Small molecules blocking the entry of severe acute respiratory syndrome coronavirus into host cells.


Severe acute respiratory syndrome coronavirus (SARS-CoV) is the pathogen of SARS, which caused a global panic in 2003. We describe here the screening of Chinese herbal medicine-based, novel small molecules that bind avidly with the surface spike protein of SARS-CoV and thus can interfere with the entry of the virus to its host cells. We achieved this by using a two-step screening method consisting of frontal affinity chromatography-mass spectrometry coupled with a viral infection assay based on a human immunodeficiency virus (HIV)-luc/SARS pseudotyped virus. Two small molecules, tetra-O-galloyl-beta-D-glucose (TGG) and luteolin, were identified, whose anti-SARS-CoV activities were confirmed by using a wild-type SARS-CoV infection system. TGG exhibits prominent anti-SARS-CoV activity with a 50% effective concentration of 4.5 microM and a selective index of 240.0. The two-step screening method described here yielded several small molecules that can be used for developing new classes of anti-SARS-CoV drugs and is potentially useful for the high-throughput screening of drugs inhibiting the entry of HIV, hepatitis C virus, and other insidious viruses into their host cells.

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@article{Yi2004SmallMB, title={Small molecules blocking the entry of severe acute respiratory syndrome coronavirus into host cells.}, author={Ling Ka Yi and Zhengquan Li and Kehu Yuan and Xiuxia Qu and Jian Qin Chen and Guangwen Wang and Hong Zhang and Hongpeng Luo and Lili Zhu and Pengfei Jiang and Lirong Chen and Yan Shen and Min Luo and Guoying Zuo and Jianhe Hu and Deliang Duan and Yuchun Nie and Xuanling Shi and Wei Wang and Yang Han and Tai-sheng Li and Yuqing Liu and Mingxiao Ding and Hongkui Deng and Xiaojie Xu}, journal={Journal of virology}, year={2004}, volume={78 20}, pages={11334-9} }