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Polyene macrolide antibiotics and their applications in human therapy

Sergey B Zotchev1

  • 1Department of Biotechnology, Norwegian University of Science and Technology, N-7491 Trondheim, Norway. sergey.zotchev@chembio.ntnu.no

Current Medicinal Chemistry
|February 7, 2003
PubMed

Insights

Polyene macrolides are effective antifungal agents but can be toxic. This review discusses their properties, toxicity, and potential new uses in treating serious diseases.

Area of Science:

  • Mycology
  • Pharmacology
  • Infectious Diseases

Background:

  • Fungal infections pose a significant threat to immunocompromised individuals, including those with HIV/AIDS, undergoing cancer therapy, or organ transplantation.
  • Pathogenic fungi exhibit rapid proliferation and resistance to conventional antimicrobial drugs, necessitating effective antifungal treatments.
  • Polyene macrolide antibiotics are potent, broad-spectrum antifungal agents with low resistance rates, making them crucial in clinical settings.

Purpose of the Study:

  • To review current knowledge on polyene macrolide biosynthesis, mechanism of action, and structure-function relationships.
  • To discuss strategies for mitigating the toxicity associated with polyene macrolide therapy.
  • To highlight emerging therapeutic applications of polyene macrolides beyond fungal infections.

Main Methods:

  • Literature review of scientific publications on polyene macrolides.
  • Analysis of data on biosynthesis pathways and mechanisms of action.
  • Evaluation of structure-function relationships and toxicity profiles.
  • Exploration of novel therapeutic applications.

Main Results:

  • Polyene macrolides exhibit potent fungicidal activity and broad-spectrum efficacy.
  • Significant toxicity, including nephrotoxicity and thrombophlebitis, limits their clinical use.
  • Ongoing research focuses on developing less toxic derivatives and novel delivery systems.
  • Potential applications in prion diseases, HIV infection, and cancer are being investigated.

Conclusions:

  • Polyene macrolides remain vital antifungal agents, but their toxicity necessitates careful management and further research.
  • Understanding biosynthesis and structure-function relationships is key to improving their therapeutic index.
  • Emerging applications suggest a broader role for polyene macrolides in treating complex diseases.

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