Synthesis and Evaluation of Glucosyl-, Acyl- and Silyl- Resveratrol Derivatives as Retinoprotective Agents: Piceid Octanoate Notably Delays Photoreceptor Degeneration in a Retinitis Pigmentosa Mouse Model

Background: Retinitis pigmentosa (RP), the leading cause of inherited blindness in adults, is marked by the progressive degeneration of rod photoreceptors in the retina. While gene therapy has shown promise in treating RP in patients with specific mutations, no effective therapies currently exist fo...

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Main Authors: Lourdes Valdés-Sánchez, Seyed Mohamadmehdi Moshtaghion, Estefanía Caballano-Infantes, Pablo Peñalver, Rosario Rodríguez-Ruiz, José Luis González-Alfonso, Francisco José Plou, Tom Desmet, Juan C. Morales, Francisco J. Díaz-Corrales
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Language:English
Published: MDPI AG 2024-11-01
Series:Pharmaceuticals
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Online Access:https://www.mdpi.com/1424-8247/17/11/1482
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author Lourdes Valdés-Sánchez
Seyed Mohamadmehdi Moshtaghion
Estefanía Caballano-Infantes
Pablo Peñalver
Rosario Rodríguez-Ruiz
José Luis González-Alfonso
Francisco José Plou
Tom Desmet
Juan C. Morales
Francisco J. Díaz-Corrales
author_facet Lourdes Valdés-Sánchez
Seyed Mohamadmehdi Moshtaghion
Estefanía Caballano-Infantes
Pablo Peñalver
Rosario Rodríguez-Ruiz
José Luis González-Alfonso
Francisco José Plou
Tom Desmet
Juan C. Morales
Francisco J. Díaz-Corrales
author_sort Lourdes Valdés-Sánchez
collection DOAJ
description Background: Retinitis pigmentosa (RP), the leading cause of inherited blindness in adults, is marked by the progressive degeneration of rod photoreceptors in the retina. While gene therapy has shown promise in treating RP in patients with specific mutations, no effective therapies currently exist for the majority of patients with diverse genetic backgrounds. Additionally, no intervention can yet prevent or delay photoreceptor loss across the broader RP patient population. Resveratrol (RES), a naturally occurring polyphenol, has shown cytoprotective effects in various neurodegenerative disease models; however, its therapeutic potential is limited by low bioavailability. Methods: In this study, we synthesized novel RES derivatives and assessed their retinoprotective effects in a murine model of RP (rd10 mice). Results: Among these derivatives, piceid octanoate (PIC-OCT) significantly delayed photoreceptor degeneration in the RP model, demonstrating superior efficacy compared to RES. Conclusions: PIC-OCT shows strong potential as a leading candidate for developing new therapeutic strategies for RP.
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series Pharmaceuticals
spelling doaj-art-744cea92009a499382e7a071cf005c6d2024-11-26T18:17:20ZengMDPI AGPharmaceuticals1424-82472024-11-011711148210.3390/ph17111482Synthesis and Evaluation of Glucosyl-, Acyl- and Silyl- Resveratrol Derivatives as Retinoprotective Agents: Piceid Octanoate Notably Delays Photoreceptor Degeneration in a Retinitis Pigmentosa Mouse ModelLourdes Valdés-Sánchez0Seyed Mohamadmehdi Moshtaghion1Estefanía Caballano-Infantes2Pablo Peñalver3Rosario Rodríguez-Ruiz4José Luis González-Alfonso5Francisco José Plou6Tom Desmet7Juan C. Morales8Francisco J. Díaz-Corrales9Department of Integrative Pathophysiology and Therapies, Andalusian Molecular Biology and Regenerative Medicine Centre (CABIMER), Junta de Andalucía, CSIC, Universidad de Sevilla, Universidad Pablo de Olavide, Avda. Américo Vespucio 24, 41092 Seville, Seville, SpainDepartment of Integrative Pathophysiology and Therapies, Andalusian Molecular Biology and Regenerative Medicine Centre (CABIMER), Junta de Andalucía, CSIC, Universidad de Sevilla, Universidad Pablo de Olavide, Avda. Américo Vespucio 24, 41092 Seville, Seville, SpainDepartment of Integrative Pathophysiology and Therapies, Andalusian Molecular Biology and Regenerative Medicine Centre (CABIMER), Junta de Andalucía, CSIC, Universidad de Sevilla, Universidad Pablo de Olavide, Avda. Américo Vespucio 24, 41092 Seville, Seville, SpainDepartment of Biochemistry and Molecular Pharmacology, Instituto de Parasitología y Biomedicina López Neyra, CSIC, PTS Granada, Avda. del Conocimiento, 17, 18016 Armilla, Granada, SpainDepartment of Biochemistry and Molecular Pharmacology, Instituto de Parasitología y Biomedicina López Neyra, CSIC, PTS Granada, Avda. del Conocimiento, 17, 18016 Armilla, Granada, SpainInstituto de Catálisis y Petroleoquímica, CSIC, Marie Curie 2, 28049 Madrid, Madrid, SpainInstituto de Catálisis y Petroleoquímica, CSIC, Marie Curie 2, 28049 Madrid, Madrid, SpainCentre for Synthetic Biology, Department of Biotechnology, Ghent University, Coupure Links 653, 9000 Ghent, BelgiumDepartment of Biochemistry and Molecular Pharmacology, Instituto de Parasitología y Biomedicina López Neyra, CSIC, PTS Granada, Avda. del Conocimiento, 17, 18016 Armilla, Granada, SpainDepartment of Integrative Pathophysiology and Therapies, Andalusian Molecular Biology and Regenerative Medicine Centre (CABIMER), Junta de Andalucía, CSIC, Universidad de Sevilla, Universidad Pablo de Olavide, Avda. Américo Vespucio 24, 41092 Seville, Seville, SpainBackground: Retinitis pigmentosa (RP), the leading cause of inherited blindness in adults, is marked by the progressive degeneration of rod photoreceptors in the retina. While gene therapy has shown promise in treating RP in patients with specific mutations, no effective therapies currently exist for the majority of patients with diverse genetic backgrounds. Additionally, no intervention can yet prevent or delay photoreceptor loss across the broader RP patient population. Resveratrol (RES), a naturally occurring polyphenol, has shown cytoprotective effects in various neurodegenerative disease models; however, its therapeutic potential is limited by low bioavailability. Methods: In this study, we synthesized novel RES derivatives and assessed their retinoprotective effects in a murine model of RP (rd10 mice). Results: Among these derivatives, piceid octanoate (PIC-OCT) significantly delayed photoreceptor degeneration in the RP model, demonstrating superior efficacy compared to RES. Conclusions: PIC-OCT shows strong potential as a leading candidate for developing new therapeutic strategies for RP.https://www.mdpi.com/1424-8247/17/11/1482neurodegenerationretinal degenerationretinitis pigmentosaresveratrolpiceid octanoateretinoprotection
spellingShingle Lourdes Valdés-Sánchez
Seyed Mohamadmehdi Moshtaghion
Estefanía Caballano-Infantes
Pablo Peñalver
Rosario Rodríguez-Ruiz
José Luis González-Alfonso
Francisco José Plou
Tom Desmet
Juan C. Morales
Francisco J. Díaz-Corrales
Synthesis and Evaluation of Glucosyl-, Acyl- and Silyl- Resveratrol Derivatives as Retinoprotective Agents: Piceid Octanoate Notably Delays Photoreceptor Degeneration in a Retinitis Pigmentosa Mouse Model
Pharmaceuticals
neurodegeneration
retinal degeneration
retinitis pigmentosa
resveratrol
piceid octanoate
retinoprotection
title Synthesis and Evaluation of Glucosyl-, Acyl- and Silyl- Resveratrol Derivatives as Retinoprotective Agents: Piceid Octanoate Notably Delays Photoreceptor Degeneration in a Retinitis Pigmentosa Mouse Model
title_full Synthesis and Evaluation of Glucosyl-, Acyl- and Silyl- Resveratrol Derivatives as Retinoprotective Agents: Piceid Octanoate Notably Delays Photoreceptor Degeneration in a Retinitis Pigmentosa Mouse Model
title_fullStr Synthesis and Evaluation of Glucosyl-, Acyl- and Silyl- Resveratrol Derivatives as Retinoprotective Agents: Piceid Octanoate Notably Delays Photoreceptor Degeneration in a Retinitis Pigmentosa Mouse Model
title_full_unstemmed Synthesis and Evaluation of Glucosyl-, Acyl- and Silyl- Resveratrol Derivatives as Retinoprotective Agents: Piceid Octanoate Notably Delays Photoreceptor Degeneration in a Retinitis Pigmentosa Mouse Model
title_short Synthesis and Evaluation of Glucosyl-, Acyl- and Silyl- Resveratrol Derivatives as Retinoprotective Agents: Piceid Octanoate Notably Delays Photoreceptor Degeneration in a Retinitis Pigmentosa Mouse Model
title_sort synthesis and evaluation of glucosyl acyl and silyl resveratrol derivatives as retinoprotective agents piceid octanoate notably delays photoreceptor degeneration in a retinitis pigmentosa mouse model
topic neurodegeneration
retinal degeneration
retinitis pigmentosa
resveratrol
piceid octanoate
retinoprotection
url https://www.mdpi.com/1424-8247/17/11/1482
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