【摘 要】
：
The wide-spreading SARS-CoV-2 virus has put the world into boiling water for more than a year,however pharmacological therapies to act effectively against coronavirus disease 2019 (COVID-19) remain elusive.Chloroquine (CQ),an antimalarial drug,was found t
【机 构】
：
State Key Laboratory of Quality Research in Chinese Medicine,Institute of Chinese Medical Sciences,U
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The wide-spreading SARS-CoV-2 virus has put the world into boiling water for more than a year,however pharmacological therapies to act effectively against coronavirus disease 2019 (COVID-19) remain elusive.Chloroquine (CQ),an antimalarial drug,was found to exhibit promising antiviral activity in vitro and in vivo at a high dosage,thus CQ was approved by the FDA for the emergency use authorization (EUA) in the fight against COVID-19 in the US,but later was revoked the EUA status due to the severe clinical toxicity.Herein,we show that supramolecular formulation of CQ by a macrocyclic host,curcurbit[7]uril (CB[7]),reduced its non-specific toxicity and improved its antiviral activity against coronavirus,working in synergy with CB[7].CB[7]was found to form 1∶1 host-guest complexes with CQ,with a binding constant of ～104 L/mol.The CQ-CB[7]formulation decreased the cytotoxicity of CQ against Vero E6 and L-02 cell lines.In particular,the cytotoxicity of CQ(60 μmol/L) against both Vero E6 cell line and L-02 cell lines was completely inhibited in the presence of 300 μmol/L and 600 μmol/L CB[7],respectively.Furthermore,the CB[7]alone showed astonishing antiviral activity in SARS-CoV-2 infected Vero E6 cells and mouse hepatitis virus strain A59 (MHV-A59) infected N2A cells,and synergistically improved the antiviral activity of CQ-CB[7],suggesting that CB[7]-based CQ formulation has a great potential as a safe and effective antiviral agent against SARS-CoV-2 and other coronavirus.
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