國家衛生研究院 NHRI:Item 3990099045/13110
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    題名: Inhibition of SARS-CoV-2 by highly potent broad-spectrum anti-coronaviral tylophorine-based derivatives
    作者: Yang, CW;Lee, YZ;Hsu, HY;Jan, JT;Lin, YL;Chang, SY;Peng, TT;Yang, RB;Liang, JJ;Liao, CC;Chao, TL;Pang, YH;Kao, HC;Huang, WZ;Lin, JH;Chang, CP;Niu, GH;Wu, SH;Sytwu, HK;Chen, CT;Lee, SJ
    貢獻者: Institute of Biotechnology and Pharmaceutical Research;National Institute of Infectious Diseases and Vaccinology
    摘要: Tylophorine-based compounds and natural cardiotonic steroids (cardenolides and bufadienolides) are two classes of transmissible gastroenteritis coronavirus inhibitors, targeting viral RNA and host cell factors, respectively. We tested both types of compounds against two types of coronaviruses, to compare and contrast their antiviral properties, and with view to their further therapeutic development. Examples of both types of compounds potently inhibited the replication of both feline infectious peritonitis virus and human coronavirus OC43 with EC<sub>50</sub> values of up to 8 and 16 nM, respectively. Strikingly, the tylophorine-based compounds tested inhibited viral yields of HCoV-OC43 to a much greater extent (7–8 log magnitudes of p.f.u./ml) than the cardiotonic steroids (about 2–3 log magnitudes of p.f.u./ml), as determined by end point assays. Based on these results, three tylophorine-based compounds were further examined for their anti-viral activities on two other human coronaviruses, HCoV-229E and SARS-CoV-2. These three tylophorine-based compounds inhibited HCoV-229E with EC<sub>50</sub> values of up to 6.5 nM, inhibited viral yields of HCoV-229E by 6–7 log magnitudes of p.f.u./ml, and were also found to inhibit SARS-CoV-2 with EC<sub>50</sub> values of up to 2.5–14 nM. In conclusion, tylophorine-based compounds are potent, broad-spectrum inhibitors of coronaviruses including SARS-CoV-2, and could be used for the treatment of COVID-19.
    日期: 2020-12-14
    關聯: Frontiers in Pharmacology. 2020 Dec 14;11:Article number 606097.
    Link to: http://dx.doi.org/10.3389/fphar.2020.606097
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=1663-9812&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000602708400001
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85098260329
    顯示於類別:[李秀珠] 期刊論文
    [陳炯東] 期刊論文
    [司徒惠康] 期刊論文
    [張竣評] 期刊論文

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