几种抑制HIV-1复制酶的植物成分

Effective components against HIV-1 replicative enzymes isolated from plants

植物活性成分结构多样性和其作用多靶点的特点,已使其成为寻找抗HIV-1药物的重要来源之一。为从植物中获得结构新颖的抗HIV-1活性先导化合物,本文应用HIV-1蛋白酶(PR)、逆转录酶(RT)和整合酶(IN)筛选模型,对45个来源于毛茛科、芸香科和五味子科等植物的结构清楚的化合物进行了体外活性测定。12个三萜类化合物中8个具有抑制HIV-1PR活性,其中2个还具有抑制IN活性;15个木脂素类化合物中2个具有抑制HIV-1RT活性。6个生物碱类、7个黄酮类及5个其他结构类型的化合物都无明显抑制3种复制酶的作用。植物来源的三萜类化合物抑制PR或IN的活性较好,值得深入研究。

Plant active components characterized of many different structures and activities on multiple targets,have made them to be the important sources of inhibitors on HIV-1.For finding leading compounds with new structure against HIV-1,three key HIV-1 replicative enzymes （reverse transcriptase,protease and integrase） were used as screening models.The in vitro activities of 45 plant derived components isolated from Schisandraceae,Rutaceae and Ranunculaceae were reported.Within twelve triterpene components isolated,eight compounds were found to inhibit HIV-1 protease,in these eight active compounds,kadsuranic acid A （7） and nigranoic acid （8）,inhibited both HIV-1 protease and integrase;Among fifteen lignans,meso-dihydroguaiaretic acid （15） and kadsurarin （16） were active on HIV-1 reverse transcriptase,and 4,4-di（4-hydroxy-3-methoxyphenly）2,3-dimethylbutanol （13） active on HIV-1 integrase.All of the six alkloids,seven flavones,and five others compounds were not active or only with low activities against HIV-1 replicative enzymes.Further studies of the triterpene components showing strong inhibitory activities on HIV-1 were warranted.