| Item type |
学術雑誌論文 / Journal Article(1) |
| 公開日 |
2025-01-20 |
| タイトル |
|
|
タイトル |
Influence of Endogenous Substances on Site-II to Site-I Displacement of Diclofenac Bound to Albumin in the Aqueous Humor of Patients with Cataract |
|
言語 |
en |
| 言語 |
|
|
言語 |
eng |
| キーワード |
|
|
言語 |
en |
|
主題Scheme |
Other |
|
キーワード |
diclofenac ophthalmic solution |
| キーワード |
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|
言語 |
en |
|
主題Scheme |
Other |
|
キーワード |
albumin |
| キーワード |
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|
言語 |
en |
|
主題Scheme |
Other |
|
キーワード |
conformational change |
| キーワード |
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|
言語 |
en |
|
主題Scheme |
Other |
|
キーワード |
aqueous humor |
| キーワード |
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|
言語 |
en |
|
主題Scheme |
Other |
|
キーワード |
fatty acid |
| 資源タイプ |
|
|
資源タイプ |
journal article |
| アクセス権 |
|
| 著者 |
Ishii, Saya
Ozaki, Mineo
Takamura, Norito
Ogata, Kenji
Tokunaga, Jin
池田, 龍二
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| 抄録 |
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|
内容記述タイプ |
Abstract |
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内容記述 |
Diclofenac instillation is useful in preventing intraoperative miosis and macular edema caused by postoperative inflammation in cataract surgery; however, optimum efficacy is not attained when the instilled diclofenac strongly binds to albumin in patients’ aqueous humor. Therefore, a method that inhibits diclofenac binding and increases the concentration of its free fraction is needed. We conducted a basic study regarding the effects of inhibitors on the binding of instilled diclofenac to albumin and endogenous substances in aqueous humor. Aqueous humor samples from 16 patients were pooled together for analysis. The free fraction of diclofenac was measured using ultrafiltration methods in various experiments with pooled and mimic aqueous humor. Free fraction of diclofenac, a site II drug, in pooled aqueous humor was 0.363 0.013. The binding of diclofenac in the presence of phenylbutazone (PB), a site I inhibitor, was significantly inhibited (free fraction 0.496 0.013); however, no significant inhibition by ibuprofen, a site II inhibitor, (free fraction 0.379 0.004), was observed. The unexpected result was due to free fatty acids (FFAs; palmitic acid (PA)) and L-tryptophan (Trp). The inhibition of diclofenac binding by PB in the mimic aqueous humor containing these endogenous substances revealed significant binding inhibition in the presence of PA and Trp. Diclofenac is strongly rebound from site II to site I in the presence of FFAs and Trp in the aqueous humor because FFAs and Trp induce a conformational change in albumin. Therefore, PB significantly inhibits the binding of diclofenac to albumin. |
|
言語 |
en |
| 内容記述 |
|
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内容記述タイプ |
Other |
|
内容記述 |
Citation: Saya Ishii, Mineo Ozaki, Norito Takamura, Kenji Ogata, Jin Tokunaga, Ryuji Ikeda, Influence of Endogenous Substances on Site-II to Site-I Displacement of Diclofenac Bound to Albumin in the Aqueous Humor of Patients with Cataract, Biological and Pharmaceutical Bulletin, 47(1), 213-220, 2024-01-20, https://doi.org/10.1248/bpb.b23-00301 |
|
言語 |
en |
| 書誌情報 |
en : Biological and Pharmaceutical Bulletin
巻 47,
号 1,
p. 213-220,
発行日 2024-01-20
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| 出版者 |
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|
出版者 |
Pharmaceutical Society of Japan |
|
言語 |
en |
| ISSN |
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収録物識別子タイプ |
PISSN |
|
収録物識別子 |
0918-6158 |
| ISSN |
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収録物識別子タイプ |
EISSN |
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収録物識別子 |
1347-5215 |
| DOI |
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関連タイプ |
isVersionOf |
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|
識別子タイプ |
DOI |
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|
関連識別子 |
https://doi.org/10.1248/bpb.b23-00301 |
| 権利 |
|
|
言語 |
en |
|
権利情報 |
© 2024 The Pharmaceutical Society of Japan |
| 著者版フラグ |
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出版タイプ |
VoR |
本文 (1.1 MB)
