Person:
León Martínez, Rafael

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First Name
Rafael
Last Name
León Martínez
URI
https://hdl.handle.net/20.500.14352/77525
Affiliation
Universidad Complutense de Madrid
Faculty / Institute
Farmacia
Department
Química en Ciencias Farmacéuticas
Area
Química Orgánica
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UCM identifierORCIDScopus Author IDWeb of Science ResearcherIDDialnet IDGoogle Scholar ID

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2015 - 20162
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Author: Abril, Sheila ×

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    New melatonin–cinnamate hybrids as multi-target drugs for neurodegenerative diseases: Nrf2-induction, antioxidant effect and neuroprotection
    (Future Medicinal Chemistry, 2015) Buendia, Izaskun; Navarro González De Mesa, Elisa; Michalska Dziama, Patrycja; Gameiro, Isabel; Egea, Javier; Abril, Sheila; López, Alicia; González-Lafuente, Laura; G. López, Manuela; León Martínez, Rafael
    Neurodegenerative diseases share many pathological pathways, such as abnormal protein aggregation, mitochondrial dysfunction, extensive oxidative stress and neuroinflammation. Cells have an intrinsic mechanism of protection, the Nrf2 transcriptional factor, known as the master regulator of redox homeostasis. Results: Based on the common features of these diseases we have designed a multi-target hybrid structure derived from melatonin and ethyl cinnamate. The obtained derivatives were Nrf2 inducers and potent-free radical scavengers. These new compounds showed a very interesting neuroprotective profile in several in vitro models of oxidative stress, Alzheimer's disease and brain ischemia. Conclusion: We have designed a new hybrid structure with complementary activities. We have identified compound 5h as an interesting Nrf2 inducer, very potent antioxidant and neuroprotectant.
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    Inclusion complex of ITH12674 with2-hydroxypropyl-beta-cyclodextrin: Preparation, physical characterization and pharmacological effect
    (Carbohydrate Polymers, 2016) Michalska Dziama, Patrycja; Wojnicz, Aneta; Ruiz-Nuño, Ana; Abril, Sheila; Buendia, Izaskun; León Martínez, Rafael
    ITH12674 is a multitarget drug, designed to exert a dual “drug-prodrug” mechanism of action, able toinduce the phase II antioxidant and anti-inflammatory response for the treatment of brain ischemia.However, its physicochemical properties limit its potential preclinical development due to its low watersolubility and instability towards heat and pH variations. In order to improve its properties, we preparedthe inclusion complex of ITH12674 with 2-hydroxypropyl- -cyclodextrin (HP- -CD) by the freeze-drying method. The formation of the inclusion complex was confirmed by FT-IR spectroscopy, PXRD,DSC,1H NMR and SEM techniques. Experimental results showed that the inclusion complex enhanced itswater solubility and stability against heat, acidic and basic conditions. Furthermore, the inclusion com-plex, prepared in water solution, exerted the same potency to induce the phase II antioxidant response asthe pure ITH12674. Thus the formation of the inclusion complex with HP- -CD is a very effective methodto stabilize and solubilize the active compound for its future preclinical development.