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Relationship between the structure of synthetic organic molecules, their behavior in the phospholipid membrane and their effect on bacteria
Brzobohatá, Hana ; Fišer, Radovan (advisor) ; Mašín, Jiří (referee)
Lipophoshopnoxins (LPPOs) are organic compounds with antimicrobial activity, which take place on the baterial membrane by forming pores. LPPOs are promising bactericidal molecules with low MIC (minimal inhibition concentration) and high HC50 (hemolytic concentration) values. Structurally, LPPOs belong to the so-called synthetic antimicrobial peptidomimetics, which do not contain any peptidic bonds, but imitate the structure and function of membrane active oligopeptides (e.g. by copying the distribution of the surface charge of the molecule). The aim of this study was to describe the antimicrobial properties of the molecules DR 7072, DR 34P1, DR 362 and DR 236, which represent LEGO-LPPOs as a new generation of this antimicrobials. The selected molecules differ in the length of linker module, in the structure of hydrophobic module or both. All tested molecules have comparable antimicrobial activity with MIC between 2 and 16 μg/ml and have the ability to permeabilize bacterial membrane of both Gram negatives (G- ; Pseudomonas aeruginosa CCM 3955) and Gram positives (G+ ; Staphylococcus aureus CCM 4223). LEGO-LPPO have different mechanism of action on S. aureus and P. aeruginosa. The molecules show different mechanism of action against the mentioned bacteria. The bactericidal effect on G+ is faster and...
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Insights into the mechanism of action of bactericidal lipophosphonoxins
Panova, Natalya ; Zborníková, Eva ; Šimák, Ondřej ; Krásný, Libor ; Kolář, M. ; Látal, T. ; Seydlová, G. ; Rejman, Dominik
The advantages offered by antibiotics in the treatment of infectious diseases are endangered due to the increase in the number of antibiotic-resistant bacterial strains. This reduces the efficiency of antibiotic treatments and poses a serious health and economical problem. Currently, the need for novel antibiotics is becoming increasingly apparent. Recently, we discovered a series of compounds termed lipophosphonoxins exhibiting selective cytotoxicity towards gram-positive bacterial cells. The attempt to elucidate the mode of action of lipophosphonoxins is presented here.
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