美人工合成抗艾新药外源凝集素 可有效抑制艾滋病病毒早期感染
发布时间： 2011-09-27 | 作者：常丽君
本报讯 据美国每日科学网9月26日报道，美国犹他州大学研究人员开发出一种新型杀菌素，能和艾滋病（HIV）病毒包膜上的糖结合，从而阻止其继续感染。该成果有望作为一种新的早期疗法，预防HIV通过性途径传播。该研究发表在近期的在线杂志《分子制药》上。
多年来，杀菌素多是凝胶形式来预防HIV通过性途径传播，但收效甚微。HIV要形成感染，必须首先进入宿主细胞，然后控制细胞复制机制来自我复制，新的HIV再去感染其它细胞。在病毒进入与复制这两步中，都为抗艾滋病药物提供了潜在靶点。论文作者、犹他州大学生物工程与制药化学副教授帕德里克·基瑟说：“但目前临床试验中所用的抗HIV药物，大部分都是瞄准病毒的复制系统；而在阻止病毒进入方面研究很少，这种方法能在病毒和目标细胞作用之前就使其失去活性，同时，这种方法成本很高且产量极低。外源凝集素（Lectins）就是这种方法中使用的药物。”
外源凝集素是自然界发现的一类分子，能和某些特殊的糖结合在一起。HIV病毒外面包着一层糖类包膜，能使它们躲过免疫系统。此前的研究显示，从植物和细菌中提取的外源凝集素能和HIV包膜上的糖结合，从而阻止其进入细胞。
但生产和提纯天然外源凝集素成本高得吓人。而基瑟和同事在一种名为（BzB）的化合物的基础上，开发出了一种人工合成的外源凝集素，能和HIV上面的糖残基结合，并加强了二者间的结合键，开发出了合成外源凝集素多聚物，由相同的亚单元构成，每个亚单元都包含了多重BzB结合位点。增加了BzB结合位点的数量和密度后，聚合物能更好地与HIV结合，大大提高了其抗病毒能力。
由于HIV变种很多，其病毒包膜上的糖也大不相同，基瑟和同事还对合成外源凝集素的光谱抗病毒性进行了评价，发现其不仅对广泛的HIV病毒种显出了同样的抵抗力，而且还是专门针对HIV的，对其它病毒的包膜没有影响。此外，他们还评价了该聚合物在一种果糖（精液中的糖，能中和外源凝集素类药物效力）中的抗HIV能力，发现其抗病毒能力在果糖中完全无损。
“这种多聚物在抗NIV方面非常有效，将一块方糖大小的BzB多聚物溶化在一浴缸的水中，其浓度足以阻止HIV感染细胞。”基瑟说，“理想的抗HIV杀菌素包括效能、广谱性、选择抑制性、生物产量以及生物适应性等多方面。这些以BzB为基础的合成外源凝集素好像符合了所有这些关键的指标，为那些HIV流行的地区，提供了一种可负担得起的，还具有升级潜力的干预式性传播预防药物”。
基瑟还表示，今后的研究将集中在对这些合成外源凝集素的效能评价上，观察它们被人体吸收后，预防HIV在组织间传播的效果，还将在灵长类动物身上进行测试。目前他们正在开发一种凝胶形式的聚合物，可预防HIV通过性途径传播。（常丽君）
(科技日报)
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| 图示∶2011年5月正式出版的《中国特色医疗金鉴》登载的刘君主任及其机构事迹 |
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U.S. anti-AIDS drugs synthetic lectin
Can inhibit HIV infection in early
Posted: 2011-09-27 | Author: Chang Lijun
http://www.stdaily.com 2011 年 09 月 27 MVP: Science and Technology Daily Author: Chang Lijun
WASHINGTON According to the U.S. Science Daily reported Sept. 26 Network, University of Utah researchers have developed a new type of spinosad, can and AIDS (HIV) viral envelope on the sugar-binding, thereby preventing it from continuing infection. The results are expected as a new early treatment, prevention of HIV through sexual transmission. The study is published in a recent online magazine "molecule drug" on.
Over the years, more than a gel form of Spinosad to prevent HIV through sexual transmission, but with little success. To the formation of HIV infection, you must first enter the host cell, and then copy the mechanisms controlling cell from my copy, go to the new HIV infection of other cells. In viral entry and replication in these two steps are to provide a potential target for anti-AIDS drug. Authors, University of Utah professor of biological engineering and pharmaceuticals 帕德里克基 Joseph said: "But the clinical trials used anti-HIV drugs, most of them are aimed at viral replication system; in terms of preventing viruses from entering rarely, this method can function in the virus and target cells before the loss of activity at the same time, this method costs high and low yield. lectin (Lectins) is the drug used in this way. "
Lectins are a class of molecules found in nature, can and some special sugar together. HIV, wrapped in a layer of sugar coating, enabling them to escape the immune system. Earlier studies have shown that extracts from plants and bacteria the lectin to the sugar and the combination of HIV envelope, thereby preventing it from entering cells.
However, the production and purification of natural lectin costs were prohibitively high. The Jise and colleagues called (BzB) compounds, based on the development of a synthetic lectin, and HIV can be above the sugar-binding residues, and to strengthen the combination between the two key, developed a synthetic polymer lectin from the same sub-unit structure, each subunit contains binding sites of multiple BzB. Increase the number of binding sites BzB and density, the polymer can better combine with HIV has greatly enhanced its anti-virus capabilities.
Because many HIV variants, the viral envelope is also different on the sugar, Jise and colleagues also synthesized lectin toxicity spectrum disease resistance was evaluated and found not only a wide range of HIV viral strains show the same resistance, but also specifically for HIV, the envelope of the virus does not affect the other. In addition, they evaluate the polymer in a fructose (the sugar in semen, to the lectin and the effectiveness of drugs) in the ability of anti-HIV, anti-virus capabilities found in the fructose is completely non-destructive.
"This polymer is very effective in anti-NIV, the size of a sugar cube melting in a polymer BzB bath water, its concentration is sufficient to prevent HIV infection in cells." Jise said, "The ideal anti-HIV spinosad including performance, broad spectrum, choose inhibition, biological yield and biological adaptation, and many of these to BzB based synthetic lectin seems to meet all these key indicators for those areas where the HIV epidemic, providing one kind of affordable, but also has upgrade potential intervention to prevent sexually transmitted type of drug. "
Jise also said that future research will focus on these synthetic lectin performance evaluation, observation they are absorbed by the body to prevent the spread of HIV in inter-organizational effectiveness, will be tested in primates. Currently they are developing a form of polymer gel can prevent HIV through sexual transmission. (Chang Lijun)
(Technology News)
