Search for compounds that are effective in both prevention and treatment of Alzheimer's disease

2019 Fiscal Year Final Research Report

• Project/Area Number: 17K08351
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Natural medicines
• Research Institution: Meiji Pharmaceutical University
• Principal Investigator: KOYAMA KIYOTAKA 明治薬科大学, 薬学部, 教授 (20225593)
• Project Period (FY): 2017-04-01 – 2020-03-31
• Keywords: アルツハイマー / アミロイドベータ / 凝集抑制 / Galactomyces / SC2051 / MPUC 239 / naphtho-gamma-pyrone / dinaphthalenone誘導体

Outline of Final Research Achievements

A study was conducted using the Th-T method (amyloid β aggregation test) as a biological test for the purpose of isolating anti-Alzheimer's disease-active compounds from marine-derived fungal cultures. As a result, one novel compound and two known compounds were isolated from the ethyl acetate extract of Galactomyces pseudocandidus (MPUC 398). Among them, the known compound SC2051 showed a strong amyloid β aggregation inhibitory activity (IC50 = 2.5 μM). Furthermore, five known compounds and one undetermined structure compound were isolated from MPUC239. Among them, the compounds with undetermined structure showed a strong amyloid β aggregation inhibitory activity (IC50 = 3.9 μM).

Free Research Field

天然物化学

Academic Significance and Societal Importance of the Research Achievements

我が国の大きな社会問題となっているアルツハイマー病は脳にアミロイドβと呼ばれる異常なタンパク質が蓄積・凝集し、神経細胞死が進行する原因不明の難病である。しかし、根本的治療薬は未だ上市されておらず、抗アルツハイマー病薬の開発が社会的に強く求められている。今回の研究で、アミロイドβの凝集を強く抑制する化合物２種が得られた。これらの化合物の構造をヒントとして、抗アルツハイマー病薬の開発が進む可能性を示した。