Anti-diabetic activity of quercetin extracted from Phyllanthus emblica L. fruit: In silico and in vivo approaches

Prabhu, S.; Vijayakumar, Sekar; Kothandaraman, Swaminathan; Palani, Manogar

doi:10.1016/j.jpha.2017.10.005

Cited by 129 publications

(66 citation statements)

References 24 publications

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“…Comparison of the 1 H and 13 C NMR data for fractions A and B revealed that these compounds are quercetin and kaempferol, respectively (Figure ) (Ibrahim, Amin, Ibrahim, Abdelzaher, & Abdelrahman, ). Interestingly, previous studies have demonstrated the antidiabetic activity of quercetin (Abdelkarem & Fadda, ; Srinivasan, Vijayakumar, Kothandaraman, & Palani, ; Yang & Kang, ) and kaempferol (Alkhalidy et al, ; Chandramohan, Al‐Numair, Alsaif, & Veeramani, ; Zang, Zhang, Igarashi, & Yu, ) in different models. The reduction in blood glucose shows that these compounds contribute to the blood glucose lowering activity of methanolic leaf extract of B. pinnatum .…”

Section: Resultsmentioning

confidence: 99%

Bioactivity-guided isolation of antidiabetic principles from the methanolic leaf extract ofBryophyllum pinnatum

et al. 2018

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The antidiabetic principles from methanolic leaf extract of Bryophyllum pinnatum were isolated. The leaf extract was fractionated on silica gel using column chromatography and identified using nuclear magnetic resonance (NMR) spectrometry. The ethylacetate fraction of the partitioned methanolic extract of B. pinnatum lowered blood glucose of alloxan‐induced diabetic rats and inhibited α‐amylase and α‐glucosidase with IC50 137.89 and 110.15 µg/mL, respectively. In addition to lowering blood glucose, fractions A and B inhibited α‐amylase with IC50 57.43 and 43.84 µg/mL and α‐glucosidase with IC50 11.15 and 25.79 µg/mL, respectively. 1H and 13C NMR showed that fractions A and B are quercetin and kaempeferol, respectively. Molecular docking revealed that kaempferol and quercetin interacted with amino acid residues that bind/hydrolyze substrate molecules These compounds reversed altered lipid profile and oxidative stress biomarkers. Our findings showed that kaempferol and quercetin are responsible for the antidiabetic activity of B. pinnatum. Practical application Bryophyllum pinnatum is an edible vegetable plant in some parts of Nigeria, and its consumption could improve diabetic condition and lower postprandial glucose. Furthermore, extract of the leaves could be developed into food supplements for managing diabetes and its associated complications including dyslipidaemia and oxidative stress.

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Section: Resultsmentioning

confidence: 99%

Bioactivity-guided isolation of antidiabetic principles from the methanolic leaf extract ofBryophyllum pinnatum

et al. 2018

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“…However, in previous reports, quercetin may reduce the risk of T2DM; by inhibition of glycogen phosphorylase which inhibited glycogenolysis, reduced hepatic glucose production [32,33]. Quercetin and rutin reduced glucose absorption from small intestine by inhibition of αamylase and αglucosidases to lowering the blood glucose level [34][35][36]. Coumarin showed antidiabetic activity by stimulating the insulin production from β-cell in pancreas by regulating the glycolysis and inhibition of gluconeogenesis [37].…”

Section: Discussionmentioning

confidence: 99%

Quercetin and Coumarin Inhibit Dipeptidyl Peptidase-IV and Exhibits Antioxidant Properties: In Silico, In Vitro, Ex Vivo

et al. 2020

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Quercetin and coumarin, two naturally occurring phytochemicals of plant origin, are known to regulate hyperglycemia and oxidative stress. The present study was designed to evaluate the inhibitory activity of quercetin and coumarin on dipeptidyl peptidase-IV (DPP-IV) and their antioxidant potential. DPP-IV inhibition assays were performed, and evaluated IC50 values of diprotin A, quercetin, coumarin, and sitagliptin were found to be 0.653, 4.02, 54.83, and 5.49 nmol/mL, respectively. Furthermore, in silico studies such as the drug-likeliness and docking efficiency of quercetin and coumarin to the DPP-IV protein were performed; the ex vivo antiperoxidative potential of quercetin and coumarin were also evaluated. The results of the present study showed that the DPP-IV inhibitory potential of quercetin was slightly higher than that of sitagliptin. Virtual docking revealed the tight binding of quercetin with DPP-IV protein. Quercetin and coumarin reduced oxidative stress in vitro and ex vivo systems. We report for the first time that both compounds inhibited the DPP-IV along with antioxidant activity and thus may be use as function food ingredients in the prevention of diabetes.

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“…Some studies also demonstrated antidiabetic properties of QC through a variety of mechanisms. [42][43][44] On the other hand, the relationship between prolonged hyperglycemia and cognitive impairment has been reported. 45 Therefore, part of the memory restoration that is found in diabetic rats could be due to the potency of QC to decrease hyperglycemia and improve other diabetic-related parameters such as dyslipidemia.…”

Section: Discussionmentioning

confidence: 99%

Effect of quercetin-conjugated superparamagnetic iron oxide nanoparticles on diabetes-induced learning and memory impairment in rats

Ebrahimpour

Esmaeili

Beheshti

2018

IJN

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BackgroundDiabetes mellitus plays a causative role in cognitive decline. Newly, neuroprotective effects of flavonoids have been widely investigated in neurodegenerative diseases. Quercetin (QC) is a phyto-derived bioactive flavone with numerous beneficial activities. However, its limited permeability to cross the blood–brain barrier, low oral bioavailability, poor aqueous solubility, and rapid gastrointestinal digestion lead to the administration of high dose of QC in clinical application.Materials and methodsIn order to overcome these limitations, we conjugated QC with superparamagnetic iron oxide nanoparticles (QCSPIONs) and supplemented streptozotocin-induced diabetic rats with it to improve diabetes-related memory impairment. In this regard, 40 rats were distributed into five groups with eight animals: control, diabetes, and diabetes treated with SPIONs, QC, and QCSPIONs. All treatments (at the dose of 25 mg/kg) were dissolved in deionized water and gavaged for 35 consecutive days.ResultsAt the end of the study, QCSPIONs possessed significantly better efficacy than free QC on the improvement of memory performance. In the Morris water maze test, QCSPIONs compared to free QC reduced much better the escape latency over training trials (P<0.01) and increased the time spent in the target quadrant in probe trial (P<0.001). In the passive avoidance test, it increased step-through latency (P<0.05) and reduced the time spent in the dark compartment (P<0.01). In addition, both free QC and QCSPIONs were able to prevent the changes in body weight and decrease blood glucose levels in diabetic rats (P<0.05).ConclusionOverall, according to these results, we conclude that QC in the conjugated state with lower dose offers significantly higher potency in ameliorating diabetes-related memory impairment. Thus, this study offers an effective combined therapy for improving learning and memory.

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Anti-diabetic activity of quercetin extracted from Phyllanthus emblica L. fruit: In silico and in vivo approaches

Cited by 129 publications

References 24 publications

Bioactivity-guided isolation of antidiabetic principles from the methanolic leaf extract ofBryophyllum pinnatum

Bioactivity-guided isolation of antidiabetic principles from the methanolic leaf extract ofBryophyllum pinnatum

Quercetin and Coumarin Inhibit Dipeptidyl Peptidase-IV and Exhibits Antioxidant Properties: In Silico, In Vitro, Ex Vivo

Effect of quercetin-conjugated superparamagnetic iron oxide nanoparticles on diabetes-induced learning and memory impairment in rats

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