scholarly journals Stimulating effect of a new triterpene derived from Anoectochilus elwesii on glucose uptake in insulin-resistant human HepG2 cells

2014 ◽  
Vol 28 (23) ◽  
pp. 2163-2168 ◽  
Author(s):  
Jinyan Cai ◽  
Lin Zhao ◽  
En Zhu ◽  
Jiao Guo
Keyword(s):  
Glucose Uptake ◽  
Hepg2 Cells ◽  
Insulin Resistant

scholarly journals Anti-Diabetic Activity of 2,3,6-Tribromo-4,5-Dihydroxybenzyl Derivatives from Symphyocladia latiuscula through PTP1B Downregulation and α-Glucosidase Inhibition

Marine Drugs ◽  
2019 ◽  
Vol 17 (3) ◽  
pp. 166 ◽  
Author(s):  
Pradeep Paudel ◽  
Su Seong ◽  
Hye Park ◽  
Hyun Jung ◽  
Jae Choi
Keyword(s):  
Glucose Uptake ◽  
Methyl Ether ◽  
In Silico ◽  
Hepg2 Cells ◽  
Halogen Bond ◽  
Biological Activities ◽  
Tyrosine Phosphatase ◽  
Docking Simulations ◽  
Insulin Resistant ◽  
Ring Number

The marine alga, Symphyocladia latiuscula (Harvey) Yamada, is a good source of bromophenols with numerous biological activities. This study aims to characterize the anti-diabetic potential of 2,3,6-tribromo-4,5-dihydroxybenzyl derivatives isolated from S. latiuscula via their inhibition of tyrosine phosphatase 1B (PTP1B) and α-glucosidase. Additionally, this study uses in silico modeling and glucose uptake potential analysis in insulin-resistant (IR) HepG2 cells to reveal the mechanism of anti-diabetic activity. This bioassay-guided isolation led to the discovery of three potent bromophenols that act against PTP1B and α-glucosidase: 2,3,6-tribromo-4,5-dihydroxybenzyl alcohol (1), 2,3,6-tribromo-4,5-dihydroxybenzyl methyl ether (2), and bis-(2,3,6-tribromo-4,5-dihydroxybenzyl methyl ether) (3). All compounds inhibited the target enzymes by 50% at concentrations below 10 μM. The activity of 1 and 2 was comparable to ursolic acid (IC50; 8.66 ± 0.82 μM); however, 3 was more potent (IC50; 5.29 ± 0.08 μM) against PTP1B. Interestingly, the activity of 1–3 against α-glucosidase was 30–110 times higher than acarbose (IC50; 212.66 ± 0.35 μM). Again, 3 was the most potent α-glucosidase inhibitor (IC50; 1.92 ± 0.02 μM). Similarly, 1–3 showed concentration-dependent glucose uptake in insulin-resistant HepG2 cells and downregulated PTP1B expression. Enzyme kinetics revealed different modes of inhibition. In silico molecular docking simulations demonstrated the importance of the 7–OH group for H-bond formation and bromine/phenyl ring number for halogen-bond interactions. These results suggest that bromophenols from S. latiuscula, especially highly brominated 3, are inhibitors of PTP1B and α-glucosidase, enhance insulin sensitivity and glucose uptake, and may represent a novel class of anti-diabetic drugs.

scholarly journals Water Extract of Mungbean (Vigna radiata L.) Inhibits Protein Tyrosine Phosphatase-1B in Insulin-Resistant HepG2 Cells

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1452
Author(s):  
Orathai Saeting ◽  
Kasemsiri Chandarajoti ◽  
Angsuma Phongphisutthinan ◽  
Parichat Hongsprabhas ◽  
Sudathip Sae-tan
Keyword(s):  
Glucose Metabolism ◽  
Glucose Uptake ◽  
Protein Tyrosine Phosphatase ◽  
Hepg2 Cells ◽  
Tyrosine Phosphatase ◽  
Water Extract ◽  
Protein Tyrosine ◽  
Insulin Resistant ◽  
Expression Of Genes ◽  
Ptp 1B

The present study aimed to investigate the effects of mungbean water extract (MWE) on insulin downstream signaling in insulin-resistant HepG2 cells. Whole seed mungbean was extracted using boiling water, mimicking a traditional cooking method. Vitexin and isovitexin were identified in MWE. The results showed that MWE inhibited protein tyrosine phosphatase (PTP)-1B (IC50 = 10 μg/mL), a negative regulator of insulin signaling. MWE enhanced cellular glucose uptake and altered expression of genes involved in glucose metabolism, including forkhead box O1 (FOXO1), phosphoenolpyruvate carboxykinase (PEPCK), and glycogen synthase kinase (GSK)-3β in the insulin-resistant HepG2 cells. In addition, MWE inhibited both α-amylase (IC50 = 36.65 mg/mL) and α-glucosidase (IC50 = 3.07 mg/mL). MWE also inhibited the formation of advanced glycation end products (AGEs) (IC50 = 2.28 mg/mL). This is the first study to show that mungbean water extract increased cellular glucose uptake and improved insulin sensitivity of insulin-resistant HepG2 cells through PTP-1B inhibition and modulating the expression of genes related to glucose metabolism. This suggests that mungbean water extract has the potential to be a functional ingredient for diabetes.

Investigations on the effects of ginsenoside-Rg1 on glucose uptake and metabolism in insulin resistant HepG2 cells

2019 ◽  
Vol 843 ◽  
pp. 277-284 ◽  
Author(s):  
Xiaoming Fan ◽  
Junyan Tao ◽  
Yulin Zhou ◽  
Yunhe Hou ◽  
Yiyu Wang ◽  
...  
Keyword(s):  
Glucose Uptake ◽  
Hepg2 Cells ◽  
Ginsenoside Rg1 ◽  
Insulin Resistant ◽  
Uptake And Metabolism

scholarly journals Theaflavins Improve Insulin Sensitivity through Regulating Mitochondrial Biosynthesis in Palmitic Acid-Induced HepG2 Cells

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3382 ◽  
Author(s):  
Tuantuan Tong ◽  
Ning Ren ◽  
Park Soomi ◽  
Jiafan Wu ◽  
Na Guo ◽  
...  
Keyword(s):  
Insulin Resistance ◽  
Palmitic Acid ◽  
Glucose Uptake ◽  
Hepg2 Cells ◽  
Molecular Mechanisms ◽  
Glucose Transporter ◽  
Mrna Level ◽  
Food Ingredients ◽  
Insulin Resistant ◽  
Mitochondrial Dna Copy Number

Theaflavins, the characteristic and bioactive polyphenols in black tea, possess the potential improving effects on insulin resistance-associated metabolic abnormalities, including obesity and type 2 diabetes mellitus. However, the related molecular mechanisms are still unclear. In this research, we investigated the protective effects of theaflavins against insulin resistance in HepG2 cells induced by palmitic acid. Theaflavins significantly increased glucose uptake of insulin-resistant cells at noncytotoxic doses. This activity was mediated by upregulating the total and membrane bound glucose transporter 4 protein expressions, increasing the phosphor-Akt (Ser473) level, and decreasing the phosphorylation of IRS-1 at Ser307. Moreover, theaflavins were found to enhance the mitochondrial DNA copy number, down-regulate the PGC-1β mRNA level and increase the PRC mRNA expression. Mdivi-1, a selective mitochondrial division inhibitor, could attenuate TFs-induced promotion of glucose uptake in insulin-resistant HepG2 cells. Taken together, these results suggested that theaflavins could improve hepatocellular insulin resistance induced by free fatty acids, at least partly through promoting mitochondrial biogenesis. Theaflavins are promising functional food ingredients and medicines for improving insulin resistance-related disorders.

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