Cassiman J J, De Clercq E, Jones A S, Walker R T, Van den Berghe H
Br Med J (Clin Res Ed). 1981 Sep 26;283(6295):817-8. doi: 10.1136/bmj.283.6295.817.
The rate of sister chromatid exchange induced by several anti-herpes agents was measured to assess their potential mutagenicity. The agents--5-iodo-deoxyuridine (IDU), 5-trifluoromethyl-deoxyuridine (TFT), and [E]-5-(2-bromovinyl)-deoxyuridine (BVDU)--were incubated at various concentrations with human lymphocytes and fibroblasts, and that rate of sister chromatid exchanges was measured. In lymphocytes and fibroblasts BVDU and IDU did not induce exchange except at concentrations of 50 mg/l, while TFT increased the rate of exchange at a concentration of 0.5 mg/l. The rate of sister chromatid exchange is a sensitive index of chromosomal damage, and these findings provide information on the safety of some of the antiherpes agents tested. TFT increased the rate of exchange at a concentration that coincides with its minimal antiviral concentration, but BVDU did not induce exchange at therapeutic concentrations.
为评估几种抗疱疹药物的潜在致突变性,对其诱导姐妹染色单体交换的速率进行了测定。将这些药物——5-碘脱氧尿苷(IDU)、5-三氟甲基脱氧尿苷(TFT)和[E]-5-(2-溴乙烯基)脱氧尿苷(BVDU)——以不同浓度与人淋巴细胞和成纤维细胞一起孵育,然后测定姐妹染色单体交换的速率。在淋巴细胞和成纤维细胞中,除了浓度为50mg/L时,BVDU和IDU不会诱导交换,而TFT在浓度为0.5mg/L时会增加交换速率。姐妹染色单体交换速率是染色体损伤的一个敏感指标,这些发现为所测试的一些抗疱疹药物的安全性提供了信息。TFT在与其最低抗病毒浓度一致的浓度下增加了交换速率,但BVDU在治疗浓度下不会诱导交换。