scholarly journals The interaction of new oxicam derivatives with lipid bilayers as measured by calorimetry and fluorescence spectroscopy

2018 ◽  
Vol 65 (2) ◽  
pp. 185-191 ◽  
Author(s):  
Jadwiga Maniewska ◽  
Justyna Gąsiorowska ◽  
Berenika Marta Szczęśniak-Sięga ◽  
Krystyna Michalak

The purpose of the present work was to assess the ability of five new oxicam analogues to interact with the lipid bilayers. To characterize the interaction of newly synthesized NSAIDs (non-steroidal anti-inflammatory drugs) analogues with DPPC lipid bilayers the two following techniques were applied – differential scanning calorimetry (DSC) and fluorescence spectroscopy. The results obtained by these experimental approaches show that new oxicams analogues interact with the lipid model membranes under consideration. As demonstrated both in calorimetric and spectroscopic studies, the greatest influence on the thermotropic properties of the lipid membrane and on the quenching of fluorescence of Laurdan and Prodan was exerted by a derivative named PR47 containing in its structure a two–carbon aliphatic linker with a carbonyl group, as well as bromine and trifluoromethyl substituents.

2011 ◽  
Vol 34 (1) ◽  
pp. 45-51 ◽  
Author(s):  
Justyna Gąsiorowska ◽  
Olga Wesołowska ◽  
Krystyna Michalak

Interaction of plant alkaloid, berberine, with zwitterionic and negatively charged phospholipid bilayers Berberine exhibits many pharmacological activities e.g. antibacterial, anti-inflammatory, antiproliferative and apoptosis-inducing. Interaction of berberine with model membranes was studied for the first time using differential scanning calorimetry, fluorescence spectroscopy and turbidity measurements. Influence of berberine on thermotropic properties of bilayers formed from zwitterionic DMPC was insignificant, whereas in bilayers formed from negatively charged DMPG berberine reduced the temperature and cooperativity of main phospholipid phase transition. In higher concentrations berberine induced complex double-peak transition, with the new peak appearing in temperature higher than the original one. It suggested the interaction of the alkaloid with lipid headgroup region of the bilayer. Additionally, berberine quenched fluorescence of Prodan to a higher extent than Laurdan that pointed to stronger interaction with membrane segments close to its surface. Berberine-induced fluorescence quenching of both probes was more pronounced in DPPG than in DPPC bilayers. It was concluded that electrostatic interactions governed berberine association with model membrane.


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