JP2018052846A - 心房性ナトリウム利尿ペプチド分泌促進用組成物 - Google Patents
心房性ナトリウム利尿ペプチド分泌促進用組成物 Download PDFInfo
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- JP2018052846A JP2018052846A JP2016189715A JP2016189715A JP2018052846A JP 2018052846 A JP2018052846 A JP 2018052846A JP 2016189715 A JP2016189715 A JP 2016189715A JP 2016189715 A JP2016189715 A JP 2016189715A JP 2018052846 A JP2018052846 A JP 2018052846A
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- natriuretic peptide
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Abstract
Description
項1.イリドイド骨格を有する化合物を含有する心房性ナトリウム利尿ペプチド分泌促進用組成物。
項2.1日投与量あたり、イリドイド骨格を有する化合物を15〜500mg含有する、項1に記載の組成物。
項3.食品組成物、医薬組成物または飼料組成物である、項1または2に記載の組成物。
項4.イリドイド骨格を有する化合物がゲニポシド酸である、項1〜3のいずれかに記載の組成物。
項5.高血圧、動脈硬化、心不全、虚血性心疾患、慢性腎臓病、肥満、癌または骨粗鬆症の予防または改善を目的として使用される、項1〜4のいずれかに記載の組成物。
(1)ゲニポシド酸(GEA)の調製
精製水に48重量%濃度になるように水酸化ナトリウムを加え50℃まで昇温した。6分間かけてゲニポシド(四川双子叶生物科技有限公司より購入)を加えて50℃にて2時間撹拌した。原料の消失を目視で確認した後、25℃付近まで冷却し、4N塩酸で中和して粗ゲニポシド酸溶液を得た。粗ゲニポシド酸溶液を希塩酸でpH3.5に調整し、水で平衡化したODS(Daisogel SP-120-40/60 ODS-B、ダイソー株式会社製)に吸着させた。次いで、脱塩のため精製水で洗浄し、50容量%メタノール水溶液にて溶出し、高純度のゲニポシド酸を得た(純度99.5%以上)。
ゲニポシド酸をラットに投与し、血中の心房性ナトリウム利尿ペプチド(ANP)濃度を測定した。具体的には、前述の方法で精製したゲニポシド酸を純水と混合し、得られた溶液を、ゲニポシド酸100mg/kgとなるように絶食後の雄性16週齢SHR(高血圧自然発症ラット)へ単回経口投与した(n=6)。コントロールとして、前記溶液と同量の純水を、別の雄性16週齢SHR(高血圧自然発症ラット)へ単回経口投与した(n=6)。
血漿中のANPを定量するにあたり、化学発光酵素免疫測定法の一種であるsandwich chemiluminescent enzyme immunoassay(サンドイッチCLEIA)法を使用した。抗ラット/マウスα-ANPポリクローナル抗体(pAb #131-7、国立循環器病研究センター提供)が固定化されたマイクロプレートへ標準溶液としてアッセイバッファーに溶解したrat/mouse a−ANP(株式会社ペプチド研究所化学合成物)を添加して一次抗体処理を行った後、抗α−ANPマウスモノクローナル抗体(anti-α-ANP mAb、塩野義製薬株式会社提供)をプレートへ入れ、二次抗体処理を行った。続いて、発光基質(CDP-star plus Emerald II enhancer、Applied Biosystems、USA)を加えた後、プレートリーダー(Molecular Devices、USA)を用いて標準溶液の発光強度(relative luminescent units(RLU))を測定し、その平均値からバックグラウンド(Non-Specific Binding(NSB))を引いた値を測定値(RLU―NSB)として算出した。
Claims (4)
- イリドイド骨格を有する化合物を含有する心房性ナトリウム利尿ペプチド分泌促進用組成物。
- 1日投与量あたり、イリドイド骨格を有する化合物を15〜500mg含有する、請求項1に記載の組成物。
- 食品組成物、医薬組成物または飼料組成物である、請求項1または2に記載の組成物。
- イリドイド骨格を有する化合物がゲニポシド酸である、請求項1〜3のいずれかに記載の組成物。
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TW106130089A TWI747945B (zh) | 2016-09-28 | 2017-09-04 | 心房排鈉肽(atrial natriuretic peptide)分泌促進用組成物 |
PCT/JP2017/034617 WO2018062122A1 (ja) | 2016-09-28 | 2017-09-26 | 心房性ナトリウム利尿ペプチド分泌促進用組成物 |
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