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Efficacy of HIV antiviral polyanionic carbosilane dendrimer G2-S16 in the presence of semen

机译:HIV抗病毒多阴离子碳硅烷树枝状晶仪G2-S16在精液存在下的功效

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The development of a safe and effective microbicide to prevent the sexual transmission of human immunodeficiency virus (HIV)-1 is urgently needed. Unfortunately, the majority of microbicides, such as poly(L-lysine)-dendrimers, anionic polymers, or antiretrovirals, have proved inactive or even increased the risk of HIV infection in clinical trials, most probably due to the fact that these compounds failed to prevent semen-exposed HIV infection. We showed that G2-S16 dendrimer exerts anti-HIV-1 activity at an early stage of viral replication, blocking the gp120/CD4/CCR5 interaction and providing a barrier to infection for long periods, confirming its multifactorial and nonspecific ability. Previously, we demonstrated that topical administration of G2-S16 prevents HIV transmission in humanized BLT mice without irritation or vaginal lesions. Here, we demonstrated that G2-S16 is active against mock- and semen-exposed HIV-1 and could be a promising microbicide against HIV infection.
机译:迫切需要安全和有效的杀微生物化剂,以防止人体免疫缺陷病毒(HIV)-1的性传播。不幸的是,大多数杀菌剂,例如聚(L-赖氨酸) - 致留剂,阴离子聚合物或抗逆转录病毒,已被证明是非活性的,甚至增加了临床试验中HIV感染的风险,大概是由于这些化合物未能发生的事实防止精液艾滋病毒感染。我们表明,G2-S16树突式的抗HIV-1活性在病毒复制的早期施用,阻断GP120 / CD4 / CCR5相互作用,并为长时间提供感染的屏障,确认其多重造影和非特异性能力。以前,我们证明了G2-S16的局部给药可防止人源化的BLT小鼠中的HIV透射,而不会刺激或阴道病变。在这里,我们证明G2-S16针对模拟和精液的HIV-1活跃,并且可以是针对HIV感染的有希望的微生物剂。

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