scholarly journals 2-Acyl-tetrahydroisoquinoline-3-carboxylic Acids: Lead Compounds with Triple Actions, Peroxisome Proliferator-Activated Receptor α/γ Agonist and Protein-Tyrosine Phosphatase 1B Inhibitory Activities

2011 ◽  
Vol 59 (7) ◽  
pp. 876-879 ◽  
Author(s):  
Kazuya Otake ◽  
Satoru Azukizawa ◽  
Kenji Takahashi ◽  
Masaki Fukui ◽  
Michiko Shibabayashi ◽  
...  
Keyword(s):  
Carboxylic Acids ◽  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Peroxisome Proliferator ◽  
Protein Tyrosine Phosphatase 1B ◽  
Peroxisome Proliferator Activated Receptor ◽  
Protein Tyrosine ◽  
Lead Compounds ◽  
Inhibitory Activities

scholarly journals Glucose Uptake Stimulatory and PTP1B Inhibitory Activities of Pimarane Diterpenes from Orthosiphon stamineus Benth

Biomolecules ◽  
2019 ◽  
Vol 9 (12) ◽  
pp. 859 ◽  
Author(s):  
Phi Hung Nguyen ◽  
Huynh Nhu Tuan ◽  
Duc Thuan Hoang ◽  
Quoc Trung Vu ◽  
Minh Quan Pham ◽  
...  
Keyword(s):  
Glucose Uptake ◽  
Insulin Signaling ◽  
Protein Tyrosine Phosphatase ◽  
Tyrosine Phosphatase ◽  
Protein Tyrosine Phosphatase 1B ◽  
Protein Tyrosine ◽  
Orthosiphon Stamineus ◽  
Potent Inhibition ◽  
Ic50 Values ◽  
Inhibitory Activities

Seven pimarane diterpenes (1–7) were isolated from Orthosiphon stamineus Benth. by assay-guided isolation. All of the isolates possessed a 2-deoxy-2-((7-nitro-2,1,3-benzoxadiazol-4-yl)amino)-d-glucose uptake effect in 3T3-L1 adipocytes at concentrations of 5 and 10 μM. Most of them showed potent inhibition against protein tyrosine phosphatase 1B with IC50 values ranging from 0.33 to 9.84 μM. In the kinetic study, all inhibition types were exposed for the examined potencies, including mixed-competitive (1), non-competitives (3 and 5), competitive (6), and uncompetitive (7). The results suggested that O. stamineus and its pimarane diterpenes might exert the hypoglycemic effect via the insulin signaling pathway targeting inhibition of protein tyrosine phosphatase 1B (PTP1B) activity.

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