Tetra-p-guanidinoethylcalix[4]arene trifluoroacetate salt (CX1) was synthesized recently as an antibacterial agent. It showed to be active in vitro against various Gram-positive and Gram-negative bacteria. To get more insight the mechanism of biological activity this derivative, it studied upon interactions with model lipid membranes. Langmuir monolayers were formed zwitterionic 1,2-dimyristoyl-sn-glycero-3-phosphocholine or 1,2-dimyristoyl-sn-glycero-3-phosphoethanolamine, anionic...

Literature data indicate that some calixarene derivatives with antimicrobial activities may be useful as drugs; one of the aspects biological activity different classes antibiotics concerns interactions lipid membranes. Here, possibility incorporation and/or translocation three amphiphilic p-tert-butylcalix[4]arene across membranes was studied using monolayers. The used have 6-aminopenicillanic acid or benzylpenicillin moieties grafted in alternate positions at lower rim;...

Meloxicam, piroxicam, and tenoxicam belong to a highly potent oxicam group of nonsteroidal anti-inflammatory drugs. Whereas the structurally similar oxicams have different pharmacokinetics, treatment efficiency, adverse effects, their common mechanism action is inhibition membrane enzyme, cyclooxygenase. Because prerequisite for accessing cyclooxygenase by drugs interaction with membrane, focus current study was comparison how meloxicam, interact lipid monolayers used as models biological...

Meloxicam, a nonsteroidal anti-inflammatory drug (NSAID), is known as selective cyclooxygenase-2 inhibitor. Cyclooxygenase-2 membrane protein, functionally coupled to an interfacial enzyme, phospholipase A2. Consequently, it may be supposed that the interactions of NSAIDs with lipid membranes play role in process. In order investigate mechanism this process, Langmuir films formed 1,2-dipalmitoyl-sn-glycero-3-phosphocholine, 1,2-dilauroyl-sn-glycero-3-phosphocholine,...

Interactions of phenantrene, anthracene, pyrene, chrysene, and benzo[a]pyrene (polyaromatic hydrocarbons) with model phospholipid membranes were probed using the Langmuir technique. The lipid monolayers prepared 1,2-dipalmitoyl-sn-glycero-3-phosphocholine, 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine, 1,2-dipalmitoyl-sn-glycero-3-phosphoglycerol, 1,2-dipalmitoyl-sn-glycero-3-phosphoserine, 1,2-myristoyl-sn-glycero-3-phosphoethanolamine, 1,2-dilauroyl-sn-glycero-3-phosphocholine,...

The two new p-tert-butylcalix[4]arene derivatives described here bear one or nalidixic acid arms linked to the lower calixarene rim via quinolone carboxylate moiety. These were synthesized in order investigate important features of molecules conceived as potential antibiotics, namely, metal cation complexation and interfacial properties, way which they interrelate. properties studied monomolecular films spread on pure water aqueous subphases containing biologically relevant mono- divalent...

Behavior of cationic tetra-p-guanidinoethylcalix[4]arene (CX1) and its building block, p-guanidinoethylphenol (mCX1) in model monolayer lipid membranes was investigated using all atom molecular dynamics simulations surface pressure measurements. Members two classes lipids were taken into account: zwitterionic 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC) anionic 1,2-dimyristoyl-sn-glycero-3-phospho-l-serine sodium salt (DMPS) as models eukaryotic bacterial cell membranes, respectively....

Abstract By reducing the surface tension of air–water interface in alveoli, lung surfactant (LS) is crucial for proper functioning lungs. It also forms first barrier against inhaled pathogens. In this study we inspect interactions LS models with a dangerous air pollutant, benzo[a]pyrene (BaP). Dipalmitoylphosphatidylcholine (DPPC), 1‐palmitoyl‐2‐oleoylphosphatidylcholine, and their 1:1 mixture are used as models. Pressure‐area isotherms employed to macroscopic properties monolayers. We find...

Doxorubicin (DOX) is a commonly used chemotherapeutic drug, from the anthracycline class, which genotoxic to neoplastic cells via DNA intercalation mechanism. It effective and universal; however, it also causes numerous side effects. The most serious of them are cardiotoxicity decrease in number myeloid cells. For this reason, targeted DOX delivery systems desirable, since they would allow lowering drug dose therefore limiting systemic Recently, synthetic dyes, particular Congo red (CR),...

Three nonsteroidal anti-inflammatory oxicam drugs, namely meloxicam, piroxicam, and tenoxicam, were used to modify the properties of monomolecular films formed with 1,2-dilauroyl-sn-glycero-3-phosphocholine, 1,2-dilauroyl-sn-glycero-3-phosphoethanolamine, or 1,2-dilauroyl-sn-glycero-3-phospho-(1-rac-glycerol). These systems examined via surface pressure electrical potential measurements, polarization modulation infrared reflection absorption spectroscopy, Brewster angle microscopy. Moreover,...

Apart from being responsible for sufficient pulmonary compliance and preventing alveolar collapse, lung surfactant (LS) also forms the first barrier uptake of inhaled pathogens. As such it is susceptible to damage caused by various deleterious compounds present in air, e.g. oxidants capable oxidizing unsaturated LS lipids. This study examines consequences 20% lipids an model: a mixed 1 : DPPC POPC monolayer. POxnoPC (1-palmitoyl-2-(9-oxo-nonanoyl)-sn-glycero-3-phosphocholine) considered as...

Two p-tert-butylcalix[4]arene derivatives bearing one or two nalidixic acid groups connected to the lower rim of through propylenic spacer were studied upon interaction with model bacterial membranes. Indeed, these developed recently as new macrocyclic antibiotic carriers for antibacterial therapy. To obtain molecular level information about between calixarene conjugates and a membrane lipid, atomistic dynamics simulation, well surface pressure, potential, polarization modulation infrared...

We introduce and study a multicomponent lipid film mimicking composition of the human lung surfactant. It consists phospholipids with various headgroups tail saturation. Furthermore, it includes cholesterol oxidized lipids. Langmuir trough fluorescence microscopy experiments are combined fully atomistic molecular dynamics simulations. The considered mixtures form complex interfacial films properties modulated by lateral compression. Cholesterol laterally condenses, lipids expand films; both...

There is evidence that serious pathologies are associated with aluminum (Al). In the present work, influence of Al on enzymatic lipolysis was studied aim to get more insight into possible link between Al-induced membrane modification and cytotoxicity trivalent cation (AlIII). Lipid monolayers were used as model membranes. The monomolecular film technique allowed monitoring Al-dependent modifications lipid monolayer properties enzyme kinetics. Two enzymes, namely, Candida rugosa lipase a...

The interaction between five gemini amphiphilic pseudopeptides (GAPs) differing by the length of central spacer and a model membrane lipid, 1,3-bis[1,2-dimyristoyl-sn-glycero-3-phospho]-sn-glycerol (cardiolipin) were studied with aim to evaluate their possible antimicrobial properties. To this end, monomolecular films formed at air/water interface pure cardiolipin or cardiolipin/GAPs mixtures; film properties determined using surface pressure potential measurements, as well...