Halliday S M, Lackman-Smith C, Bader J P, Rice W G, Clanton D J, Zalkow L H, Buckheit R W
Virology Research Group, Southern Research Institute, Frederick Research Center, MD 21701, USA.
Antiviral Res. 1996 Dec;33(1):41-53. doi: 10.1016/s0166-3542(96)00994-1.
The anti-HIV sulfonated dye, resobene, was found to be a potent inhibitor of the attachment of HIV to target cells, the fusion of envelope- and CD4-expressing cells, and the cell-to-cell transmission of virus. Resobene inhibited the infection of phenotypically distinct, established human cell lines and fresh human peripheral blood lymphocytes and macrophages by laboratory-derived isolates of human immunodeficiency virus type 1 (HIV-1) and type 2 (HIV-2), and a panel of biologically diverse primary clinical isolates, including syncytium-inducing and non-syncytium-inducing viruses and strains representative of the various virus clades found worldwide. The compound was also active against all drug-resistant virus isolates tested. Cell-based and biochemical mechanism of action studies demonstrated that the compound inhibits the attachment of infectious virus and fusion of virus-infected cells to uninfected target cells by binding to the cationic V3 loop of the envelope glycoprotein. Resobene effectively inhibited the infection of cell populations which do and do not express cell surface CD4. Resobene prevented infection of the cervical epithelial cell line ME180, suggesting the compound may effectively act as a topical microbicide to prevent the sexual transmission of HIV.
抗艾滋病毒磺化染料雷索苯被发现是一种有效的抑制剂，可抑制艾滋病毒与靶细胞的附着、包膜表达细胞与CD4表达细胞的融合以及病毒的细胞间传播。雷索苯抑制了1型人类免疫缺陷病毒（HIV-1）和2型（HIV-2）的实验室衍生分离株以及一组生物学特性多样的原发性临床分离株对表型不同的已建立人类细胞系、新鲜人类外周血淋巴细胞和巨噬细胞的感染，这些临床分离株包括合胞体诱导病毒和非合胞体诱导病毒以及代表全球发现的各种病毒进化枝的毒株。该化合物对所有测试的耐药病毒分离株也具有活性。基于细胞和生化作用机制的研究表明，该化合物通过与包膜糖蛋白的阳离子V3环结合，抑制感染性病毒的附着以及病毒感染细胞与未感染靶细胞的融合。雷索苯有效抑制了表达和不表达细胞表面CD4的细胞群体的感染。雷索苯可预防宫颈上皮细胞系ME180的感染，这表明该化合物可能有效地作为一种局部杀菌剂来预防艾滋病毒的性传播。
