Chlorpromazine associates with phosphatidylserines to cause an increase in the lipid's own interfacial molecular area — role of the fatty acyl composition

Interactions of bioactive molecules & nanomaterials with Langmuir monolayers as cell membrane models

“…The compression isotherms of DPPC/PS/drug monolayers revealed film expansion with increasing gel-fluid domain boundary length as confirmed by fluorescence microscopy [228]. The increase in mean molecular area was observed by many research groups investigating chlorpromazine -the most frequently studied cationic phenothiazine derivative [231][232][233]. The effect observed in penetration experiments was interpreted as being due to incorporation and interaction with acyl chains of phospholipids, being stronger for saturated vs.…”

“…Typical examples include: antimicrobials [117,, anti-tumorals [116,, antiinflammatory [77,[214][215][216][217], anesthesics [218][219][220][221][222][223][224][225][226][227], anti-psychotics [228][229][230][231][232][233][234][235][236][237], cardiac [238][239][240][241][242][243][244][245] and antihistaminic [246] drugs. To address this issue, Langmuir monolayers have been used involving AmB alone as well as mixed with membrane sterols.…”

Drug–Membrane Interactions: Molecular Mechanisms Underlying Therapeutic and Toxic Effects of Drugs

“…In fact, the use of monolayers of phospholipids as a membrane model has regained interest recently, since it is half of a lipid bilayer and thus constitutes a very convenient first step to approach the two-dimensional structure of biomembranes [110][111][112][113][114][115][116][117]. Phospholipidic monolayers dispersed on the top of an aqueous subphase provide a highly informative approach for studying drug-lipid interactions at the air-water interface, as there is no curvature effect (unlike vesicles) and the lateral packing can be precisely controlled [111,113,118].…”

The Role of the Membrane Actions of Phenothiazines and Flavonoids as Functional Modulators

“…However, the comparison of the effect of CPZ (9) with that exerted by simple monovalent cations makes the authors conclude that CPZ (9) interacted with lipid acyl chains. This hypothesis was corroborated by further studies in which monolayers composed of saturated or unsaturated PS species were used [43]. It was demonstrated that the work of insertion of CPZ (9) between lipid molecules was the smallest, when the most unsaturated PS species was used to form the monolayer.…”

“…The effect of daidzein (40) and formononetin (41) was quite weak and not concentrationdependent. On the other hand, clear concentration dependence was visible in the case of genistein (42) and biochanin A (43). Both compounds caused a slight increase of T m at an isoflavone : lipid molar ratio of 0.2 accompanied by a strong decrease at higher concentrations.…”