Cell lines

pcDNA3-FADDdn-transfected BJAB cells

Preparation method

The solubility of this compound in DMSO is >12.2mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

15 to 100 μM for 36 h.

Applications

Piceatannol-induced apoptosis in BJAB cells was mediated by loss of mitochondrial membrane. Piceatannol led to a significant loss of the mitochondrial membrane potential at relatively low concentrations of 15 and 25μM. Piceatannol at concentrations< 100μM significantly did not reduce viability of BJAB cells thereby indicating that a membrane disrupting effect of this naturally occurring polyhydroxystilbenes, ie unspecific necrosis, did not play a role for their death-inducing potency. Apoptosis induction was concentration-dependent with a half-maximum concentration of 25μM for piceatannol.

Animal models

Six-week-old female BALB/c mice

Dosage form

1, 2.5, 5, or 10 mg/kg of body weight by gavage for 7 days

Application

The DAI (disease activity index) decreased significantly in the mice receiving piceatannol (2.5–10 mg/kg) compared with the mice receiving vehicle treatment. And piceatannol (2.5–10 mg/kg) treatment reduced weight loss in mice with colitis. NO and PGE2 are considered important inflammatory mediators, playing a key role in the pathogenesis of IBD (Inflammatory bowel disease). Oral administration of piceatannol reduced NO and PGE2 production in a concentration-dependent manner at day 10. Piceatannol administration (10 mg/kg) prevented significant increases in IL-1β, IL-6, and TNF-α levels. Administration of piceatannol 10 mg/kg significantly decreased the translocation of phospho-STAT3 and of the p65 subunit of NF-κB to enterocyte nuclei. Thus 10 mg/kg of piceatannol dramatically reduced MCP-1 and KC production in the colon. This indicated that piceatannol exerted anti-inflammatory effects by reducing monocyte and neutrophil infiltration into the colonic mucosa.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

Piceatannol is a selective inhibitor of protein tyrosine kinase Syk. It could inhibit ICa,L, Ito, IKr, Ca2+ transients and Na+-Ca2+ exchange except IK1. Shows multiple biological activities such as anti-inflammatory, antiproliferative and immunomodulatory effects.In vitro: The treatment of human myeloid cells with piceatannol suppressed TNF-induced DNA binding activity of NF-κB. The effect of piceatannol was not restricted to myeloid cells, as TNF-induced NF-κB activation was also suppressed in lymphocyte and epithelial cells. Piceatannol also inhibited NF-κB activated by H2O2, PMA, LPS, okadaic acid, and ceramide. [1]

References:
[1]. Kazuhiro Ashikawa et al. Piceatannol Inhibits TNF-Induced NF-κB Activation and NF-κB-Mediated Gene Expression Through Suppression of IκBα Kinase and p65 Phosphorylation. J Immunol, 2002 Dec 1, 169(11):6490-7.
[2]. Wen-Pin Chen et al. Piceatannol, a derivative of resveratrol, moderately slows INa inactivation and exerts antiarrhythmic action in ischaemia-reperfused rat hearts. Br J Pharmacol.2009 Jun, 157(3), 381-391.