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].

MCE 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

406.38

C₂₀H₂₂O₉

94356-26-0

白皮杉醇 3′-O-葡萄糖苷

Room temperature in continental US; may vary elsewhere.

4deg;C, protect from light

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

In Vitro:;

DMSO : 50 mg/mL (123.04 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  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); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.15 mM，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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  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); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.15 mM，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。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

  Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.15 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  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.

  [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.

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].

MCE 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].

MCE 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.

  [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.