scholarly journals Protein Tyrosine Phosphatase 1B Inhibition and Glucose Uptake Potentials of Mulberrofuran G, Albanol B, and Kuwanon G from Root Bark of Morus alba L. in Insulin-Resistant HepG2 Cells: An In Vitro and In Silico Study

2018 ◽  
Vol 19 (5) ◽  
pp. 1542 ◽  
Author(s):  
Pradeep Paudel ◽  
Ting Yu ◽  
Su Seong ◽  
Eun Kuk ◽  
Hyun Jung ◽  
...  
Keyword(s):  
Glucose Uptake ◽  
Protein Tyrosine Phosphatase ◽  
In Silico ◽  
Hepg2 Cells ◽  
Tyrosine Phosphatase ◽  
Root Bark ◽  
Protein Tyrosine Phosphatase 1B ◽  
Insulin Resistant ◽  
In Silico Study

Pyrazoles as novel protein tyrosine phosphatase 1B (PTP1B) inhibitors: An in vitro and in silico study

2021 ◽  
Vol 181 ◽  
pp. 1171-1182
Author(s):  
Sónia Rocha ◽  
Mariana Lucas ◽  
Vera L.M. Silva ◽  
Pedro M.O. Gomes ◽  
Artur M.S. Silva ◽  
...  
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
In Silico ◽  
Tyrosine Phosphatase ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine ◽  
In Silico Study ◽  
Ptp1b Inhibitors ◽  
Novel Protein

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 Synthesis, in vitro and in silico screening of ethyl 2-(6-substituted benzo[d]thiazol-2-ylamino)-2-oxoacetates as protein-tyrosine phosphatase 1B inhibitors

2012 ◽  
Vol 53 ◽  
pp. 346-355 ◽  
Author(s):  
Gabriel Navarrete-Vazquez ◽  
Marleth Ramírez-Martínez ◽  
Samuel Estrada-Soto ◽  
Carlos Nava-Zuazo ◽  
Paolo Paoli ◽  
...  
Keyword(s):  
Protein Tyrosine Phosphatase ◽  
In Silico ◽  
Tyrosine Phosphatase ◽  
Protein Tyrosine Phosphatase 1B ◽  
In Silico Screening ◽  
Protein Tyrosine

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.

Isolation and Identification of a Potent PTP1B Inhibitor, Ursolic Acid, from Carolina Jasmine (Gelsemium sempervirens (L.) J.St.-Hil.)

2020 ◽  
Vol 17 (12) ◽  
pp. 939-943
Author(s):  
Toshiro Noshita ◽  
Yusuke Kakizoe ◽  
Satoshi Tanabe ◽  
Hidekazu Ouchi ◽  
Akihiro Tai
Keyword(s):  
Ursolic Acid ◽  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Active Agent ◽  
Protein Tyrosine Phosphatase 1B ◽  
Inhibiting Activity ◽  
Inhibition Activity ◽  
Isolation And Identification ◽  
Gelsemium Sempervirens

Extracts of Carolina jasmine (Gelsemium sempervirens (L.) J.St.-Hil.) petals were evaluated in vitro for inhibition activity against protein tyrosine phosphatase 1B (PTP1B). The principle active agent was also isolated from the extract and identified as ursolic acid (1). This is the first report of ursolic acid from G. sempervirens and of PTP1B-inhibiting activity in the genus Gelsemium.

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