Reviving chloroquine for anti-SARS-CoV-2 treatment with cucurbit[7]uril-based supramolecular formulation

查看全文 作　　者：Cheryl [1]H.T.Kwong;Jingfang [2]Mu;Shengke [1]Li;Yaohui [2]Fang;Qianyun [3]Liu;Xiangjun [1]Zhang;Hiotong [1]Kam;Simon [1]M.Y.Lee;Yu [3]Chen;Fei [2]Deng;Xi [2,3]Zhou;Ruibing [1]Wang

机构地区：[1]State Key Laboratory of Quality Research in Chinese Medicine,Institute of Chinese Medical Sciences,University of Macao,Macao 999078,China;[2]State Key Laboratory of Virology,Wuhan Institute of Virology,Center for Biosafety Mega-Science,Chinese Academy of Sciences(CAS),Wuhan 430071,China;[3]State Key Laboratory of Virology,College of Life Sciences,Wuhan University,Wuhan 430072,China

出　　处：《Chinese Chemical Letters》索引2021年第32卷第10期,共4页

基　　金：supported by the Science and Technology Development Fund,Macao SAR(No.0007/2020/A);International Partnership Program of Chinese Academy of Sciences(No.153B42KYSB20200004 to X.Zhou and R.Wang);the Strategic Priority Research Program of CAS(No.XDB29010300);the National Natural Science Foundation of China(Nos.21871301,22071275,31970169,31800140,31800140 and 31670161);the Yunde Hou Academician Fund from National Institute for Viral Disease Control and Prevention(No.2019HYDQNJJ10)。 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 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CQ was approved by the FDA for the emergency use authorization(EUA)in the fight against COVID-19 in the US,but later was revoked the EUA status due to the severe clinical toxicity.Herein,we show that supramolecular formulation of CQ by a macrocyclic host,curcurbit[7]uril(CB[7]),reduced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 mmol/L)against both Vero E6 cell line and L-02 cell lines was completely inhibited in the presence of 300 mmol/L and 600 mmol/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 N2 A 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. 关键词：HOST-GUEST CHLOROQUINE Cucurbit[7]uril SARS-CoV-2 COVID-19

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Reviving chloroquine for anti-SARS-CoV-2 treatment with cucurbit[7]uril-based supramolecular formulation

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