Anthraquinones as a new class of antiviral agents against human immunodeficiency virus.
Various anthraquinones substituted with hydroxyl, amino, halogen, carboxylic acid, substituted aromatic group, and sulfonate were tested to determine their activity against human immunodeficiency virus type 1 (HIV-1) in primary human lymphocytes. Among the compounds tested, polyphenolic and/or polysulfonate substituted anthraquinones were found to possess the most potent antiviral activity. Hypericin, an anthraquinone dimer previously shown to have activity against nonhuman retroviruses also exhibited anti-HIV-1 activity in lymphocytes. the active anthraquinones inhibited HIV-1 reverse transcriptase. However, this enzyme inhibition was selective only for 1,2,5,8-tetrahydroanthraquinone and hypericin. Hypericin interacts nonspecifically with protein suggesting that this effect may dictate its inhibitory activity against the viral reverse transcriptase.
Veterans Affairs Medical Center, Decatur, GA 30033.
R F
RF
Schinazi
C K
CK
Chu
J R
JR
Babu
B J
BJ
Oswald
V
V
Saalmann
D L
DL
Cannon
B F
BF
Eriksson
M
M
Nasr
D000163:Acquired Immunodeficiency Syndrome / Q000188:drug therapy*; D000880:Anthraquinones / Q000494:pharmacology*; D000998:Antiviral Agents / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology / Q000254:growth & development; D006801:Humans; D008214:Lymphocytes / Q000382:microbiology; D012194:RNA-Directed DNA Polymerase / Q000378:metabolism; D014779:Virus Replication / Q000187:drug effects
D000880:Anthraquinones; D000998:Antiviral Agents; D012194:RNA-Directed DNA Polymerase