| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Polyphyllin H potently inhibits the activities of CYP1A2 (IC50 = 6.44 µM, competitive), CYP2D6 (IC50 = 13.88 µM, competitive) and CYP3A4 (IC50 = 4.52 µM, non-competitive, time-dependent). It downregulates the expression of ABCB1 and ABCC3, binds to membrane cholesterol and disrupts lipid raft structures. Additionally, it targets P-glycoprotein and has been identified as a potential "Q-marker" for antiplatelet aggregation activity.
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| ln Vitro |
Polyphyllin H has demonstrated significant anti-inflammatory properties and exhibits a reparative effect on the skin barrier, surpassing the efficacy of dexamethasone in certain experimental models. It restores the sensitivity of paclitaxel-resistant breast cancer cells to paclitaxel. As a bioactive natural product, it inhibits tumor cell proliferation and induces apoptosis through modulation of PI3K/Akt and NF-κB signaling pathways.
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| ln Vivo |
In vivo studies have shown that Polyphyllin H can be analyzed in beagle dog plasma using liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS), highlighting its detectability and quantifiability. It has been used in studies of inflammation, fractures, and convulsions. The compound exhibits antimicrobial and hemostatic effects in animal models. Further in vivo investigations are ongoing to fully characterize its therapeutic potential and pharmacokinetic properties.
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| Enzyme Assay |
Non-cellular enzyme/receptor binding assays for Polyphyllin H typically employ LC-MS/MS analysis to quantify the compound in biological matrices such as plasma. Cytochrome P450 inhibition assays are conducted using standard fluorogenic or luminogenic substrates to determine IC50 values for CYP1A2, CYP2D6, and CYP3A4. Membrane cholesterol binding can be assessed using lipid raft disruption assays with fluorescent membrane probes. These cell-free systems allow for the characterization of the compound's direct interactions with its molecular targets without the complexity of cellular metabolism.
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| Cell Assay |
Cellular assays for Polyphyllin H typically utilize cancer cell lines to evaluate its antiproliferative and pro-apoptotic effects. Paclitaxel-resistant breast cancer cells are used to assess the compound's ability to restore chemosensitivity. Cells are treated with varying concentrations of Polyphyllin H, and cell viability is measured using MTT or CCK-8 assays. Apoptosis is evaluated through flow cytometry using Annexin V/PI staining, while signaling pathway modulation (PI3K/Akt and NF-κB) is analyzed via Western blotting.
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| Animal Protocol |
In vivo animal studies of Polyphyllin H have been conducted in beagle dogs for pharmacokinetic analysis, where the compound is administered and plasma samples are collected for LC-MS/MS quantification. The compound has also been studied in models of inflammation, fractures, and convulsions. Typical protocols involve oral or intravenous administration, followed by monitoring of therapeutic endpoints such as tumor growth inhibition, inflammatory marker reduction, or seizure suppression.
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| ADME/Pharmacokinetics |
Dosing and administration details for Polyphyllin H in pharmacokinetic studies involve analysis in beagle dog plasma using LC-MS/MS, with the compound being detectable and quantifiable. As a steroidal saponin with high molecular weight (871.02 g/mol), it likely exhibits limited oral bioavailability and may require formulation strategies to enhance absorption. The compound's interaction with CYP450 enzymes suggests potential drug-drug interactions. Comprehensive PK parameters such as half-life, Cmax, and AUC have not been fully characterized in published literature.
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| Toxicity/Toxicokinetics |
Toxicological data for Polyphyllin H are limited, though as a steroidal saponin, it may exhibit concentration-dependent cytotoxicity. The compound's inhibition of CYP450 enzymes (CYP1A2, CYP2D6, CYP3A4) suggests potential for drug-drug interactions and hepatotoxicity concerns at high doses. It has been shown to downregulate ABCB1 and ABCC3 expression, which could affect multidrug resistance and toxicity profiles. Further comprehensive toxicological studies are needed to establish safety margins.
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| References | |
| Additional Infomation |
Reports indicate that Paris polyphylla var. chinensis, Paris mairei, and Paris polyphylla contain parisin H, and relevant data are available for reference.
Polyphyllin H is a natural steroidal saponin primarily used as a research tool in oncology and pharmacology. It has not been approved for clinical use or entered human trials. Its mechanism of action involves inhibition of CYP450 enzymes, downregulation of ABC transporters, and disruption of membrane lipid rafts. The compound is valuable for studying drug resistance mechanisms, particularly in paclitaxel-resistant breast cancer, and for investigating anti-inflammatory and antiplatelet aggregation pathways. |
| Molecular Formula |
C44H70O17
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|---|---|
| Molecular Weight |
871.02
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| Exact Mass |
870.461
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| CAS # |
81917-50-2
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| PubChem CID |
101615586
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| Appearance |
White to off-white solid powder
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| LogP |
0.2
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
61
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| Complexity |
1620
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| Defined Atom Stereocenter Count |
25
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| SMILES |
C[C@@H]1CC[C@@]2([C@H]([C@]3([C@@H](O2)C[C@@H]4[C@@]3(CC[C@H]5[C@H]4CC=C6[C@@]5(CC[C@@H](C6)O[C@H]7[C@@H]([C@H]([C@@H]([C@H](O7)CO)O[C@H]8[C@@H]([C@H]([C@@H](O8)CO)O)O)O)O[C@H]9[C@@H]([C@@H]([C@H]([C@@H](O9)C)O)O)O)C)C)O)C)OC1
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| InChi Key |
DEUSODBYLVUUQI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C44H70O17/c1-19-8-13-43(54-18-19)21(3)44(53)29(61-43)15-26-24-7-6-22-14-23(9-11-41(22,4)25(24)10-12-42(26,44)5)56-40-37(60-38-34(51)32(49)30(47)20(2)55-38)35(52)36(28(17-46)58-40)59-39-33(50)31(48)27(16-45)57-39/h6,19-21,23-40,45-53H,7-18H2,1-5H3
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| Chemical Name |
2-[5-[3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]oxy-4-hydroxy-6-(hydroxymethyl)-2-(8-hydroxy-5',7,9,13-tetramethylspiro[5-oxapentacyclo[10.8.0.02,9.04,8.013,18]icos-18-ene-6,2'-oxane]-16-yl)oxyoxan-3-yl]oxy-6-methyloxane-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 |
| 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: ≥ 100 mg/mL (114.81 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (2.87 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (2.87 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 (2.87 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 | 1.1481 mL | 5.7404 mL | 11.4808 mL | |
| 5 mM | 0.2296 mL | 1.1481 mL | 2.2962 mL | |
| 10 mM | 0.1148 mL | 0.5740 mL | 1.1481 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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