Complex formation between primycin and ergosterol: Entropy-driven initiation of modification of the fungal plasma membrane structure

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Abstract

The interaction of the antibiotic primycin with the main fungal sterol, ergosterol, was investigated in vitro in order to monitor the effect of primycin on the fungal plasma membrane at the molecular level. The thermodynamic parameters of complex formation were determined by measuring Rayleigh scattering as a signal sensitive to particle size. The Benesi-Hildebrand method validated the 1: 1 stoichiometry of the primycin-ergosterol complexes. A very low enthalpy change (ΔH=1.14 kJ mol-1) was measured during the complex formation, which itself cannot be responsible for the molecular association. However, the entropy production (ΔS=29.78 J mol K-1) observed during the complex formation can describe the molecular interaction. This effect is probably due to the partial destruction of the solvation shell of the interacting species before the interlinking of the molecules. The results highlight the importance of ergosterol as concerns the mode of effect of primycin in the treatment of fungal infections. As the entropy has a determinant role in the ergosterol-primycin interaction, this interaction exhibits a very high temperature dependence, with the important consequence that the effect exerted by primycin on the cell membranes increases with rising temperature, and the effect is therefore pronounced in fevered bodies.

Original languageEnglish
Pages (from-to)193-196
Number of pages4
JournalJournal of Antibiotics
Volume65
Issue number4
DOIs
Publication statusPublished - Apr 2012

Fingerprint

Ergosterol
Entropy
Cell Membrane
Temperature
Mycoses
Sterols
Thermodynamics
Particle Size
primycin
Anti-Bacterial Agents

Keywords

  • antibiotic
  • ergosterol
  • interaction
  • membrane
  • primycin

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

Cite this

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title = "Complex formation between primycin and ergosterol: Entropy-driven initiation of modification of the fungal plasma membrane structure",
abstract = "The interaction of the antibiotic primycin with the main fungal sterol, ergosterol, was investigated in vitro in order to monitor the effect of primycin on the fungal plasma membrane at the molecular level. The thermodynamic parameters of complex formation were determined by measuring Rayleigh scattering as a signal sensitive to particle size. The Benesi-Hildebrand method validated the 1: 1 stoichiometry of the primycin-ergosterol complexes. A very low enthalpy change (ΔH=1.14 kJ mol-1) was measured during the complex formation, which itself cannot be responsible for the molecular association. However, the entropy production (ΔS=29.78 J mol K-1) observed during the complex formation can describe the molecular interaction. This effect is probably due to the partial destruction of the solvation shell of the interacting species before the interlinking of the molecules. The results highlight the importance of ergosterol as concerns the mode of effect of primycin in the treatment of fungal infections. As the entropy has a determinant role in the ergosterol-primycin interaction, this interaction exhibits a very high temperature dependence, with the important consequence that the effect exerted by primycin on the cell membranes increases with rising temperature, and the effect is therefore pronounced in fevered bodies.",
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