Key Laboratory of Resource Biology and Biotechnology in Western China (Northwest University), Ministry of Education, Biomedicine Key Laboratory of Shaanxi Province, Northwest University, Xi'an 710069, China; Sorbonne Universités, UPMC Univ Paris 06, Institut Parisien de Chimie Moléculaire, CNRS UMR 8232, 4 place Jussieu, 75005 Paris, France.
Key Laboratory of Resource Biology and Biotechnology in Western China (Northwest University), Ministry of Education, Biomedicine Key Laboratory of Shaanxi Province, Northwest University, Xi'an 710069, China.
Eur J Med Chem. 2017 Apr 21;130:308-319. doi: 10.1016/j.ejmech.2017.02.028. Epub 2017 Feb 21.
Based on classical drug design theory, a novel series of gentiopicroside derivatives was designed and synthesized. All synthesized compounds were then biologically evaluated for their inhibition of influenza virus and anti-HCV activity in vitro. Some of the gentiopicroside derivatives, such as 11a, 13d and 16 showed interesting anti-influenza virus activity with IC at 39.5 μM, 45.2 μM and 44.0 μM, respectively. However, no significant anti-HCV activity was found for all of gentiopicroside derivatives. The preliminary results indicate that modification of the sugar moiety on gentiopicroside was helpful for enhancing the anti-influenza activities. Our works demonstrate the importance of secoiridoid natural products as new leads in the development of potential antiviral inhibitors.
基于经典的药物设计理论，设计并合成了一系列新的龙胆苦苷衍生物。然后对所有合成的化合物进行了体外抗流感病毒和抗 HCV 活性的生物评价。一些龙胆苦苷衍生物，如 11a、13d 和 16，表现出有趣的抗流感病毒活性，IC 值分别为 39.5 μM、45.2 μM 和 44.0 μM。然而，所有龙胆苦苷衍生物均未表现出显著的抗 HCV 活性。初步结果表明，对龙胆苦苷糖基部分的修饰有助于增强其抗流感活性。我们的工作表明，裂环环烯醚萜类天然产物作为新型抗病毒抑制剂先导化合物的重要性。
