Qian-Cutrone J, Huang S, Trimble J, Li H, Lin P F, Alam M, Klohr S E, Kadow K F
Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, Connecticut 06492, USA.
J Nat Prod. 1996 Feb;59(2):196-9. doi: 10.1021/np9600560.
During the screening of natural products for their ability to inhibit the binding of HIV-REV protein to [33P]-labeled RRE RNA, one novel compound, niruriside (1), was isolated from the MeOH extract of the dried leaf of Phyllanthus niruri L. by bioassay-guided fractionation. The structure of niruriside was determined by spectroscopic methods. Niruriside showed specific inhibitory activity against the binding of REV protein to RRE RNA with an IC50 value of 3.3 microM; however, niruriside did not protect CEM-SS cells from acute HIV infection at concentrations up to 260 microM using an XTT dye reduction assay.
在筛选天然产物抑制HIV-REV蛋白与[33P]标记的RRE RNA结合能力的过程中，通过生物活性导向分离从余甘子干燥叶的甲醇提取物中分离出一种新型化合物——余甘子苷（1）。余甘子苷的结构通过光谱方法确定。余甘子苷对REV蛋白与RRE RNA的结合表现出特异性抑制活性，IC50值为3.3微摩尔；然而，使用XTT染料还原测定法，在浓度高达260微摩尔时，余甘子苷并不能保护CEM-SS细胞免受急性HIV感染。
