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Miltefosine impacts small molecule transport in Gram-positive bacteria

Marea J Blake1, Eleanor F Page1, Madeline E Smith1

  • 1University of Tennessee Knoxville TN USA trcalhoun@utk.edu.

RSC Chemical Biology
|October 4, 2024
PubMed

Insights

Miltefosine (MLT) does not alter bacterial membrane structure in Staphylococcus aureus. However, MLT significantly impacts the transport of certain small molecules across bacterial membranes, suggesting its potential as a drug delivery adjuvant.

Area of Science:

  • Membrane Biophysics
  • Antimicrobial Drug Action
  • Bacterial Physiology

Background:

  • Miltefosine (MLT), an alkylphosphocholine, is recognized for its anticancer and antiparasitic properties.
  • MLT's interaction with eukaryotic lipid rafts is established, with emerging evidence suggesting effects on bacterial membrane microdomains.
  • Conflicting reports exist regarding MLT's influence on bacterial plasma membrane fluidity.

Purpose of the Study:

  • To investigate the impact of MLT on the global ordering and lipid packing of Staphylococcus aureus membranes.
  • To determine how MLT affects the transport of various small molecules across the membranes of Staphylococcus aureus and Bacillus subtilis.

Main Methods:

  • Steady-state fluorescence techniques, including generalized polarization of laurdan and anisotropy of diphenylhexatriene, were used to assess membrane properties.
  • Time-resolved second harmonic scattering was employed to study the transport of small molecules across bacterial membranes.

Main Results:

  • Miltefosine (MLT) was found to have no significant effect on the overall ordering and lipid packing of Staphylococcus aureus membranes.
  • MLT significantly altered the transport of certain small molecules across the membranes of S. aureus and B. subtilis, though not all molecules were affected.

Conclusions:

  • MLT does not disrupt the global membrane structure of S. aureus.
  • MLT's ability to modulate small molecule transport suggests its potential as an adjuvant for enhancing drug delivery in bacteria.

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