Lipid conjugates of antiretroviral agents. II. Disodium palmityl phosphonoformate: Anti-HIV activity, physical properties, and interaction with plasma proteins

• Published in: Biochemical and biophysical research communications Vol. 171; no. 1; pp. 458 - 464
• Main Authors: Neto, Catherine Camaioni, Steim, Joseph M., Sarin, Prem S., Sun, Daisy K., Bhongle, Nandkumar N., Piratla, Rao K., Turcotte, Joseph G.
• Format: Journal Article
• Language: English
• Published: San Diego, CA Elsevier Inc 31.08.1990; Elsevier
• Subjects: AIDS/HIV; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiviral Agents; Biological and medical sciences; Cell Fusion - drug effects; Cell Line; Chemical Phenomena; Chemistry, Physical; Foscarnet; HIV - drug effects; HIV - growth & development; In Vitro Techniques; Lipoproteins - metabolism; Medical sciences; Palmitates; Palmitic Acids; Pharmacology. Drug treatments; Phosphonoacetic Acid - analogs & derivatives; Retroviridae Proteins - metabolism; Serum Albumin, Bovine - metabolism; PBS; HDL; BSA; HIV; LDL; Virus; Proteins; Retroviridae; Antiviral; Molecular interaction; Lipids; Conjugation; Human immunodeficiency virus; Biological activity; Dose activity relation
• ISSN: 0006-291X; 1090-2104
• DOI: 10.1016/0006-291X(90)91415-O

Disodium palmityl phosphonoformate, a novel lipid phosphoester of the anti HIV agent phosphonoformate (foscarnet), inhibits HIV replication in H9 cells and syncytia formation in MOLT-3 cells as effectively as foscarnet itself, as shown by dose-response data from assays for expression of p17 and p24 viral antigens and syncytia formation. Protein binding studies indicate that in serum, the derivative exists bound to albumin and the lipoproteins, and would therefore be likely to exhibit improved serum lifetime in vivo.