Identification of Cyanidin-3-arabinoside Extracted from Blueberry as a Selective Protein Tyrosine Phosphatase 1B Inhibitor
Tian JL, Liao XJ, Wang YH, Si X, Shu C, Gong ES, Xie X, Ran XL, Li B
Journal of agricultural and food chemistry · 52 citations
Review labels
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How it was studied
- Design
- In vitro/mechanistic study (classified by our AI screen)
- Studied in
- Cells or lab samples
- Main outcome
- Mechanisms only
Who paid for it
- Funding
- Independent funding
- Government
- National Natural Science Foundation of China
- Government
- Natural Science Foundation of Liaoning Province
- Government
- Shenyang Science and Technology Bureau
- University or hospital
- Shenyang Agricultural University
- Government
- Key Laboratory of Fruit and Vegetable Processing, Ministry of Agriculture
- Government
- Department of Human Resources of Liaoning Province
- Government
- Liaoning Province
- Government
- Innovative Talent Support Program for Institution of Higher Learning of Liaoning Province
- Grants
- Natural Science Foundation of Liaoning Province (20180550776); Shenyang Agricultural University (880418027); National Natural Science Foundation of China (31671863); Shenyang Science and Technology Bureau (RC170247)
Based on 8 listed funder(s).
Publication
- Published
- 2019-11-19 · J Agric Food Chem · vol. 67 · issue 49 · pp. 13624–13634
- Publisher
- American Chemical Society
- Cited
- 73 citations · more than 92% of similar papers · 2.8× the field average
- Impact
- Top 10% most cited in its field
- References
- 30 works
- Access
- Paywalled
- Research areas
- Protein Tyrosine Phosphatases · Microbial Metabolites in Food Biotechnology · Seaweed-derived Bioactive Compounds
- Keywords
- Oleanolic acid, Chemistry, Biochemistry, Protein tyrosine phosphatase, IC50, Phosphatase, Protein kinase B, GSK-3, Enzyme, Pharmacology, Phosphorylation, Biology, In vitro
- MeSH
- humans, fruit, anthocyanins, glucosides, plant extracts, enzyme inhibitors, molecular structure, kinetics, protein tyrosine phosphatase, non-receptor type 1, phosphatidylinositol 3-kinases, molecular docking simulation, blueberry plants
9 authors
From CN
- Jinlong TianShenyang Agricultural University
- Xiao-Jun LiaoBeijing Advanced Innovation Center for Food Nutrition and Human Health; China Agricultural University
- Yuehua WangShenyang Agricultural University
- Xu SiShenyang Agricultural University
- Chi ShuShenyang Agricultural University
- Er Sheng GongShenyang Agricultural University
Abstract
Protein tyrosine phosphatase 1B (PTP1B) is an important target for type 2 diabetes. PTP1B inhibitors can reduce blood glucose levels by increasing insulin sensitivity. Anthocyanins often play a hypoglycemic effect, but the research about them have mainly focused on glucosidase. At present, the research about protein tyrosine phosphatase 1B (PTP1B) target is less, and the corresponding molecular mechanism is still unclear. Therefore, in this present study, anthocyanins isolated from blueberry were used to study the inhibitory activity on PTP1B. The isolated cyanidin-3-arabinoside (Cya-3-Ara) exhibited a better inhibitory activity with IC50 = 8.91 ± 0.63 μM, which was higher than the positive control (oleanolic acid, IC50 = 13.9 ± 1.01 μM), and the mechanism of PTP1B inhibition was reversible mixed pattern. The structure-activity relationship (SAR) between anthocyanins and PTP1B inhibition was investigated. The enzyme activity inhibition and molecular docking showed that anthocyanins had high selectivity for PTP1B inhibition. Further study showed that Cya-3-Ara could promote glycogen synthesis through ameliorating PTP1B-involved IRS-1/PI3K/Akt/GSK3β pathways. Cya-3-Ara could also be regarded as a synergistic inhibitor (CI ≤ 0.54) of oleanolic acid to obtain a better inhibitory effect on PTP1B. Taken together, our study clearly illustrates the SAR between anthocyanins and PTP1B inhibition and the mechanism of Cya-3-Ara in the insulin signaling pathway.
Abstract via Europe PMC. Copyright remains with the authors or publisher.
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