Macrolides: From Toxins to Therapeutics

Toxins (Basel). 2021 May 12;13(5):347. doi: 10.3390/toxins13050347.

Abstract

Macrolides are a diverse class of hydrophobic compounds characterized by a macrocyclic lactone ring and distinguished by variable side chains/groups. Some of the most well characterized macrolides are toxins produced by marine bacteria, sea sponges, and other species. Many marine macrolide toxins act as biomimetic molecules to natural actin-binding proteins, affecting actin polymerization, while other toxins act on different cytoskeletal components. The disruption of natural cytoskeletal processes affects cell motility and cytokinesis, and can result in cellular death. While many macrolides are toxic in nature, others have been shown to display therapeutic properties. Indeed, some of the most well known antibiotic compounds, including erythromycin, are macrolides. In addition to antibiotic properties, macrolides have been shown to display antiviral, antiparasitic, antifungal, and immunosuppressive actions. Here, we review each functional class of macrolides for their common structures, mechanisms of action, pharmacology, and human cellular targets.

Keywords: antibiotic; antifungal; antiparasitic; antiviral; immunosuppressant; macrolide; toxin.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Anti-Bacterial Agents / isolation & purification
  • Anti-Bacterial Agents / pharmacology*
  • Anti-Bacterial Agents / toxicity
  • Cytoskeleton / drug effects
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Macrolides / isolation & purification
  • Macrolides / pharmacology*
  • Macrolides / toxicity
  • Marine Toxins / isolation & purification
  • Marine Toxins / pharmacology*
  • Marine Toxins / toxicity

Substances

  • Anti-Bacterial Agents
  • Macrolides
  • Marine Toxins