Evaluation of molecular mechanisms of riboflavin anti-COVID-19 action reveals anti-inflammatory efficacy rather than antiviral activity.
Biochim Biophys Acta Gen Subj
; 1868(5): 130582, 2024 May.
Article
em En
| MEDLINE
| ID: mdl-38340879
ABSTRACT
BACKGROUND:
Riboflavin (vitamin B2) is one of the most important water-soluble vitamins and a coenzyme involved in many biochemical processes. It has previously been shown that adjuvant therapy with flavin mononucleotide (a water-soluble form of riboflavin) correlates with normalization of clinically relevant immune markers in patients with COVID-19, but the mechanism of this effect remains unclear. Here, the antiviral and anti-inflammatory effects of riboflavin were investigated to elucidate the molecular mechanisms underlying the riboflavin-induced effects.METHODS:
Riboflavin was evaluated for recombinant SARS-CoV-2 PLpro inhibition in an enzyme kinetic assay and for direct inhibition of SARS-CoV-2 replication in Vero E6 cells, as well as for anti-inflammatory activity in polysaccharide-induced inflammation models, including endothelial cells in vitro and acute lung inflammation in vivo.RESULTS:
For the first time, the ability of riboflavin at high concentrations (above 50 µM) to inhibit SARS-CoV-2 PLpro protease in vitro was demonstrated; however, no inhibition of viral replication in Vero E6 cells in vitro was found. At the same time, riboflavin exerted a pronounced anti-inflammatory effect in the polysaccharide-induced inflammation model, both in vitro, preventing polysaccharide-induced cell death, and in vivo, reducing inflammatory markers (IL-1ß, IL-6, and TNF-α) and normalizing lung histology.CONCLUSIONS:
It is concluded that riboflavin reveals anti-inflammatory rather than antiviral activity for SARS-CoV-2 infection. GENERALSIGNIFICANCE:
Riboflavin could be suggested as a promising compound for the therapy of inflammatory diseases of broad origin.Palavras-chave
Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Células Endoteliais
/
COVID-19
Idioma:
En
Ano de publicação:
2024
Tipo de documento:
Article