Synthesis, Structure Activity Relationship and Anti-influenza A Virus Evaluation of Oleanolic Acid-Linear Amino Derivatives

  • Li Weijia
    Medical School of Kunming University of Science and Technology
  • Yang Fan
    Medical School of Kunming University of Science and Technology
  • Meng Lingkuan
    Medical School of Kunming University of Science and Technology
  • Sun Jiaqi
    State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University
  • Su Yangqing
    Medical School of Kunming University of Science and Technology
  • Shao Liang
    Medical School of Kunming University of Science and Technology
  • Zhou Demin
    State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University
  • Yu Fei
    Medical School of Kunming University of Science and Technology

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<p>Oleanolic acid (OA) was discovered as a mild influenza hemagglutinin (HA) inhibitor in our earlier studies. In the present work, 20 compounds were prepared by structural modifications of OA, and their antiviral activities against influenza A/WSN/33 (H1N1) virus in Madin–Darby canine kidney (MDCK) cells were evaluated. Based on the biological result, structure–activity relationship (SAR) was discussed. Compound 10 with six-carbon chain and a terminal hydroxyl group showed the strongest anti-influenza activity with an IC50 of 2.98 µM, which is an order of magnitude more potent than OA. Hemagglutination inhibition and Surface plasmon resonance (SPR) assay indicated that compound 10 might interfere with influenza invasion by interacting with HA protein.</p>

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