Lactoferrin Inhibition of the Complex Formation between ACE2 Receptor and SARS CoV-2 Recognition Binding Domain

Int J Mol Sci. 2022 May 13;23(10):5436. doi: 10.3390/ijms23105436.

Abstract

The present investigation focuses on the analysis of the interactions among human lactoferrin (LF), SARS-CoV-2 receptor-binding domain (RBD) and human angiotensin-converting enzyme 2 (ACE2) receptor in order to assess possible mutual interactions that could provide a molecular basis of the reported preventative effect of lactoferrin against CoV-2 infection. In particular, kinetic and thermodynamic parameters for the pairwise interactions among the three proteins were measured via two independent techniques, biolayer interferometry and latex nanoparticle-enhanced turbidimetry. The results obtained clearly indicate that LF is able to bind the ACE2 receptor ectodomain with significantly high affinity, whereas no binding to the RBD was observed up to the maximum "physiological" lactoferrin concentration range. Lactoferrin, above 1 µM concentration, thus appears to directly interfere with RBD-ACE2 binding, bringing about a measurable, up to 300-fold increase of the KD value relative to RBD-ACE2 complex formation.

Keywords: SARS-CoV-2 receptor-binding domain (RBD); angiotensin-converting enzyme 2 (ACE2); biolayer interferometry; kinetic analysis; lactoferrin; nanoparticle enhanced turbidimetry.

MeSH terms

  • Angiotensin-Converting Enzyme 2* / antagonists & inhibitors
  • Angiotensin-Converting Enzyme 2* / metabolism
  • COVID-19* / metabolism
  • COVID-19* / virology
  • Humans
  • Lactoferrin* / metabolism
  • Peptidyl-Dipeptidase A / metabolism
  • Protein Interaction Domains and Motifs
  • SARS-CoV-2* / metabolism
  • Spike Glycoprotein, Coronavirus / metabolism

Substances

  • Spike Glycoprotein, Coronavirus
  • spike protein, SARS-CoV-2
  • Peptidyl-Dipeptidase A
  • ACE2 protein, human
  • Angiotensin-Converting Enzyme 2
  • Lactoferrin

Grants and funding

The research leading to these results was also supported by a European Research Council Synergy grant ASTRA (n. 855923).