Active phytochemicals of Pueraria tuberosa for DPP-IV inhibition: in silico and experimental approach
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TLDR
Through molecular docking, this study found Puerarone and Robinin to be the most potential phytochemicals of PTWE for DPP-IV inhibition, and provides the novel active components that contribute to the D PP-IV inhibitory property ofPTWE.Abstract:
We had earlier reported that the extract of Pueraria tuberosa significantly inhibits DPP-IV enzyme, resulting in glucose tolerance response in rats. In this study, we have explored the active phytochemicals responsible for this potential. The results have been validated in both fasting and postprandial states in the plasma of normal rats and also in fasting blood and intestinal homogenates of diabetic models. Pueraria tuberosa water extract (PTWE) was administered to normal Charles Foster rats for 35 days and to diabetic model (65 mg/kg bw) for 10 days. After treatments, oral glucose tolerance test (OGTT) and insulin was done for 90 min, and the changes in the levels of GLP-1, GIP, and DPP-IV activities were monitored in fasting and postprandial states. In the case of the diabetic model, DPP-IV activity was measured in intestinal homogenate and basal insulin in plasma. The components of PTWE were analyzed via HPLC-MS based on their chemical formula, molecular mass, and retention time. Using the molecular docking study, we have selected the top five components having strong binding energy with DPP-IV. The increase in secretion of GLP-1 and GIP was significantly higher in the postprandial state when compared to fasting condition. GLP-1 plasma concentration increased by 5.8 and 2.9 folds and GIP increased by 8.7 and 2.4 folds in PTWE and control rats, respectively. In contrast, the postprandial decrease in DPP-IV specific activities was recorded at 2.3 and 1.4 folds. The response in OGTT and insulin was also consistent with these changes. In comparison to diabetic controls, PTWE-administered rats showed decreased DPP-IV activity in the intestine, leading to enhanced basal insulin concentration. Through molecular docking, we found Puerarone and Robinin to be the most potential phytochemicals of PTWE for DPP-IV inhibition. Binding energy (kcal/mol) and dissociation constant (pM) of Robinin with DPP-IV protein were found to be 7.543 and 2,957,383.75, respectively. For Puerarone, it was 7.376 and 3,920,309, respectively. Thus, this study provides the novel active components that contribute to the DPP-IV inhibitory property of PTWE.read more
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DPP-IV Inhibitory Potentials of Flavonol Glycosides Isolated from the Seeds of Lens culinaris: In Vitro and Molecular Docking Analyses
TL;DR: Three flavonol glycosides (1–3) were isolated from the seeds of Lens culinaris Medikus and tested for their DPP-IV–inhibitory activity, and it was demonstrated for the first time, that compounds 1–3 inhibited D PP-IV activity in a concentration-dependent manner in the in vitro bioassay system.
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The Emerging Role of Polyphenols in the Management of Type 2 Diabetes
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Pueraria tuberosa: A Review on Traditional Uses, Pharmacology, and Phytochemistry
Ram Bharti,Ram Bharti,Bhupinder Singh Chopra,Bhupinder Singh Chopra,Sachin Raut,Sachin Raut,Neeraj Khatri,Neeraj Khatri +7 more
TL;DR: Pueraria tuberosa (Roxb. ex Willd.) DC. as mentioned in this paper is a perennial herb distributed throughout India and other Asian countries, and its extracts have been reported for nutritional and medicinal properties in Ayurveda as well as in Chinese traditional practices.
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Plasma dipeptidyl peptidase-IV activity in patients with type-2 diabetes mellitus correlates positively with HbAlc levels, but is not acutely affected by food intake
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