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Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Chin+Chem+Lett 2021 ; 32 (10): 3019-3022 Nephropedia Template TP
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Reviving chloroquine for anti-SARS-CoV-2 treatment with cucurbit 7 uril-based supramolecular formulation #MMPMID33840982
Kwong CHT; Mu J; Li S; Fang Y; Liu Q; Zhang X; Kam H; Lee SMY; Chen Y; Deng F; Zhou X; Wang R
Chin Chem Lett 2021[Oct]; 32 (10): 3019-3022 PMID33840982show ga
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CQ was approved by the FDA for the emergency use authorization (EUA) in the fight against COVID-19 in the US, but later was revoked the EUA status due to the severe clinical toxicity.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 approximately 10(4) 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 mumol/L) against both Vero E6 cell line and L-02 cell lines was completely inhibited in the presence of 300 mumol/L and 600 mumol/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.