1. Anthraquinones as a new class of antiviral agents against human immunodeficiency virus
- Author
-
Vanessa Saalmann, Deborah L. Cannon, Bertil F.H. Eriksson, Barbara J. Oswald, Mohamed Nasr, Chung K. Chu, Raymond F. Schinazi, and J. Ramesh Babu
- Subjects
Pharmacology ,chemistry.chemical_classification ,Acquired Immunodeficiency Syndrome ,Carboxylic acid ,Biological activity ,Anthraquinones ,RNA-Directed DNA Polymerase ,Biology ,Virus Replication ,Antiviral Agents ,Reverse transcriptase ,Virus ,Hypericin ,chemistry.chemical_compound ,Enzyme ,Biochemistry ,chemistry ,Mechanism of action ,Virology ,medicine ,HIV-1 ,Humans ,Lymphocytes ,medicine.symptom - Abstract
Various anthraquinones substituted with hydroxyl, amino, halogen, carboxylic acid, substituted aromatic group, and sulfonate were tested to determine their activity against human immunodeficiency virus type 1 (HIV-1) in primary human lymphocytes. Among the compounds tested, polyphenolic and/or polysulfonate substituted anthraquinones were found to possess the most potent antiviral activity. Hypericin, an anthraquinone dimer previously shown to have activity against nonhuman retroviruses also exhibited anti-HIV-1 activity in lymphocytes. the active anthraquinones inhibited HIV-1 reverse transcriptase. However, this enzyme inhibition was selective only for 1,2,5,8-tetrahydroanthraquinone and hypericin. Hypericin interacts nonspecifically with protein suggesting that this effect may dictate its inhibitory activity against the viral reverse transcriptase.
- Published
- 1990