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.
University of Chinese Academy of Sciences, Yuquan Rd 19 A, Beijing, 100049, People's Republic of China.
Mol Divers. 2019 Feb;23(1):1-9. doi: 10.1007/s11030-018-9840-5. Epub 2018 Jul 3.
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 H NMR, C NMR, HRMS spectra. Among them, compounds 3b and 3c exhibited potent activities against influenza H1N1 with micromolar IC values and might serve as new lead compounds for the treatment of influenza.
流感病毒是造成季节性流行疾病和偶发性大流行疾病的原因，会导致严重的发病率和死亡率。尽管市场上有几种药物（金刚烷胺和神经氨酸酶抑制剂）可用，但具有抗药性的流感病毒株在全球范围内的传播，迫切需要新型抗病毒药物。黄花蒿是一种民间药物，用于治疗感冒。在本文中，我们对黄花蒿中的生物活性成分岩白菜素进行了结构修饰，合成了一系列 2-取代岩白菜素甲酯（3a-3o）。它们的结构通过 1H NMR、13C NMR 和高分辨质谱（HRMS）得到了充分的表征。其中，化合物 3b 和 3c 对 H1N1 流感病毒表现出很强的抑制活性，其半数抑制浓度（IC50）值为微摩尔级，可能成为治疗流感的新型先导化合物。
