2. Metabolic Enzyme/Protease Membrane Transporter/Ion Channel
  3. Cytochrome P450 P-glycoprotein
  4. Polyphyllin H

Polyphyllin H is a steroidal saponin. Polyphyllin H is isolated from Paris polyphylla. 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). Polyphyllin H downregulates the expression of ABCB1 and ABCC3. Polyphyllin H binds to membrane cholesterol and disrupts lipid raft structures. Polyphyllin H restores the sensitivity of paclitaxel-resistant breast cancer cells to paclitaxel.

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Polyphyllin H

Polyphyllin H Chemical Structure

CAS No. : 81917-50-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
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10 mg In-stock
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Based on 1 publication(s) in Google Scholar

Polyphyllin H Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Polyphyllin H

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Polyphyllin H is a steroidal saponin. Polyphyllin H is isolated from Paris polyphylla. 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). Polyphyllin H downregulates the expression of ABCB1 and ABCC3. Polyphyllin H binds to membrane cholesterol and disrupts lipid raft structures. Polyphyllin H restores the sensitivity of paclitaxel-resistant breast cancer cells to paclitaxel[1][2].

IC50 & Target[1]

CYP1A2

6.44 μM (IC50)

CYP2D6

13.88 μM (IC50)

CYP3A4

4.52 μM (IC50)

In Vitro

Polyphyllin H (0-100 μM; 1 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) in pooled HLMs in a concentration-dependent manner[1].
Polyphyllin H (5-50 μM) specifically binds to cholesterol-containing membranes and induces calcein release in a dose-dependent manner, whereas it has no effect on cholesterol-free membranes[2].
Polyphyllin H (100-300 μM) binds directly to cholesterol in a concentration-dependent manner, which is evidenced by the enhanced fluorescence intensity of DHE[2].
Polyphyllin H (1 μM; 48 h) reverses paclitaxel resistance in MCF-7/PTX cells and reduces the IC50 of paclitaxel to 119.229 nM[2].
Polyphyllin H (1-2 μM) disrupts the plasma membrane integrity of MCF-7/PTX cells in a concentration-dependent manner in vitro[2].
Polyphyllin H (1 μM; 48 h) downregulates the protein expression of efflux transporters in MCF-7/PTX cells[2].
Polyphyllin H (1-2 μM) disrupts the plasma membrane integrity of MCF-7/PTX cells in a concentration-dependent manner in vitro[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Polyphyllin H Related Antibodies

Cell Cytotoxicity Assay[2]

Cell Line: paclitaxel-resistant MCF-7/PTX human breast cancer cells
Concentration: 1 μM (in combination with paclitaxel); 200 μM exogenous cholesterol (co-incubated with 1 μM Polyphyllin H and paclitaxel)
Incubation Time: 48 h
Result: Reduced the IC50 of paclitaxel in MCF-7/PTX cells to 119.229 nM, resulting in a resistance reversal fold of 5.5.
Had this effect significantly attenuated by addition of exogenous cholesterol.

Western Blot Analysis[2]

Cell Line: paclitaxel-resistant MCF-7/PTX human breast cancer cells
Concentration: 1 μM; 200 μM exogenous cholesterol (co-incubated with 1 μM Polyphyllin H)
Incubation Time: 48 h
Result: Significantly reduced protein expression levels of lipid raft marker CAV-1, and efflux transporters ABCB1 and ABCC3 in MCF-7/PTX cells.
Had this downregulation partially restored by co-treatment with exogenous cholesterol.
In Vivo

Polyphyllin H (2.5 mg/kg; i.p.; every 2 days; 21 days) alone reduces tumor growth and tumor cholesterol levels in paclitaxel-resistant breast cancer xenografts, and when combined with paclitaxel (5 mg/kg; i.v.; every 2 days; 21 days), achieves an ~80% tumor inhibition rate by downregulating tumor cholesterol levels and lipid raft-associated ABC transporter expression, with good biosafety[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude (female, 4 weeks old)[2]
Dosage: 2.5 mg/kg (monotherapy); 2.5 mg/kg + 5 mg/kg paclitaxel (combination therapy)
Administration: i.p.; every 2 days; 21 days (monotherapy); i.p. (Polyphyllin H) + i.v. (paclitaxel); every 2 days; 21 days (combination therapy)
Result: Reduced tumor volume and weight compared to the control group.
Reduced total cholesterol levels in tumor tissue compared to the control and paclitaxel-only groups.
Achieved an ~80% tumor inhibition rate (based on final tumor volume), significantly higher than the 55% inhibition rate of lovastatin plus paclitaxel.
Significantly reduced total cholesterol levels in tumor tissue compared to lovastatin plus paclitaxel.
Markedly downregulated protein expression of CAV-1, ABCB1, and ABCC3 in tumor tissue to a greater degree than lovastatin plus paclitaxel.
Caused no significant pathological changes in heart, liver, spleen, lungs, or kidneys of treated mice.
Molecular Weight

871.02

Formula

C44H70O17
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@@]([C@](O[C@]1(OC2)CC[C@H]2C)([H])C[C@@]3([H])[C@@](CC=C(C4)[C@@]5(CC[C@@H]4O[C@H](O[C@@H]6CO)[C@@H]([C@H]([C@@H]6O[C@@H]([C@@H]([C@H]7O)O)O[C@H]7CO)O)O[C@H](O[C@H]8C)[C@@H]([C@@H]([C@H]8O)O)O)C)([H])[C@]5([H])CC9)([C@@H]1C)[C@]39C
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (114.81 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (2.87 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1481 mL 5.7404 mL 11.4808 mL 28.7020 mL
5 mM 0.2296 mL 1.1481 mL 2.2962 mL 5.7404 mL
10 mM 0.1148 mL 0.5740 mL 1.1481 mL 2.8702 mL
15 mM 0.0765 mL 0.3827 mL 0.7654 mL 1.9135 mL
20 mM 0.0574 mL 0.2870 mL 0.5740 mL 1.4351 mL
25 mM 0.0459 mL 0.2296 mL 0.4592 mL 1.1481 mL
30 mM 0.0383 mL 0.1913 mL 0.3827 mL 0.9567 mL
40 mM 0.0287 mL 0.1435 mL 0.2870 mL 0.7175 mL
50 mM 0.0230 mL 0.1148 mL 0.2296 mL 0.5740 mL
60 mM 0.0191 mL 0.0957 mL 0.1913 mL 0.4784 mL
80 mM 0.0144 mL 0.0718 mL 0.1435 mL 0.3588 mL
100 mM 0.0115 mL 0.0574 mL 0.1148 mL 0.2870 mL
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Polyphyllin H Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Polyphyllin H81917-50-2Cytochrome P450P-glycoproteinCYPsP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243ABC transporterCYP1A2paclitaxel-resistant breast cancerABCC3cholesterolMCF-7/PTX cellsCYP2D6CYP3A4cytochrome P450Inhibitorinhibitorinhibit

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