Studies of the mechanisms of action of neovibsanins toward the development of therapeutic agents for Alzheimer's disease
Project/Area Number |
23590033
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Research Category |
Grant-in-Aid for Scientific Research (C)
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Allocation Type | Multi-year Fund |
Section | 一般 |
Research Field |
Chemical pharmacy
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Research Institution | Tokushima Bunri University |
Principal Investigator |
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Project Period (FY) |
2011 – 2013
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Project Status |
Completed (Fiscal Year 2013)
|
Budget Amount *help |
¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2013: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2012: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2011: ¥2,600,000 (Direct Cost: ¥2,000,000、Indirect Cost: ¥600,000)
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Keywords | 有機化学 / 生物活性 / アルツハイマー病 / 神経科学 / 薬学 / 光親和性標識 / 有機合成化学 / 神経変性疾患 / 神経栄養因子 / PC12細胞 / ネオビブサニン類 / 神経突起伸展活性 / 生理活性 |
Research Abstract |
Neovibsanins were originally isolated from Viburnum awabuki by Fukuyama and co-workers in 1996. These natural products were found to display neurite outgrowth activity in PC12 cells, suggesting neovibsanin-type compounds could be promising candidates for the development of novel therapeutic agents to treat Alzheimer-type dementia. However, the detailed mechanism for the activity is still unknown. We carried out the syntheses of several kinds of neovibsanin derivatives on the basis of the tricyclic acetal which is a minimum essential structure expressing the activity, to clarify the detailed structure-activity relationship of neovibsanins. As the results, it was revealed that the C11 of neovibsanin skeleton is a suitable position for the substitution with photoaffinity-functional group. On the basis of these knowledge, the synthesis of the photoaffinity-labeled neovibsanin derivative, which is useful in order to find the target molecules having an affinity for neovibsanin, was achieved.
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Report
(4 results)
Research Products
(36 results)
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[Journal Article] Novel inhibitor of bacterial sphingomyelinase, SMY-540, developed based on three-dimensional structure analysis2014
Author(s)
Oda, H. Imagawa, R. Kato, K. Yabiku, T. Yoshikawa, T. Takemoto, H. Takahashi, H. Yamamoto, M. Nishizawa, J. Sakurai, M. Nagahama
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Journal Title
J. Enzyme Inhib. Med. Chem.
Volume: 29
Issue: 3
Pages: 1-8
DOI
Related Report
Peer Reviewed
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[Journal Article] Novel inhibitor of bacterial sphingomyelinase, SMY-540, developed based on three-dimensional structure analysis2013
Author(s)
M. Oda, H. Imagawa, R. Kato, K. Yabiku, T. Yoshikawa, T. Takemoto, H. Takahashi, H. Yamamoto, M. Nishizawa, J. Sakurai, M. Nagahama
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Journal Title
J. Enzyme Inhib. Med. Chem
Volume: (Ahead of Print)
Pages: 1-8
Related Report
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[Journal Article] Concise synthesis of a probe molecule enabling analysis and imaging of vizantin2013
Author(s)
H. Yamamoto, M. Oda, M. Nakano, K. Yabiku, M. Shibutani, T. Nakanishi, M. Suenaga, M. Inoue, H. Imagawa, M. Nagahama, Y. Matsunaga, S. Himeno, K. Setsu, J. Sakurai, Nishizawa
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Journal Title
Chem. Pharm. Bull
Volume: 61(4)
Pages: 452-459
Related Report
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[Journal Article] Development of vizantin, a safe immunostimulant, based on the structure−activity relationship of trehalose-6,6′-dicorynomycolate2013
Author(s)
H. Yamamoto, M. Oda, M. Nakano, N. Watanabe, K. Yabiku, M. Shibutani, M. Inoue, H. Imagawa, M. Nagahama, S. Himeno, K. Setsu, J. Sakurai, M. Nishizawa
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Journal Title
J. Med. Chem
Volume: 56
Pages: 381-385
Related Report
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[Journal Article] Yellow pigments, fomitellanols A and B, and TBAF (1.5 eq) drimane sesquiterpenoids, cryptoporic acids P and Q, from fomitella fraxinea and their inhibitory activity against COX and 5-LO2013
Author(s)
K. Yoshikawa, K. Koso, M. Shimomura, M. Tanaka, H. Yamamoto, H. Imagawa, S. Arihara, T. Hashimoto
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Journal Title
Molecules
Volume: 18
Pages: 4181-4191
Related Report
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[Journal Article] Concise synthesis of a probe molecule enabling analysis and imaging of vizantin2013
Author(s)
H. Yamamoto, M. Oda, M. Nakano, K. Yabiku, M. Shibutani, T. Nakanishi, M. Suenaga, M. Inoue, H. Imagawa, M. Nagahama, Y. Matsunaga, S. Himeno, K. Setsu, J. Sakurai, M. Nishizawa
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Journal Title
Chem. Pharm. Bull
Volume: 61
Pages: 452-459
Related Report
Peer Reviewed
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[Journal Article] Development of vizantin, a safe immunostimulant, based on the structure-activity relationship of trehalose-6,6′-dicorynomycolate2013
Author(s)
H. Yamamoto, M. Oda, M. Nakano, N. Watanabe, K. Yabiku, M. Shibutani, M. Inoue, H. Imagawa, M. Nagahama, S. Himeno, K. Setsu, J. Sakurai, M. Nishizawa
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Journal Title
J. Med. Chem
Volume: 56
Issue: 1
Pages: 381-385
DOI
Related Report
Peer Reviewed
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[Journal Article] Yellow pigments, fomitellanols A and B, and drimane sesquiterpenoids, cryptoporic acids P and Q, from fomitella fraxinea and their inhibitory activity against COX and 5-LO2013
Author(s)
K. Yoshikawa, K. Koso, M. Shimomura, M. Tanaka, H. Yamamoto, H. Imagawa, S. Arihara, T. Hashimoto
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Journal Title
Molecules
Volume: 18
Issue: 4
Pages: 4181-4191
DOI
Related Report
Peer Reviewed
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[Journal Article] Syntheses of Structurally-simplified and Fluorescently-labeled Neovibsanin Derivatives and Analysis of their Neurite Outgrowth Activity in PC12 cells2012
Author(s)
H. Imagawa, H. Saijo, H. Yamaguchi, K. Maekawa, T. Kurisaki, H. Yamamoto, M. Nishizawa, M. Oda, M. Kabura, M. Nagahama, J. Sakurai, M. Kubo, M. Nakai, K. Makino, M. Ogata, H. Takahashi, Y. Fukuyama
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Journal Title
Bioorg. Med. Chem. Lett
Volume: 22
Pages: 2089-2093
Related Report
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[Journal Article] Syntheses of Structurally-simplified and Fluorescently-labeled Neovibsanin Derivatives and Analysis of their Neurite Outgrowth Activity in PC12 Cells.2012
Author(s)
H.Imagawa, H. Siajo, H. Yamaguchi, K. Maekwa, T. Kurisaki, H. Yamamoto, M. Nishizawa, M. Oda, M. Kaubura, M. Nagahama, J. Sakurai, M. Nakai, K. Makino, M. Ogata, H. Takahashi, Y. Fukuyama
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Journal Title
Bioorg. Med. Chem. Lett.
Volume: 22,(5)
Issue: 5
Pages: 2089-2093
DOI
Related Report
Peer Reviewed
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[Journal Article] Halichonines A, B, and C, Novel Sesquiterpene Alkaloids from the Marine Sponge Halichondria okadai Kadota2011
Author(s)
O. Ohno, T. Chiba, S. Todoroki, H. Yoshimura, Maru, K. Maekawa, H. Imagawa, K. Yamada, A. Wakamiya, K. Suenaga, D. Uemura
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Journal Title
Chem. Commun
Volume: 47
Pages: 12453-12455
Related Report
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[Journal Article] Halichonines A, B, and C, Novel Sesquiterpene Alkaloids from the Marine Sponge Halichondria okadai2011
Author(s)
Kadota. O. Ohno, T. Chiba, S. Todoroki, H. Yoshimura, N. Maru, K. Maekawa, H. Imagawa, K. Yamada, A. Wakamiya, K. Suenaga, D. Uemura
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Journal Title
Chem. Commun.
Volume: 47
Pages: 12453-12455
Related Report
Peer Reviewed
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[Presentation] Syntheses of Structurally-simplified Neovibsanin Derivatives and Analysis of their Neurite Outgrowth Activity2013
Author(s)
Hiroshi Imagawa, Hayato Saijo, Hitomi Yamaguchi, Ken Maekawa, Takahiro Kurisaki, Hirofumi Yamamoto, Mugio Nishizawa, Masataka Oda, Michiko Kabura, Masahiro Nagahama, Jun Sakurai, Miwa Kubo, Megumi Nakai, Kosho Makino, Mitsuko Ogata, Hironobu Takahashi, Yoshiyasu Fukuyama
Organizer
23rd French-Japanese Symposium on medicinal and fine chemistry(第23回日仏医薬精密化学会議)
Place of Presentation
長崎
Related Report
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[Presentation] Syntheses of Structurally-simplified Neovibsanin Derivatives and Analysis of their Neurite Outgrowth Activity2013
Author(s)
Hiroshi Imagawa, Hayato Saijo, Hitomi Yamaguchi, Ken Maekawa, Takahiro Kurisaki, Hirofumi Yamamoto, Mugio Nishizawa, Masataka Oda, Michiko Kabura, Masahiro Nagahama, Jun Sakurai, Miwa Kubo, Megumi Nakai, Kosho Makino, Mitsuko Ogata, Hironobu Takahashi, Yoshiyasu Fukuyama
Organizer
23rd French-Japanese Symposium on medicinal and fine chemistry
Place of Presentation
長崎
Related Report
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[Presentation] 磁性ビーズ担持型ビザヒンチンの定量法の検討2013
Author(s)
中野真代,山本博文,今川 洋,櫻井純,西沢麦夫,樽井敬史,渋谷昌弘,大林寿美代,玉城糊太,小田真隆,永浜政博
Organizer
日本薬学会 第133年会
Place of Presentation
横浜
Related Report
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[Presentation] 光親和性標識を持つネオビブサニン誘導体の合成研究2012
Author(s)
今川洋,○山口仁美,前川健,杉本実希子,西條速人,栗崎貴啓,山本博文,西澤麦夫,小田真隆,永浜政博,櫻井純,久保美和,牧野宏章,福山愛保
Organizer
日本薬学会第132年会
Place of Presentation
札幌
Related Report
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