Synthesis and anti-hepatitis C virus effect of juglorubin and its derivatives

2022 Fiscal Year Final Research Report

• Project/Area Number: 20K05868
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Review Section: Basic Section 38040:Bioorganic chemistry-related
• Research Institution: Tokyo University of Science
• Principal Investigator: Kuramcohi Kouji 東京理科大学, 理工学部応用生物科学科, 教授 (90408708)
• Project Period (FY): 2020-04-01 – 2023-03-31
• Keywords: 1,4-ナフトキノン / C型肝炎ウイルス / ジュグロルビン

Outline of Final Research Achievements

Juglorubin is a natural dye isolated from the culture of Streptomyces sp. 3094, 815, and GW4184. It has been previously synthesized via the biomimetic dimerization of juglomycin C, a plausible genetic precursor. In this study, the derivatives of juglorubin, 1-O-acetyljuglorubin dimethyl ester and juglorubin dimethyl ester, were found to exhibit antiviral activity against hepatitis C virus (HCV) without exerting any remarkable cytotoxicity against host Huh7 cells. They also inhibited liver X receptor activation and lipid droplet accumulation in Huh7 cells. These findings suggest that 1-O-acetyljuglorubin dimethyl ester and juglorubin dimethyl ester targeted the host factors required for HCV production.

Free Research Field

生物有機化学

Academic Significance and Societal Importance of the Research Achievements

本研究で、C型肝炎ウイルスの複製を阻害する誘導体を見出すことができた。非常に低濃度で抗ウイルス活性を発揮することや、宿主細胞には毒性が少ないことから、抗ウイルス剤としての実用化が期待できる。さらには抗ウイルス薬の開発で鍵となる作用機構を明らかにすることができた。