Potential treatment - pre-clinical evidence
Baicalein is a natural trihydroxyflavone bioactive compound (with e. g. anti-inflammatory, antioxidant, or hormone antagonist properties) (ChEBI). It potentially acts against SARS-CoV-2 infection through inhibition of mitochondrial oxidative phosphorylation via mitochondrial permeability transition pore activity modulation (Huang et al., 2020).
Discovery of baicalin and baicalein as novel, natural product inhibitors of SARS-CoV-2 3CL protease in vitro
Potential Treatment of Chinese and Western Medicine Targeting Nsp14 of SARS-CoV-2
nsp14 Small molecule In silico
Predicted to bind the SARS-CoV-2 nsp14 protein.
The comprehensive study on the therapeutic effects of baicalein for the treatment of COVID-19 in vivo and in vitro
Small molecule Animal model In vitro
|Vero E6 cells; hACE2 mice; BALB/c mice; male SD rats (pharmacokinetics).
Reduction in SARS-CoV-2-induced cell damage assessed by changes in morphology in vitro at concentrations of 0.1 μM or more (which were achievable in rats). Inhibition of viral replication in lungs, relief of lung lesions, and reduction of weigth loss in hACE2 mice. In a LPS-induced acute lung injury murine model, bacalein improved respiratory function and reduced inflammatory markers.
Baicalein inhibits SARS-CoV-2/VSV replication with interfering mitochondrial oxidative phosphorylation in a mPTP dependent manner
Small molecule In vitro Mechanism
|Vero E6 cells
Inhibits SARS-CoV-2 infection in sub-toxic concentrations in vitro. Reduces oxygen consumption through partial oxidative phosphorylation inhibition, potentially via mitochondrial permeability transition pore regulation.
Scutellaria baicalensis extract and baicalein inhibit replication of SARS-CoV-2 and its 3C-like protease in vitro
Small molecule Enzyme assay In vitro In silico
|in silico; in vitro enzyme assay; Vero cells; HEK293T cell lysates; SARS-CoV-2 isolate C-Tan-nCoV Wuhan strain 01
Inhibits SARS-CoV-2 3C-like protease in vitro with IC50 of 0.39 µM and blocks SARS-CoV-2 replication with EC50 of 2.9 µM in Vero cells. It acts mainly at the post-entry stages of infection.
Baicalein and Baicalin Inhibit SARS-CoV-2 RNA-Dependent-RNA Polymerase
RdRpol Biophysical assay Small molecule Enzyme assay In vitro In silico
|in silico; in vitro biophysical assay; in vitro enzyme assay; Vero CCL-81 cells; SARS-CoV-2 strain USA-WA/2020; (VSV) SARS-CoV-2 pseudovirus
Inhibited SARS-CoV-2 RNA-dependent RNA polymerase (more potently than baicalin) and displayed antiviral activity in vitro (EC50 of 4.5 µM).