Biochimica et Biophysica Acta (BBA) - Biomembranes
Regular paperThe active metabolite hydroxytamoxifen of the anticancer drug tamoxifen induces structural changes in membranes
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Anticancer drugs tamoxifen and 4hydroxytamoxifen as effectors of phosphatidylethanolamine lipid polymorphism
2022, Chemistry and Physics of LipidsOptimization of nanoemulsified systems containing lamellar phases for co-delivery of celecoxib and endoxifen to the skin aiming for breast cancer chemoprevention and treatment
2022, Colloids and Surfaces A: Physicochemical and Engineering AspectsCitation Excerpt :The authors also reported increased bilayer thickness and chain order parameters, suggesting that the increased calcein translocation could result from transient defects caused by tamoxifen. Similarly, hydroxytamoxifen, another tamoxifen metabolite, was described to broaden the transition profile of dipalmitoylphosphatidylcholine and to shift its main transition temperature to lower values, among other effects that depended on the fatty acyl chain length [65]. This increase in viscosity might aid topical application.
Dissimilar action of tamoxifen and 4-hydroxytamoxifen on phosphatidylcholine model membranes
2021, Biophysical ChemistryCitation Excerpt :Concerning HTMX, very few works have addressed the study of its interaction with phospholipid membranes. Briefly, it has been reported that HTMX decreases membrane fluidity in ox-brain phospholipid liposomes [12], or presents temperature-dependent ordering or disordering effects [13]. Up to date, high sensitivity calorimetric and X-ray scattering studies on the influence of TMX and HTMX on the thermotropic properties of phospholipid membranes, or its permeability properties, have not been published.
Mitochondria: The gateway for tamoxifen-induced liver injury
2014, ToxicologyThe antiestrogen endoxifen protects rat liver mitochondria from permeability transition pore opening and oxidative stress at concentrations that do not affect the phosphorylation efficiency
2013, Toxicology and Applied PharmacologyCitation Excerpt :TAM is a highly hydrophobic molecule that strongly partitions in biomembranes (Custódio et al., 1991), affecting the dynamic properties of lipids (Custódio et al., 1993b; Kazanci and Severcan, 2007). Similar effects were reported for OHTAM (Custódio et al., 1993a). Although the effects of EDX on biomembranes have not yet been described, it is plausible that due to its structural resemblance with OHTAM, which has an additional N-methyl group, it may also affect membrane dynamics.