title: In vitro activity of polyhydroxycarboxylates against herpesviruses and HIV.
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.
authors.affiliation: Institute for Antiviral Chemotherapy, Friedrich-Schiller University, Jena, Germany. Astrid.Meerbach@med.uni-jena.de
authors.forename: A
authors.initials: A
authors.lastname: Meerbach
authors.forename: J
authors.initials: J
authors.lastname: Neyts
authors.forename: J
authors.initials: J
authors.lastname: Balzarini
authors.forename: B
authors.initials: B
authors.lastname: Helbig
authors.forename: E
authors.initials: E
authors.lastname: De Clercq
authors.forename: P
authors.initials: P
authors.lastname: Wutzler
mesh_terms: D000998:Antiviral Agents / Q000737:chemistry* / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D003587:Cytomegalovirus / Q000187:drug effects; D015195:Drug Design; D006678:HIV / Q000187:drug effects*; D006564:Herpesviridae / Q000187:drug effects*; D006801:Humans; D008970:Molecular Weight; D010636:Phenols / Q000737:chemistry* / Q000494:pharmacology*; D011108:Polymers / Q000737:chemistry / Q000494:pharmacology; D018139:Simplexvirus / Q000187:drug effects; D013937:Thymidine Kinase / Q000378:metabolism
chemical_list: D000998:Antiviral Agents; D010636:Phenols; D011108:Polymers; D013937:Thymidine Kinase