Abstract
Glycyrrhizin (GL) was shown to inhibit SARS-coronavirus (SARS-CoV) replication in vitro. Here the anti-SARS-CoV activity of 15 GL derivatives was tested. The introduction of 2-acetamido-beta-d-glucopyranosylamine into the glycoside chain of GL resulted in 10-fold increased anti-SARS-CoV activity compared to GL. Amides of GL and conjugates of GL with two amino acid residues and a free 30-COOH function presented up to 70-fold increased activity against SARS-CoV but also increased cytotoxicity resulting in decreased selectivity index.
MeSH terms
- Animals
- Antiviral Agents / chemical synthesis*
- Antiviral Agents / chemistry
- Antiviral Agents / pharmacology
- Chlorocebus aethiops
- Glycyrrhizic Acid / analogs & derivatives*
- Glycyrrhizic Acid / chemical synthesis*
- Glycyrrhizic Acid / chemistry
- Glycyrrhizic Acid / pharmacology
- Severe acute respiratory syndrome-related coronavirus / drug effects*
- Severe acute respiratory syndrome-related coronavirus / isolation & purification
- Structure-Activity Relationship
- Vero Cells
- Virus Replication / drug effects
Substances
- Antiviral Agents
- Glycyrrhizic Acid