Search of natural compounds for prevention age-related disease due to inhibition the formation of Advanced Glycation End-products, and synthesis of related derivatives.

2023 Fiscal Year Final Research Report

• Project/Area Number: 22K20730
• Research Category: Grant-in-Aid for Research Activity Start-up
• Allocation Type: Multi-year Fund
• Review Section: 0801:Pharmaceutical sciences and related fields
• Research Institution: Sojo University
• Principal Investigator: Nakashima Keisuke 崇城大学, 薬学部, 助教 (50964441)
• Project Period (FY): 2022-08-31 – 2024-03-31
• Keywords: 終末糖化産物 / カテコール基 / ガロイル基 / プレニル関連化合物 / ホップ / ノブドウ / 抗CMAモノクローナル抗体 / 抗CMLモノクローナル抗体

Outline of Final Research Achievements

The findings on the CMA and CML formation inhibitory activity of Epimedii Herba (EH), which is the premise of this study, were submitted and accepted for publication. In addition, 7 prenylated compounds from Humulus lupulus (hops) were isolated and evaluated the activity. As the result, Xanthohumol D (XHD), isolated as racemic compound and each enantiomer (XHD1, D2) had CMA formation inhibitory activity at a final concentration of 1 mM. The findings with EH and hops revealed that the core structure for activity is a phenolic hydroxyl group, with at least two hydroxyl groups (catechol or galloyl groups).
Therefore, a study was conducted to identify active compounds from Ampelopsis glandulosa var. heterophylla (wild grape), which has been reported to contain a large amount of phenolic compounds. As a result, 7 compounds were identified and found to have significant activity, as expected.

Free Research Field

薬用植物学・天然物化学

Academic Significance and Societal Importance of the Research Achievements

本検討からフェノール性水酸基を豊富に含む天然資源には強力な抗糖化作用が期待されることが明らかとなった。中でも本検討で用いたノブドウは、生育は容易で繁殖力もあるため育成は容易であるが、味等の問題から商業的に利用が難しい未利用資源に分類される植物である。このような未利用資源であっても、今回のような抗糖化活性を有することが明らかとなれば商業的な利用価値を付与できる可能性があり、未利用資源の利活用につながることが期待される。またノブドウから活性化合物を精製し、それを原料としてより強力な活性を有する化合物を創出する等、本検討が抗糖化を介した疾病予防薬創出の足掛かりとなることが期待される。