el-Mekkawy S, Meselhy M R, Kusumoto I T, Kadota S, Hattori M, Namba T
Research Institute for Wakan-Yaku (Traditional Sino-Japanese Medicines), Toyama Medical and Pharmaceutical University, Japan.
Chem Pharm Bull (Tokyo). 1995 Apr;43(4):641-8. doi: 10.1248/cpb.43.641.
Extracts of 41 medicinal plants used in Egyptian folk medicine were screened for their inhibitory effects on human immunodeficiency virus-1 reverse transcriptase. The extracts of fruits of Phyllanthus emblica, Quercus pedunculata, Rumex cyprius, Terminalia bellerica, Terminalia chebula and Terminalia horrida showed significant inhibitory activity with IC50 < or = 50 micrograms/ml. Through a bioassay guided-fractionation of the methanol extract of the fruit of P. emblica, putranjivain A (1) was isolated as a potent inhibitory substance with IC50 = 3.9 microM, together with 1,6-di-O-galloyl-beta-D-glucose (2), 1-O-galloyl-beta-D-glucose (3), kaempferol-3-O-beta-D-glucoside (4), quercetin-3-O-beta-D-glucoside (5) and digallic acid (6). The inhibitory mode of action by 1, 2 and 6 was non-competitive with respect to the substrate but competitive with respect to a template-primer. Furthermore, the stereochemistry of 1 was established in this paper by nuclear magnetic resonance spectroscopy.
对埃及民间医学中使用的41种药用植物提取物进行了筛选，以研究它们对人类免疫缺陷病毒1型逆转录酶的抑制作用。余甘子、无梗花栎、塞浦路斯酸模、毗黎勒、诃子和粗毛诃子果实的提取物表现出显著的抑制活性，半数抑制浓度（IC50）≤50微克/毫升。通过对余甘子果实甲醇提取物进行生物测定导向的分级分离，分离出了具有强效抑制作用的普特兰吉文A（1），其IC50 = 3.9微摩尔，同时还分离出了1,6-二-O-没食子酰基-β-D-葡萄糖（2）、1-O-没食子酰基-β-D-葡萄糖（3）、山柰酚-3-O-β-D-葡萄糖苷（4）、槲皮素-3-O-β-D-葡萄糖苷（5）和双没食子酸（6）。1、2和6的抑制作用模式对底物而言是非竞争性的，但对模板引物而言是竞争性的。此外，本文通过核磁共振光谱确定了1的立体化学结构。
