7-O-Methylaromadendrin Stimulates Glucose Uptake and Improves Insulin Resistance in Vitro

Zhang, Wei Yun; Lee, Jung‐Jin; Kim, In-Su; Kim, Young S.; Park, Jeong Sook; Myung, Chang‐Seon

doi:10.1248/bpb.33.1494

Cited by 52 publications

(32 citation statements)

References 31 publications

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“…Kinetic studies demonstrated that the inhibition produced by the flavonoid mixture and pheophytin A as well as the TFMS inhibitor of PTP1B enzyme indicates they were competitive inhibitors. Such compounds from plants including phenols, flavonoids and other compounds have been reported as PTP1B inhibitors (Zhang et al, 2010;Na et al, 2006a, b). These reports show that PTP1B enzyme inhibiting compounds from plants belong to diverse chemical classes.…”

Section: Discussion and Conclusionconclusionmentioning

confidence: 99%

In vitro anti-diabetic activity of flavonoids and pheophytins from Allophylus cominia Sw . on PTP1B, DPPIV, alpha-glucosidase and alpha-amylase enzymes

Semaan

Igoli

Young

et al. 2017

Journal of Ethnopharmacology

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BackgroundEthno-botanical information from diabetic patients in Cuba led to the identification of Allophylus cominia as a possible source of new drugs for the treatment of type 2 diabetes mellitus (T2-DM). ExperimentalChemical characterization of the extracts from A. cominia was carried out using chromatographic and spectroscopic methods. The extracts were tested for their activity on PTP1B, DPPIV, α-glucosidase enzymes and α-amylase. ResultsThe flavonoid rich fractions from A. cominia inhibited DPPIV enzyme (75.3±2.33%) at 30 µg/ml and produced a concentration-dependent inhibition against DPPIV with a Ki value of 2.6 µg/ml. At 30 µg/ml, flavonoids and pheophytins extracts significantly inhibited PTP1B enzyme (100±2.6% and 68±1% respectively). The flavonoids, pheophytin A and pheophytin B fractions showed significant concentration-dependent inhibition against PTP1Bwith Ki values of 3 µg/ml, 0.64 µg/ml and 0.88 µg/ml respectively. At 30 µg/ml, the flavonoid fraction significantly inhibited α-glucosidase enzyme (86±0.3%) in a concentration-dependent pattern with a Ki value of 2 µg/ml.None of the fractions showed significant effects on α-amylase. Fatty acids, tannins, pheophytins A and B, and a mixture of flavonoids were detected in the methanolic extract from A. cominia. The identified flavonoids were mearnsitrin, quercitrin, quercetin-3-alloside, and naringenin-7-glucoside.

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Section: Discussion and Conclusionconclusionmentioning

confidence: 99%

In vitro anti-diabetic activity of flavonoids and pheophytins from Allophylus cominia Sw . on PTP1B, DPPIV, alpha-glucosidase and alpha-amylase enzymes

Semaan

Igoli

Young

et al. 2017

Journal of Ethnopharmacology

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“…The glucose uptake assay using the 2-NBDG screening system was performed as described previously (Zhang et al 2010). Briefly, IEC-6 cells were seeded at 1 × 10 4 cells/well into 96-well plates for 24 h and then treated with or without a given concentration of dexamethasone and 50 µM of the SGK1 inhibitor EMD638683 in the absence or presence of 100 µM 2-NBDG for 1 h. The fluorescence intensity of 2-NBDG was recorded in the FL1 channel using a FACScaanto TM flow cytometer (Becton Dickinson, Franklin Lakes, NJ, USA).…”

Section: Glucose Uptake Measurement Using Flow Cytometrymentioning

confidence: 99%

SGK1 inhibitor reverses hyperglycemia partly through decreasing glucose absorption

Hao

Pan

et al. 2016

Journal of Molecular Endocrinology

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This study investigates the effectiveness and mechanisms of a serum-and glucocorticoidinducible kinase 1 (SGK1) inhibitor in counteracting hyperglycemia. In an in vivo experiment, we demonstrated that after an 8-week treatment with an SGK1 inhibitor, the fasting blood glucose and HbA1c level significantly decreased in db/db mice. RT-PCR and western blot analyses revealed that intestinal SGK1 and sodium glucose co-transporter 1 (SGLT1) expression were enhanced in db/db mice. Treatment with an SGK1 inhibitor decreased excessive SGLT1 expression in the intestine of db/db mice. In vitro experiments with intestinal IEC-6 cells showed that the co-administration of an SGK1 inhibitor partly reversed the SGLT1 expression and glucose absorption that were induced by dexamethasone. In conclusion, this study revealed that the favorable effect of an SGK1 inhibitor on hyperglycemia is partly due to decreased glucose absorption through SGLT1 in the small intestine. These data collectively suggest that SGK1 may be a potent target for the treatment of diabetes and other metabolic disorders.

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“…Insulin-resistant HepG2 cells were induced with high glucose as described previously [12,13,24,25] with minor modifications. Briefly, 3 !…”

Section: Induction Of Insulin-resistant Hepg2 Cells and Immunoblottingmentioning

confidence: 99%

Stimulation of Glucose Uptake and Improvement of Insulin Resistance by Aromadendrin

et al. 2011

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Agents that stimulate glucose uptake and improve insulin resistance may be useful in the management of type 2 diabetes mellitus (DM). Thus, the aims of this study were to assess the effects of aromadendrin, a flavonoid from Gleditsia sinensis Lam., on stimulation of glucose uptake and improvement of insulin resistance and to characterize the molecular mechanisms underlying these activities. Insulin-stimulated glucose uptake was measured in HepG2 cells and in differentiated 3T3-L1 adipocytes using 2-[N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino]-2-deoxy-D-glucose (2-NBDG), a fluorescent D-glucose analog. Expression of the peroxisome proliferator-activated receptor-γ2 (PPARγ2) and adipocyte-specific fatty acid binding protein (aP2) mRNAs and the PPARγ2 protein was analyzed in adipocytes using RT-PCR and immunoblotting, respectively. Insulin-stimulated protein kinase B (Akt/PKB) phosphorylation was measured in high glucose-induced, insulin-resistant HepG2 cells. Similar to 30 µmol/l rosiglitazone, treatment with 30 µmol/l aromadendrin significantly stimulated insulin-sensitive glucose uptake in both HepG2 cells and 3T3-L1 adipocytes. Aromadendrin treatment also enhanced adipogenesis and caused increases in the expression of PPARγ2 and aP2 mRNAs and the PPARγ2 protein in differentiated 3T3-L1 adipocytes. In high glucose-induced, insulin-resistant HepG2 cells, aromadendrin reversed the inhibition of Akt/PKB phosphorylation in response to insulin, which could be abrogated by pretreatment with LY294002, a phosphatidylinositol 3-kinase (PI3K) inhibitor. Aromadendrin treatment induced adipogenesis by increases in PPARγ2 expression, resulting in stimulation of glucose uptake and ameliorated insulin resistance. These findings suggest that aromadendrin may represent a potential therapeutic candidate for the management of type 2 DM.

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7-O-Methylaromadendrin Stimulates Glucose Uptake and Improves Insulin Resistance in Vitro

Cited by 52 publications

References 31 publications

In vitro anti-diabetic activity of flavonoids and pheophytins from Allophylus cominia Sw . on PTP1B, DPPIV, alpha-glucosidase and alpha-amylase enzymes

In vitro anti-diabetic activity of flavonoids and pheophytins from Allophylus cominia Sw . on PTP1B, DPPIV, alpha-glucosidase and alpha-amylase enzymes

SGK1 inhibitor reverses hyperglycemia partly through decreasing glucose absorption

Stimulation of Glucose Uptake and Improvement of Insulin Resistance by Aromadendrin

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