JP2017031146A - Nik阻害剤 - Google Patents
Nik阻害剤 Download PDFInfo
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- JP2017031146A JP2017031146A JP2016147543A JP2016147543A JP2017031146A JP 2017031146 A JP2017031146 A JP 2017031146A JP 2016147543 A JP2016147543 A JP 2016147543A JP 2016147543 A JP2016147543 A JP 2016147543A JP 2017031146 A JP2017031146 A JP 2017031146A
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- mangiferin
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- nik
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- ZTGSICGSZVMZDH-UHFFFAOYSA-N 4-[1-(2-amino-5-chloropyrimidin-4-yl)-2,3-dihydroindol-6-yl]-2-(3-methyl-1,2,4-oxadiazol-5-yl)but-3-yn-2-ol Chemical compound CC1=NOC(C(C)(O)C#CC=2C=C3N(CCC3=CC=2)C=2C(=CN=C(N)N=2)Cl)=N1 ZTGSICGSZVMZDH-UHFFFAOYSA-N 0.000 title claims abstract description 11
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
【解決手段】マンギフェリンを有効成分とするNIK阻害剤は、NIKだけを選択的に阻害することができ、NF−κBが恒常的に活性化している悪性腫瘍に対して有用な医薬組成物とすることができる。
【選択図】図1
Description
多発性骨髄腫細胞株であるIM9細胞を用いて、マンギフェリン投与によるNIK阻害作用について、イムノブロッティングで検討した結果、NIKの活性化阻害を認めた(図1)。
マンギフェリン投与により、NIKの下流シグナルであるIKK、IκB、NF−κBの活性動態について、イムノブロッティングで検討した結果、IKK、IκBの活性化阻害、IκBの発現増加、NF−κBおよびNF−κB2の核移行阻害を認めた(図2)。
マンギフェリン投与によるNIK/IKK/NF−κB経路以外の生存シグナル因子であるERK、JNK、mTORの活性動態について、イムノブロッティングで検討した結果、ERK、JNK、mTORの活性動態に変化を認めなかった(図3)。
多発性骨髄腫細胞株を用いて、マンギフェリンによる細胞死誘導効果について、トリパンブルーダイ法で検討した結果、図4に示されるように、全ての多発性骨髄腫細胞株においてマンギフェリンにより細胞死誘導効果を認めた。
悪性黒色腫細胞を用いてマンギフェリンによる腫瘍増殖抑制効果について検討した結果、図7に示されるようにマンギフェリン投与により腫瘍増殖抑制効果を認めた。
In vivoでのマンギフェリンのNIK抑制効果について悪性黒色腫細胞にて担癌マウスを作製し、検討を行った結果、図8に示されるようにマンギフェリン投与によりNIK、IKK及びNF−κBの抑制効果を認めた。
Claims (3)
- マンギフェリンを有効成分とするNIK阻害剤。
- マンギフェリンを有効成分とする癌若しくは炎症性疾患の予防薬。
- マンギフェリンを有効成分とする癌若しくは炎症性疾患の治療薬。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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JP2015150702 | 2015-07-30 | ||
JP2015150702 | 2015-07-30 |
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JP2017031146A true JP2017031146A (ja) | 2017-02-09 |
JP6488264B2 JP6488264B2 (ja) | 2019-03-20 |
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JP2016147543A Active JP6488264B2 (ja) | 2015-07-30 | 2016-07-27 | Nik阻害剤 |
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JP (1) | JP6488264B2 (ja) |
Cited By (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2019150087A1 (en) * | 2018-01-30 | 2019-08-08 | Olusola Clement Idowu | Mangiferin as a protective agent against mitochondrial dna damage and skin-care compositions comprising same |
WO2020130102A1 (ja) * | 2018-12-19 | 2020-06-25 | 学校法人近畿大学 | 自己免疫疾患の改善用組成物 |
WO2020162638A1 (ja) * | 2019-02-08 | 2020-08-13 | 学校法人近畿大学 | 悪性腫瘍疾患の改善用組成物 |
WO2022138735A1 (ja) | 2020-12-22 | 2022-06-30 | 学校法人近畿大学 | 悪性腫瘍疾患の改善用医薬組成物 |
WO2023234312A1 (ja) * | 2022-05-30 | 2023-12-07 | 学校法人近畿大学 | 自己免疫系疾患の改善用医薬組成物 |
WO2024029528A1 (ja) * | 2022-08-02 | 2024-02-08 | 学校法人近畿大学 | アレルギー性疾患の改善用医薬組成物 |
Citations (4)
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CN1977855A (zh) * | 2005-12-09 | 2007-06-13 | 海南盛科天然药物研究院有限公司 | 含芒果苷的药用组合物及其制备方法 |
JP2009023935A (ja) * | 2007-07-19 | 2009-02-05 | Univ Kinki | 消炎剤、関節炎における炎症性疾患治療剤 |
JP2012530078A (ja) * | 2009-06-16 | 2012-11-29 | 海南徳澤薬物研究有限公司 | マンギフェリンベルベリン塩およびその調製方法と用途 |
JP2014516976A (ja) * | 2011-07-06 | 2014-07-17 | 南京工▲業▼大学 | フルクトシル化マンギフェリン並びにその調製方法及び用途 |
-
2016
- 2016-07-27 JP JP2016147543A patent/JP6488264B2/ja active Active
Patent Citations (4)
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CN1977855A (zh) * | 2005-12-09 | 2007-06-13 | 海南盛科天然药物研究院有限公司 | 含芒果苷的药用组合物及其制备方法 |
JP2009023935A (ja) * | 2007-07-19 | 2009-02-05 | Univ Kinki | 消炎剤、関節炎における炎症性疾患治療剤 |
JP2012530078A (ja) * | 2009-06-16 | 2012-11-29 | 海南徳澤薬物研究有限公司 | マンギフェリンベルベリン塩およびその調製方法と用途 |
JP2014516976A (ja) * | 2011-07-06 | 2014-07-17 | 南京工▲業▼大学 | フルクトシル化マンギフェリン並びにその調製方法及び用途 |
Non-Patent Citations (3)
Title |
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CANCER LETTERS, vol. 305, JPN6018007655, 2011, pages 21 - 31, ISSN: 0003850651 * |
THE JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 279, JPN6018007659, 25 May 2004 (2004-05-25), pages 33768 - 33781, ISSN: 0003850649 * |
TOXICOLOGY AND APPLIED PHARMACOLOGY, vol. 272, JPN6018007652, 22 May 2013 (2013-05-22), pages 180 - 190, ISSN: 0003850650 * |
Cited By (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2019150087A1 (en) * | 2018-01-30 | 2019-08-08 | Olusola Clement Idowu | Mangiferin as a protective agent against mitochondrial dna damage and skin-care compositions comprising same |
WO2020130102A1 (ja) * | 2018-12-19 | 2020-06-25 | 学校法人近畿大学 | 自己免疫疾患の改善用組成物 |
JP7479695B2 (ja) | 2018-12-19 | 2024-05-09 | 学校法人近畿大学 | 自己免疫疾患の改善用組成物 |
WO2020162638A1 (ja) * | 2019-02-08 | 2020-08-13 | 学校法人近畿大学 | 悪性腫瘍疾患の改善用組成物 |
WO2022138735A1 (ja) | 2020-12-22 | 2022-06-30 | 学校法人近畿大学 | 悪性腫瘍疾患の改善用医薬組成物 |
WO2023234312A1 (ja) * | 2022-05-30 | 2023-12-07 | 学校法人近畿大学 | 自己免疫系疾患の改善用医薬組成物 |
WO2024029528A1 (ja) * | 2022-08-02 | 2024-02-08 | 学校法人近畿大学 | アレルギー性疾患の改善用医薬組成物 |
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