Comprehensive insights into the therapeutic effects of baicalein and baicalin against SARS-COV-2 infection

Abstract

Background

The coronavirus disease 2019 (COVID-19) pandemic is caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The emergence of new SARS-CoV-2 variants has reduced the effectiveness of existing vaccines. Current treatments, including corticosteroids, antiviral agents, and monoclonal antibody-based immunomodulators, often have limitations, including adverse side effects, limited efficacy, and high costs, especially for patients with comorbidities. These challenges have spurred interest in phytochemicals, known for their anti-inflammatory, antiviral, and antioxidant properties.

Purpose

This review aims to provide a comprehensive analysis of the anti-SARS-CoV-2 efficacy and anti-inflammatory activity of baicalein and its 7-O-glucuronide derivative, baicalin, are the main components derived from Scutellaria baicalensis. We focus on their mechanisms of action against SARS-CoV-2 and their potential role in mitigating COVID-19-related inflammation.

Materials and Methods

A comprehensive literature search was conducted using databases such as PubMed, Web of Science, and Scopus. Studies investigating the effects of baicalein and baicalin on viral infections, inflammatory pathways, and COVID-19-specific targets, including spike protein, 3C-like protease (3CLpro) and PLpro, were included.

Results

Baicalein and baicalin exhibit anti-SARS-CoV-2 activity by inhibiting viral entry through blockade of the interaction between the spike protein and angiotensin-converting enzyme II (ACE2) receptor. They also suppress viral replication by targeting 3CLpro, RNA-dependent RNA polymerase (RdRp), and helicase. Moreover, baicalein and baicalin mitigate COVID-19-associated inflammation by regulating nod-like receptor pyrin domain-containing 3 (NLRP3) inflammasome and toll-like receptor pathways. They inhibit nuclear factor kappa B (NF-κB) and mitogen-activated protein kinase (MAPK) pathways, thereby reducing pro-inflammatory cytokines such as IL-6, IL-1β, IFN-γ, and TNF-α.

Conclusion

Baicalein and Baicalin hold therapeutic potential for managing viral infections and inflammation. Further preclinical and clinical research is essential to validate these findings and advance baicalein and baicalin as viable therapeutic candidates for COVID-19.