The Brief Overview, Antivirus and Anti-SARS-CoV-2 Activity, Quantitative Methods, and Pharmacokinetics of Cepharanthine: A Potential Small-Molecule Drug Against COVID-19

July 2023 in “ Frontiers in Pharmacology ”

Binbin Xia, Zheng Li, Yali Li, Wenfang Sun, Yang Liu, Liushui Li, Jingyao Pang, Jing Chen, Jiaxin Li, Hua Cheng

cepharanthine bisbenzylisoquinoline alkaloid alopecia

Studysummary This review highlights cepharanthine as a promising candidate for COVID-19 treatment due to its antiviral activity against SARS-CoV-2 and favorable pharmacokinetic and safety profile, but reports no new clinical results.

Our plain-language summary. Not medical advice or a treatment recommendation. Consult a qualified healthcare professional before changing treatment. Full disclaimer

Cepharanthine (CEP) is a bisbenzylisoquinoline alkaloid with potential as a small-molecule drug against COVID-19 due to its significant antiviral properties against SARS-CoV-2. Studies have shown that CEP effectively inhibits viral replication and entry by targeting specific viral proteins and cellular pathways, demonstrating greater efficacy than remdesivir in vitro. Despite its promise, CEP's poor oral bioavailability poses a challenge, though alternative administration routes like pulmonary delivery and nanotechnology-based systems have shown to enhance its bioavailability. CEP has been used safely since 1951 for various conditions, including alopecia, and its safety profile supports its potential as a COVID-19 therapeutic. However, further research is needed to optimize its pharmacokinetics and confirm its clinical efficacy.

View this study on frontiersin.org →

Discuss this study in the Community →

Research cited in this study

10 / 10 results

research The Antiviral Activity of a Small Molecule Drug Targeting the NSP1-Ribosome Complex Against Omicron, Especially in Elderly Patients

6 citations , March 2023 in “Frontiers in Cellular and Infection Microbiology”

This study found that Golvatinib, Gliquidone, and Dihydroergotamine may inhibit the binding of SARS-CoV-2's Nsp1 protein to the host ribosomal subunit, suggesting potential as treatments against COVID-19 variants.

research The Common Regulatory Pathway of COVID-19 and Multiple Inflammatory Diseases and the Molecular Mechanism of Cepharanthine in the Treatment of COVID-19

15 citations , July 2022 in “Frontiers in Pharmacology”

This study suggests that Cepharanthine, a monomer in traditional Chinese medicine, may help treat COVID-19 by affecting multiple signaling pathways, and that TNF and IL-17 inhibitors used in rheumatoid arthritis, ankylosing spondylitis, and gouty arthritis might also be beneficial.

research Bioavailability Enhancement of Cepharanthine via Pulmonary Administration in Rats and Its Therapeutic Potential for Pulmonary Fibrosis Associated with COVID-19 Infection

14 citations , April 2022 in “Molecules”

This study found that pulmonary delivery of cepharanthine significantly improved bioavailability and may provide protective effects against pulmonary fibrosis related to COVID-19 infection in a rat model.

research Cepharanthine Suppresses Herpes Simplex Virus Type 1 Replication Through the Downregulation of the PI3K/Akt and p38 MAPK Signaling Pathways

30 citations , December 2021 in “Frontiers in Microbiology”

In this study, researchers found that cepharanthine significantly inhibited HSV-1 replication in vitro by interfering with specific signaling pathways, arresting the cell cycle, and inducing apoptosis in infected cells, highlighting its potential as an antiviral agent.

research Evaluating Cepharanthine Analogues as Natural Drugs Against SARS-CoV-2

29 citations , November 2021 in “FEBS Open Bio”

In this study, molecular docking simulations and cell-based assays suggested that certain analogues of cepharanthine might possess anti-SARS-CoV-2 activity.

Comparison of Viral RNA–Host Protein Interactomes Across Pathogenic RNA Viruses Informs Rapid Antiviral Drug Discovery for SARS-CoV-2

research Comparison of Viral RNA–Host Protein Interactomes Across Pathogenic RNA Viruses Informs Rapid Antiviral Drug Discovery for SARS-CoV-2

100 citations , November 2021 in “Cell Research”

This study found that SARS-CoV-2 hijacks the host factor IGF2BP1 to stabilize its RNA and enhance translation, and identified Cepharanthine and Trifluoperazine as potential treatments against the virus.

The Brief Overview, Antivirus and Anti-SARS-CoV-2 Activity, Quantitative Methods, and Pharmacokinetics of Cepharanthine: A Potential Small-Molecule Drug Against COVID-19

Research cited in this study

research The Antiviral Activity of a Small Molecule Drug Targeting the NSP1-Ribosome Complex Against Omicron, Especially in Elderly Patients

research The Common Regulatory Pathway of COVID-19 and Multiple Inflammatory Diseases and the Molecular Mechanism of Cepharanthine in the Treatment of COVID-19

research Bioavailability Enhancement of Cepharanthine via Pulmonary Administration in Rats and Its Therapeutic Potential for Pulmonary Fibrosis Associated with COVID-19 Infection

research Cepharanthine Suppresses Herpes Simplex Virus Type 1 Replication Through the Downregulation of the PI3K/Akt and p38 MAPK Signaling Pathways

research Evaluating Cepharanthine Analogues as Natural Drugs Against SARS-CoV-2

research Comparison of Viral RNA–Host Protein Interactomes Across Pathogenic RNA Viruses Informs Rapid Antiviral Drug Discovery for SARS-CoV-2

research Preparation and Evaluation of Self-Emulsifying Drug Delivery System of Cepharanthine

research Discovery of COVID-19 Inhibitors Targeting the SARS-CoV-2 Nsp13 Helicase

research Cepharanthine: A Review of the Antiviral Potential of a Japanese-Approved Alopecia Drug in COVID-19

research Cepharanthine: An Update of Its Mode of Action, Pharmacological Properties, and Medical Applications