Bioactive Metabolites of Marine Origin Have Unusual Effects on Model Membrane Systems.

Marine sponges and soft corals have yielded novel compounds with antineoplastic and antimicrobial activities. Their mechanisms of action are poorly understood, and in most cases, little relevant experimental evidence is available on this topic. In the present study, we investigated whether agelasine D (compound 1) and three agelasine analogs (compound 2-4) as well as malonganenone J (compound 5), affect the physical properties of a simple lipid model system, consisting of dioleoylphospahtidylcholine and dioleoylphosphatidylethanolamine. The data indicated that all the tested compounds increased stored curvature elastic stress, and therefore, tend to deform the bilayer which occurs without a reduction in the packing stress of the hexagonal phase. Furthermore, lower concentrations (1%) appear to have a more pronounced effect than higher ones (5-10%). For compounds 4 and 5, this effect is also reflected in phospholipid headgroup mobility assessed using 31P chemical shift anisotropy (CSA) values of the lamellar phases. Among the compounds tested, compound 4 stands out with respect to its effects on the membrane model systems, which matches its efficacy against a broad spectrum of pathogens. Future work that aims to increase the pharmacological usefulness of these compounds could benefit from taking into account the compound effects on the fluid lamellar phase at low concentrations.

Staphylococcus epidermidis biofilm on implant material is reduced by a covalently linked thiophenone.

AIMS: The present aims were firstly to coat metal implant material with a quorum sensing inhibitory thiophenone molecule, and secondly to assess the inhibitory effect on Staphylococcus epidermidis biofilm accumulation on thiophenone-coated coupons. METHOD AND RESULTS: Thiophenone- and control-coated metal coupons were prepared by silane hydrolysis and dip coating. The linking of thiophenone to the surface was confirmed by X-ray photoelectron spectroscopy analyses. Biofilm by Staph. epidermidis, a frequent cause of implant-associated infections, was allowed to form under flowing conditions for 48 h. The biofilm accumulations were significantly reduced on the thiophenone-coated coupons. This was confirmed by confocal scanning microscopy. CONCLUSION: This study showed for the first time how a synthetic thiophenone may be covalently linked to a stainless steel surface, and that biofilm accumulations on such surfaces are significantly reduced. SIGNIFICANCE AND IMPACT OF THE STUDY: Functionalizing surfaces by covalent linking of thiophenones might open a wide array of applications. Thiophenone coating of medical implants represents a novel and promising approach to prevent implant-associated infections.