Prevention of HIV-1 infection by phthalocyanines.
Prevention of HIV-1 infection by phthalocyanines.
复制标题
通过酞菁预防 HIV-1 感染。
DOI：
10.1016/s0166-3542(03)00035-4
复制
发表时间：
2003
影响因子：
7.6
通讯作者：
Dixon,DabneyW
中科院分区：
文献类型：
--
作者：
Vzorov,AndreiN;Marzilli,LuigiG;Compans,RichardW;Dixon,DabneyW
已在具有整合的LTR-β-半乳糖苷酶基因的上皮HeLa-CD 4细胞系中评价了所选酞菁和金属酞菁阻断HIV感染的能力。磺化酞菁本身（PcS），以及它的铜，镍和钒基螯合物，是最有效的阻断病毒感染。这些化合物在阻断病毒Env蛋白的融合活性方面也非常有效。预期所有这些化合物都弱结合或根本不结合轴向配体。相比之下，磺化酞菁承载金属预期结合轴向配体更紧密（铝，钴，铬，铁，硅，和锌）在阻断HIV感染，也不太有效抑制融合。发现许多活性化合物阻断gp 120与CD 4的结合。选择阳离子和羧基酞菁，以及四氮杂卟啉，也进行了评价。我们的结果表明，至少有一些化合物使病毒无感染性，即它们是杀病毒的。这些化合物具有作为杀微生物剂的潜力，可用于提供对性传播HIV的保护。
The ability of selected phthalocyanines and metallophthalocyanines to block HIV infection has been evaluated in an epithelial HeLa–CD4 cell line with an integrated LTR-β-galactosidase gene. Sulfonated phthalocyanine itself (PcS), as well as its copper, nickel, and vanadyl chelates, were the most effective in blocking viral infection. These compounds were also very effective in blocking the fusion activity of the viral Env proteins. All of these compounds are expected to bind axial ligands weakly or not at all. In contrast, sulfonated phthalocyanines bearing metals expected to bind axial ligands more tightly (aluminum, cobalt, chromium, iron, silicon, and zinc) were less effective in blocking HIV infection and also less effective at inhibiting fusion. A number of active compounds were found to block binding of gp120 to CD4. Selected cationic and carboxy phthalocyanines, as well as porphyrazines, were also evaluated. Our results indicate that at least some of the compounds render the virus noninfectious, i.e. that they are virucidal. These compounds have potential as microbicides that might be used to provide protection against sexually transmitted HIV.