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).
Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium.
D
D
Schols
P
P
Wutzler
R
R
Klöcking
B
B
Helbig
E
E
De Clercq
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