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CAS No.: 10083-24-6

Piceatannol/白皮杉醇 Catalog No. CSN12330

Synonyms: Astringenin;trans-Piceatannol;trans-Picetannol

Piceatannol, a natural stilbene, is selective Syk inhibitor extracted from the rhizomes of Polygonum cuspidatum Sieb. et Zucc..

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述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 (V_max) 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].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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	22765896

动物研究
剂量
Rat: 10 mg/kg, 30 mg/kg^[3] (i.v.) Mice: 50 mg/kg/day for 2 weeks^[4] (i.p.); 1 mg/kg, 5 mg/kg^[5] (p.o.)

给药途径
i.v., i.p., p.o.
参考文献

动物研究
剂量	Rat: 10 mg/kg, 30 mg/kg^[3] (i.v.) Mice: 50 mg/kg/day for 2 weeks^[4] (i.p.); 1 mg/kg, 5 mg/kg^[5] (p.o.)
给药途径	i.v., i.p., p.o.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.0943 mL
- 20.4714 mL
- 40.9429 mL
- 5 mM
- 0.8189 mL
- 4.0943 mL
- 8.1886 mL
- 10 mM
- 0.4094 mL
- 2.0471 mL
- 4.0943 mL

技术信息

CAS号

10083-24-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H12O4

运输

蓝冰

分子量

244.24

别名

Astringenin;trans-Piceatannol;trans-Picetannol;trans-3,3',4,5'-Tetrahydroxystilbene;NSC-622471;白皮杉醇

溶解度

DMSO	48.0 mg/mL (196.5 mM)
Water	Insoluble
Ethanol	47.0 mg/mL (192.4 mM)

动物实验配方

5%DMSO+40% PEG300+5% Tween+50%water

4 mg/mL

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