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.
Highlights
Physical Chemistry and Applied Spectroscopy, Chemistry Division, Los Alamos National Laboratory, Abstract: Macrolides are a diverse class of hydrophobic compounds characterized by a macrocyclic lactone ring and distinguished by variable side chains/groups
Bryostatin-1 can have an adverse effect in the treatment of HIV, since it stimulates the expression of several silent genes in unrelated cells, including the expression of inflammatory factors, but this can be controlled by pairing it with other latent reversal agents to mediate side effects [107]
Macrolides, well known for their cytotoxic activity, display a variety of beneficial bioactivities that are important to human health
Summary
The study of macrolides over the past few decades has revealed a varied group of molecules with a range of structures and functions. Many macrolides have been discovered that display pharmaceutical properties, giving them potential as antibiotic, antiviral, antiparasitic, antimycotic, or immunosuppressant drugs [2,3]. While naturally produced macrolides may have limited use as drugs due to their instability in stomach acid, poor pharmacokinetics, and adverse side effects, synthetic macrolide derivatives have been developed to overcome these issues [1]. One of the largest classes of macrolides is toxins, many of which are produced from marine sources [4]. The focus of this review was to compare and contrast five major functional classes of macrolides from a variety of natural sources: toxins, antibiotics, antivirals/antiparasitics, antifungals, and immunosuppressants.
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