1. Synthesis of Denosomin-Vitamin D3 Hybrids and Evaluation of Their Anti-Alzheimer's Disease Activities.
- Author
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Sugimoto K, Yajima H, Hayashi Y, Minato D, Terasaki S, Tohda C, and Matsuya Y
- Subjects
- Amyloid beta-Peptides metabolism, Cell Membrane metabolism, Cholecalciferol chemistry, Cholecalciferol pharmacology, Dehydroepiandrosterone chemical synthesis, Dehydroepiandrosterone chemistry, Dehydroepiandrosterone pharmacology, Molecular Structure, Neurons pathology, Alzheimer Disease drug therapy, Cholecalciferol chemical synthesis, Dehydroepiandrosterone analogs & derivatives
- 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 1,25D(3)-membrane-associated, rapid response steroid-binding protein (1,25D(3)-MARRS) pathway. The biological assay revealed that the hybridization of characteristic δ-lactone in denosomin and the triene moiety in VD(3) was effective to enhance the nerve re-extension activity in amyloid β (Aβ)-damaged neurons.
- Published
- 2015
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