Cho Jin-Beom, Lee Jin-Moo, Ahn Hee-Chul, Jeong Yong-Joo
Department of Bio and Nanochemistry, Kookmin University, Seoul 136-702, Republic of Korea.
Department of Pharmacy, Dongguk University-Seoul, Goyang 410-820, Republic of Korea.
J Microbiol Biotechnol. 2015 Dec 28;25(12):2007-10. doi: 10.4014/jmb.1507.07078.
A new chemical inhibitor against severe acute respiratory syndrome (SARS) coronavirus helicase, 7-ethyl-8-mercapto-3-methyl-3,7-dihydro-1H-purine-2,6-dione, was identified. We investigated the inhibitory effect of the compound by conducting colorimetry-based ATP hydrolysis assay and fluorescence resonance energy transfer-based double-stranded DNA unwinding assay. The compound suppressed both ATP hydrolysis and double-stranded DNA unwinding activities of helicase with IC50 values of 8.66 ± 0.26 μM and 41.6 ± 2.3 μM, respectively. Moreover, we observed that the compound did not show cytotoxicity up to 80 µMconcentration. Our results suggest that the compound might serve as a SARS coronavirus inhibitor.
一种针对严重急性呼吸综合征（SARS）冠状病毒解旋酶的新型化学抑制剂——7-乙基-8-巯基-3-甲基-3,7-二氢-1H-嘌呤-2,6-二酮被鉴定出来。我们通过进行基于比色法的ATP水解试验和基于荧光共振能量转移的双链DNA解旋试验，研究了该化合物的抑制作用。该化合物抑制解旋酶的ATP水解和双链DNA解旋活性，IC50值分别为8.66±0.26μM和41.6±2.3μM。此外，我们观察到该化合物在浓度高达80μM时未表现出细胞毒性。我们的结果表明，该化合物可能作为一种SARS冠状病毒抑制剂。
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