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 1,25D(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.
authors.affiliation: Graduate School of Medicine and Pharmaceutical Sciences, and ‡Institute of Natural Medicine, University of Toyama , 2630 Sugitani, Toyama 930-0194, Japan.
authors.forename: Kenji
authors.initials: K
authors.lastname: Sugimoto
authors.affiliation: Graduate School of Medicine and Pharmaceutical Sciences, and ‡Institute of Natural Medicine, University of Toyama , 2630 Sugitani, Toyama 930-0194, Japan.
authors.forename: Hisanari
authors.initials: H
authors.lastname: Yajima
authors.affiliation: Graduate School of Medicine and Pharmaceutical Sciences, and ‡Institute of Natural Medicine, University of Toyama , 2630 Sugitani, Toyama 930-0194, Japan.
authors.forename: Yusuke
authors.initials: Y
authors.lastname: Hayashi
authors.affiliation: Graduate School of Medicine and Pharmaceutical Sciences, and ‡Institute of Natural Medicine, University of Toyama , 2630 Sugitani, Toyama 930-0194, Japan.
authors.forename: Daishiro
authors.initials: D
authors.lastname: Minato
authors.affiliation: Graduate School of Medicine and Pharmaceutical Sciences, and ‡Institute of Natural Medicine, University of Toyama , 2630 Sugitani, Toyama 930-0194, Japan.
authors.forename: Sayuri
authors.initials: S
authors.lastname: Terasaki
authors.affiliation: Graduate School of Medicine and Pharmaceutical Sciences, and ‡Institute of Natural Medicine, University of Toyama , 2630 Sugitani, Toyama 930-0194, Japan.
authors.forename: Chihiro
authors.initials: C
authors.lastname: Tohda
authors.affiliation: Graduate School of Medicine and Pharmaceutical Sciences, and ‡Institute of Natural Medicine, University of Toyama , 2630 Sugitani, Toyama 930-0194, Japan.
authors.forename: Yuji
authors.initials: Y
authors.lastname: Matsuya
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy*; D016229:Amyloid beta-Peptides / Q000378:metabolism; D002462:Cell Membrane / Q000378:metabolism; D002762:Cholecalciferol / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D003687:Dehydroepiandrosterone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D009474:Neurons / Q000473:pathology
chemical_list: D016229:Amyloid beta-Peptides; C543747:denosomin; D002762:Cholecalciferol; D003687:Dehydroepiandrosterone