Diammonium Glycyrrhizinate Exerts Broad-Spectrum Antiviral Activity Against Human Coronaviruses by Interrupting Spike-Mediated Cellular Entry.

Publication date: Jun 30, 2025

Glycyrrhizic acid (GA) and its derivatives have been reported to have potent pharmacological effects against viral infections, including SARS-CoV and SARS-CoV-2. However, their antiviral mechanisms against coronaviruses are not fully understood. In this study, we found that diammonium glycyrrhizinate (DG) can effectively reduce infections of several human coronaviruses, including HCoV-OC43, HCoV-229E, and SARS-CoV-2, as well as newly emerged variants, with EC values ranging from 115 to 391 μg/mL being recorded. Time-of-addition and pseudotype virus infection studies indicated that DG treatment dramatically inhibits the process of virus entry into cells. Furthermore, we demonstrated that DG broadly binds to the RBD of human coronaviruses, thereby blocking spike-mediated cellular entry, by using TR-FRET-based receptor-binding domain (RBD)-ACE2 interaction assay, capillary electrophoresis (CE), and surface plasmon resonance (SPR) assay. In support of this notion, studies of molecular docking and amino acid mutation showed that DG may directly bind to a conserved hydrophobic pocket of the RBD of coronaviruses. Importantly, intranasal administration of DG had a significant protective effect against viral infection in a HCoV-OC43 mouse model. Finally, we found that combinations of DG and other coronavirus inhibitors exhibited antiviral synergy. In summary, our studies strongly reveal that DG exerts broad-spectrum antiviral activity against human coronaviruses by interrupting spike-mediated cellular entry, demonstrating the pharmacological feasibility of using DG as a candidate for alternative treatment and prevention of coronavirus infection.

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Concepts Keywords
Antiviral Angiotensin-Converting Enzyme 2
Coronaviruses Angiotensin-Converting Enzyme 2
Docking Animals
Pharmacological Antiviral Agents
Potent Antiviral Agents
broad spectrum
coronavirus
Coronavirus 229E, Human
Coronavirus Infections
Coronavirus OC43, Human
COVID-19
COVID-19 Drug Treatment
diammonium glycyrrhizinate
Glycyrrhizic Acid
Glycyrrhizic Acid
HEK293 Cells
Humans
Mice
Molecular Docking Simulation
RBD-binding activity
SARS-CoV-2
Spike Glycoprotein, Coronavirus
Spike Glycoprotein, Coronavirus
spike protein, SARS-CoV-2
spike-mediated cellular entry
Virus Internalization

Semantics

Type Source Name
drug DRUGBANK Glycyrrhizic acid
disease MESH viral infections
disease MESH infections
disease IDO process
disease IDO assay
disease MESH coronavirus infection
disease MESH COVID 19 pandemic
disease MESH respiratory diseases
disease MESH tic
disease MESH liver diseases
disease MESH chronic hepatitis
disease IDO immunodeficiency
disease MESH hepatitis
disease MESH herpes simplex
disease MESH influenza
disease IDO replication
disease IDO infection
disease MESH reinfection
drug DRUGBANK Phosphate ion
disease IDO protein
disease MESH dissociation
drug DRUGBANK Amino acids
drug DRUGBANK Water
disease MESH weight loss
disease MESH paralysis
disease MESH ataxia
drug DRUGBANK Pentaerythritol tetranitrate
disease MESH body weight change
disease MESH atrophy
disease MESH inflammation
drug DRUGBANK Ribavirin
drug DRUGBANK Azithromycin
disease IDO host
disease MESH brain inflammation
disease MESH lung diseases
disease MESH hepatocellular carcinoma
pathway KEGG Hepatocellular carcinoma
disease MESH hepatoblastoma
drug DRUGBANK Methylergometrine
drug DRUGBANK Streptomycin
drug DRUGBANK Ammonium chloride
disease IDO reagent
drug DRUGBANK Trestolone
disease IDO cell
pathway KEGG Endocytosis
drug DRUGBANK Dimethyl sulfoxide
drug DRUGBANK Sodium acetate
drug DRUGBANK Flunarizine
drug DRUGBANK Gold
drug DRUGBANK Ethanolamine
disease MESH immobilization
disease IDO facility
disease IDO pathogen
disease MESH morbidity
drug DRUGBANK Formaldehyde
drug DRUGBANK Coenzyme M
disease MESH severe acute respiratory syndrome
disease MESH pneumonia
drug DRUGBANK (S)-Des-Me-Ampa
drug DRUGBANK Sulfasalazine
drug DRUGBANK Guanosine
drug DRUGBANK Diethylstilbestrol
drug DRUGBANK Chlorcyclizine
drug DRUGBANK Carboxyamidotriazole
pathway REACTOME Metabolism
disease MESH Shock
disease MESH portal hypertension
drug DRUGBANK Curcumin

Original Article

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