Theonella : A Treasure Trove of Structurally Unique and Biologically Active Sterols

• Published in: Marine drugs Vol. 21; no. 5; p. 291
• Main Authors: Festa, Carmen, De Marino, Simona, Zampella, Angela, Fiorucci, Stefano
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 08-05-2023; MDPI
• Subjects: Acids; Animals; Bile; Biocompatibility; Biological activity; Biomarkers; cytotoxic activity; Cytotoxicity; Homeostasis; Human diseases; Humans; Ligands; Liver cirrhosis; Liver diseases; Marine environment; Marine invertebrates; marine sponge; Metabolism; Metabolites; Natural products; nuclear receptor ligands; Nuclear receptors; Peptides; Phytosterols; Receptors, Cytoplasmic and Nuclear; Review; Secondary metabolites; Steroids; Sterols; Sterols - chemistry; Sterols - pharmacology; Terpenes; Theonella; Toxicity; secondary metabolites; Theonella; marine sponge; cytotoxic activity; sterols; structure–activity relationship (SAR); nuclear receptor ligands
• ISSN: 1660-3397; 1660-3397
• DOI: 10.3390/md21050291

The marine environment is considered a vast source in the discovery of structurally unique bioactive secondary metabolites. Among marine invertebrates, the sponge
spp. represents an arsenal of novel compounds ranging from peptides, alkaloids, terpenes, macrolides, and sterols. In this review, we summarize the recent reports on sterols isolated from this amazing sponge, describing their structural features and peculiar biological activities. We also discuss the total syntheses of solomonsterols A and B and the medicinal chemistry modifications on theonellasterol and conicasterol, focusing on the effect of chemical transformations on the biological activity of this class of metabolites. The promising compounds identified from
spp. possess pronounced biological activity on nuclear receptors or cytotoxicity and result in promising candidates for extended preclinical evaluations. The identification of naturally occurring and semisynthetic marine bioactive sterols reaffirms the utility of examining natural product libraries for the discovery of new therapeutical approach to human diseases.