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Synthesis of Denosomin–Vitamin D3 Hybrids and Evaluation of Their Anti-Alzheimer’s Disease Activities
- Sugimoto, Kenji, Yajima, Hisanari, Hayashi, Yusuke, Minato, Daishiro, Terasaki, Sayuri, Tohda, Chihiro, Matsuya, Yuji
- Organic letters 2015 v.17 no.23 pp. 5910-5913
- amyloid, bioassays, chemical reactions, moieties, nerve tissue, neurites, organic compounds
- 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.