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Piceatannol 3'-O-glucoside is a natural product from Rhubarb, acting as a potent inhibitor of arginase activity. It can activate endothelial nitric oxide (NO) synthase through inhibition of arginase activity. It inhibits arginase I and arginase II with IC50s of 11.22 µM and 11.06 µM, respectively.
| ln Vitro |
Piceatannol 3'-O-glucoside (Piceatannol-3'-O-β-D-glucopyranoside; PG) is the active component of stilbene, which inhibits the enzymes arginase I and II in lysates of mouse kidney and liver, respectively. in an active, dose-dependent way. The Griess assay showed that treatment with Piceatannol 3'-O-glucoside dramatically inhibited arginase activity and enhanced nitrite and nitrate (NOx) generation in human umbilical vein endothelial cells. Arginase I activity was considerably reduced in liver lysates upon incubation with varying concentrations of piceatannol 3'-O-glucoside (75 ± 5% at 1 µM, 3 72±7% at µM, and 62±1% at 10 µM) (100±9%). Following incubation with 1, 3, and 10 µM piceatannol 3'-O-glucoside, the residual arginase activity in kidney lysates were 75±6, 74±5, and 53±8%, respectively. Using liver and kidney lysates with varying doses of piceatannol 3'-O-glucoside (0 to 120 µM), arginase activity was determined. For both liver and kidney lysates, the 50% inhibitory concentration (IC50) was 11.22 µM and 11.06 µM, respectively. Software called Graphpad Prizm 4.0 was used to obtain these values. In HUVECs, piceatannol 3'-O-glucoside enhances NO generation while inhibiting arginase activity. With an IC50 value of 69 µM, piceatannol 3'-O-glucoside inhibits lipoxygenase activity by up to 66% at a dose of 100 µM[1].
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| ln Vivo |
The aim of this work is to investigate potential underlying mechanisms and assess the effects of piceatannol 3'-O-glucoside (PG) on vascular function in wild-type (WT) and atherosclerosis model mice (apolipoprotein E-deficient mice, ApoE-/-) animals. The vasoconstrictive response to phenylephrine (PE) and normal diet (ND)-fed WT mice was decreased by preincubating the aorta arteries with picatannol 3'-O-glucoside. In contrast, endothelium-dependent animals showed a considerably improved vasodilatory response to acetylcholine (ACh). In the aortic rings of high-cholesterol diet (HCD)-fed ApoE-/-mice, piceatannol 3'-O-glucoside therapy dramatically increases acetylcholine (Ach)-dependent vasodilatory response while attenuating phenylephrine (PE)-dependent contractile responses. When ApoE-/-mice fed HCD were given drinking water containing piceatannol 3'-O-glucoside, the production of fatty streaks was greatly decreased [2].
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| References |
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| Additional Infomation |
Piceatannol 3'-O-glucoside has been reported in Rheum undulatum, Rheum rhaponticum, and Rheum rhabarbarum with data available.
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| Molecular Formula |
C20H22O9
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|---|---|
| Molecular Weight |
406.38328
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| Exact Mass |
406.126
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| CAS # |
94356-26-0
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| PubChem CID |
11968990
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
721.6±60.0 °C at 760 mmHg
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| Flash Point |
390.2±32.9 °C
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| Vapour Pressure |
0.0±2.5 mmHg at 25°C
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| Index of Refraction |
1.761
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| LogP |
0.04
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
534
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C1=CC(=C(C=C1/C=C/C2=CC(=CC(=C2)O)O)O[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O)O
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| InChi Key |
UMGCIIXWEFTPOC-CUYWLFDKSA-N
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| InChi Code |
InChI=1S/C20H22O9/c21-9-16-17(25)18(26)19(27)20(29-16)28-15-7-10(3-4-14(15)24)1-2-11-5-12(22)8-13(23)6-11/h1-8,16-27H,9H2/b2-1+/t16-,17-,18+,19-,20-/m1/s1
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| Chemical Name |
(2S,3R,4S,5S,6R)-2-[5-[(E)-2-(3,5-dihydroxyphenyl)ethenyl]-2-hydroxyphenoxy]-6-(hydroxymethyl)oxane-3,4,5-triol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~123.04 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4608 mL | 12.3038 mL | 24.6075 mL | |
| 5 mM | 0.4922 mL | 2.4608 mL | 4.9215 mL | |
| 10 mM | 0.2461 mL | 1.2304 mL | 2.4608 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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