Cardellina J H, Munro M H, Fuller R W, Manfredi K P, McKee T C, Tischler M, Bokesch H R, Gustafson K R, Beutler J A, Boyd M R
Laboratory of Drug Discovery Research and Development, National Cancer Institute, Frederick, MD 21702-1201.
J Nat Prod. 1993 Jul;56(7):1123-9. doi: 10.1021/np50097a016.
A relatively high percentage (ca. 15%) of aqueous extracts from terrestrial plants, cyanobacteria, and marine invertebrates and algae has exhibited activity in the National Cancer Institute's primary AIDS-antiviral screen. By removal of anionic polysaccharides in a first stage of dereplication, we have eliminated from further consideration a considerable number of these extracts. However, a still substantial proportion of the active extracts remained, from which we wished to select and prioritize a small percentage for our detailed bioassay-directed fractionation studies. Therefore, a chemical screening protocol, utilizing various solid-phase extraction cartridges, has been developed for a second-stage dereplication and to assist in prioritization of these extracts for our further investigations.
在国立癌症研究所的原发性抗艾滋病病毒筛选中，来自陆生植物、蓝细菌、海洋无脊椎动物和藻类的水提取物中有相对较高比例（约15%）表现出活性。在初次去除重复成分的阶段，通过去除阴离子多糖，我们已将相当数量的这些提取物排除在进一步研究之外。然而，仍有相当一部分活性提取物留存下来，我们希望从中挑选一小部分并确定其优先级，以便进行详细的生物测定导向分级分离研究。因此，已开发出一种利用各种固相萃取柱的化学筛选方案，用于第二阶段的去除重复成分，并协助确定这些提取物的优先级以便我们进一步研究。
