Lipid–Drug Interaction and Colligative Properties in Phospholipid Vesicles

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

“…Morin (30) was a very effective modulator that increased daunomycin (78) and vinblastine accumulation which achieved the level of 500% of the control. Morin (30) and other flavonoids influenced te cellular content of GSH; however, only morin (30) increased GSH concentration, and instead other flavonoids decreased cellular GSH.…”

“…Flavonoids were found to effectively protect erythrocytes against free radical-induced lysis. When the flavonoids were used at 0.25 mM concentration, quercetin (29) turned out to be the most potent protective agent, followed by myricetin (31), morin (30), kaempferol (28), and apigenin (23). Quercetin was also an active antihemolytic agent at a concentration two times lower.…”

“…Nguyen et al [226] have studied the influence of 22 flavonoids on the transport of daunomycin (78) and vinblastine in Panc-1 cells, which are a human pancreatic adenocarcinoma cell line expressing MRP1. Biochanin A (43), genistein (42), quercetin (29), chalcone (65), silymarin, phloretin (66), morin (30), and kaempferol (28) at 100 µM concentrations all significantly increased the accumulation of both daunomycin (78) and vinblastine in these cells. Morin (30) was a very effective modulator that increased daunomycin (78) and vinblastine accumulation which achieved the level of 500% of the control.…”

“…The authors claimed that at intermediate CPZ (9) concentrations (above 2 × 10 -6 M), next to drug partitioning into the lipid bilayer some type of electrostatic interaction of CPZ (9) with anionic groups of membrane components also took place. On the other hand, Banerjee et al [30], based on calorimetric experiments, suggested that binding of CPZ (9) and imipramine with dipalmitoylphosphatidylcholine (DPPC) liposomes could not be ruled solely by electrostatic interactions. It was proposed that nonspecific "dilution" of drugs into a hydrophobic lipid phase was crucial for their interaction with membranes ("simple partition" model).…”

“…Kitagawa et al [215] have studied the effects of flavonoids naringenin (33) (flavanone), baicalein (26) (flavone), kaempferol (28), quercetin (29), myricetin (31), morin (30), and fisetin (32) (flavonols), as well as two glycosides of quercetin (29), on P-gp function in multidrug-resistant P-gp overexpressing KB-C2 cells. Kaempferol and quercetin (29) increased the accumulation of Rh123 in resistant cells.…”