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Piceatannol 3'-O-glucoside inhibits arginase I and arginase II with IC50 values of 11.22 μM and 11.06 μM, respectively. By inhibiting arginase, it increases L-arginine availability for eNOS, thereby activating eNOS and enhancing nitric oxide (NO) production.
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| 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].
In vitro, Piceatannol 3'-O-glucoside inhibits arginase activity and activates eNOS in endothelial cells, leading to increased NO production. It has been shown to increase pulmonary blood oxygen partial pressure. |
| 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].
In vivo, this compound has been studied for its vasodilatory effects through eNOS activation. It may have potential therapeutic applications in cardiovascular diseases and pulmonary hypertension. |
| Enzyme Assay |
Arginase inhibitory activity is measured using purified arginase I and II enzymes. The enzyme is incubated with L-arginine as substrate, and urea production is measured colorimetrically. Inhibition is determined by comparing activity in the presence and absence of the compound.
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| Cell Assay |
Endothelial cells (e.g., HUVECs) are cultured and treated with Piceatannol 3'-O-glucoside. NO production is measured using the Griess reagent or a fluorescent NO probe. eNOS phosphorylation is assessed by Western blotting.
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| Animal Protocol |
Animal models of pulmonary hypertension or cardiovascular disease are used to evaluate in vivo effects. The compound is administered orally or intravenously, and parameters such as blood pressure, pulmonary oxygen partial pressure, and NO levels are measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties are not extensively characterized. As a glycoside, it is expected to undergo deglycosylation and metabolism. Oral bioavailability may be limited, but the compound has demonstrated in vivo activity.
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| Toxicity/Toxicokinetics |
Specific toxicity data are limited. Stilbenoids are generally considered to have a favorable safety profile. No significant adverse effects have been reported at research doses.
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| References |
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| Additional Infomation |
According to reports, plants of the genus Rheum undulatum, Rheum rhaponticum, and Rheum rhabarbarum contain 3'-O-glucoside of paclitaxel, and relevant data are available for reference.
Piceatannol 3'-O-glucoside is a research compound with no clinical trial or regulatory approval status. It is used primarily as a reference standard and in pharmacological studies of arginase inhibition and eNOS activation. |
| 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 |
|---|---|
| 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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