Synthesis of Denosomin-Vitamin D3 Hybrids and Evaluation of Their Anti-Alzheimer's Disease Activities

Kenji Sugimoto; Hisanari Yajima; Yusuke Hayashi; Daishiro Minato; Sayuri Terasaki; Chihiro Tohda; Yuji Matsuya

doi:10.1021/acs.orglett.5b03138

Synthesis of Denosomin-Vitamin D₃ Hybrids and Evaluation of Their Anti-Alzheimer's Disease Activities

Kenji Sugimoto, Hisanari Yajima, Yusuke Hayashi, Daishiro Minato, Sayuri Terasaki, Chihiro Tohda, Yuji Matsuya^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

11 Scopus citations

Abstract

As an extension of previously conducted studies on developing an anti-Alzheimer's disease agent, denosomin (1-deoxy-24-norsominone, an artificial inducer of neurite elongation), derivatives were designed and synthesized based on the hypothesis that our denosomin would exhibit axonal extension activity via a 1,25D₃-membrane-associated, rapid response steroid-binding protein (1,25D₃-MARRS) pathway. The biological assay revealed that the hybridization of characteristic δ-lactone in denosomin and the triene moiety in VD₃ was effective to enhance the nerve re-extension activity in amyloid β (Aβ)-damaged neurons.

Original language	English
Pages (from-to)	5910-5913
Number of pages	4
Journal	Organic Letters
Volume	17
Issue number	23
DOIs	https://doi.org/10.1021/acs.orglett.5b03138
State	Published - 2015/11/20

ASJC Scopus subject areas

Biochemistry
Physical and Theoretical Chemistry
Organic Chemistry

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10.1021/acs.orglett.5b03138

Cite this

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title = "Synthesis of Denosomin-Vitamin D3 Hybrids and Evaluation of Their Anti-Alzheimer's Disease Activities",

abstract = "As an extension of previously conducted studies on developing an anti-Alzheimer's disease agent, denosomin (1-deoxy-24-norsominone, an artificial inducer of neurite elongation), derivatives were designed and synthesized based on the hypothesis that our denosomin would exhibit axonal extension activity via a 1,25D3-membrane-associated, rapid response steroid-binding protein (1,25D3-MARRS) pathway. The biological assay revealed that the hybridization of characteristic δ-lactone in denosomin and the triene moiety in VD3 was effective to enhance the nerve re-extension activity in amyloid β (Aβ)-damaged neurons.",

author = "Kenji Sugimoto and Hisanari Yajima and Yusuke Hayashi and Daishiro Minato and Sayuri Terasaki and Chihiro Tohda and Yuji Matsuya",

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AU - Sugimoto, Kenji

AU - Yajima, Hisanari

AU - Hayashi, Yusuke

AU - Minato, Daishiro

AU - Terasaki, Sayuri

AU - Tohda, Chihiro

AU - Matsuya, Yuji

PY - 2015/11/20

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AB - As an extension of previously conducted studies on developing an anti-Alzheimer's disease agent, denosomin (1-deoxy-24-norsominone, an artificial inducer of neurite elongation), derivatives were designed and synthesized based on the hypothesis that our denosomin would exhibit axonal extension activity via a 1,25D3-membrane-associated, rapid response steroid-binding protein (1,25D3-MARRS) pathway. The biological assay revealed that the hybridization of characteristic δ-lactone in denosomin and the triene moiety in VD3 was effective to enhance the nerve re-extension activity in amyloid β (Aβ)-damaged neurons.

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