Barnard D L, Fairbairn D W, O'Neill K L, Gage T L, Sidwell R W
Department of A.D.V.S., Utah State University, Logan 84322-5600, USA.
Antiviral Res. 1995 Dec;28(4):317-29. doi: 10.1016/0166-3542(95)00057-7.
Sulfonated anthraquinones and other anthraquinone derivatives were evaluated for anti-human cytomegalovirus (HCMV) activity, cytotoxicity and genotoxicity. Acid blues 40 and 129, acid black 48, alizarin violet R and reactive blue 2 were the most active compounds having selective indices of greater than 30 and EC50 values of 4-30 microM. When tested against a clinical isolate, the 4 compounds were 2- to 5-fold less active. The antiviral activity was distinctly separate from the virucidal activity (> 1000 microM). The compounds were weakly toxic to either log phase or stationary cells in most of the following cytotoxicity assays: neutral red uptake assay, lactic acid dehydrogenase assay, trypan blue exclusion assay and radiolabeled macromolecular precursor uptake assays. Using a genotoxicity assay, the comet assay, only reactive blue 2 and acid black 48 were found to cause DNA strand breakage. This occurred at concentrations of 30 and 170 microM, respectively. These results suggest that these compounds could be a prototype for synthesizing even more effective HCMV-inhibitory anthraquinone derivatives.
对磺化蒽醌及其他蒽醌衍生物进行了抗人巨细胞病毒（HCMV）活性、细胞毒性和遗传毒性评估。酸性蓝40和129、酸性黑48、茜素紫R和活性蓝2是活性最强的化合物，其选择性指数大于30，半数有效浓度（EC50）值为4 - 30微摩尔。在针对临床分离株进行测试时，这4种化合物的活性降低了2至5倍。抗病毒活性与杀病毒活性明显不同（>1000微摩尔）。在以下大多数细胞毒性试验中，这些化合物对对数期或稳定期细胞的毒性较弱：中性红摄取试验、乳酸脱氢酶试验、台盼蓝排斥试验和放射性标记大分子前体摄取试验。使用遗传毒性试验彗星试验，仅发现活性蓝2和酸性黑48会导致DNA链断裂，分别发生在30和170微摩尔的浓度下。这些结果表明，这些化合物可能是合成更有效HCMV抑制性蒽醌衍生物的原型。
