Abstract

The review highlights the main results of two decades of research on climacostol (5-[(2Z)-non-2-en-1-yl]benzene-1,3-diol), the resorcinolic lipid produced and used by the ciliated protozoan Climacostomum virens for chemical defense against a wide range of predators, and to assist its carnivorous feeding. After the first studies on the physiological function of climacostol, the compound and some analogues were chemically synthesized, thus allowing us to explore both its effect on different prokaryotic and eukaryotic biological systems, and the role of its relevant structural traits. In particular, the results obtained in the last 10 years indicate climacostol is an effective antimicrobial and anticancer agent, bringing new clues to the attempt to design and synthesize additional novel analogues that can increase or optimize its pharmacological properties.

Highlights

  • Aquatic organisms live in environments which are exceptionally full of competitive biodiversity and for this reason have evolved a great number of adaptive strategies to survive and reproduce, which in eukaryotic unicellular microbes appear well represented

  • The results showed an appreciable and comparable antimicrobial activity of the three compounds, which were effective against Gram-positive bacteria and C. albicans with Minimum Inhibitory Concentrations (MIC) and Minimum Bactericidal Concentration (MBC) ranging from 8 to 32 mg L−1

  • Drosophila flies fed directly with acidic nutrients containing increasing concentrations of MOMO showed a significant reduction in oviposition and survival of larvae, which exhibited apoptotic

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Summary

Introduction

Aquatic organisms live in environments which are exceptionally full of competitive biodiversity and for this reason have evolved a great number of adaptive strategies to survive and reproduce, which in eukaryotic unicellular microbes (protists) appear well represented. At the molecular level, ciliated protists show adaptive strategies based on at least two classes of compounds, pheromones and secondary metabolites. Secondary metabolites produced by ciliates include toxic substances either stored in the cell cytoplasm or inside ejectable organelles (known as extrusomes) that are anchored to the cell cortex before being used in predator-prey and cell-environment interactions [2,3]. These secondary metabolites are synthesized through different biogenetic routes and have been named from the taxonomic names of their source organisms. OOrigriignianlal mmicircoropphhotootgorgarpahphof Co. vfirenCs. byvYi.reTnsus kiib(yProtYis.t InTfosrumkaiition(PSreorvtiesrt, htItpn:f/o/prmroatitsito.in.hosSeei.ravce. r, htjtpp/:P//rpotriosti_smt.ie.nhuoEse.hi.tamc.lj)p. /Protist_menuE.html)

Climacostol Mediates Predator–Prey Interactions
Climacostol Reduces Tumor Progression via p53-Dependent Apoptosis
Climacostol Induces Dysfunctional Autophagy in Tumor Cells
The Synthetic Analogues of Climacostol for Biotechnological Applications
Antitumour Activity
Antimicrobial Activity
Findings
Conclusions
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