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The interactions of amphotericin B with various sterols in relation to its possible use in anticancer therapy

C Charbonneau1, I Fournier, S Dufresne

  • 1Département de Chimie-Biologie, Université du Québec à Trois-Rivières, B.P. 500, Trois-Rivières, Québec, Canada G9A 5H7.

Biophysical Chemistry
|June 29, 2001
PubMed

Insights

Amphotericin B (AmB) selectively binds to 7-dehydrocholesterol (7-DHC), a cholesterol precursor linked to cancer therapy, with higher affinity than to ergosterol. This interaction with 7-DHC and cholesterol oxidation products is crucial for AmB administration.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Mycology

Background:

  • Amphotericin B (AmB) is a vital antifungal agent targeting fungal ergosterol but causing host toxicity via cholesterol interaction.
  • AmB may also interact with cholesterol precursors like lanosterol and 7-dehydrocholesterol (7-DHC), and cholesterol oxidation products.

Purpose of the Study:

  • To investigate the solution-phase interactions between Amphotericin B and various sterols, including cholesterol precursors and oxidation products.
  • To elucidate the binding affinities and selectivity of AmB towards these sterols based on structural differences.

Main Methods:

  • UV-Vis spectroscopy was employed to monitor interactions in solution.
  • Differential scanning calorimetry was utilized to assess the thermodynamic properties of AmB-sterol interactions.

Main Results:

  • Amphotericin B demonstrated selective interaction with 7-dehydrocholesterol (7-DHC).
  • The binding affinity of AmB for 7-DHC was found to be greater than its affinity for ergosterol.
  • Selective interaction was also observed between AmB and 7-ketocholesterol, a major cholesterol oxidation product.

Conclusions:

  • AmB exhibits preferential binding to 7-DHC, a sterol implicated in hepatocellular carcinoma therapeutic strategies.
  • The high affinity of AmB for 7-DHC and its interaction with cholesterol oxidation products necessitate careful consideration during antifungal therapy.

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