Research on seeds from unique ring skeletal limonoids for drug discovery

2018 Fiscal Year Final Research Report

• Project/Area Number: 16K08309
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Natural medicines
• Research Institution: Hoshi University
• Principal Investigator: Morita Hiroshi 星薬科大学, 薬学部, 教授 (70220069)
• Project Period (FY): 2016-04-01 – 2019-03-31
• Keywords: リモノイド / ceramicine B / 脂肪滴蓄積抑制作用 / メラニン産生抑制作用

Outline of Final Research Achievements

During our search for bioactive limonoids from medicinal plants, we have isolated ceramicines, which are a series of limonoids from the bark of Chisocheton ceramicus (Meliaceae). Ceramicine B has shown a strong lipid droplets accumulation (LDA) inhibitory activity and also anti-melanin deposition activity.
With the purpose of discovering compounds with stronger activity than ceramicine B, we further investigated the constituents of C. ceramicus. As a result, several new ceramicines were isolated, and their structures were determined on the basis of spectroscopic analyses. We also investigated the effect of the substituent by synthesizing several derivatives and evaluating their LDA inhibitory activity. Furthermore, some new limonoids from Walsura chrysogyne and Chukrasia velutina, were isolated and their structures were elucidated.

Free Research Field

天然物化学

Academic Significance and Societal Importance of the Research Achievements

これまでリモノイド類の作用として着目されてこなかったメラニン産生抑制作用および脂肪滴蓄積抑制作用の作用機序を解明する。これらの作用機序を解明することにより、特に ceramicine類の活性の本質を解明する。また、Chisocheton ceramicus に主成分として含有されるceramicine B を利用して、構造変換を行うことにより、新たな創薬素材分子を設計する。さらに、熱帯未利用植物抽出エキスをスクリーニングすることで、特異的な環骨格を有するリモノイドの探索を行い天然物特有の多様性に富んだ新規創薬シードを見出す。