Tewtrakul Supinya, Subhadhirasakul Sanan, Cheenpracha Sarot, Karalai Chatchanok
Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla, 90112, Thailand.
Phytother Res. 2007 Nov;21(11):1092-5. doi: 10.1002/ptr.2252.
The bioassay-guided fractionation for anti-HIV-1 integrase activity led to the isolation of six compounds from the whole plant extract of Eclipta prostrata extract. They were identified as 5-hydroxymethyl-(2,2':5',2'')-terthienyl tiglate (1), 5-hydroxymethyl-(2,2':5',2'')-terthienyl agelate (2), 5-hydroxymethyl-(2,2':5',2'')-terthienyl acetate (3), ecliptal (4), orobol (5) and wedelolactone (6). Of these, compound 6 showed the highest activity against HIV-1 integrase (IN) with an IC50 value of 4.0+/-0.2 microm, followed by compound 5 (IC50=8.1+/-0.5 microm), whereas the four terthiophene compounds (1-4) were inactive (IC50>100 microm). Regarding HIV-1 protease (PR) inhibitory activity, compound 1 exhibited appreciable activity against HIV-1 PR with an IC50 of 58.3+/-0.8 microm, followed by compound 4 (IC50=83.3+/-1.6 microm) and compound 3 (IC50=93.7+/-0.8 microm), while compounds 2, 5 and 6 were inactive against HIV-1 PR (IC50>100 microm). This is the first report of anti-HIV-1 IN activities for wedelolactone (6), a coumarin derivative, and orobol (5), an isoflavone derivative. This study supports the use of E. prostrata in AIDS patients, which is in accord with its traditional use by Thai traditional doctors for curing blood related diseases.
针对抗HIV-1整合酶活性进行的生物测定导向分级分离，从鳢肠全株提取物中分离出了六种化合物。它们分别被鉴定为5-羟甲基-(2,2':5',2'')-三联噻吩替格列酸酯（1）、5-羟甲基-(2,2':5',2'')-三联噻吩阿魏酸酯（2）、5-羟甲基-(2,2':5',2'')-三联噻吩乙酸酯（3）、墨旱莲素（4）、紫铆因（5）和蟛蜞菊内酯（6）。其中，化合物6对HIV-1整合酶（IN）表现出最高活性，IC50值为4.0±0.2微摩尔，其次是化合物5（IC50 = 8.1±0.5微摩尔），而四种噻吩类化合物（1 - 4）无活性（IC50>100微摩尔）。关于HIV-1蛋白酶（PR）抑制活性，化合物1对HIV-1 PR表现出可观的活性，IC50为58.3±0.8微摩尔，其次是化合物4（IC50 = 83.3±1.6微摩尔）和化合物3（IC50 = 93.7±0.8微摩尔），而化合物2、5和6对HIV-1 PR无活性（IC50>100微摩尔）。这是关于香豆素衍生物蟛蜞菊内酯（6）和异黄酮衍生物紫铆因（5）抗HIV-1 IN活性的首次报道。本研究支持在艾滋病患者中使用鳢肠，这与其在泰国传统医学中用于治疗血液相关疾病的传统用途相符。
