The adamantane-derived bananins are potent inhibitors of the helicase activities and replication of SARS coronavirus.

The adamantane-derived bananins are potent inhibitors of the helicase activities and replication of SARS coronavirus.
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DOI:
10.1016/j.chembiol.2005.01.006
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发表时间:
2005-03
影响因子:
--
通讯作者:
Huang JD
Huang JD
中科院分区:
生物1区
文献类型:
--
作者:
Tanner JA;Zheng BJ;Zhou J;Watt RM;Jiang JQ;Wong KL;Lin YP;Lu LY;He ML;Kung HF;Kesel AJ;Huang JD

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香蕉素是一类具有独特结构特征的抗病毒化合物,其包含与吡哆醛衍生物共价结合的三氧杂金刚烷部分。这类化合物的六个成员:bananin,iodobananin,vanillinbananin,ansabananin,eubananin和adeninobanin被合成和测试作为SARS冠状病毒(SCV)解旋酶的抑制剂。Bananin、iodobananin、vanillinbananin和eubananin是SCV解旋酶ATP酶活性的有效抑制剂,IC 50值在0.5-3 μM范围内。使用基于FRET的荧光测定,观察到类似的趋势,尽管在略高的抑制剂浓度下,解旋酶活性的抑制。在SCV细胞培养体系中,香蕉素的EC_(50)小于10 μM,CC_(50)大于300 μM。抑制动力学与香蕉素抑制细胞内过程或涉及SCV复制的过程一致。
Bananins are a class of antiviral compounds with a unique structural signature incorporating a trioxa-adamantane moiety covalently bound to a pyridoxal derivative. Six members of this class of compounds: bananin, iodobananin, vanillinbananin, ansabananin, eubananin, and adeninobananin were synthesized and tested as inhibitors of the SARS Coronavirus (SCV) helicase. Bananin, iodobananin, vanillinbananin, and eubananin were effective inhibitors of the ATPase activity of the SCV helicase with IC50 values in the range 0.5–3 μM. A similar trend, though at slightly higher inhibitor concentrations, was observed for inhibition of the helicase activities, using a FRET-based fluorescent assay. In a cell culture system of SCV, bananin exhibited an EC50 of less than 10 μM and a CC50 of over 300 μM. Kinetics of inhibition are consistent with bananin inhibiting an intracellular process or processes involved in SCV replication.
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