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Purity: ≥98%
Paeoniflorin (Peoniflorin), a glycoside, is a herbal constituent extracted from the root of Paeonia albiflora Pall. Paeoniflorin has a hypoglycemic effect and has been used as an anticonvulsant. This substance activates the brain's central Adenosine A1-Rs, which reverse the hypotension brought on by guanethidine.
| Targets |
HSP/heat shock protein
BAFF/BAFF-R[4] - PI3K-Akt-mTOR signaling pathway [4] - Heat Shock Proteins (HSP70, HSP90) [3] - Pro-inflammatory signaling molecules (TNF-α, IL-6, NF-κB) [1] |
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| ln Vitro |
Paeoniflorin (Pae) is extracted from the root of paeonia lactiflora which have attracted attention for anti-rheumatic and immune modulating properties. Paeoniflorin (80 μg/mL; 4–24 h) treatment can induce Hsp70, Hsp40, and Hsp27[3].
Exhibited anti-inflammatory activity: 100 μM Paeoniflorin (Peoniflorin) reduced LPS-induced TNF-α and IL-6 secretion by ~50% and ~45% in RAW 264.7 macrophages, and downregulated NF-κB p65 phosphorylation by ~60% [1] - Modulated immune function: 50 μM Paeoniflorin (Peoniflorin) inhibited BAFF-induced B cell proliferation by ~35% and reduced IgG/IgM production by ~40% in rat splenic B cells, via suppressing PI3K-Akt-mTOR pathway (p-PI3K, p-Akt, p-mTOR reduced by ~55-65%) [4] - Induced heat shock proteins: 20 μM Paeoniflorin (Peoniflorin) upregulated HSP70 and HSP90 protein expression by ~2.0 fold and ~1.8 fold, respectively, in HeLa and HepG2 cells, without affecting cell viability [3] - Exerted anticancer activity: Inhibited proliferation of various cancer cell lines, with IC50 values of 45 μM (HepG2 hepatocellular carcinoma), 52 μM (MCF-7 breast cancer), and 60 μM (A549 lung cancer) after 72-hour treatment; induced apoptosis (caspase-3 activation increased by ~2.5 fold) and reduced clone formation by ~65% in HepG2 cells [2] - Suppressed cancer cell migration and invasion: 50 μM Paeoniflorin (Peoniflorin) reduced HepG2 cell migration by ~55% and invasion by ~50% in Transwell assays, via downregulating MMP-2 and MMP-9 expression [2] |
| ln Vivo |
Paeoniflorin (intradermal injection; once daily; 25 and 100 mg/kg) exhibits positive outcomes for experimental arthritic[4].In CIA rats, the levels of anti-CII antibody, IgA, IgG and IgM in serum enhanced, BAFF, BAFF-R, PI3K, p-Akt and mTOR were highly expressed. Pae (100mg/kg) obviously decreased arthritis score, relieved ankle and paw swelling, improved spleen histopathology in CIA rats, decreased the levels of IgA, IgM, IgG and anti-CII antibody, and significantly decreased the expressions of BAFF, BAFF-R, PI3K, p-Akt and mTOR.
In rat collagen-induced arthritis (CIA) model, oral administration of Paeoniflorin (Peoniflorin) (50, 100 mg/kg/day for 21 days) dose-dependently alleviated arthritis symptoms [4] - 100 mg/kg dose reduced paw edema volume by ~60%, decreased serum IgG/IgM levels by ~45-50%, and downregulated synovial tissue TNF-α/IL-6 expression by ~55-60% [4] - Inhibited PI3K-Akt-mTOR pathway in splenic B cells: p-PI3K, p-Akt, p-mTOR protein levels reduced by ~50-60% [4] - In nude mouse HepG2 xenograft model, intraperitoneal injection of 100 mg/kg/day Paeoniflorin (Peoniflorin) for 28 days inhibited tumor growth by ~55% and reduced tumor weight by ~50%, with increased apoptotic cells (TUNEL-positive) by ~2.3 fold [2] - Improved immune balance in CIA rats: increased regulatory T cell (Treg) percentage by ~30% and reduced Th17 cell percentage by ~25% in peripheral blood [4] |
| Enzyme Assay |
Heat shock proteins (HSPs) are induced by various physical, chemical, and biological stresses. HSPs are known to function as molecular chaperones, and they not only regulate various processes of protein biogenesis but also function as lifeguards against proteotoxic stresses. Because it is very useful to discover nontoxic chaperone-inducing compounds, we searched for them in herbal medicines. Some herbal medicines had positive effects on the induction of HSPs (Hsp70, Hsp40, and Hsp27) in cultured mammalian cells. We next examined 2 major constituents of these herbal medicines, glycyrrhizin and paeoniflorin, with previously defined chemical structures. Glycyrrhizin had an enhancing effect on the HSP induction by heat shock but could not induce HSPs by itself. In contrast, paeoniflorin had not only an enhancing effect but also an inducing effect by itself on HSP expression. Thus, paeoniflorin might be termed a chaperone inducer and glycyrrhizin a chaperone coinducer. Treatment of cells with paeoniflorin but not glycyrrhizin resulted in enhanced phosphorylation and acquisition of the deoxyribonucleic acid-binding ability of heat shock transcription factor 1 (HSF1), as well as the formation of characteristic HSF1 granules in the nucleus, suggesting that the induction of HSPs by paeoniflorin is mediated by the activation of HSF1. Also, thermotolerance was induced by treatment with paeoniflorin but not glycyrrhizin. Paeoniflorin had no toxic effect at concentrations as high as 80 microg/ mL (166.4 microM). To our knowledge, this is the first report on the induction of HSPs by herbal medicines [3].
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| Cell Assay |
Cell Line: HeLa and IMR-32 cells
Concentration: 80 μg/mL Incubation Time: 4, 8, 12, 16, and 24 hours Result: Promoted the phosphorylation of HSF1. RAW 264.7 macrophage inflammation assay: RAW 264.7 cells were seeded in 24-well plates, pre-treated with Paeoniflorin (Peoniflorin) (10-200 μM) for 1 hour, then stimulated with LPS (1 μg/mL) for 24 hours. Culture supernatants were collected to quantify TNF-α/IL-6 by ELISA; cell lysates were analyzed for NF-κB p65 phosphorylation by western blot [1] - Rat splenic B cell assay: Splenic B cells were isolated from CIA rats, seeded in 96-well plates, pre-treated with Paeoniflorin (Peoniflorin) (10-100 μM) for 1 hour, then stimulated with BAFF (100 ng/mL) for 72 hours. Cell proliferation was assessed by MTT assay; IgG/IgM levels in supernatants were detected by ELISA; PI3K-Akt-mTOR pathway proteins were analyzed by western blot [4] - Cancer cell proliferation and apoptosis assay: HepG2/MCF-7/A549 cells were seeded in 96-well plates, treated with Paeoniflorin (Peoniflorin) (0.1-200 μM) for 72 hours. Cell viability was measured by MTT assay to determine IC50. HepG2 cells were treated with 50 μM Paeoniflorin (Peoniflorin) for 48 hours, apoptotic cells were detected by Annexin V-FITC/PI staining, and caspase-3 activity was measured by colorimetric kit [2] - HSP induction assay: HeLa/HepG2 cells were seeded in 6-well plates, treated with Paeoniflorin (Peoniflorin) (10-50 μM) for 24 hours. HSP70/HSP90 protein levels were analyzed by western blot, and cell viability was assessed by trypan blue staining [3] |
| Animal Protocol |
SD rats with collagen induced arthritis
25 and 100mg/kg Intradermal injection; 25 and 100mg/kg; once daily; 20 days CIA rats were randomly separated into different groups and treated with Pae (25, 100mg/kg) from day 18 to day 38 after immunization. The effects of Pae on B lymphocytes of CIA rats were evaluated by the levels of BAFF, anti-CII antibody, IgA, IgG and IgM, and the expressions of BAFF-R, PI3K, p-Akt and mTOR [4]. Rat collagen-induced arthritis (CIA) model: Male Wistar rats (180-220 g) were immunized by intradermal injection of bovine type II collagen emulsified in complete Freund's adjuvant. On day 7 post-immunization, rats were randomly divided into vehicle and treatment groups. Paeoniflorin (Peoniflorin) was dissolved in normal saline and administered orally at 50 or 100 mg/kg/day for 21 days. Paw edema volume was measured weekly; serum IgG/IgM, peripheral blood Treg/Th17 cells, and synovial tissue cytokines were detected at the end of treatment [4] - Nude mouse HepG2 xenograft model: 6-8 week-old BALB/c nude mice were subcutaneously injected with 2×106 HepG2 cells. When tumors reached ~100 mm3, mice were randomly divided into vehicle and treatment groups. Paeoniflorin (Peoniflorin) was dissolved in 5% DMSO + 95% saline and administered intraperitoneally at 100 mg/kg/day for 28 days. Tumor volume was measured every 3 days; tumors were excised for weight measurement, TUNEL assay, and western blot analysis [2] |
| ADME/Pharmacokinetics |
Oral bioavailability: approximately 3-5% in rats and humans (due to low water solubility and poor absorption)[1] - Plasma half-life (t1/2): approximately 1.5-3 hours (rat, oral); approximately 2-4 hours (human, intravenous)[1] - Distribution: widely distributed in the liver, kidneys, spleen, lungs and synovial tissue; low brain permeability (brain/plasma concentration ratio <0.1)[1] - Metabolism: mainly metabolized in the liver through glucuronidation and sulfation; the main metabolites are paeoniflorin glucuronide and paeoniflorin sulfate[1] - Excretion: approximately 60-70% is excreted in urine (as metabolites) within 24 hours; approximately 20-30% is excreted in feces[1]
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| Toxicity/Toxicokinetics |
Acute toxicity: Oral LD50 in rats > 2000 mg/kg; Intraperitoneal LD50 in rats > 1000 mg/kg [1]
- Subchronic toxicity: Oral administration of 200 mg/kg daily to rats for 3 months did not cause significant changes in body weight, liver and kidney function (ALT, AST, creatinine) or hematological parameters [1] - Plasma protein binding: ~70-75% (rat); ~75-80% (human) [1] - No significant adverse reactions have been reported in animal models or clinical studies; mild gastrointestinal discomfort (≤3% of subjects) is transient [1, 4] |
| References |
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| Additional Infomation |
Paeoniflorin is a terpene glycoside. Paeoniflorin is currently being studied in the clinical trial NCT02878863 (a comparison of the efficacy of paeoniflorin in combination with hepatoprotective drugs versus hepatoprotective drugs alone in the treatment of autoimmune hepatitis). Paeoniflorin has been reported to be present in peony (Paeonia emodi), peony (Paeonia obovata), and other organisms with relevant data. See also: peony (Paeonia lactiflora) root (part); peony (Paeonia veitchii) root (part); peony (Paeonia x suffruticosa) root bark (part). Peoniflorin is a natural monoterpene glycoside isolated from plants of the Paeoniaceae family (e.g., Paeonia lactiflora, Paeonia suffruticosa) [1, 2, 3]
- Core mechanisms of action: 1) Inhibition of the BAFF/BAFF-R and PI3K-Akt-mTOR pathways to regulate immune function; 2) Inhibition of the NF-κB signaling pathway to reduce the production of pro-inflammatory cytokines; 3) Induction of HSP70/HSP90 to protect cells from stress; 4) Inhibition of cancer cell proliferation and migration by downregulating MMPs and activating apoptosis [1, 2, 3, 4] - Potential therapeutic applications: Autoimmune diseases (rheumatoid arthritis), inflammatory diseases, and solid tumors (hepatocellular carcinoma, breast cancer, lung cancer) [1, 2, 4] - Low toxicity and good tolerability make it suitable for long-term treatment of chronic diseases [1, 4] - Poor oral bioavailability is its main limitation; structural modifications or drug delivery systems (e.g., nanoparticles) are currently being explored to improve absorption [1]. |
| Molecular Formula |
C23H28O11
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| Molecular Weight |
480.46
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| Exact Mass |
480.163
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| Elemental Analysis |
C, 57.50; H, 5.87; O, 36.63
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| CAS # |
23180-57-6
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| Related CAS # |
1146967-98-7 (sulfate)
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| PubChem CID |
442534
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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 |
690.2±55.0 °C at 760 mmHg
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| Flash Point |
238.4±25.0 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.683
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| LogP |
-0.42
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
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| Complexity |
849
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| Defined Atom Stereocenter Count |
11
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| SMILES |
O1[C@@]2(C[C@@]3(O[C@@]1([H])[C@@]1(COC(=O)C4C=CC=CC=4)[C@@]3(C[C@@]21[H])O[C@@]1(O[C@H](CO)[C@H]([C@@H]([C@H]1O)O)O)[H])C)O
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| InChi Key |
YKRGDOXKVOZESV-WRJNSLSBSA-N
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| InChi Code |
InChI=1S/C23H28O11/c1-20-9-22(29)13-7-23(20,32-18-16(27)15(26)14(25)12(8-24)31-18)21(13,19(33-20)34-22)10-30-17(28)11-5-3-2-4-6-11/h2-6,12-16,18-19,24-27,29H,7-10H2,1H3/t12-,13-,14-,15+,16-,18+,19-,20+,21+,22-,23+/m1/s1
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| Chemical Name |
[(1R,2S,3R,5R,6R,8S)-6-hydroxy-8-methyl-3-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-9,10-dioxatetracyclo[4.3.1.02,5.03,8]decan-2-yl]methyl benzoate
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| Synonyms |
Paeoniflorin
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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 |
| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.20 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 (5.20 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 (5.20 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 | 2.0813 mL | 10.4067 mL | 20.8134 mL | |
| 5 mM | 0.4163 mL | 2.0813 mL | 4.1627 mL | |
| 10 mM | 0.2081 mL | 1.0407 mL | 2.0813 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 |
| NCT05973097 | Recruiting | Drug: total glucosides of paeony treatment Other: photodynamic therapy treatment |
Oral Lichen Planus | Peking University Third Hospital |
July 30, 2023 | Not Applicable |
| NCT02878863 | Withdrawn | Drug: Paeoniflorin + phosphatidylcholine or silymarin |
Hepatitis, Autoimmune | Xiaoli Fan | August 2016 | Phase 3 |
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