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 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.
Cardellina
J H
JH
Laboratory of Drug Discovery Research and Development, National Cancer Institute, Frederick, MD 21702-1201.
Munro
M H
MH
Fuller
R W
RW
Manfredi
K P
KP
McKee
T C
TC
Tischler
M
M
Bokesch
H R
HR
Gustafson
K R
KR
Beutler
J A
JA
Boyd
M R
MR
D015496:CD4-Positive T-Lymphocytes / Q000187:drug effects; D002478:Cells, Cultured; D004353:Drug Evaluation, Preclinical; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D010936:Plant Extracts / Q000032:analysis / Q000494:pharmacology*; D013634:Tannins / Q000302:isolation & purification / Q000494:pharmacology; D014779:Virus Replication / Q000187:drug effects*
D010936:Plant Extracts; D013634:Tannins