HIV-inhibitory natural products. 11. Comparative studies of sulfated sterols from marine invertebrates.
A total of 22 sulfated sterols isolated from marine sponges, ophiuroids (brittle stars), and asteroids (sea stars) were comparatively evaluated for their antiviral activity against HIV-1 and HIV-2. In general, sterols with sulfate groups at position 2, 3, or 6 were the most active, with EC50 values of 3-13 microM against HIV-1 (RF) and 2-8 microM against HIV-2 (CBL20). Those compounds which were sulfated on the sterol D ring were completely inactive against both HIV-1 and HIV-2. Overall, sulfated sterols active against HIV-1 were also active against HIV-2.
McKee
T C
TC
Laboratory of Drug Discovery Research and Development, National Cancer Institute, Frederick, Maryland 21702-1201.
Cardellina
J H
JH
Riccio
R
R
D'Auria
M V
MV
Iorizzi
M
M
Minale
L
L
Moran
R A
RA
Gulakowski
R J
RJ
McMahon
J B
JB
Buckheit
R W
RW
D000818:Animals; D000998:Antiviral Agents / Q000302:isolation & purification* / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004447:Echinodermata / Q000737:chemistry*; D015497:HIV-1 / Q000187:drug effects*; D015498:HIV-2 / Q000187:drug effects*; D006801:Humans; D008826:Microbial Sensitivity Tests; D011161:Porifera / Q000737:chemistry*; D013261:Sterols / Q000302:isolation & purification* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013463:Sulfuric Acid Esters / Q000302:isolation & purification* / Q000494:pharmacology*
D000998:Antiviral Agents; D013261:Sterols; D013463:Sulfuric Acid Esters