Abstract
In the pursuit of bioactive phytochemicals as a therapeutic strategy to manage metabolic risk factors for type 2 diabetes (T2D), aspalathin, C-glucosyl dihydrochalcone from rooibos (Aspalathus linearis), has received much attention, along with its C-glucosyl flavone derivatives and phlorizin, the apple O-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 C-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.
Highlights
There are three main types of diabetes, namely, type 1 diabetes, type 2 diabetes (T2D), and diabetes in pregnancy, with T2D accounting for approximately 90% of the total [1,2].Diabetes, especially global prevalence of T2D, is increasing as reported by the InternationalDiabetes Federation
The expression of genes involved in mitochondrial function, such as uncoupling protein 2 (Ucp 2), mitochondrial complex 1/3, Sirt1, nuclear respiratory factor 1 (Nrf 1), and mitochondrial transcription factor (Tfam) suggests that aspalathin and its flavone derivatives could protect against mitochondrial dysfunction in C2C12 skeletal muscle cells [148]
This review provided new insights into the potential antidiabetic activities of aspalathin and related compounds, focusing on recently published therapeutic targets, which include enhancing insulin signaling via AMPK and AKT activation and improving mitochondrial function
Summary
There are three main types of diabetes, namely, type 1 diabetes, type 2 diabetes (T2D), and diabetes in pregnancy, with T2D accounting for approximately 90% of the total [1,2]. This review describes recent studies on preventive and/or alleviating effects of aspalathin, a flavonoid and C-glucosyl dihydrochalcone from an endemic South African plant, Aspalathus linearis, better known as rooibos, against T2D and diabetes-related disorders. Inclusion of the minor rooibos O-glucosyl dihydrochalcone, phloridzin [5] is motivated by its structural similarity to aspalathin and potential in managing diabetes [6,7]. Their bioavailability and microbial biotransformation are addressed, as both are fundamental to the bioefficacy of these compounds.
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