Acylhydrazones Contribute to Serum Glucose Homeostasis Through Dual Physiological Targets

Frederico, Marisa Jádna Silva; Castro, Allisson Jhonatan Gomes; Mascarello, Alessandra; Mendes, Camila Pires; Kappel, Virgínia Demarchi; Stumpf, Taisa; Leal, Paulo Ademar Martins; Nunes, Ricardo José; Yunes, Rosendo A.; Silva, Fátima

doi:10.2174/1568026611212190003

Cited by 12 publications

(42 citation statements)

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“…4A shows the stimulatory effect of triterpene 2 on calcium influx was not significantly altered in the presence of tolbutamide. However, when diazoxide, an agonist of K + -ATP channels [32], was pre-incubated before the addition of triterpene 2, it blocked the stimulatory effect of triterpene 2 on calcium influx (Fig. 4B).…”

Section: Ca 2+ Influx In Pancreatic Isletmentioning

confidence: 91%

“…The reaction was refluxed under nitrogen for 36 h. Dichloromethane (30 mL) was added and the organic phase was washed with three 25-mL portions of 2 M aq HCl solution, three 25-mL portions of 10% aq NaHCO 3 solution, dried over Na 2 SO 4 , filtered 23 27.9 1.01 s C-4 C-5, C-24 24 16.2 0.91 s C-4 C-5 25 26.1 1.14 s C-10 C-1, C-5, C-9 26 15.3 0.74 s C-14 C-8, C-15 27 15.8 0.81 s C-13 28 13.9 0.76 s C-17 C-16, C-18, C-21 29 23 …”

Section: Synthesis Of Triterpenementioning

confidence: 99%

“…We halted incubation using the technique reported by Batra and Sjogren [28] with modifications [29]. One mL of cold buffer with lanthanum chloride (10 mM) at 2°C was added to the samples to stop calcium fluxes.…”

Section: Studies On 45 Ca 2+ Influx In Rat Isolated Pancreatic Isletmentioning

confidence: 99%

“…Nifedipine (1 μM), an L-VDCC blocker [16,33], inhibited the effect of triterpene 2. In addition, the influence of intracellular Ca 2+ in the stimulatory effect of triterpene 2 on 45 Ca 2+ influx was investigated using BAPTA-AM, an intracellular Ca 2+ -chelator [30,32]. Fig.…”

Section: Ca 2+ Influx In Pancreatic Isletmentioning

confidence: 99%

“…The genus Croton shows terpenoids as predominant secondary metabolites with important biological properties. Although the recent report that the triterpene 3β-hydroxyhop-22 (29)ene isolated and characterized from Croton heterodoxus Baillon induces insulin secretion mediated by incretin release and ionic channels modulation [10], the mechanism of action of triterpenes on insulin secretion and glucose regulation is not fully understood.…”

Section: Introductionmentioning

confidence: 99%

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Triterpene derivative: A potential signaling pathway for the fern-9(11)-ene-2α,3β-diol on insulin secretion in pancreatic islet

et al. 2016

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Section: Ca 2+ Influx In Pancreatic Isletmentioning

confidence: 91%

Section: Synthesis Of Triterpenementioning

confidence: 99%

Section: Studies On 45 Ca 2+ Influx In Rat Isolated Pancreatic Isletmentioning

confidence: 99%

Section: Ca 2+ Influx In Pancreatic Isletmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Triterpene derivative: A potential signaling pathway for the fern-9(11)-ene-2α,3β-diol on insulin secretion in pancreatic islet

et al. 2016

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Incretinomimetic and Insulinomimetic Effect of (2E)‐N′‐(1′‐Naphthyl)‐3,4,5‐Trimethoxybenzohydrazide for Glycemic Homeostasis

Frederico

Mascarello

Castro

et al. 2015

J of Cellular Biochemistry

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To characterize the role and the mechanism of action of (2E)-N'-(1'-naphthyl)-3,4,5-trimethoxybenzohydrazide (BZD) on incretin secretion, glucose uptake in skeletal muscle and α-glucosidase activity on intestine, targets for glucose homeostasis. It was assayed on glucose tolerance test (GTT) to analyze GLP-1 secretion and the activity of DPP-4 enzyme in vitro. In skeletal muscle, mechanism of action on glucose uptake was carried out by in vitro experiments. The activity of intestinal disaccharidases was performed after in vivo and in vitro experiments. The compound improved the glucose tolerance around 30%, 25%, and 20% at 15, 30, and 60 min, respectively and potentiated the sitagliptin effect, an inhibitor of the enzyme that removes GLP-1, about 50, 45, and 54% at 15, 30, and 60 min, respectively. Additionally, BZD did not modify the activity of DPP-4 enzyme. The acute effect of BZD on glucose uptake is mediated by increasing GLUT4 expression (around 140%) and its translocation to the plasma membrane in soleus muscle. The genomic effect as well as GLUT4 translocation involve the activation of PI-3K and MAPK pathways and require the microtubules integrity to the complete stimulatory effect of this compound on glucose uptake. Beyond, BZD acts in an alternative target to ameliorate glycaemia, intestinal disaccharidases. In a whole, these data point an incretino- and insulinomimetic effect of the compound for glycemic control.

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Bis‐Pyrano Prenyl Isoflavone Improves Glucose Homeostasis by Inhibiting Dipeptidyl Peptidase‐4 in Hyperglycemic Rats

Altenhofen

Luz

Frederico

et al. 2016

J of Cellular Biochemistry

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Isoflavones widely distributed in plants prevent diabetes. This study investigated the in vivo and in vitro effect of 3',4'-dihydroxy-6″,6″,6″',6″'-tetramethylbis(pyrano[2″,3″:5,6::2″',3″':7,8]isoflavone (bis-pyrano prenyl isoflavone) on glucose homeostasis in hyperglycemic rats. The ethyl acetate fraction from aerial parts of Polygala molluginifolia that contain isoflavones was assayed on glucose tolerance, on in vitro maltase activity and on protein glycation. The isoflavone bis-pyrano prenyl isolated from this fraction was investigated on glucose homeostasis. The in vivo action of the isoflavone exhibits an anti-hyperglycemic effect by improving glucose tolerance, augmenting the liver glycogen, inhibiting maltase activity, and stimulating glucagon-like peptide-1 (GLP-1) and insulin secretion. The in vitro isoflavone inhibits dipeptidyl peptidase-4 (DPP-4) activity since the glucose tolerance was improved in the presence of the isoflavone as much as sitagliptin, an inhibitor of DPP-4. However, the co-incubation with isoflavone and sitagliptin exhibited an additive anti-hyperglycemic action. The isoflavone increased the GLP-1 faster than the positive hyperglycemic group, which shows that the intestine is a potential target. Thus, to clarify the main site of action in which isoflavone improves glucose balance, the in vitro mechanism of action of this compound was tested in intestine using calcium influx as a trigger for the signal pathways for GLP-1 secretion. The isoflavone stimulates calcium influx in intestine and its mechanism involves voltage-dependent calcium channels, phospholipase C, protein kinase C, and stored calcium contributing for GLP-1 secretion. In conclusion, the isoflavone regulates glycaemia by acting mainly in a serum target, the DPP-4 inhibitor. Furthermore, the long-term effect of isoflavone prevents protein glycation. J. Cell. Biochem. 118: 92-103, 2017. © 2016 Wiley Periodicals, Inc.

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Acylhydrazones Contribute to Serum Glucose Homeostasis Through Dual Physiological Targets

Cited by 12 publications

References 0 publications

Triterpene derivative: A potential signaling pathway for the fern-9(11)-ene-2α,3β-diol on insulin secretion in pancreatic islet

Triterpene derivative: A potential signaling pathway for the fern-9(11)-ene-2α,3β-diol on insulin secretion in pancreatic islet

Incretinomimetic and Insulinomimetic Effect of (2E)‐N′‐(1′‐Naphthyl)‐3,4,5‐Trimethoxybenzohydrazide for Glycemic Homeostasis

Bis‐Pyrano Prenyl Isoflavone Improves Glucose Homeostasis by Inhibiting Dipeptidyl Peptidase‐4 in Hyperglycemic Rats

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