中草药中HIV-1三大酶类抑制剂研究进展

来源:岁月联盟 作者: 时间:2015-06-05

  4  展望
   
  由于AIDS在全球的迅速蔓延及流行,各国政府都投入了大量的人力、物力、财力来用于艾滋病的预防和治疗,科学家们也在加紧寻找新的具有抗HIV活性的化合物。目前已上市的21种药物均由化学方法合成而来,具有毒副作用强、价格昂贵、不能彻底杀灭病毒等缺点,使得其在应用上受到一定程度的限制。而天然产物是生物活性化合物的丰富来源,科学家们寄希望从中找到新的具有抗AIDS作用的先导化合物,并大大加强了对天然药物的开发与研究,且已取得较好的研究成果。
   
  目前,研究者们已成功地找到了多种类型的抗HIV-1天然化合物,这些先导化合物要么结构独特,要么具有新的作用机制。科学家们在试图阐明它们的作用靶点及其作用机制的同时,通过结构活性相关性(Structure-Activity Relationship, SAR)的分析来优化这些先导化合物,使之成为一个候选药物,为开发新药和临床用药提供科学的指导。在已发现的具有抗HIV-1活性的中草药中,从作用的靶点可以看出,作用于HIV-1逆转录酶的天然化合物居多,而作用于HIV-1整合酶和蛋白酶的化合物相对少些,因此,继续从中草药中研究开发作用于HIV-1复制周期各个环节的有效化合物仍具有非常广阔的空间,同时这也是寻找有效抗艾滋病病毒药物的主要途径之一。

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