Concentration dependent different action of tamoxifen on membrane fluidity.
Tamoxifen (TAM) is a non-steroidal antiestrogen drug, which is widely used to prevent and treat breast, liver, pancreas and brain cancers. The present work investigates, in detail, the concentration dependent behavior of TAM (varying from 1 mol% to 45 mol%) on membrane fluidity. The differential scanning calorimetry (DSC) studies showed that tamoxifen eliminates the pre-transition and decreases the main phase transition to lower temperatures. Using visible spectroscopy at 440 nm and Fourier transform infrared (FTIR) spectroscopy it was found that membrane dynamics decreases for 1 and 3 mol% tamoxifen in both the gel and liquid crystalline phases. Above these concentrations up to 18-24 mol%, it increases and reaches its maximum values. As tamoxifen concentration was further increased, the membrane dynamics is found to be gradually decreased, although TAM still has fluidifying effect in comparison to pure phospholipid membrane. These findings are important for the effective use of tamoxifen in the cancer therapy to eliminate its dose dependent side effects reported in the literature.
Kazanci
Nadide
N
Department of Physics, Faculty of Science, Ege University, Izmir, Turkey.
Severcan
Feride
F
D015060:1,2-Dipalmitoylphosphatidylcholine / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D004305:Dose-Response Relationship, Drug; D004965:Estrogen Antagonists / Q000494:pharmacology* / Q000627:therapeutic use; D005260:Female; D006801:Humans; D008081:Liposomes / Q000737:chemistry*; D008560:Membrane Fluidity / Q000187:drug effects*; D009369:Neoplasms / Q000188:drug therapy; D017550:Spectroscopy, Fourier Transform Infrared; D013629:Tamoxifen / Q000494:pharmacology* / Q000627:therapeutic use; D013696:Temperature
D004965:Estrogen Antagonists; D008081:Liposomes; D013629:Tamoxifen; D015060:1,2-Dipalmitoylphosphatidylcholine