| Size | Price | Stock | Qty |
|---|---|---|---|
| 1g |
|
||
| 2g |
|
||
| 5g |
|
||
| 10g | |||
| Other Sizes |
Purity: ≥98%
Polydatin (Reservatrol 3-β-mono-D-Glucoside; Piceid) is a naturally occuring stilbene and a precursor of resveratrol as well as a crystal component extracted from the root stem of perennial herbage Polygonum Cuspidatum Sieb.et Zucc. It is also known as a PLA2 inhibitor which reduces Phospholipase A2 (PLA2) activity and sPLA2-IIA mRNA expression and mitigates LPS-induced lung injury by increasing increased Clara cell secretory protein (CCSP) expression.
| Targets |
Polydatin up-regulates Clara cell secretory protein (CCSP) and inhibits phospholipase A2 (PLA2), specifically secretory phospholipase A2 type IIA (sPLA2-IIA). [1]
|
|---|---|
| ln Vitro |
In vitro activity: Polydatin, known as a PLA2 inhibitor, reduces Phospholipase A2 (PLA2) activity and sPLA2-IIA mRNA expression and mitigates LPS-induced lung injury by increasing increased Clara cell secretory protein (CCSP) expression. In vitro experiments were performed using BEAS-2B cells (human bronchial epithelial cells transformed by SV40 T-antigen). MTT assay determined the suitable concentration of Polydatin to be 0.5 mmol/L and LPS to be 100 ng/mL. LPS challenge (100 ng/mL for 28 hours) reduced CCSP mRNA and protein expression in BEAS-2B cells. Polydatin (0.5 mmol/L) promoted CCSP expression not only in normal BEAS-2B cells but also in LPS-induced BEAS-2B cells, as shown by real-time PCR and western blotting. CCSP expression in the PD pretreatment group (PD for 4 hours then LPS for 24 hours) was greater than in the PD treatment group (LPS for 24 hours then PD for 4 hours). The change in CCSP mRNA was consistent with CCSP protein expression. [1] |
| ln Vivo |
Pretreatment with Polydatin (15, 45, and 100 mg/kg) dose-dependently reduces sepsis-induced mortality and lung injury in cecal ligation and puncture (CLP-)induced sepsis mice through inhibiting CLP-induced serum tumor necrosis factor-alpha (TNF-alpha) and interleukin-6 (IL-6) production, lung cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase isoform (iNOS) protein expressions and NF-kappaB activation. LD50: Mice 1g/kg (i.p.).
In vivo experiments were conducted in male Sprague-Dawley rats (7-week-old, 200-250 g). LPS (10 mg/kg, intravenous) induced acute lung injury and decreased CCSP mRNA and protein expression in rat lung. Polydatin (0.5% solution, intravenous at doses of 1, 5, 10, 30 mg/kg) increased CCSP mRNA and protein expression in a dose-dependent manner, and also decreased sPLA2 and cPLA2 mRNA expression in a dose-dependent manner. The PD pretreatment group (PD given 0.5 hours before LPS) showed significantly higher CCSP expression and lower sPLA2/cPLA2 expression compared to the PD treatment group (PD given 1 hour after LPS). Serum CCSP level, measured by ELISA, was increased in the LPS group but decreased by Polydatin treatment in a dose-dependent manner. Immunohistochemistry showed that the percentage of CCSP-positive cells in lung tissue was increased by Polydatin in a dose-dependent manner (e.g., PD pretreatment: 40.2±2.3% at 1 mg/kg, 54±3% at 5 mg/kg, 63.5±2.6% at 10 mg/kg, 79±3% at 30 mg/kg; PD treatment: 37.4±2.4% at 1 mg/kg, 46±3% at 5 mg/kg, 56.8±2.4% at 10 mg/kg, 70±4% at 30 mg/kg). [1] |
| Cell Assay |
BEAS-2B cells were cultured in LHC-8 medium at 37°C in an atmosphere of 5% CO2 and 95% air. The medium was replaced every second day, and cells were passaged when >85% confluent by washing with Ca2+ and Mg2+-free PBS and dislodging with 0.05% trypsin. MTT assay was used to determine suitable concentrations of Polydatin (0.5 mmol/L) and LPS (100 ng/mL). Cells were divided into five groups: normal control (normal conditions for 28 hours); LPS group (100 ng/mL LPS for 28 hours); PD treatment group (100 ng/mL LPS for 24 hours followed by 0.5 mmol/L PD for 4 hours); PD pretreatment group (0.5 mmol/L PD for 4 hours followed by 100 ng/mL LPS for 24 hours); PD control group (0.5 mmol/L PD for 28 hours). Total RNA was isolated using Trizol reagent, purified with RNeasy Mini Kit, treated with DNase I, and reverse-transcribed. Quantitative gene expression analysis was performed using ABI Prism 7000 Sequence Detection System with SYBR Green PCR Master Mix. Primers for CCSP and β-actin were used (CCSP forward: 5'-GAAACTCGCTGTCACCCCTACC-3', reverse: 5'-TTAATGATGCTTTCTCTGG-3'; β-actin forward: 5'-CCTGTACGCCAACACAGTGGC-3', reverse: 5'-ATACCTCCTGCTTGCTGATCC-3'). For protein detection, cells were washed with PBS, lysed in lysis buffer, and subjected to SDS-PAGE and western blotting with anti-CCSP antibody (1:100). Immunopositive bands were visualized by enhanced chemiluminescence, and blots were reprobed with GAPDH antibody (1:2000) as a loading control. [1]
|
| Animal Protocol |
Rats: Rats are divided into six groups by random assignment andtreated as follows: in normal group and polydatin control group: ratsare administrated with CMC-Na and polydatin (200 μmol/kg) by gavagerespectively, and given normal saline (NS) by tail intravenous (iv)injection with the same volume; in DOX group: rats are injected with DOXby cauda vein for 4 weeks (3 mg/kg per week), the cumulative dosage is12 mg/kg similar to that in the research of Chang et al. Mice:Polydatin is dissolved in dimethyl sulfoxide (DMSO) and diluted inDulbecco’s modified Eagle’s medium (DMEM). Sixty adult female postpartumand lactating BALB/c mice (6–8 weeks old, weighing 35–40 g) areobtained. Control group (CG): The mice are treated with 100 μL of PBS asa vehicle control. Polydatin groups: 24h after S aureus infection, the mouse model of S aureus mastitis is intraperitoneally administered polydatin at 15, 30 and 45 mg/kg Rats and Mice Male Sprague-Dawley rats (7-week-old, 200-250 g, clean grade) were housed at 24±2°C with 12h dark/12h light cycle. Rats were randomly divided into five groups (n=10 each): sham operation (normal saline); endotoxic shock (LPS 10 mg/kg body weight); PD treatment group (LPS 10 mg/kg, then 0.5% Polydatin solution 0.2 ml/kg body weight, final concentration 1 mg/kg, 1 hour later); PD pretreatment group (0.5% PD solution 0.2 ml/kg, then LPS 10 mg/kg 0.5 hours later); PD control group (PD solution only). The PD treatment and pretreatment groups were further divided into four subgroups (n=6 each) receiving 1, 5, 10, or 30 mg/kg PD. PD was administered as a 0.5% solution (0.2 ml per kg body weight). Rats were anesthetized with 20% urethane (5-6 ml/kg body weight) intraperitoneally. The left common carotid artery was catheterized to measure mean arterial pressure (MAP) using an MS302 biology signal recording system. The right cervical vein was catheterized for LPS or PD injection. LPS (Sigma, 10 mg/kg) was injected from the right cervical vein. After injection, MAP fell from normal to shock levels. After six hours of observation, rats were sacrificed by cervical dislocation, and lung tissues and blood were collected. Total RNA was isolated from lung tissue using Trizol, purified, and reverse transcribed. Real-time PCR and RT-PCR were performed using primers for CCSP, sPLA2, cPLA2, and β-actin. For western blotting, protein was isolated from lung homogenate, resolved by SDS-PAGE, transferred to membrane, incubated with primary antibody (anti-CCSP) and peroxidase-conjugated secondary antibody, and detected with chemiluminescent substrate. Serum CCSP concentration was measured by ELISA according to manufacturer's instructions. Immunohistochemistry: lung biopsies were fixed in Bouin's fluid, paraffin-embedded, cut into 6-μm sections, and CCSP-immunoreactive cells were detected with uteroglobin antibody and immunoperoxidase technique. The proportion of CCSP-positive cells was expressed as a percentage of the whole bronchiolar epithelium cell population. [1] |
| Toxicity/Toxicokinetics |
Polydatin is a monocrystalline compound extracted from Polygonum cuspidatum Sieb et Zucc, a traditional Chinese medicinal herb. It has been shown to have prophylactic and therapeutic effects on acutely injured lungs in rats with endotoxic shock by inhibiting phospholipase A2 activity and the gene expression of secretory phospholipase A2 type IIA (sPLA2-IIA). The present study demonstrates that Polydatin up-regulates CCSP expression, which in turn inhibits PLA2 activation, providing a crucial protective mechanism in LPS-induced acute lung injury. CCSP is an endogenous inhibitor of PLA2. Polydatin increased CCSP-positive cell percentage, up-regulated CCSP mRNA and protein expression in lung tissue during LPS-induced acute lung injury, and the effect was dose-dependent. PD pretreatment showed greater efficacy than PD treatment, suggesting competitive inhibition of CCSP between PD and LPS. The study provides evidence for potential efficacy of Polydatin in clinical use for lung injury. [1]
|
| References |
BMC Cell Biol.2011 Jul 25;12:31;Mediators Inflamm.2013;2013:354087.
|
| Additional Infomation |
Trans-piceid is a stilbene compound, a product of trans-resveratrol with a β-D-glucose residue at the 3-position. It has multiple functions, including as a metabolite, potassium channel regulator, antiarrhythmic drug, hepatoprotective agent, antioxidant, nephroprotective agent, and anti-aging agent. It is a stilbene compound, polyphenol, β-D-glucoside, and monosaccharide derivative. Its function is related to trans-resveratrol. Polydatin, also known as Piceid, is the natural precursor and glycosidic form of resveratrol, possessing a single-crystal structure. Although it is isolated from the bark of Picea sitchensis or Polygonum cuspidatum, resveratrol glycosides may also be found in grapes, peanuts, hop cones, red wine, hop kernels, cocoa products, chocolate products, and many everyday foods. Resveratrol glycosides possess anti-inflammatory, immunomodulatory, antioxidant, and antitumor activities. Studies have shown that they can exert cytotoxic effects on colorectal cancer cells by inducing cell cycle arrest and apoptosis. Resveratrol glycosides have been reported to be found in hops, resveratrol, and other organisms with relevant data.
|
| Molecular Formula |
C20H22O8
|
|
|---|---|---|
| Molecular Weight |
390.38
|
|
| Exact Mass |
407.134
|
|
| CAS # |
65914-17-2
|
|
| Related CAS # |
|
|
| PubChem CID |
5281718
|
|
| Appearance |
White to off-white solid powder
|
|
| Density |
1.521 g/cm3
|
|
| Boiling Point |
707.7ºC at 760 mmHg
|
|
| Melting Point |
130 - 140 °C
|
|
| Flash Point |
381.8ºC
|
|
| LogP |
0.496
|
|
| Hydrogen Bond Donor Count |
6
|
|
| Hydrogen Bond Acceptor Count |
8
|
|
| Rotatable Bond Count |
5
|
|
| Heavy Atom Count |
28
|
|
| Complexity |
506
|
|
| Defined Atom Stereocenter Count |
5
|
|
| SMILES |
C1=CC(=CC=C1/C=C/C2=CC(=CC(=C2)O[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O)O)O
|
|
| InChi Key |
HSTZMXCBWJGKHG-CUYWLFDKSA-N
|
|
| InChi Code |
InChI=1S/C20H22O8/c21-10-16-17(24)18(25)19(26)20(28-16)27-15-8-12(7-14(23)9-15)2-1-11-3-5-13(22)6-4-11/h1-9,16-26H,10H2/b2-1+/t16-,17-,18+,19-,20-/m1/s1
|
|
| Chemical Name |
(2S,3R,4S,5S,6R)-2-[3-hydroxy-5-[(E)-2-(4-hydroxyphenyl)ethenyl]phenoxy]-6-(hydroxymethyl)oxane-3,4,5-triol
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.40 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 (6.40 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 (6.40 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 | 2.5616 mL | 12.8080 mL | 25.6161 mL | |
| 5 mM | 0.5123 mL | 2.5616 mL | 5.1232 mL | |
| 10 mM | 0.2562 mL | 1.2808 mL | 2.5616 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05867693 | Recruiting | Dietary Supplement: palmithoylethanolamide/polydatin |
Irritable Bowel Syndrome | University of Roma La Sapienza | April 19, 2023 | Not Applicable |
| NCT02372903 | Completed | Drug: Administration of micronized Palmitoylethanolamide (PEA)- Transpolydatin |
Endometriosis Chronic Pelvic Pain |
University of Cagliari | October 2013 | Not Applicable |
| NCT04912947 | Completed | Dietary Supplement: Immusystem Other: Placebo |
Oxidative Stress | Complife Italia Srl | October 30, 2020 | Not Applicable |
|
|---|
|
 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
