WEKO3
アイテム
Kinetics and metabolism of apocynin in the mouse brain assessed with positron-emission tomography
https://repo.qst.go.jp/records/48400
https://repo.qst.go.jp/records/484003807b6a8-7467-420a-8ed1-838a24457646
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2017-12-05 | |||||
| タイトル | ||||||
| タイトル | Kinetics and metabolism of apocynin in the mouse brain assessed with positron-emission tomography | |||||
| 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_6501 | |||||
| 資源タイプ | journal article | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Okamura, Toshimitsu
× Okamura, Toshimitsu× Okada, Maki× Kikuchi, Tatsuya× Wakizaka, Hidekatsu× Zhang, Ming-Rong× 岡村 敏充× 岡田 真希× 菊池 達矢× 脇坂 秀克× 張 明栄 |
|||||
| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Background: Apocynin is a constituent of the medicinal herb Picrorhiza kurroa. It is an inhibitor of nicotinamide adenine dinucleotide phosphate oxidase. This compound shows potential anti-inflammatory and antioxidant effects and has been tested as a neuroprotectant in many animal models of brain disease. In such studies, understanding the brain kinetics of apocynin would be important for interpreting its in vivo efficacy; however, little has been reported on the kinetics of apocynin in the brain. Purpose: The purpose of this study is to investigate the kinetics and metabolism of apocynin in the brain of mice. Study design: The kinetics and metabolism of apocynin were examined using [11C]apocynin and positronemission tomography (PET). Methods: In vivo PET scanning was performed in mice for 20 min after intraperitoneal administration of an apocynin solution containing [11C]apocynin. Metabolites in the brain were analyzed using high-performance liquid chromatography. The doses of apocynin used ranged from <1.5 μg/kg (tracer dose) to 100 mg/kg. Results: Brain radioactivity during the period of 0 to 20 min after administration was negligible at the tracer dose and extremely low at the dose of 10 mg/kg. Moderate radioactivity was observed in the brain a few minutes after administration at the doses of 25 and 50 mg/kg and rapidly decreased thereafter. At a dose of 100 mg/kg, [11C] apocynin resulted in a high uptake of radioactivity followed by a gradual washout. In contrast to the brain, a clear dose-dependent increase in radioactivity was not observed in the blood. The fraction of the unchanged form in the brain decreased with time, and the degree of the reduction depended on apocynin doses: apocynin was rapidly metabolized in the brain at lower doses, whereas it was slowly decomposed at higher doses. On the basis of these data, the maximum apocynin concentrations in the brain were calculated to be 10 μM (10 mg/kg), 49 μM (25 mg/kg), 150 μM (50 mg/kg), and 380 μM (100 mg/kg). A metabolite observed in the brain was found to be apocynin glucuronide but not diapocynin, an active metabolite. Conclusion: These results would be useful for an evaluation of the potential efficacy of apocynin as a neuroprotective agent. |
|||||
| 書誌情報 |
Phytomedicine 巻 38, p. 84-89, 発行日 2018-01 |
|||||
| 出版者 | ||||||
| 出版者 | ELSEVIER | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0944-7113 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1016/j.phymed.2017.05.006 | |||||
