol phase. The increase in lipophilicity of enalaprilat by metal complexation suggests that the long-term administration of enalapril could be a possible risk factor for the disrupted distribution of those metal ions in biological systems.<br> | |||||
| 内容記述 | ||||||
| 内容記述タイプ | Other | |||||
| 内容記述 | Enalaprilat (H<sub>2</sub>L), which is the active metabolite of the pro-drug enalapril, is an angiotensin-converting enzyme inhibitor. Some side effects such as neurodegeneration and taste disorder can be related to copper or zinc deficiency, which would be caused by the metal complex formation of dianionic elalaprilat (L<sup>2−</sup>). For a better understanding of this phenomenon, we investigated the solution species of enalaprilat in the presence of copper(II) or zinc(II) ions by pH titration analysis with <i>I</i>=0.10 <small>M</small> (NaCl) at 25℃. The 1:1 complex formation constants (<i>K</i><sub>ML</sub>=[ML]/[M<sup>2+</sup>][L<sup>2−</sup>] <small>M</small><sup>−1</sup>) of 10<sup>7.4</sup> for CuL and 10<sup>4.4</sup> for ZnL complexes were evaluated, indicating the presence of those complexes at a physiological pH. Furthermore, partition experiments with a two-phase system of 1-butanol/water at 25℃ disclosed that copper(II) and zinc(II) complexes of enalaprilat were partially extracted into the organic layer. In the absence of those metal ions, enalaprilat was not soluble in the 1-butanol phase. The increase in lipophilicity of enalaprilat by metal complexation suggests that the long-term administration of enalapril could be a possible risk factor for the disrupted distribution of those metal ions in biological systems.<br> | |||||
| 書誌情報 |
福山大学薬学部研究年報 en : Annual report of the Faculty of Pharmacy & Pharmaceutical Sciences, Fukuyama University 巻 3, 号 32, p. 22-22, 発行日 2014-12-25 |
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| 出版者 | ||||||
| 出版者 | 福山大学薬学部 | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0288-724X | |||||
| 書誌レコードID | ||||||
| 収録物識別子タイプ | NCID | |||||
| 収録物識別子 | AN10064550 | |||||
