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Antiviral chemistry & chemotherapy

Publication date: 2001-11-01
Volume: 12 Pages: 337 - 45
Publisher: SAGE Publishing

Author:

Meerbach, A
Neyts, Johan ; Balzarini, Jan ; Helbig, B ; De Clercq, Erik ; Wutzler, P

Keywords:

Antiviral Agents, Cell Division, Cell Line, Cytomegalovirus, Drug Design, HIV, Herpesviridae, Humans, Molecular Weight, Phenols, Polymers, Simplexvirus, Thymidine Kinase, Science & Technology, Life Sciences & Biomedicine, Biochemistry & Molecular Biology, Pharmacology & Pharmacy, Virology, polyanionic compounds, phenolic polymers, herpesvirus, cytomegalovirus, vaginal microbicide, HUMAN-IMMUNODEFICIENCY-VIRUS, HERPES-SIMPLEX VIRUS, DEXTRAN SULFATE, IN-VITRO, POLYANIONIC COMPOUNDS, SELECTIVE INHIBITORS, VAGINAL MICROBICIDES, ANTIVIRAL ACTIVITY, ENVELOPED VIRUSES, REPLICATION, 0304 Medicinal and Biomolecular Chemistry, 0601 Biochemistry and Cell Biology, 1117 Public Health and Health Services, 3404 Medicinal and biomolecular chemistry

Abstract:

The antiviral activity of 17 polyhydroxycarboxylates derived from phenolic compounds was evaluated against herpesviruses and HIV. When present during virus adsorption several of the polymers exhibited potent activity against herpes simplex virus type 1 (HSV-1), HSV-2, thymidine kinase deficient HSV-1, human cytomegalovirus (HCMV) and HIV-1 and HIV-2 at concentrations that were not toxic to the host cells. A close correlation was found between the 50% inhibitory concentrations of the polyhydroxycarboxylates against HCMV-induced cytopathicity, their inhibitory effect on the expression of HCMV-specific immediate early antigens and their inhibitory effects on HCMV adsorption to the cells. The antiviral activity of the phenolic polymers was dependent on the presence of a sufficient number of carboxylic groups. The mechanism of antiviral action of the polyhydroxycarboxylates can thus be ascribed to inhibition of virus adsorption. This type of compound may have potential in a vaginal gel to prevent sexual transmission of HSV and HIV.