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G2-S16 树枝状聚合物作为一种用于预防女性 HIV-1 感染的杀微生物剂候选物。

G2-S16 dendrimer as a candidate for a microbicide to prevent HIV-1 infection in women.

机构信息

Section Immunology and Laboratorio Inmuno Biología Molecular, Hospital General Universitario Gregorio Marañón (HGUGM), Madrid, Spain.

出版信息

Nanoscale. 2017 Jul 13;9(27):9732-9742. doi: 10.1039/c7nr03034g.

Abstract

Unprotected heterosexual intercourse is the first route for sustaining the global spread of human immunodeficiency virus type 1 (HIV-1), being responsible for 80% of new HIV-1 infections in the world. The presence of inflammation in the female reproductive tract and the presence of semen increases the risk of heterosexual HIV-1 transmission. This state-of-the-art research based on an innovative nanotechnology design was focused on a toxicological study of the limitation of the activity of the novel HO-soluble anionic carbosilane dendrimer G2-S16 in the adult cervical and foreskin epithelia. The G2-S16 dendrimer did not cause any irritation or inflammation in the vaginal epithelium, proving that this dendrimer is a safe nanocompound for vaginal application to control viral transmission. It was shown that no significant differences were found in mortality, sublethal or teratogenic effects when the zebra fish embryos were treated with G2-S16. In short, G2-S16 seems to be an ideal candidate for the development of a topical microbicide against HIV-1 infection and the next step is try in clinical trials, because of its great in vivo biocompatibility, as well as its ability to halt HIV-1 infection in the presence of semen.

摘要

无保护的异性性行为是导致全球人类免疫缺陷病毒 1 型(HIV-1)传播的首要途径,占全球新感染 HIV-1 的 80%。生殖道炎症和精液的存在增加了异性 HIV-1 传播的风险。这项基于创新纳米技术设计的最新研究集中于研究新型 HO 可溶性阴离子碳硅烷树枝状大分子 G2-S16 在成人宫颈和包皮上皮中的活性限制的毒理学研究。G2-S16 树枝状大分子不会引起阴道上皮的任何刺激或炎症,证明这种树枝状大分子是一种安全的纳米化合物,可用于阴道应用以控制病毒传播。结果表明,当用 G2-S16 处理斑马鱼胚胎时,在死亡率、亚致死或致畸作用方面没有发现显著差异。简而言之,G2-S16 似乎是开发针对 HIV-1 感染的局部杀微生物剂的理想候选物,下一步是尝试临床试验,因为它具有良好的体内生物相容性,以及在存在精液的情况下阻止 HIV-1 感染的能力。

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