Coates J A, Cammack N, Jenkinson H J, Jowett A J, Jowett M I, Pearson B A, Penn C R, Rouse P L, Viner K C, Cameron J M
Department of Virology, Glaxo Group Research Ltd., Middlesex, United Kingdom.
Antimicrob Agents Chemother. 1992 Apr;36(4):733-9. doi: 10.1128/AAC.36.4.733.
The (-)-enantiomer of 2'-deoxy-3'-thiacytidine (3TC) was found to be a potent and selective inhibitor of human immunodeficiency virus types 1 (HIV-1) and 2 (HIV-2) in vitro. We determined its antiviral activity against a number of laboratory strains of HIV-1 and HIV-2 in a range of CD4-bearing lymphocyte cell lines (mean 50% inhibitory concentration [IC50] range, 4 nM to 0.67 microM). 3TC was also active against a range of HIV-1 strains in peripheral blood lymphocytes (mean IC50 range, 2.5 to 90 nM). The IC50 for cytotoxicity in seven lymphocyte cell cultures, including human peripheral blood lymphocytes, ranged from 0.5 to 6 mM. 3TC had no detectable antiviral activity against a range of other viruses or in cells chronically infected with HIV-1 or HIV-2. The effects of time of addition of the compound and varying the multiplicity of infection on the antiviral activity of 3TC were determined. The results showed that 3TC is a potent and selective inhibitor of HIV-1 and HIV-2 replication in vitro.
2'-脱氧-3'-硫代胞苷（3TC）的（-）-对映体在体外被发现是1型人类免疫缺陷病毒（HIV-1）和2型人类免疫缺陷病毒（HIV-2）的强效且选择性抑制剂。我们在一系列携带CD4的淋巴细胞系中测定了其对多种HIV-1和HIV-2实验室毒株的抗病毒活性（平均50%抑制浓度[IC50]范围为4 nM至0.67 μM）。3TC在外周血淋巴细胞中对一系列HIV-1毒株也有活性（平均IC50范围为2.5至90 nM）。在包括人外周血淋巴细胞在内的七种淋巴细胞培养物中，其细胞毒性的IC50范围为0.5至6 mM。3TC对一系列其他病毒或慢性感染HIV-1或HIV-2的细胞没有可检测到的抗病毒活性。我们还测定了添加该化合物的时间以及改变感染复数对3TC抗病毒活性的影响。结果表明，3TC在体外是HIV-1和HIV-2复制的强效且选择性抑制剂。
