Spleen tyrosine kinase (Syk) is a cytosolic non-receptor protein tyrosine kinase (PTK) and is mainly expressed in hematopoietic cells. Syk was recognized as a critical element in the B-cell receptor signaling pathway. Syk is also a key component in signal transduction from other immune receptors like Fc receptors and adhesion receptors[3]. Piceatannol, an anti-inflammatory, immunomodulatory, and anti-proliferative stilbene, is a selective Syk inhibitor, about 10-fold more sensitive than Lyn[4]. The treatment of human myeloid cells with piceatannol suppressed TNF-induced DNA binding activity of NF-κB. TNF-induced NF-κB activation was also suppressed in lymphocyte and epithelial cells. It also inhibited NF-κB activated by H2O2, PMA, LPS, okadaic acid, and ceramide[5]. In rat ventricular cells, piceatannol (3 - 30 µmol/L) prolonged the action potential durations (APDs) and decreased the maximal rate of upstroke (Vmax) without altering Ca2+ transients. Piceatannol (1 – 10 µmol/L) exerted antiarrhythmic activity in isolated rat hearts subjected to ischaemia‐reperfusion injury[6]. Oral piceatannol administration in BALB/c mice with dextran sulfate sodium (DSS)-induced colitis was associated with a remarkable amelioration of the disruption of the colonic architecture, a significant reduction in colonic myeloperoxidase (MPO) activity, and a decrease in production of inflammatory mediators such as nitric oxide (NO), prostaglandin (PG) E2, and pro-inflammatory cytokines[7].
Piceatannol suppressed the rises in blood glucose levels at early stages and improved the impaired glucose tolerance at late stages in db/db mice[8].
Piceatannol 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
human A2780 cells
Proliferation assay
2 days
Antiproliferative activity against human A2780 cells after 2 days by Alamar Blue assay, IC50=41 μM
24239390
human lung mast cells
Function assay
Inhibition of SYK in human lung mast cells assessed as reduction in anti-IgE-stimulated histamine release, EC50=25 μM
22257213
mouse 3T3L1 cells
10 to 50 μM
Function assay
48 h
Reduction in triglyceride level in mouse 3T3L1 cells at 10 to 50 uM after 48 hrs
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