天然产物来源的抗HIV-1多靶点抑制剂研究进展  

Advances in studies on HIV-1 multi-target drugs from natural products

作　　者：李凯[1] 李爱秀[1,2] 靳玉瑞[1] 罗力[1] 

机构地区：[1]武警后勤学院基础部药物设计实验室,天津300309 [2]武警后勤学院,天津市职业与环境危害防治重点实验室,天津300309

出　　处：《中草药》2015年第12期1840-1848,共9页Chinese Traditional and Herbal Drugs

基　　金：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)

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1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。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.

关 键 词：天然产物 抗HIV-1 多靶点抑制剂 先导化合物 艾滋病 

分 类 号：R284[医药卫生—中药学] R285[医药卫生—中医学]