title: Structure activity relationship study of curcumin analogues toward the amyloid-beta aggregation inhibitor.
abstract: Inhibition of the amyloid β aggregation process could possibly prevent the onset of Alzheimer's disease. In this article, we report a structure-activity relationship study of curcumin analogues for anti amyloid β aggregation activity. Compound 7, the ideal amyloid β aggregation inhibitor in vitro among synthesized curcumin analogues, has not only potent anti amyloid β aggregation effects, but also water solubility more than 160 times that of curcumin. In addition, new approaches to improve water solubility of curcumin-type compounds are proposed.
authors.affiliation: Department of Biochemical Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510, Japan.
authors.forename: Hitoshi
authors.initials: H
authors.lastname: Endo
authors.affiliation: Department of Biochemical Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510, Japan.
authors.forename: Yuri
authors.initials: Y
authors.lastname: Nikaido
authors.affiliation: Department of Biochemical Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510, Japan.
authors.forename: Mamiko
authors.initials: M
authors.lastname: Nakadate
authors.affiliation: Department of Biochemical Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510, Japan.
authors.forename: Satomi
authors.initials: S
authors.lastname: Ise
authors.affiliation: Department of Biochemical Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510, Japan. Electronic address: konno@yz.yamagata-u.ac.jp.
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Konno
mesh_terms: D016229:Amyloid beta-Peptides / Q000037:antagonists & inhibitors* / Q000378:metabolism; D003474:Curcumin / Q000138:chemical synthesis / Q000737:chemistry*; D006801:Humans; D007700:Kinetics; D008968:Molecular Conformation; D011485:Protein Binding; D011789:Quantum Theory; D012995:Solubility; D013329:Structure-Activity Relationship
chemical_list: D016229:Amyloid beta-Peptides; D003474:Curcumin
keywords: Aggregation inhibitor; Alzheimer’s disease; Amyloid-beta; Curcumin; Water solubility