John P. Troup, Ph.D.
Megan Koscinski, MS, RD
Blueroot Health, Inc
ABSTRACT:
Introduction
The popularity of GLP-1 RA prescription medications has grown in the last few years with nearly 60% of consumers aware of its benefit. In spite of this, a lost appreciation exists on importance and need for dietary use of selected nutrients that play a role in the activation of GLP1 receptors (most in the digestive tract). The objective of this study was to demonstrate that selected nutrients and botanicals can effectively activate and balance the GLP-1 response system, serve to inhibit DPP-IV enzymes to sustain GLP1 availability and balance metabolic systems for support of healthy weight.
Methods
Using cell culture models, a dose response assessment of select compounds ability to activate receptors known to modulate metabolic systems and their mechanisms of action was carried out. Cell cultures utilizing human reporter functional assays and compared to the established reference agonists with specific receptors assessed for Cannabinoid receptor-2 (CB2), Glucagon-Like Peptide-1 (GLP1) Receptor, bitter receptors and also the ability to inhibit DPP-IV enzyme activity. Selected nutrients and natural products assessed included protein hydrolyzed isolates (PHI), resistant starch (potato)(RS), partially hydrolyzed guar gum (PHGG), standardized hops extract (20% xanthohumalone) (XnT), copaiba oil (standardized 10% beta-caryophyllene) (BCP). A follow-up assessment of feeding selected blends of these ingredients and measuring circulating GLP-1 hormone levels was also evaluated.
Results
Results from the experimental study revealed that the nutrients and botanicals (PHI, XnT, BCP) significantly activated GLP-1 receptors (p< 0.01) vs control vehicle. BCP activated CB2 receptors and bitter receptors while PH, PHGG and RS did not activateGLP-1 receptors but inhibited DPP-IV enzyme activity resulting in sustained availability of GLP-1 levels. When a blended mix of XnT and BCP was assessed, significant increase in activation levels of both GLP-1 and CB-2 receptors was observed vs single component activation by 10% (p< 0.05). When a blend of XnT with PHGG and RS was assessed in a follow-up experimental feeding response in an animal model (rats) GLP-1 circulating levels were higher and were sustained for longer periods of time vs a blend without PHGG and RS (p< 0.01).
Conclusion
These results suggest that selected nutritional and botanical ingredients are able to activate the GLP-1 receptors resulting in significantly high levels of GLP-1 hormone response. Further, when blended combinations were assessed for synergistic effect of GLP-1 receptor activation with inhibition of DPP-IV activity, higher and sustained levels of GLP-1 levels were observed. These data suggest that natural products delivered in the diet and supplementation can effectively increase GLP-1 availability. Further studies are required in humans to verify the clinical benefits of these ingredients.
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