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Opto-Chemical and laser properties of a novel fluorescent antiestrogen derivative and its potential applications in breast cancer photodynamic chemotherapy

AuthorsDíaz, Mario; Scholz, Laura E.; Boto, Alicia ; Marín, Raquel; Puertas-Avedaño, Ricardo; Lobo, Fernando ; Hernández, Dácil ; Quinto-Alemany, David; Lahoz Zamarro, Fernando
Issue Date13-Nov-2017
CitationSHIFT 2017-Spectral Shaping for Biomedical and Energy Applications (2017)
AbstractTamoxifen is the most common antiestrogen used in the chronic treatment of breast cancer. In these cells, it mainly binds to intracellular receptors (estrogen receptor alpha, ER) and antagonizes the binding of its cognate ligand, 17ß-estradiol, thereby preventing uncontrolled hormonedependent cellular proliferation and growth. In the last decade, in our laboratories we have developed and characterized different tamoxifen derivatives, including a novel fluorescent tamoxifen conjugate: FLTX1. FLTX1 is formed by the covalent binding of tamoxifen to a common fluorescent biomarker NBD. This new prodrug was originally designed as a fluorescent biomarker to localize intracellular targets, which not only keeps the pharmacological activity of tamoxifen but also adds a luminescent functionality. Strikingly, the quantum efficiency of FLTX1 is so high that laser emission has been obtained as an emerging property. In this presentation, we will show its laser properties under three different configurations. First, as amplified spontaneous emission or mirrorless laser; second, through the evanescent field of WGMs of a ring resonator around an optical fiber; and finally as random laser in uterine tissues impregnated with the prodrug. In consideration of these properties, we have moved a step forward, under the hypothesis that in combination with a photosensitizer, such Rose Bengal (RB), FLTX1 might be used for photodynamic therapy. Under this paradigm, the new complex would act as a sensitizer in ER - overexpressing cells (which feature the most prevalent form of hormone-dependent breast cancer). Thus, when optically excited, FLTX1 would transfer its energy to RB, which, in turn, would relax producing reactive oxygen species (ROS) that eventually would induce cell death. The advantage of using FLTX1 to activate RB is the selectivity exhibited by FLTX1 to target cells overexpressing ER , i.e. estrogen-dependent breast cancer cells. This approach would reduce the damage of other non-cancer (healthy) cells or surrounding tissues. We show here the results that confirm efficient energy transfer (FRET) between FLTX1 and RB, and demonstrate the subsequent generation of ROS. Moreover, we have designed a new FLTX1-RB complex covalently bound through a short linker and explored its opto-chemical properties. This is an original cancer therapy strategy that combines the pharmacological properties of tamoxifen and its laser dye features with a highly selective photodynamic therapy.
DescriptionTrabajo presentado en SHIFT 2017-Spectral Shaping for Biomedical and Energy Applications, celebrado en Tenerife (España) del 13 al 17 de noviembre de 2017.
Appears in Collections:(IPNA) Comunicaciones congresos
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