Role of seminal plasma in the anti-HIV-1 activity of candidate microbicides.
Role of seminal plasma in the anti-HIV-1 activity of candidate microbicides.
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精确血浆在候选微生物抗HIV-1活性中的作用。
DOI：
10.1186/1471-2334-6-150
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发表时间：
2006-10-16
影响因子：
3.7
通讯作者：
Li, Yun-Yao
中科院分区：
文献类型：
--
作者：
Neurath, A. Robert;Strick, Nathan;Li, Yun-Yao
在猕猴阴道感染模型中对杀微生物剂预防HIV-1感染的评价表明，保护所需的活性化合物浓度远远超过足以在体外完全抑制感染的水平。这些实验是在没有精浆（SP）的情况下进行的，精浆是病毒性传播的媒介。为了深入了解SP对所选杀微生物剂性能的可能影响，测定了它们在存在和不存在SP的情况下的抗HIV-1活性。使用TZM-bl指示细胞测定化合物对X4病毒HIV-1 IIIB和R5病毒HIV-1 BaL的抑制活性，并通过测量感染诱导的β-半乳糖苷酶来定量。测定了1，2-苯二甲酸醋酸纤维素（CAP）在SP存在下的杀病毒性能，CAP是唯一以水不溶性微粒化形式提供的杀微生物剂。聚合物杀微生物剂，聚（萘磺酸盐），硫酸纤维素，角叉菜胶，CAP（可溶性形式）和聚苯乙烯磺酸盐的HIV-1抑制活性，分别在SP（33.3%）的存在下，显着（范围1.44至1.73倍）减少。微粒化CAP的制剂，即使在SP体积过量的情况下也提供酸性缓冲系统，有效地灭活HIV-1感染性。本文提供的数据表明，作为HIV-1进入抑制剂的聚合物杀微生物剂的体内功效可能至少部分地由于SP的不可避免的存在而受到损害。这些可能的缺点可以通过将相应的聚合物与酸性pH缓冲系统组合来克服（用于微粉化CAP制剂的内置）或与其他抗HIV-1化合物（其活性不受SP影响，例如逆转录酶和锌指抑制剂）一起使用。
Evaluation of microbicides for prevention of HIV-1 infection in macaque models for vaginal infection has indicated that the concentrations of active compounds needed for protection by far exceed levels sufficient for complete inhibition of infection in vitro. These experiments were done in the absence of seminal plasma (SP), a vehicle for sexual transmission of the virus. To gain insight into the possible effect of SP on the performance of selected microbicides, their anti-HIV-1 activity in the presence, and absence of SP, was determined. The inhibitory activity of compounds against the X4 virus, HIV-1 IIIB, and the R5 virus, HIV-1 BaL was determined using TZM-bl indicator cells and quantitated by measuring β-galactosidase induced by infection. The virucidal properties of cellulose acetate 1,2-benzene-dicarboxylate (CAP), the only microbicide provided in water insoluble, micronized form, in the presence of SP was measured. The HIV-1 inhibitory activity of the polymeric microbicides, poly(naphthalene sulfonate), cellulose sulfate, carrageenan, CAP (in soluble form) and polystyrene sulfonate, respectively, was considerably (range ≈ 4 to ≈ 73-fold) diminished in the presence of SP (33.3%). Formulations of micronized CAP, providing an acidic buffering system even in the presence of an SP volume excess, effectively inactivated HIV-1 infectivity. The data presented here suggest that the in vivo efficacy of polymeric microbicides, acting as HIV-1 entry inhibitors, might become at least partly compromised by the inevitable presence of SP. These possible disadvantages could be overcome by combining the respective polymers with acidic pH buffering systems (built-in for formulations of micronized CAP) or with other anti-HIV-1 compounds, the activity of which is not affected by SP, e.g. reverse transcriptase and zinc finger inhibitors.
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影响因子：
3.8
作者：
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通讯作者：
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