New Insights into the Efficacy of Aspalathin and Other Related Phytochemicals in Type 2 Diabetes—A Review

In the pursuit of bioactive phytochemicals as a therapeutic strategy to manage metabolic risk factors for type 2 diabetes (T2D), aspalathin, <i>C</i>-glucosyl dihydrochalcone from rooibos (<i>Aspalathus linearis</i>), has received much attention, along with its <i>C<...

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Main Authors: Christo J. F. Muller, Elizabeth Joubert, Nireshni Chellan, Yutaka Miura, Kazumi Yagasaki
Format: Article
Language:English
Published: MDPI AG 2021-12-01
Series:International Journal of Molecular Sciences
Subjects:
Online Access:https://www.mdpi.com/1422-0067/23/1/356
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author Christo J. F. Muller
Elizabeth Joubert
Nireshni Chellan
Yutaka Miura
Kazumi Yagasaki
author_facet Christo J. F. Muller
Elizabeth Joubert
Nireshni Chellan
Yutaka Miura
Kazumi Yagasaki
author_sort Christo J. F. Muller
collection DOAJ
description In the pursuit of bioactive phytochemicals as a therapeutic strategy to manage metabolic risk factors for type 2 diabetes (T2D), aspalathin, <i>C</i>-glucosyl dihydrochalcone from rooibos (<i>Aspalathus linearis</i>), has received much attention, along with its <i>C</i>-glucosyl flavone derivatives and phlorizin, the apple <i>O</i>-glucosyl dihydrochalcone well-known for its antidiabetic properties. We provided context for dietary exposure by highlighting dietary sources, compound stability during processing, bioavailability and microbial biotransformation. The review covered the role of these compounds in attenuating insulin resistance and enhancing glucose metabolism, alleviating gut dysbiosis and associated oxidative stress and inflammation, and hyperuricemia associated with T2D, focusing largely on the literature of the past 5 years. A key focus of this review was on emerging targets in the management of T2D, as highlighted in the recent literature, including enhancing of the insulin receptor and insulin receptor substrate 1 signaling via protein tyrosine phosphatase inhibition, increasing glycolysis with suppression of gluconeogenesis by sirtuin modulation, and reducing renal glucose reabsorption via sodium-glucose co-transporter 2. We conclude that biotransformation in the gut is most likely responsible for enhancing therapeutic effects observed for the <i>C</i>-glycosyl parent compounds, including aspalathin, and that these compounds and their derivatives have the potential to regulate multiple factors associated with the development and progression of T2D.
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spelling doaj.art-e21f75c9df264da4bc59fef440305c192023-11-23T11:38:44ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672021-12-0123135610.3390/ijms23010356New Insights into the Efficacy of Aspalathin and Other Related Phytochemicals in Type 2 Diabetes—A ReviewChristo J. F. Muller0Elizabeth Joubert1Nireshni Chellan2Yutaka Miura3Kazumi Yagasaki4Biomedical Research and Innovation Platform (BRIP), South African Medical Research Council (MRC), Tygerberg 7505, South AfricaPlant Bioactives Group, Post-Harvest & Agro-Processing Technologies, Agricultural Research Council, Infruitec-Nietvoorbij, Stellenbosch 7599, South AfricaBiomedical Research and Innovation Platform (BRIP), South African Medical Research Council (MRC), Tygerberg 7505, South AfricaDivision of Applied Biological Chemistry, Institute of Agriculture, Tokyo University of Agriculture and Technology, Tokyo 183-8509, JapanDivision of Applied Biological Chemistry, Institute of Agriculture, Tokyo University of Agriculture and Technology, Tokyo 183-8509, JapanIn the pursuit of bioactive phytochemicals as a therapeutic strategy to manage metabolic risk factors for type 2 diabetes (T2D), aspalathin, <i>C</i>-glucosyl dihydrochalcone from rooibos (<i>Aspalathus linearis</i>), has received much attention, along with its <i>C</i>-glucosyl flavone derivatives and phlorizin, the apple <i>O</i>-glucosyl dihydrochalcone well-known for its antidiabetic properties. We provided context for dietary exposure by highlighting dietary sources, compound stability during processing, bioavailability and microbial biotransformation. The review covered the role of these compounds in attenuating insulin resistance and enhancing glucose metabolism, alleviating gut dysbiosis and associated oxidative stress and inflammation, and hyperuricemia associated with T2D, focusing largely on the literature of the past 5 years. A key focus of this review was on emerging targets in the management of T2D, as highlighted in the recent literature, including enhancing of the insulin receptor and insulin receptor substrate 1 signaling via protein tyrosine phosphatase inhibition, increasing glycolysis with suppression of gluconeogenesis by sirtuin modulation, and reducing renal glucose reabsorption via sodium-glucose co-transporter 2. We conclude that biotransformation in the gut is most likely responsible for enhancing therapeutic effects observed for the <i>C</i>-glycosyl parent compounds, including aspalathin, and that these compounds and their derivatives have the potential to regulate multiple factors associated with the development and progression of T2D.https://www.mdpi.com/1422-0067/23/1/356aspalathinbioavailabilitydiabetes<i>C</i>-glucosyl flavonesgut microbiotahyperuricemia
spellingShingle Christo J. F. Muller
Elizabeth Joubert
Nireshni Chellan
Yutaka Miura
Kazumi Yagasaki
New Insights into the Efficacy of Aspalathin and Other Related Phytochemicals in Type 2 Diabetes—A Review
International Journal of Molecular Sciences
aspalathin
bioavailability
diabetes
<i>C</i>-glucosyl flavones
gut microbiota
hyperuricemia
title New Insights into the Efficacy of Aspalathin and Other Related Phytochemicals in Type 2 Diabetes—A Review
title_full New Insights into the Efficacy of Aspalathin and Other Related Phytochemicals in Type 2 Diabetes—A Review
title_fullStr New Insights into the Efficacy of Aspalathin and Other Related Phytochemicals in Type 2 Diabetes—A Review
title_full_unstemmed New Insights into the Efficacy of Aspalathin and Other Related Phytochemicals in Type 2 Diabetes—A Review
title_short New Insights into the Efficacy of Aspalathin and Other Related Phytochemicals in Type 2 Diabetes—A Review
title_sort new insights into the efficacy of aspalathin and other related phytochemicals in type 2 diabetes a review
topic aspalathin
bioavailability
diabetes
<i>C</i>-glucosyl flavones
gut microbiota
hyperuricemia
url https://www.mdpi.com/1422-0067/23/1/356
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