Selective inhibitory activity of polyhydroxycarboxylates derived from phenolic compounds against human immunodeficiency virus replication.
Polyhydroxycarboxylates (MW: 3,800-14,000) derived from phenolic (PDP) compounds have been found to inhibit the cytopathicity of HIV-1 and HIV-2 in MT-4 cells at concentrations that are not toxic to the host cells. The PDP compounds also inhibited syncytium formation in cocultures of MOLT-4 cells with HIV-1- or HIV-2-infected HUT-78 cells. They also interfered with the binding of OKT4A/leu3a monoclonal antibody (mAb) to the CD4 receptor, the binding of anti-gp120 mAb to HIV-1 gp120, and attachment of HIV-1 virions to MT-4 cells. The anti-HIV activity in this series of compounds can be ascribed to inhibition of the gp120-CD4 interaction and seems to depend on the presence of the anionic carboxylate groups. Their mechanism of action is similar to that of the heterogeneous polymer aurintricarboxylic acid (ATA).
Schols
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Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium.
Wutzler
P
P
Klöcking
R
R
Helbig
B
B
De Clercq
E
E
D000327:Adsorption; D000911:Antibodies, Monoclonal / Q000276:immunology; D000998:Antiviral Agents / Q000494:pharmacology*; D015704:CD4 Antigens / Q000276:immunology; D015496:CD4-Positive T-Lymphocytes / Q000276:immunology; D002264:Carboxylic Acids / Q000737:chemistry* / Q000494:pharmacology; D002478:Cells, Cultured; D015726:Giant Cells / Q000382:microbiology; D015699:HIV Envelope Protein gp120 / Q000276:immunology; D015497:HIV-1 / Q000187:drug effects* / Q000254:growth & development / Q000276:immunology; D015498:HIV-2 / Q000187:drug effects* / Q000254:growth & development / Q000276:immunology; D010636:Phenols / Q000737:chemistry* / Q000494:pharmacology; D011948:Receptors, Antigen, T-Cell / Q000276:immunology; D014779:Virus Replication / Q000187:drug effects*
D000911:Antibodies, Monoclonal; D000998:Antiviral Agents; D015704:CD4 Antigens; D002264:Carboxylic Acids; D015699:HIV Envelope Protein gp120; D010636:Phenols; D011948:Receptors, Antigen, T-Cell