A CHEMICAL-SCREENING STRATEGY FOR THE DEREPLICATION AND PRIORITIZATION OF HIV-INHIBITORY AQUEOUS NATURAL-PRODUCTS EXTRACTS

A relatively high percentage (ca. 15 %) of aqueous extracts from terre strial plants, cyanobacteria, and marine invertebrates and algae has e xhibited activity in the National Cancer Institute's primary AIDS-anti viral screen. By removal of anionic polysaccharides in a first stage o f dereplication, we have eliminated from further consideration a consi derable number of these extracts. However, a still substantial proport ion of the active extracts remained, from which we wished to select an d prioritize a small percentage for our detailed bioassay-directed fra ctionation studies. Therefore, a chemical screening protocol, utilizin g various solid-phase extraction cartridges, has been developed for a second-stage dereplication and to assist in prioritization of these ex tracts for our further investigations.