Antiretroviral activities of anthraquinones and their inhibitory effects on reverse transcriptase.
Alizarin complexone (AC), alizarin Red S (ARS) and various other anthraquinones were evaluated for their inhibitory effects on Rous-associated virus 2 reverse transcriptase (RAV-2 RT). Some 1,2-dihydroxyanthraquinones were active against this enzyme and AC was the most potent inhibitor among these compounds [50% inhibitory concentration (IC50): 3.8 micrograms/ml]. AC slightly inhibited Rous sarcoma virus RT (RSV RT) and human immunodeficiency virus type 1 RT (HIV-1 RT) (IC50: 100 micrograms/ml and 45 micrograms/ml, respectively). However, AC efficiently inhibited focus formation by Rous sarcoma virus (RSV) and cytopathogenicity of human immunodeficiency virus type 1 (HIV-1). Simultaneous administration of AC with RSV to newborn chickens also delayed tumor induction by RSV.
Higuchi
H
H
Research Institute for Molecular Genetics, Tsumura and Co., Ibaraki, Japan.
Mori
K
K
Kato
A
A
Ohkuma
T
T
Endo
T
T
Kaji
H
H
Kaji
A
A
D000818:Animals; D000880:Anthraquinones / Q000494:pharmacology* / Q000627:therapeutic use; D000998:Antiviral Agents / Q000494:pharmacology* / Q000627:therapeutic use; D001354:Avian Leukosis Virus / Q000187:drug effects / Q000201:enzymology; D001358:Avian Sarcoma Viruses / Q000187:drug effects / Q000201:enzymology; D015496:CD4-Positive T-Lymphocytes; D002461:Cell Line, Transformed; D002478:Cells, Cultured; D002645:Chickens; D003588:Cytopathogenic Effect, Viral; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology; D006801:Humans; D007700:Kinetics; D012190:Retroviridae / Q000187:drug effects* / Q000201:enzymology; D018894:Reverse Transcriptase Inhibitors; D001357:Sarcoma, Avian / Q000188:drug therapy*; D014407:Tumor Cells, Cultured; D010948:Viral Plaque Assay
D000880:Anthraquinones; D000998:Antiviral Agents; D018894:Reverse Transcriptase Inhibitors; C070804:alizarin complexone; C004468:Alizarin Red S; C010078:alizarin