Structure of Polydatin
CAS No.: 27208-80-6
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Polydatin, extracted from the roots ofPolygonum cuspidatumSieb, a widely used traditional Chinese remedies, possesses anti-inflammatory activity in several experimental models.
Synonyms: Piceid; trans-Polydatin; 3,4,5-Trihydroxystilbene-3-beta-monoglucoside
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CAS No. : | 27208-80-6 |
Formula : | C20H22O8 |
M.W : | 390.38 |
SMILES Code : | O([C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)C2=CC(/C=C/C3=CC=C(O)C=C3)=CC(O)=C2 |
Synonyms : |
Piceid; trans-Polydatin; 3,4,5-Trihydroxystilbene-3-beta-monoglucoside
|
MDL No. : | MFCD00210592 |
InChI Key : | HSTZMXCBWJGKHG-CUYWLFDKSA-N |
Pubchem ID : | 5281718 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H312 |
Precautionary Statements: | P280 |
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
BRL-3A cells | 10, 20, 40 µM | 1 hour | To investigate the effect of Polydatin on fructose-induced ZEB1 nuclear translocation in BRL-3A cells. Results showed that Polydatin significantly decreased nuclear ZEB1 protein levels and increased cytoplasm ZEB1 protein levels. | J Cell Mol Med. 2020 Nov;24(22):13208-13222 |
Human conjunctival cells (HCC) | 0.1, 1, or 10 µM | 1 hour to 24 hours | To investigate the effect of Polydatin on hyperosmolar stress-induced inflammation. Results showed that Polydatin significantly inhibited hyperosmolar stress-induced mRNA expression of IL-6, TNF-α, IL-1β, and MMP9, and suppressed NF-κB nuclear translocation and COX-2 expression. | Nutrients. 2019 Nov 15;11(11):2792 |
BRL-3A cells | 10, 20, 40 µM | 12 hours | To investigate the effect of Polydatin on fructose-induced miR-203 expression in BRL-3A cells. Results showed that Polydatin significantly increased miR-203 expression levels. | J Cell Mol Med. 2020 Nov;24(22):13208-13222 |
Human podocytes | 20, 40, 80 µM | 12, 24, 72 hours | Polydatin attenuated high fructose-induced podocyte oxidative stress and injury by suppressing HIF-1α/NOX4 pathway. | Pharmaceutics. 2022 Oct 16;14(10):2202 |
BRL-3A cells | 10, 20, 40 µM | 24 hours | To investigate the effect of Polydatin on fructose-induced survivin and TGF-β1 protein levels in BRL-3A cells. Results showed that Polydatin significantly down-regulated survivin and TGF-β1 protein levels. | J Cell Mol Med. 2020 Nov;24(22):13208-13222 |
HepG2 cells | 5, 10, 20, 40 µM | 24 hours | In insulin-resistant HepG2 cells, polydatin upregulated the protein levels of LDLR and GCK but repressed PCSK9 protein expression, besides, polydatin also inhibited the combination between PCSK9 and LDLR. | Cardiovasc Diabetol. 2016 Feb 1;15:19 |
HepG2 cells | 5, 10, 20 µM | 24 hours | Polydatin significantly reduced the accumulation of lipid droplets in PA-induced HepG2 cells, decreased cellular TG content, and reduced LDH release and apoptosis. | Int J Biol Sci. 2018 Jul 30;14(11):1411-1425 |
Rat glomerular mesangial cells | 10, 20, 40 µM | 24 hours | Polydatin significantly reduced the expression of FN and ICAM-1 in HG-exposed GMCs and decreased ROS production | Acta Pharmacol Sin. 2020 Dec;41(12):1587-1596. |
Young HUVEC (yHUVEC) | 10 µM | 24 hours | Significantly decreased the expression of IL-8 and ROS production | Antioxidants (Basel). 2022 May 24;11(6):1037 |
HCT116 cells | 20-120 µM | 24 hours, 48 hours, 72 hours | To evaluate the effects of PD on proliferation and apoptosis of HCT116 cells. Results showed that PD alone had no significant effect on HCT116 cell proliferation, but combined treatment with IR significantly inhibited proliferation and promoted apoptosis. | Int J Biol Sci. 2019 Jan 1;15(2):430-440. |
CT26 cells | 20-120 µM | 24 hours, 48 hours, 72 hours | To evaluate the effects of PD on proliferation and apoptosis of CT26 cells. Results showed that PD alone had no significant effect on CT26 cell proliferation, but combined treatment with IR significantly inhibited proliferation and promoted apoptosis. | Int J Biol Sci. 2019 Jan 1;15(2):430-440. |
Lgr5+ CSCs | 40 µM | 3, 5, 7 days | To evaluate the effects of PD on proliferation and apoptosis of Lgr5+ CSCs. Results showed that PD significantly inhibited proliferation and promoted apoptosis of Lgr5+ CSCs, and the effect was more pronounced when combined with IR. | Int J Biol Sci. 2019 Jan 1;15(2):430-440. |
C33A cells | 200 µM | 48 hours | To evaluate the effect of PD on the cell cycle, results showed that PD induced G0/G1 phase cell cycle arrest | Front Cell Dev Biol. 2021 Apr 12;9:587218 |
CaSki cells | 200 µM | 48 hours | To evaluate the effect of PD on the cell cycle, results showed that PD induced G0/G1 phase cell cycle arrest | Front Cell Dev Biol. 2021 Apr 12;9:587218 |
HL-7702 cells | 50, 100, 200, 250, 300 µM | 48 hours | PD selectively blocked the proliferation of HCC cells but showed low toxicity in normal cells. | Cells. 2023 Jan 4;12(2):222. |
SK-HEP1 cells | 50, 100, 200, 250, 300 µM | 48 hours | PD selectively blocked the proliferation of HCC cells but showed low toxicity in normal cells. | Cells. 2023 Jan 4;12(2):222. |
HepG2 cells | 50, 100, 200, 250, 300 µM | 48 hours | PD selectively blocked the proliferation of HCC cells but showed low toxicity in normal cells. | Cells. 2023 Jan 4;12(2):222. |
MC3T3-E1 cells | 20, 40, 80 mM | 7 days | Evaluate the reversal effect of POL on the osteoporosis model, results showed that POL could partially reverse the reduction of bone turnover markers by DXM in a dose-dependent manner | Front Cell Dev Biol. 2021 Sep 29;9:730362 |
BEAS-2B | 0-600 µM | 72 hours | PD showed less cytotoxicity against normal human cells | Int J Oncol. 2024 Aug;65(2):77 |
Induced neurons (iNs) | 10 µM | 7 days | Increased immunofluorescence signals of EF-G1 and MtCO2, indicating upregulation of mitochondrial protein synthesis | Biomolecules. 2024 May 18;14(5):598 |
GFM1 mutant fibroblasts | 10 µM | 7 days | Increased GFM1 transcript and protein expression levels, improved mitochondrial protein synthesis and cellular bioenergetics | Biomolecules. 2024 May 18;14(5):598 |
Bone marrow mesenchymal stem cells (BMSCs) | 1 µM and 10 µM | 7 days (ALP staining) and 21 days (ARS staining) | Promoted proliferation and osteogenic differentiation of BMSCs, upregulated expression of OCN, ALP, and COL1A1 | Int J Surg. 2025 Jan 1;111(1):411-425. |
H460 | 0-600 µM | 72 hours | PD significantly inhibited NSCLC cell proliferation with IC50 values of ~500 µM | Int J Oncol. 2024 Aug;65(2):77 |
H1299 | 0-600 µM | 72 hours | PD significantly inhibited NSCLC cell proliferation with IC50 values of ~500 µM | Int J Oncol. 2024 Aug;65(2):77 |
Senescent HUVEC (sHUVEC) | 10 µM | 72 hours | Significantly decreased the expression of IL-1β, IL-8, ROS production and RAGE expression | Antioxidants (Basel). 2022 May 24;11(6):1037 |
Human umbilical vein endothelial cells (HUVECs) | 1 µM | 8 hours (migration assay) and 24 hours (scratch wound assay) | POL indirectly promoted HUVECs migration and tube formation via BMSCs | Int J Surg. 2025 Jan 1;111(1):411-425. |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Wistar rats | Dry eye disease (DED) model induced by exorbital lacrimal gland excision | Eye drops | 0.05% and 0.5% Polydatin eye drops | Three times daily for 7 days | To investigate the therapeutic effect of Polydatin on dry eye disease. Results showed that Polydatin significantly restored tear volume, improved corneal irregularity and conjunctival goblet cell density, and inhibited NLRP3 inflammasome expression. | Nutrients. 2019 Nov 15;11(11):2792 |
Mice | Subarachnoid hemorrhage model | Intraperitoneal injection | 10, 20, and 30 mg/kg | Single dose, lasting 24 hours | PD significantly reduced brain edema and Evans blue extravasation after SAH, improving neurological function. | Front Pharmacol. 2024 Sep 4;15:1450238 |
Mice | Db/db mouse model | Oral | 100 mg/kg | Once daily for 5 weeks | To investigate the improvement effect of polydatin on diabetes-induced hyposalivation. Results showed that polydatin ameliorated hypofunction of the salivary gland and inhibited diabetes-related salivary cell injury. | Pharmaceutics. 2021 Dec 27;14(1):51 |
Db/db mice | Type 2 diabetes model | Gavage | 100 mg/kg | 6 days per week for 4 weeks | In the db/db mice model, we found that polydatin markedly enhanced GCK and LDLR protein levels, and inhibited PCSK9 expression in the liver. | Cardiovasc Diabetol. 2016 Feb 1;15:19 |
Nude mice (BALB/c) | Cervical cancer xenograft model | Injection | 100 mg/kg | Once daily for about 3 weeks | To evaluate the inhibitory effect of PD on tumor growth, results showed that PD significantly inhibited tumor growth | Front Cell Dev Biol. 2021 Apr 12;9:587218 |
C57BL/6 mice | STZ-induced diabetic mouse model | Gavage | 100 mg/kg | 6 days a week for 12 weeks | Polydatin improved renal function and fibrosis in diabetic mice by restoring Cx32 expression and reducing Nox4 expression | Acta Pharmacol Sin. 2020 Dec;41(12):1587-1596. |
Guinea pigs | Cisplatin-induced hearing loss model | Intraperitoneal injection | 20 mg/kg, 40 mg/kg, 80 mg/kg | Once daily for 3 days | Polydatin reduces cisplatin-induced hearing loss and hair cell damage by activating the Nrf2/HO-1 signaling pathway | Front Pharmacol. 2022 Aug 4;13:887833 |
C57BL/6 mice | AOM/DSS-induced CRC model | Intraperitoneal injection | 25mg/kg | Once a week, total of 4 times | To evaluate the therapeutic effects of PD combined with IR in a CRC mouse model. Results showed that PD combined with IR significantly prolonged survival time, reduced tumor number and volume, inhibited tumor cell proliferation and promoted apoptosis. | Int J Biol Sci. 2019 Jan 1;15(2):430-440. |
Pig | Intrauterine growth retardation (IUGR) model | Dietary supplementation | 250 mg/kg | From 21 to 35 days of age, lasting for 14 days | To evaluate the protective effects of polydatin against liver injury and mitochondrial dysfunction induced by IUGR. Polydatin decreased hepatic apoptotic rate, improved mitochondrial damage features, inhibited mitochondrial swelling and superoxide anion formation, and preserved mitochondrial membrane potential. Concurrently, polydatin promoted mitochondrial biogenesis, increased SIRT1 activity, and upregulated the expression levels of several genes related to mitochondrial function and fitness. Polydatin also facilitated mitochondrial oxidative metabolism with a beneficial outcome of increased energy production. Furthermore, polydatin mitigated the IUGR-induced reduction in Mn-SOD activity and prevented the excessive accumulation of oxidative damaging products in the liver. | Antioxidants (Basel). 2022 Mar 30;11(4):666 |
C57BL/6 mice | CLP-induced sepsis model | Tail vein injection | 30 mg/kg | Single dose, 2 hours before CLP surgery | To evaluate the protective effect of Polydatin on sepsis-induced acute kidney injury, results showed that Polydatin significantly reduced renal tubular damage scores and serum BUN, Scr levels | Cell Death Dis. 2021 Feb 26;12(2):217 |
Sprague-Dawley rats | Lateral fluid percussion brain injury model | Intraperitoneal injection | 30 mg/kg | Immediately after TBI | Polydatin protects neuronal mitochondria by upregulating SIRT1 expression and activity, inhibiting the p38 phosphorylation-mediated mitochondrial apoptotic pathway, thereby alleviating secondary brain injury after traumatic brain injury | Neural Regen Res. 2019 Sep;14(9):1573-1582 |
Sprague-Dawley rats | Permanent middle cerebral artery occlusion (MCAO) model | Intraperitoneal injection | 30 mg/kg | The first dose was administered 30 min before ischemia, and the second dose was administered within 1 h after ischemia | Polydatin treatment reduced the infarction volume and mitigated the neurobehavioral deficits, sequentially rescued neuronal apoptosis. Ischemic stroke induced an elevation of neuroinflammation and reactive oxygen species, which could be attenuated by polydatin via the reduced activation of p38 mitogen-activated protein kinase and c-Jun N-terminal kinase. In addition, polydatin upregulated the endogenous antioxidant nuclear factor erythroid 2-related factor 2, heme oxygenase-1, the thioredoxin pathway, and eventually reversed ischemic-stroke-induced elevation of ROS and inflammation in ischemic cortical tissue. | Front Pharmacol. 2019 Jun 26;10:663 |
C57BL/6 mice | DSS-induced ulcerative colitis model | Gavage | 30 mg/kg/day | Once daily for 7 days | To evaluate the protective effect of PD on DSS-induced ulcerative colitis, results showed that PD significantly reduced colon length shortening, decreased disease activity index (DAI) scores, and alleviated intestinal mucosal morphological damage | Front Pharmacol. 2025 Jan 14;15:1513020 |
Balb/c mice | CPP crystal-induced arthritis model | Gavage | 40 mg/kg | Prophylactic model: administered at 24, 15 and 1 h before and 1, 6 and 24 h after crystal injection; Therapeutic model: administered 1, 6 and 24 h after crystal injection | Prophylactic PD treatment significantly reduced ankle swelling after 48 h from crystal injection, decreased leukocyte infiltration, necrosis, edema, and synovitis, and reduced circulating levels of IL-1? and CXCL1 as well as their tissue expression; therapeutic PD administration did not show any beneficial effects | Nutrients. 2021 Mar 13;13(3):929 |
C57BL/6 mice | Bleomycin-induced pulmonary fibrosis model | Intragastric administration | 40 mg/kg | Once per day for four weeks | To investigate the effect and mechanism of polydatin on BLM-induced pulmonary fibrosis. Results showed that polydatin effectively reduced fibrosis, decreased levels of inflammatory factors TNF-α, LPS, IL-6, and IL-1β, and altered gut microbiota composition. | J Cell Mol Med. 2023 Dec;27(23):3717-3728 |
Sprague-Dawley rats | Ovariectomy-induced osteoporotic bone defect rat model | Intragastric administration | 40 mg/kg/day | Once daily for 4 weeks | POL accelerated osteoporotic bone repair by activating PI3K/AKT/GSK-3β/β-catenin pathway, enhancing osteogenesis and angiogenesis | Int J Surg. 2025 Jan 1;111(1):411-425. |
C57BL/6 mice | Methionine-choline deficient (MCD) diet-induced NASH and liver fibrosis model | Intraperitoneal injection | 5 mg/kg | Every other day for 4 weeks | Polydatin treatment significantly reduced serum ALT and AST levels, hepatic lipid deposition, oxidative stress, inflammation, and fibrosis in MCD diet-fed mice. | Int J Biol Sci. 2018 Jul 30;14(11):1411-1425 |
BALB/c nude mice | H460 xenograft model | Intraperitoneal injection | 50 mg/kg PD every two days | Every two days for two weeks | Combined treatment with PD and cisplatin significantly inhibited tumor growth | Int J Oncol. 2024 Aug;65(2):77 |
Sprague-Dawley rats | Fructose-induced liver fibrosis model | Oral | 7.5, 15, 30 mg/kg | Once daily for 11 weeks | To investigate the effect of Polydatin on fructose-induced liver fibrosis in rats. Results showed that Polydatin significantly alleviated liver fibrosis, decreased serum concentrations of insulin, TG, IL-1β and TNF-α, improved insulin resistance, and reduced liver fibrotic area. | J Cell Mol Med. 2020 Nov;24(22):13208-13222 |
Sprague-Dawley rats | High fructose diet-induced kidney injury model | Intragastric gavage | 7.5, 15, 30 mg/kg | Once daily for 7 weeks | Polydatin attenuated high fructose-induced podocyte oxidative stress and injury by suppressing HIF-1α/NOX4 pathway, improving renal function. | Pharmaceutics. 2022 Oct 16;14(10):2202 |
Tags: Polydatin | Piceid | Autophagy | Apoptosis | Mitophagy | Mitochondrial Autophagy | 27208-80-6 |
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H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
H335 | May cause respiratory irritation |
H336 | May cause drowsiness or dizziness |
H340 | May cause genetic defects |
H341 | Suspected of causing genetic defects |
H350 | May cause cancer |
H351 | Suspected of causing cancer |
H360 | May damage fertility or the unborn child |
H361 | Suspected of damaging fertility or the unborn child |
H361d | Suspected of damaging the unborn child |
H362 | May cause harm to breast-fed children |
H370 | Causes damage to organs |
H371 | May cause damage to organs |
H372 | Causes damage to organs through prolonged or repeated exposure |
H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
Code | Phrase |
H400 | Very toxic to aquatic life |
H401 | Toxic to aquatic life |
H402 | Harmful to aquatic life |
H410 | Very toxic to aquatic life with long-lasting effects |
H411 | Toxic to aquatic life with long-lasting effects |
H412 | Harmful to aquatic life with long-lasting effects |
H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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