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Rhanteriol, a New Rhanterium suaveolens Desf. Lignan with Pharmacological Potential as an Inhibitor of Enzymes Involved in Neurodegeneration and Type 2 Diabetes

Several specialized plant metabolites are reported to be enzyme inhibitors. In this investigation, the phytochemical composition and the biological activity of Rhanterium suaveolens Desf. were studied. One new lignan (rhanteriol 1) and seven known secondary metabolites were isolated from the aerial...

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Autores principales: Belaabed, Soumia, Khalfaoui, Ayoub, Parisi, Valentina, Santoro, Valentina, Russo, Daniela, Ponticelli, Maria, Monné, Magnus, Rebbas, Khellaf, Milella, Luigi, Donadio, Giuliana
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9865629/
https://www.ncbi.nlm.nih.gov/pubmed/36679017
http://dx.doi.org/10.3390/plants12020301
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author Belaabed, Soumia
Khalfaoui, Ayoub
Parisi, Valentina
Santoro, Valentina
Russo, Daniela
Ponticelli, Maria
Monné, Magnus
Rebbas, Khellaf
Milella, Luigi
Donadio, Giuliana
author_facet Belaabed, Soumia
Khalfaoui, Ayoub
Parisi, Valentina
Santoro, Valentina
Russo, Daniela
Ponticelli, Maria
Monné, Magnus
Rebbas, Khellaf
Milella, Luigi
Donadio, Giuliana
author_sort Belaabed, Soumia
collection PubMed
description Several specialized plant metabolites are reported to be enzyme inhibitors. In this investigation, the phytochemical composition and the biological activity of Rhanterium suaveolens Desf. were studied. One new lignan (rhanteriol 1) and seven known secondary metabolites were isolated from the aerial parts of R. suaveolens by using different chromatographic procedures. The biological properties of the R. suaveolens extracts and the new compound were evaluated by measuring their ability to inhibit the cholinesterase and carbohydrate-hydrolyzing enzymes, using cell-free in vitro methods. The new lignan, rhanteriol, was shown to inhibit α-amylase and α-glucosidase (IC(50) = 46.42 ± 3.25 μM and 26.76 ± 3.29 μM, respectively), as well as butyrylcholinesterase (IC(50) = 10.41 ± 0.03 μM), with an effect comparable to that of the respective standards, acarbose and galantamine. Furthermore, docking studies were performed suggesting the interaction mode of rhanteriol with the active sites of the investigated enzymes. The obtained data demonstrated that the aerial part of R. suaveolens could represent a source of active molecules, such as rhanteriol, usable in the development of treatments for preventing or treating type 2 diabetes mellitus and neurodegeneration.
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spelling pubmed-98656292023-01-22 Rhanteriol, a New Rhanterium suaveolens Desf. Lignan with Pharmacological Potential as an Inhibitor of Enzymes Involved in Neurodegeneration and Type 2 Diabetes Belaabed, Soumia Khalfaoui, Ayoub Parisi, Valentina Santoro, Valentina Russo, Daniela Ponticelli, Maria Monné, Magnus Rebbas, Khellaf Milella, Luigi Donadio, Giuliana Plants (Basel) Article Several specialized plant metabolites are reported to be enzyme inhibitors. In this investigation, the phytochemical composition and the biological activity of Rhanterium suaveolens Desf. were studied. One new lignan (rhanteriol 1) and seven known secondary metabolites were isolated from the aerial parts of R. suaveolens by using different chromatographic procedures. The biological properties of the R. suaveolens extracts and the new compound were evaluated by measuring their ability to inhibit the cholinesterase and carbohydrate-hydrolyzing enzymes, using cell-free in vitro methods. The new lignan, rhanteriol, was shown to inhibit α-amylase and α-glucosidase (IC(50) = 46.42 ± 3.25 μM and 26.76 ± 3.29 μM, respectively), as well as butyrylcholinesterase (IC(50) = 10.41 ± 0.03 μM), with an effect comparable to that of the respective standards, acarbose and galantamine. Furthermore, docking studies were performed suggesting the interaction mode of rhanteriol with the active sites of the investigated enzymes. The obtained data demonstrated that the aerial part of R. suaveolens could represent a source of active molecules, such as rhanteriol, usable in the development of treatments for preventing or treating type 2 diabetes mellitus and neurodegeneration. MDPI 2023-01-09 /pmc/articles/PMC9865629/ /pubmed/36679017 http://dx.doi.org/10.3390/plants12020301 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Belaabed, Soumia
Khalfaoui, Ayoub
Parisi, Valentina
Santoro, Valentina
Russo, Daniela
Ponticelli, Maria
Monné, Magnus
Rebbas, Khellaf
Milella, Luigi
Donadio, Giuliana
Rhanteriol, a New Rhanterium suaveolens Desf. Lignan with Pharmacological Potential as an Inhibitor of Enzymes Involved in Neurodegeneration and Type 2 Diabetes
title Rhanteriol, a New Rhanterium suaveolens Desf. Lignan with Pharmacological Potential as an Inhibitor of Enzymes Involved in Neurodegeneration and Type 2 Diabetes
title_full Rhanteriol, a New Rhanterium suaveolens Desf. Lignan with Pharmacological Potential as an Inhibitor of Enzymes Involved in Neurodegeneration and Type 2 Diabetes
title_fullStr Rhanteriol, a New Rhanterium suaveolens Desf. Lignan with Pharmacological Potential as an Inhibitor of Enzymes Involved in Neurodegeneration and Type 2 Diabetes
title_full_unstemmed Rhanteriol, a New Rhanterium suaveolens Desf. Lignan with Pharmacological Potential as an Inhibitor of Enzymes Involved in Neurodegeneration and Type 2 Diabetes
title_short Rhanteriol, a New Rhanterium suaveolens Desf. Lignan with Pharmacological Potential as an Inhibitor of Enzymes Involved in Neurodegeneration and Type 2 Diabetes
title_sort rhanteriol, a new rhanterium suaveolens desf. lignan with pharmacological potential as an inhibitor of enzymes involved in neurodegeneration and type 2 diabetes
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9865629/
https://www.ncbi.nlm.nih.gov/pubmed/36679017
http://dx.doi.org/10.3390/plants12020301
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