Peng Zong-gen, Xu Li-jia, Ye Wen-cai, Xiao Pei-gen, Chen Hong-shan
Institute of Medicinal and Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
Yao Xue Xue Bao. 2010 Feb;45(2):235-40.
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 alkaloids, 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.
植物活性成分具有多种不同结构且对多个靶点有活性，这使其成为HIV-1抑制剂的重要来源。为了寻找针对HIV-1的具有新结构的先导化合物，使用了三种关键的HIV-1复制酶（逆转录酶、蛋白酶和整合酶）作为筛选模型。报道了从五味子科、芸香科和毛茛科分离得到的45种植物衍生成分的体外活性。在分离出的12种三萜成分中，发现8种化合物可抑制HIV-1蛋白酶，在这8种活性化合物中，南五味子酸A（7）和黑老虎酸（8）同时抑制HIV-1蛋白酶和整合酶；在15种木脂素中，中-二氢愈创木酸（15）和南五味子素（16）对HIV-1逆转录酶有活性，4,4-二（4-羟基-3-甲氧基苯基）-2,3-二甲基丁醇（13）对HIV-1整合酶有活性。所有6种生物碱、7种黄酮类化合物及其他5种化合物对HIV-1复制酶无活性或仅有低活性。对显示出对HIV-1有强抑制活性的三萜成分进行进一步研究很有必要。
