Collaborative Innovation Center of New Drug Research and Safety Evaluation, Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou University, Zhengzhou, Henan, China.
Key Laboratory of "Runliang" Antiviral Medicines Research and Development, Institute of Drug Discovery and Development, Zhengzhou University, Zhengzhou, China.
J Med Virol. 2020 Jan;92(1):17-25. doi: 10.1002/jmv.25586. Epub 2019 Sep 10.
A series of butene lactones were synthesized and these compounds were tested for anti-respiratory syncytial virus (RSV) activity in vitro. Three compounds exhibited an antiviral effect, the highest of which was compound 6b3 with an effective concentration 50% of 6.35 μM. The effects of 6b3 were then evaluated in vivo and a significant reduction in the lung index caused by RSV was detected. Reduced inflammatory infiltration and necrosis of the lungs were revealed by histopathology and gross pathology. Activation of an early immune response by 6b3 was also observed by cytokine analysis via a real-time polymerase chain reaction. These results indicated that 6b3 has an anti-RSV effect both in vitro and in vivo, and is a possible candidate compound for the development of an anti-RSV drug in the future.
合成了一系列丁烯内酯,并对这些化合物进行了体外抗呼吸道合胞病毒(RSV)活性测试。三种化合物表现出抗病毒作用,其中最高的是化合物 6b3,其有效浓度 50%为 6.35 μM。然后在体内评估了 6b3 的作用,发现其显著降低了 RSV 引起的肺指数。组织病理学和大体病理学显示,炎症浸润和肺部坏死减少。通过实时聚合酶链反应的细胞因子分析也观察到 6b3 对早期免疫反应的激活。这些结果表明,6b3 具有体外和体内的抗 RSV 作用,是未来开发抗 RSV 药物的潜在候选化合物。