Piceatannol 3′-O-glucoside, an active component of Rhubarb, activates endothelial nitric oxide (NO) synthase through inhibition of arginase activity with IC₅₀s of 11.22 µM and 11.06 µM against arginase I and arginase II, respectively.

NO synthase^[1]
IC50: 11.22 μM (Arginase I), 11.06 μM (Arginase II)^[1]

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^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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^[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

406.38

C₂₀H₂₂O₉

94356-26-0

固体

White to off-white

白皮杉醇 3′-O-葡萄糖苷

• Phenols
• Polyphenols

• Stilbenes

• 植物
• 蓼科
• 大黄

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

DMSO 中的溶解度 : 50 mg/mL (123.04 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

• 方案 一

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

  Solubility: ≥ 2.5 mg/mL (6.15 mM); 澄清溶液

  此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

  生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。

• 方案 二

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

  Solubility: ≥ 2.5 mg/mL (6.15 mM); 澄清溶液

  此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

  20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

• 方案 三

  请依序添加每种溶剂： 10% DMSO    90% Corn Oil

  Solubility: ≥ 2.5 mg/mL (6.15 mM); 澄清溶液

  此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Woo A, et al. Piceatannol-3′-O-beta-D-glucopyranoside as an active component of rhubarb activates endothelial nitric oxide synthase through inhibition of arginase activity. Exp Mol Med. 2010 Jul 31;42(7):524-32.  [Content Brief]

  [2]. Woo A, et al. Arginase inhibition by piceatannol-3′-O-β-D-glucopyranoside improves endothelial dysfunctionvia activation of endothelial nitric oxide synthase in ApoE-null mice fed a high-cholesterol diet. Int J Mol Med. 2013 Apr;31(4):803-10.  [Content Brief]

Tissue lysates are prepared using lysis buffer (50 mM Tris-HCl, pH 7.5, 0.1 mM EDTA and protease inhibitors) by homogenization at 4°C followed by centrifugation for 20 min at 14,000× g at 4°C. The supernatants are used to assay for arginase activity. The livers or kidneys from C57BL/6 mice (10 weeks) are homogenized in the buffer (50 mM Tris-HCl, 150 mM NaCl, 1% Nonidet P-40, 1 mM EDTA, 1 µg/mL of leupeptin, 1 µg/mL of pepstatin, 1 µg/mL of aprotinin, 1 mM phenylmethylsulfonylflouride, 1 mM sodium orthovanadate, and 1 mM NaF) and centrifuged for 30 min at 14,000× g. The protein amount of the supernatant is analyzed by the Bradford method. Protein (100 µg) are separated in a 10% SDS-PAGE and then transferred to a nitrocellulose membrane. The blots are incubated with a monoclonal anti-arginase I, anti-arginase II, anti-endothelial nitric oxide synthase (eNOS), or anti-β-tubulin antibodies followed by the secondary antibody. The signals are detected using an enhanced chemiluminescence detection reagent with X-ray films^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Mice^[2]
Twenty 10-week-old male wild-type (WT) (C57BL/6J) and ApoE^-/- mice are studied. To determine the effect of Piceatannol 3′-O-glucoside on vascular reactivity, aortic rings isolated from 20 male C57BL/6J WT mice fed a normal diet (ND) and 20 male ApoE^-/- mice fed an HCD are studied for 6 weeks. Aortic rings are incubated with or without Piceatannol 3′-O-glucoside (50 μM) for 18 h. For the pathological assay, Piceatannol 3′-O-glucoside is administered in the drinking water to ApoE^-/- mice for 6 weeks when the mice are started on the HCD. Given that each mouse consumes ~10 mL water/day this represents a daily dose of ~500 μg/mouse/day of Piceatannol 3′-O-glucoside^[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Woo A, et al. Piceatannol-3′-O-beta-D-glucopyranoside as an active component of rhubarb activates endothelial nitric oxide synthase through inhibition of arginase activity. Exp Mol Med. 2010 Jul 31;42(7):524-32.  [Content Brief]

  [2]. Woo A, et al. Arginase inhibition by piceatannol-3′-O-β-D-glucopyranoside improves endothelial dysfunctionvia activation of endothelial nitric oxide synthase in ApoE-null mice fed a high-cholesterol diet. Int J Mol Med. 2013 Apr;31(4):803-10.  [Content Brief]