Parameters of inhibition of HIV-1 infection by small anionic microbicides.
Parameters of inhibition of HIV-1 infection by small anionic microbicides.
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DOI：
10.1016/j.antiviral.2006.07.008
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发表时间：
2007
影响因子：
7.6
通讯作者：
A. Vzorov;J. Bozja;D. Dixon;L. Marzilli;R. Compans
中科院分区：
文献类型：
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作者：
A. Vzorov;J. Bozja;D. Dixon;L. Marzilli;R. Compans
磺化卟啉和酞菁已被证明具有抗艾滋病毒活性，并被考虑用作杀菌剂。这两类化合物都是带负电荷的小分子，之前都被证明可以抑制 HIV Env 蛋白诱导的细胞融合，并阻断 gp120 与 CD4 受体的结合。在本研究中，我们表明这些化合物可抑制细胞相关 HIV 的传播，使多种 HIV-1 初级分离株失活，并对 DS 聚阴离子抗性病毒具有活性。测试的化合物在一定的 pH 值范围内具有活性，并且对正常细菌菌群没有可检测到的活性。这些结果支持这样的结论：阴离子四吡咯是有前途的候选杀微生物剂，用于预防艾滋病毒。
Sulfonated porphyrins and phthalocyanines have been shown to have anti-HIV activity and are under consideration as microbicides. Both categories of compounds are small negatively charged molecules and both were previously shown to inhibit cell fusion induced by the HIV Env protein and to block binding of gp120 to the CD4 receptor. In the present study we show that these compounds inhibit transmission of cell-associated HIV, inactivate a broad range of HIV-1 primary isolates and are active against DS polyanion-resistant virus. The compounds tested are active over a range of pH values, and possess no detectable activity against normal bacterial flora. These results support the conclusion that anionic tetrapyrroles are promising candidates as microbicides for HIV prevention.