1. Apoptosis Immunology/Inflammation
  2. Apoptosis Pyroptosis
  3. Polyphyllin VI

Polyphyllin VI, an active saponin, possess anti-cancer activities. Polyphyllin VI induces G2/M cell cycle arrest and triggers apoptosis. Polyphyllin VI induces caspase-1-mediated pyroptosis via the induction of ROS/NF-κB/NLRP3/GSDMD signal axis in non-small cell lung cancer.

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Polyphyllin VI Chemical Structure

Polyphyllin VI Chemical Structure

CAS No. : 55916-51-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 257 In-stock
Solution
10 mM * 1 mL in DMSO USD 257 In-stock
Solid
5 mg USD 100 In-stock
10 mg USD 160 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Polyphyllin VI:

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Polyphyllin VI, an active saponin, possess anti-cancer activities. Polyphyllin VI induces G2/M cell cycle arrest and triggers apoptosis. Polyphyllin VI induces caspase-1-mediated pyroptosis via the induction of ROS/NF-κB/NLRP3/GSDMD signal axis in non-small cell lung cancer[1][2][3].

Cellular Effect
Cell Line Type Value Description References
HL-60 IC50
5.2 μg/mL
Compound: 5
Cytotoxicity against human HL60 cells by MTT assay
Cytotoxicity against human HL60 cells by MTT assay
[PMID: 11000027]
In Vitro

Polyphyllin VI (0-16 μM; 48 h) significantly decreases the viability of A549, NCI-H1299 and HepaRG cells in a dose-dependent manner[1][2].
Polyphyllin VI (0.5-2 μM-1 μM; 24 h) significantly increases the percentage of A549, and NCI-H1299 cells in the G2/M stage in a dose-dependent manner[1].
Polyphyllin VI (0-12 μM-1 μM; 24 h) arrests HepaRG cells at S stage [2].
Polyphyllin VI (0-6 μM-1 μM; 24 h) activates the NLRP3 inflammasome[3].
Polyphyllin VI (0-6 μM-1 μM; 24 h) induces pyroptosis via ROS/NF-κB pathway om A549 and NCI-H1299 cells[3].

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

Cell Viability Assay[1][3]

Cell Line: A549, NCI-H1299, and HepaRG cells
Concentration: 0 μM, 2.5 μM, 5.0 μM, 7.5 μM, 10 μM, 12.5 μM (A549, NCI-H1299), 0 μM, 2 μM, 4.0 μM, 6.0 μM, 8.0 μM, 10.0 μM, 12.0 μM, 16.0 μM (HepaRG)
Incubation Time: 48 h (A549, NCI-H1299), 24 h and 48 h (HepaRG)
Result: Showed the IC50 value in NCI-H1299 cells after 48h treatment was 1.87±0.09 μM, 1.59±0.12 μM in A549[1].
Demonstrated the reduction of HepaRG cell viability ranged from 88.90% to 1.07% after 24 h, and from 79.06% to 0.71% after 48 h[2].

Cell Viability Assay[1]

Cell Line: A549, NCI-H1299 cells
Concentration: 0.5 μM, 1.0 μM, 2.0 μM
Incubation Time: 24 h
Result: Showed those of A549 cells in G2/M phase were 25.14%±3.31%, 28.40%±4.63%, and 42.66%±1.30%, and NCI-H1299 cells were 27.99%±4.68%, 30.24%±3.61% and 38.51%±5.10% after treatment with 0.5, 1, and 2μM for 24 h, respectively.

Cell Cycle Analysis[2]

Cell Line: HepaRG cells
Concentration: 0 μM, 2.0 μM, 4.0 μM, 6.0 μM, 8.0 μM, 12.0 μM
Incubation Time: 24 h
Result: Resulted the ratios of cells in the S and G0/G1 phase changed from 23.62%±0.14% to 34.01%±0.32%, 66.88%±1.15% to 54.00%±0.71%, respectively.

Western Blot Analysis[3]

Cell Line: A549, NCI-H1299 cells
Concentration: 0 μM, 3 μM, 4 μM, 5 μM, 6 μM
Incubation Time: 24 h
Result: Resulted dose-dependently increasing the protein expression of NLRP3 and ASC, and the cleaved form of caspase-1, IL-1β, IL-18 and GSDMD in A549 and NCI-H1299 cells.

Immunofluorescence[3]

Cell Line: A549, NCI-H1299 cells
Concentration: 0 μM, 3 μM, 4 μM, 5 μM, 6 μM
Incubation Time: 24 h
Result: Resulted the expression of caspase-1 was significantly inhibited by N-acetyl-L-cysteine (NAC) in Polyphyllin VI -treated A549 and NCI-H1299 cells.
In Vivo

Polyphyllin VI (2-4 mg/kg; i.p.; five times a week for 4 weeks) inhibits the growth of lung cancer tumor xenografts[1].
Polyphyllin VI (2.5-10 mg/kg; i.p.; 10 consecutive days) activates NLRP3 inflammasome in A549-bearing athymic nude mice[3].

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

Animal Model: A549 tumor xenografts subcutaneously inoculated into the right flank of the nude mice[1]
Dosage: 2 mg/kg, 3 mg/kg, 4 mg/kg
Administration: Intraperitoneal Injection (i.p.)
Result: Resulted the reduction of tumor volume to 25.63%, 41.71%, and 40.41%, respectively, after 2 mg/kg, 3 mg/kg and 4 mg/kg treatment.
Animal Model: A549 tumor xenografts subcutaneously inoculated into the right flank of the nude mice[3]
Dosage: 2.5 mg/kg, 5 mg/kg, 10 mg/kg
Administration: Intraperitoneal Injection (i.p.)
Result: Showed the expression of NLRP3, caspase-1, IL-1β and GSDMD was increasing in a dose manner.
Molecular Weight

738.90

Formula

C39H62O13

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@]1([C@@]2([H])O[C@]3(CC[C@@H](C)CO3)[C@H]1C)[C@]([C@@]4([H])C2)(CC[C@@]5([H])[C@@]4([H])CC=C6[C@@]5(CC[C@H](O[C@@](O[C@H](CO)[C@@H](O)[C@@H]7O)([H])[C@@H]7O[C@@](O[C@@H](C)[C@H](O)[C@H]8O)([H])[C@@H]8O)C6)C)C

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (135.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3534 mL 6.7668 mL 13.5336 mL
5 mM 0.2707 mL 1.3534 mL 2.7067 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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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: ≥ 1 mg/mL (1.35 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (1.35 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: 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

Purity: 98.41%

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.3534 mL 6.7668 mL 13.5336 mL 33.8341 mL
5 mM 0.2707 mL 1.3534 mL 2.7067 mL 6.7668 mL
10 mM 0.1353 mL 0.6767 mL 1.3534 mL 3.3834 mL
15 mM 0.0902 mL 0.4511 mL 0.9022 mL 2.2556 mL
20 mM 0.0677 mL 0.3383 mL 0.6767 mL 1.6917 mL
25 mM 0.0541 mL 0.2707 mL 0.5413 mL 1.3534 mL
30 mM 0.0451 mL 0.2256 mL 0.4511 mL 1.1278 mL
40 mM 0.0338 mL 0.1692 mL 0.3383 mL 0.8459 mL
50 mM 0.0271 mL 0.1353 mL 0.2707 mL 0.6767 mL
60 mM 0.0226 mL 0.1128 mL 0.2256 mL 0.5639 mL
80 mM 0.0169 mL 0.0846 mL 0.1692 mL 0.4229 mL
100 mM 0.0135 mL 0.0677 mL 0.1353 mL 0.3383 mL
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  • 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.

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Polyphyllin VI
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