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A Combination Approach in Inhibiting Type 2 Diabetes-Related Enzymes Using Ecklonia radiata Fucoidan and Acarbose

Although there are chemotherapeutic efforts in place for Type 2 diabetes mellitus (T2DM), there is a need for novel strategies (including natural products) to manage T2DM. Fucoidan, a sulphated polysaccharide was extracted from Ecklonia radiata. The integrity of the fucoidan was confirmed by structu...

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Autores principales: Mabate, Blessing, Daub, Chantal Désirée, Malgas, Samkelo, Edkins, Adrienne Lesley, Pletschke, Brett Ivan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8619669/
https://www.ncbi.nlm.nih.gov/pubmed/34834394
http://dx.doi.org/10.3390/pharmaceutics13111979
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author Mabate, Blessing
Daub, Chantal Désirée
Malgas, Samkelo
Edkins, Adrienne Lesley
Pletschke, Brett Ivan
author_facet Mabate, Blessing
Daub, Chantal Désirée
Malgas, Samkelo
Edkins, Adrienne Lesley
Pletschke, Brett Ivan
author_sort Mabate, Blessing
collection PubMed
description Although there are chemotherapeutic efforts in place for Type 2 diabetes mellitus (T2DM), there is a need for novel strategies (including natural products) to manage T2DM. Fucoidan, a sulphated polysaccharide was extracted from Ecklonia radiata. The integrity of the fucoidan was confirmed by structural analysis techniques such as FT-IR, NMR and TGA. In addition, the fucoidan was chemically characterised and tested for cell toxicity. The fucoidan was investigated with regards to its potential to inhibit α-amylase and α-glucosidase. The fucoidan was not cytotoxic and inhibited α-glucosidase (IC(50) 19 µg/mL) more strongly than the standard commercial drug acarbose (IC(50) 332 µg/mL). However, the fucoidan lacked potency against α-amylase. On the other hand, acarbose was a more potent inhibitor of α-amylase (IC(50) of 109 µg/mL) than α-glucosidase. Due to side effects associated with the use of acarbose, a combination approach using acarbose and fucoidan was investigated. The combination showed synergistic inhibition (>70%) of α-glucosidase compared to when the drugs were used alone. The medicinal implication of this synergism is that a regimen with a reduced acarbose dose may be used, thus minimising side effects to the patient, while achieving the desired therapeutic effect for managing T2DM.
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spelling pubmed-86196692021-11-27 A Combination Approach in Inhibiting Type 2 Diabetes-Related Enzymes Using Ecklonia radiata Fucoidan and Acarbose Mabate, Blessing Daub, Chantal Désirée Malgas, Samkelo Edkins, Adrienne Lesley Pletschke, Brett Ivan Pharmaceutics Article Although there are chemotherapeutic efforts in place for Type 2 diabetes mellitus (T2DM), there is a need for novel strategies (including natural products) to manage T2DM. Fucoidan, a sulphated polysaccharide was extracted from Ecklonia radiata. The integrity of the fucoidan was confirmed by structural analysis techniques such as FT-IR, NMR and TGA. In addition, the fucoidan was chemically characterised and tested for cell toxicity. The fucoidan was investigated with regards to its potential to inhibit α-amylase and α-glucosidase. The fucoidan was not cytotoxic and inhibited α-glucosidase (IC(50) 19 µg/mL) more strongly than the standard commercial drug acarbose (IC(50) 332 µg/mL). However, the fucoidan lacked potency against α-amylase. On the other hand, acarbose was a more potent inhibitor of α-amylase (IC(50) of 109 µg/mL) than α-glucosidase. Due to side effects associated with the use of acarbose, a combination approach using acarbose and fucoidan was investigated. The combination showed synergistic inhibition (>70%) of α-glucosidase compared to when the drugs were used alone. The medicinal implication of this synergism is that a regimen with a reduced acarbose dose may be used, thus minimising side effects to the patient, while achieving the desired therapeutic effect for managing T2DM. MDPI 2021-11-22 /pmc/articles/PMC8619669/ /pubmed/34834394 http://dx.doi.org/10.3390/pharmaceutics13111979 Text en © 2021 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
Mabate, Blessing
Daub, Chantal Désirée
Malgas, Samkelo
Edkins, Adrienne Lesley
Pletschke, Brett Ivan
A Combination Approach in Inhibiting Type 2 Diabetes-Related Enzymes Using Ecklonia radiata Fucoidan and Acarbose
title A Combination Approach in Inhibiting Type 2 Diabetes-Related Enzymes Using Ecklonia radiata Fucoidan and Acarbose
title_full A Combination Approach in Inhibiting Type 2 Diabetes-Related Enzymes Using Ecklonia radiata Fucoidan and Acarbose
title_fullStr A Combination Approach in Inhibiting Type 2 Diabetes-Related Enzymes Using Ecklonia radiata Fucoidan and Acarbose
title_full_unstemmed A Combination Approach in Inhibiting Type 2 Diabetes-Related Enzymes Using Ecklonia radiata Fucoidan and Acarbose
title_short A Combination Approach in Inhibiting Type 2 Diabetes-Related Enzymes Using Ecklonia radiata Fucoidan and Acarbose
title_sort combination approach in inhibiting type 2 diabetes-related enzymes using ecklonia radiata fucoidan and acarbose
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8619669/
https://www.ncbi.nlm.nih.gov/pubmed/34834394
http://dx.doi.org/10.3390/pharmaceutics13111979
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