Exploring the Mechanism of β-Cyclodextrin-Encased Phenolic Acids Functionalized with TPP for Antioxidant Activity and Targeting

Oxidative stress on the mitochondria in a human cell is attributed to several life-risking conditions, and as such, the importance of molecular structures packed with antioxidant properties and structural characteristics to enter the cell to help prevent such stress has been substantially relevant i...

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Main Authors: Christopher Sbarbaro, Valeria Márquez-Miranda, Matías Leal, Ricardo Pino-Rios, Pedro Olivares, Makarena González, Ignacio Díaz-Franulic, Fernando González-Nilo, Osvaldo Yáñez, Yorley Duarte
Format: Article
Language:English
Published: MDPI AG 2025-04-01
Series:Antioxidants
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Online Access:https://www.mdpi.com/2076-3921/14/4/465
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author Christopher Sbarbaro
Valeria Márquez-Miranda
Matías Leal
Ricardo Pino-Rios
Pedro Olivares
Makarena González
Ignacio Díaz-Franulic
Fernando González-Nilo
Osvaldo Yáñez
Yorley Duarte
author_facet Christopher Sbarbaro
Valeria Márquez-Miranda
Matías Leal
Ricardo Pino-Rios
Pedro Olivares
Makarena González
Ignacio Díaz-Franulic
Fernando González-Nilo
Osvaldo Yáñez
Yorley Duarte
author_sort Christopher Sbarbaro
collection DOAJ
description Oxidative stress on the mitochondria in a human cell is attributed to several life-risking conditions, and as such, the importance of molecular structures packed with antioxidant properties and structural characteristics to enter the cell to help prevent such stress has been substantially relevant in recent years. In this study, we investigated the antioxidant properties of triphenylphosphonium (TPP)-conjugated phenolic acids encapsulated in β-cyclodextrin (β-CD). We synthesized TPP conjugates of caffeic, coumaric, and cinnamic acids and formed inclusion complexes with β-CD. Our results showed successful encapsulation of TPP conjugates in β-CD with high efficiency. The TPP conjugates maintained antioxidant activity, with slight reductions observed in β-CD complexes. Furthermore, cell viability studies showed low cytotoxicity of the dds. Computational analyses revealed that TPP conjugation preserved the chemical reactivity of the phenolic acids. Molecular dynamics simulations demonstrated stable inclusion complexes with β-CD and the free energy calculations indicated that TPP conjugation significantly enhanced the ability of caffeic acid to translocate across mitochondrial membranes. These results highlight the potential of TPP-conjugated phenolic acids encapsulated in β-CD as effective antioxidants with improved mitochondrial targeting capabilities.
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spelling doaj-art-edf6b2c7464e4bd58807a6bda50ccd6e2025-08-20T03:14:16ZengMDPI AGAntioxidants2076-39212025-04-0114446510.3390/antiox14040465Exploring the Mechanism of β-Cyclodextrin-Encased Phenolic Acids Functionalized with TPP for Antioxidant Activity and TargetingChristopher Sbarbaro0Valeria Márquez-Miranda1Matías Leal2Ricardo Pino-Rios3Pedro Olivares4Makarena González5Ignacio Díaz-Franulic6Fernando González-Nilo7Osvaldo Yáñez8Yorley Duarte9Center for Bioinformatics and Integrative Biology, Facultad de Ciencias de la Vida, Universidad Andrés Bello, Santiago 8370035, ChileCenter for Bioinformatics and Integrative Biology, Facultad de Ciencias de la Vida, Universidad Andrés Bello, Santiago 8370035, ChileDepartamento de Química Orgánica y Fisicoquímica, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Santiago 8380494, ChileInstituto de Ciencias Exactas y Naturales (ICEN), Universidad Arturo Prat, Playa Brava 3256, Iquique 1111346, ChileCenter for Bioinformatics and Integrative Biology, Facultad de Ciencias de la Vida, Universidad Andrés Bello, Santiago 8370035, ChileCenter for Bioinformatics and Integrative Biology, Facultad de Ciencias de la Vida, Universidad Andrés Bello, Santiago 8370035, ChileCenter for Bioinformatics and Integrative Biology, Facultad de Ciencias de la Vida, Universidad Andrés Bello, Santiago 8370035, ChileCenter for Bioinformatics and Integrative Biology, Facultad de Ciencias de la Vida, Universidad Andrés Bello, Santiago 8370035, ChileCentro de Modelación Ambiental y Dinámica de Sistemas (CEMADIS), Universidad de las Américas, Santiago 7500975, ChileCenter for Bioinformatics and Integrative Biology, Facultad de Ciencias de la Vida, Universidad Andrés Bello, Santiago 8370035, ChileOxidative stress on the mitochondria in a human cell is attributed to several life-risking conditions, and as such, the importance of molecular structures packed with antioxidant properties and structural characteristics to enter the cell to help prevent such stress has been substantially relevant in recent years. In this study, we investigated the antioxidant properties of triphenylphosphonium (TPP)-conjugated phenolic acids encapsulated in β-cyclodextrin (β-CD). We synthesized TPP conjugates of caffeic, coumaric, and cinnamic acids and formed inclusion complexes with β-CD. Our results showed successful encapsulation of TPP conjugates in β-CD with high efficiency. The TPP conjugates maintained antioxidant activity, with slight reductions observed in β-CD complexes. Furthermore, cell viability studies showed low cytotoxicity of the dds. Computational analyses revealed that TPP conjugation preserved the chemical reactivity of the phenolic acids. Molecular dynamics simulations demonstrated stable inclusion complexes with β-CD and the free energy calculations indicated that TPP conjugation significantly enhanced the ability of caffeic acid to translocate across mitochondrial membranes. These results highlight the potential of TPP-conjugated phenolic acids encapsulated in β-CD as effective antioxidants with improved mitochondrial targeting capabilities.https://www.mdpi.com/2076-3921/14/4/465antioxidantphenolic acidscomplexoxidative stresstriphenylphosphonium (TPP)-conjugated
spellingShingle Christopher Sbarbaro
Valeria Márquez-Miranda
Matías Leal
Ricardo Pino-Rios
Pedro Olivares
Makarena González
Ignacio Díaz-Franulic
Fernando González-Nilo
Osvaldo Yáñez
Yorley Duarte
Exploring the Mechanism of β-Cyclodextrin-Encased Phenolic Acids Functionalized with TPP for Antioxidant Activity and Targeting
Antioxidants
antioxidant
phenolic acids
complex
oxidative stress
triphenylphosphonium (TPP)-conjugated
title Exploring the Mechanism of β-Cyclodextrin-Encased Phenolic Acids Functionalized with TPP for Antioxidant Activity and Targeting
title_full Exploring the Mechanism of β-Cyclodextrin-Encased Phenolic Acids Functionalized with TPP for Antioxidant Activity and Targeting
title_fullStr Exploring the Mechanism of β-Cyclodextrin-Encased Phenolic Acids Functionalized with TPP for Antioxidant Activity and Targeting
title_full_unstemmed Exploring the Mechanism of β-Cyclodextrin-Encased Phenolic Acids Functionalized with TPP for Antioxidant Activity and Targeting
title_short Exploring the Mechanism of β-Cyclodextrin-Encased Phenolic Acids Functionalized with TPP for Antioxidant Activity and Targeting
title_sort exploring the mechanism of β cyclodextrin encased phenolic acids functionalized with tpp for antioxidant activity and targeting
topic antioxidant
phenolic acids
complex
oxidative stress
triphenylphosphonium (TPP)-conjugated
url https://www.mdpi.com/2076-3921/14/4/465
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