Art. -Nr.: HY-N2382

Polyphyllin H

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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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Reinheit: 99.89%
CAS. Nr.: 81917-50-2
Formel: C₄₄H₇₀O₁₇
Molecular Weight:871.02

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Polyphyllin H Chemical Structure

CAS. Nr.: 81917-50-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CYP1A2

6.44 μM (IC₅₀)

CYP2D6

13.88 μM (IC₅₀)

CYP3A4

4.52 μM (IC₅₀)

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen :

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.

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.

Chemical Information

CAS. Nr. 81917-50-2
Appearance Solid
Molecular Weight 871.02
Formel C₄₄H₇₀O₁₇
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
- Steroids
Initial Source
- Plants
- other families
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

EMBO Mol Med

AI-identified CD133-targeting natural compounds demonstrate differential anti-tumor effects and mechanisms in pan-cancer models. [Abstract]

2025 Oct 2. PMID: 41039172

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Wang E, et al. Probe substrates assay estimates the effect of polyphyllin H on the activity of cytochrome P450 enzymes in human liver microsomes. Pharmacol Res Perspect. 2024;12(5):e70002. [Content Brief]

[2]. Ye Z, et al. Polyphyllin H Reverses Paclitaxel Resistance in Breast Cancer by Binding Membrane Cholesterol to Inhibit Both ABCB1 and ABCC3. Pharmaceuticals (Basel). 2025;18(11):1699. Published 2025 Nov 9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Polyphyllin H

1 Cited Publications

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Polyphyllin H

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Publications Citing Use of MedChemExpress (MCE) Polyphyllin H

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Polyphyllin H Related Classifications

Art. -Nr.: HY-N2382