2. Academic Validation
  3. Structural modification on rupestonic acid leads to highly potent inhibitors against influenza virus

Structural modification on rupestonic acid leads to highly potent inhibitors against influenza virus

  • Mol Divers. 2019 Feb;23(1):1-9. doi: 10.1007/s11030-018-9840-5.
Mamateli Obul 1 2,  Xincheng Wang 1 2,  Jiangyu Zhao 1,  Gen Li 1,  Haji Akber Aisa 3,  Guozheng Huang 4
Affiliations

Affiliations

  • 1 Key Laboratory of Plant Resources and Chemistry of Arid Zone, State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, 830011, People's Republic of China.
  • 2 University of Chinese Academy of Sciences, Yuquan Rd 19 A, Beijing, 100049, People's Republic of China.
  • 3 Key Laboratory of Plant Resources and Chemistry of Arid Zone, State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, 830011, People's Republic of China. haji@ms.xjb.ac.cn.
  • 4 Key Laboratory of Plant Resources and Chemistry of Arid Zone, State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi, 830011, People's Republic of China. g.huang@ms.xjb.ac.cn.
PMID: 29971616 DOI: 10.1007/s11030-018-9840-5
Abstract

Influenza viruses are responsible for seasonal epidemics and occasional pandemics, which cause significant morbidity and mortality. Although several drugs (adamantanes and neuraminidase inhibitors) are available in the market, the worldwide spread of drug-resistant influenza strains poses an urgent need for novel Antiviral drugs. Artemisia rupestris L. is a folk medicine used to treat cold. In this paper, we structurally modified rupestonic acid, a bioactive component of A. rupestris, to synthesize a series of 2-substituted rupestonic acid methyl esters (3a-3o). Their structures were fully characterized by 1H NMR, 13C NMR, HRMS spectra. Among them, compounds 3b and 3c exhibited potent activities against influenza H1N1 with micromolar IC50 values and might serve as new lead compounds for the treatment of influenza.

Keywords

Artemisia rupestris; Benzylation; Influenza virus; Rupestonic acid.

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