[关键词]
[摘要]
在复杂疾病的治疗过程中, 发现使用单靶点药物治疗越来越难得到预期的疗效。基于系统生物学和网络药理学的发展, 对于复杂疾病的发病机制和病理过程的研究更加深入透彻, 发现使用多靶点药物治疗复杂疾病能够克服单靶点药物的许多缺陷。多靶点药物包括多组分多靶点药物和单组分多靶点药物, 而单组分多靶点药物较多组分多靶点药物更有优势。艾滋病的治疗是当今世界难题, 先后采用单靶点药物和多组分多靶点联合用药(高效抗逆转录疗法)治疗艾滋病, 但是由于病毒的高度变异性和药物严重的毒副作用制约了2种疗法的广泛应用, 因此开发低毒、高效的单组分多靶点抗免疫缺陷病毒I型(HIV-1)药物成为治疗艾滋病的重要方向。抗HIV-1单组分多靶点药物主要通过合理药物设计合成或筛选得到, 其中天然产物来源广泛, 种类繁多, 不乏抑制HIV-1的活性化合物, 是发现抗HIV-1多靶点先导化合物的重要途径。对天然产物来源的具有多靶点抗HIV-1活性的化合物进行了综述。
[Key word]
[Abstract]
During the curing of complex disease, prospective therapeutic effect has been more and more difficult to achieve by using single-target inhibitors. Along with the development of systems biology and network pharmacology, the nosogenesis and the pathological process have been studied in depth, and people find that multi-target inhibitors can overcome many defects by using single-target inhibitors. Multi-target inhibitors include multicomponent and single component, but single component takes more advantages. The treatment of AIDS is a world problem, single-target inhibitors and multicomponent multi-target inhibitors (i.e. HAART) are used; However, viral height variability and severe drug resistance restrict the wide application of the two therapeutics. Therefore, the single component multi-target inhibitors with low toxicity and highperformance have been the most important choice to treat AIDS caused by HIV-1. The single component multi-target HIV-1 inhibitors mostly come from rational drug design and screening. Some HIV-1 inhibitors have been discovered from the natural products which have extensive sources and wide variety of kinds. That is an important way to develop lead compounds of HIV-1 inhibitors. This paper summarizes the advances in studies on HIV-1 multi-target drugs from natural products.
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[基金项目]
国家自然科学基金资助项目(81241114, 30472166);天津市科技攻关计划重点科技攻关专项基金资助项目(06YFGZSH07000)