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Piceatannol 3＇-O-glucoside

CAS No. : 94356-26-0

MCE 站：Piceatannol 3＇-O-glucoside

产品活性：Piceatannol 3＇-O-glucoside 是 Rhubarb 的一种活性成分，通过抑制精氨酸酶 (Arginase) 活性激活内皮细胞一氧化氮合酶 (NO synthase)，抑制 Arginase I 和 Arginase II，IC₅₀ 值分别为 11.22 μM 和 11.06 μM。

研究领域：Immunology/Inflammation  |  Metabolic Enzyme/Protease

作用靶点：NO Synthase  |  Arginase

In Vitro: Piceatannol 3＇-O-glucoside (Piceatannol-3＇-O-β-D-glucopyranoside; PG) is a potent component of stilbenes, inhibits the activity of arginase I ａnd II prepared from mouse liver ａnd kidney lysates, respectively, in a dose-dependent manner. In human umbilical vein endothelial cells, incubation of Piceatannol 3＇-O-glucoside markedly blocks arginase activity ａnd increases nitrite ａnd nitrate (NOx) production, as measured by Griess assay. In liver lysates, incubation of different concentrations of Piceatannol 3＇-O-glucoside significantly decreases arginase I activity (75±5% at 1 µM, 72±7% at 3 µM, 62±1% at 10 µM) compared to untreated control (100±9%). In kidney lysates, the residual arginase activities after incubation of 1, 3 ａnd 10 µM Piceatannol 3＇-O-glucoside are 75±6, 74±5, ａnd 53±8%, respectively. Arginase activity is measured in the presence of different concentration of Piceatannol 3＇-O-glucoside (from 0 to 120 µM) using liver lysate ａnd kidney lysate. The 50% inhibitory concentrations (IC₅₀) are 11.22 µM for the liver lysate ａnd 11.06 µM for kidney lysate. The values are obtained using the software of Graphpad prizm 4.0. Piceatannol 3＇-O-glucoside inhibits arginase activity ａnd increases NO production in HUVECs. Piceatannol 3＇-O-glucoside inhibits lipoxygenase activity upto 66% at the concentration of 100 µM ａnd IC₅₀ value is 69 µM.

In Vivo: In order to ascertain whether Piceatannol 3＇-O-glucoside (PG) ameliorates vascular function in wild-type (WT) ａnd atherogenic model mice [apolipoprotein E-null mice (ApoE^-/-)] ａnd to investigate the possible underlying mechanism. Preincubation of aortic vessels from WT mice fed a normal diet (ND) with Piceatannol 3＇-O-glucoside attenuates vasoconstriction response to U46619 ａnd phenylephrine (PE), while the vasorelaxant response to acetylcholine (Ach) is markedly enhanced in an endothelium-dependent manner. Piceatannol 3＇-O-glucoside treatment attenuates the phenylephrine (PE)-dependent contractile response, ａnd significantly improves the acetylcholine (Ach)-dependent vasorelaxation response in aortic rings from ApoE^-/- mice fed a high-cholesterol diet (HCD). Piceatannol 3＇-O-glucoside administration in the drinking water significantly reduces fatty streak formation in ApoE^-/- mice fed an HCD.

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