Please use this identifier to cite or link to this item: http://hdl.handle.net/2445/59237
Title: Shogaol-huprine hybrids: Dual antioxidant and anticholinesterase agents with beta-amyloid and tau anti-aggregating properties
Author: Pérez-Areales, F. Javier
Di Pietro, O.
Espargaró Colomé, Alba
Vallverdú i Queralt, Anna
Galdeano Cantador, Carlos
Ragusa, Ilaria M.
Viayna, Elisabet
Guillou, C.
Clos Guillén, M. Victòria
Pérez Fernández, Belén
Sabaté Lagunas, Raimon
Lamuela Raventós, Rosa Ma.
Luque Garriga, F. Xavier
Muñoz-Torrero López-Ibarra, Diego
Keywords: Disseny de medicaments
Malaltia d'Alzheimer
Antioxidants
Inhibidors enzimàtics
Pèptids
Drug design
Alzheimer's disease
Antioxidants
Enzyme inhibitors
Peptides
Issue Date: 1-Oct-2014
Publisher: Elsevier Ltd
Abstract: Multitarget compounds are increasingly being pursued for the effective treatment of complex diseases. Herein, we describe the design and synthesis of a novel class of shogaol<br>huprine hybrids, purported to hit several key targets involved in Alzheimer"s disease. The hybrids have been tested in vitro for their inhibitory activity against human acetylcholinesterase and butyrylcholinesterase and antioxidant activity (ABTS.+, DPPH and Folin-Ciocalteu assays), and in intact Escherichia coli cells for their Aβ42 and tau anti-aggregating activity. Also, their brain penetration has been assessed (PAMPA-BBB assay). Even though the hybrids are not as potent AChE inhibitors or antioxidant agents as the parent huprine Y and [4]-shogaol, respectively, they still exhibit very potent anticholinesterase and antioxidant activities and are much more potent Aβ42 and tau anti-aggregating agents than the parent compounds. Overall, the shogaol<br>huprine hybrids emerge as interesting brain permeable multitarget anti-Alzheimer leads.
Note: Versió postprint del document publicat a: http://dx.doi.org/10.1016/j.bmc.2014.07.053
It is part of: Bioorganic & Medicinal Chemistry, 2014, vol. 22, num. 19, p. 5298-5307
Related resource: http://dx.doi.org/10.1016/j.bmc.2014.07.053
URI: http://hdl.handle.net/2445/59237
ISSN: 0968-0896
Appears in Collections:Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)
Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica)
Articles publicats en revistes (Institut de Nanociència i Nanotecnologia (IN2UB))
Articles publicats en revistes (Institut de Biomedicina (IBUB))

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