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Polyphyllin VI

Cat No.:V30137 Purity: ≥98%
Polyphyllin VI is an active saponin with anti-cancer effect.
Polyphyllin VI
Polyphyllin VI Chemical Structure CAS No.: 55916-51-3
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
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1mg
5mg
10mg
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Product Description
Polyphyllin VI is an active saponin with anti-cancer effect. Polyphyllin VI induces G2/M cell cycle arrest and triggers apoptosis. Polyphyllin VI induces caspase-1-mediated pyroptosis by inducing the ROS/NF-κB/NLRP3/GSDMD signaling axis in non-small cell lung cancer.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
The viability of A549, NCI-H1299, and HepaRG cells is drastically reduced in a dose-quantitative manner by polyphyllin VI (0-16 μM; 48 hours) [1][2]. The percentage of A549 and NCI-H1299 cells in the G2/M phase is dose-wise considerably increased by polyphyllin VI (0.5-2 μM-1 μM; 24 hours) [1]. HepaRG cells are arrested in the S phase for 24 hours by polyphyllin VI (0-12 μM-1 μM) [2]. In a 24-hour period, Polyphyllin VI (0–6 μM–1 μM) stimulates the NLRP3 signalosome [3]. Through the ROS/NF-κB pathway, Polyphyllin VI (0-6 μM-1 μM; 24 hours) detects A549 and NCI.[3]
ln Vivo
Lung cancer xenograft growth is inhibited by polyphyllin VI (2-4 mg/kg; intraperitoneally; 5 times per week for 4 weeks) [1]. Intraperitoneal injection of Polyphyllin VI (2.5–10 mg/kg) administered over a 10-day period
Cell Assay
Cell viability assay[1][3]
Cell Types: A549, NCI-H1299 and HepaRG cell
Tested Concentrations: 0 μM, 2.5 μM, 5.0 μM, 7.5 μM, 10 μM, -H1299 cell pyroptosis[3]. 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 Duration: 48 hrs (hours) (A549, NCI-H1299), 24 h and 48 h (HepaRG)
Experimental Results: the IC50 value of NCI-H1299 cells after treatment for 48 hrs (hours) was 1.87±0.09 μM, and that of A549 was 1.59±0.12 μM[1]. Studies have shown that HepaRG cell viability diminished by 88.90% to 1.07% after 24 hrs (hours) and by 79.06% to 0.71% after 48 hrs (hours) [2]. Cell viability determination [1]
Cell Types: A549, NCI-H1299 cell
Tested Concentrations: 0.5 μM, 1.0 μM, 2.0 μM
Incubation Duration: 24 h
Experimental Results: The G2/M phase of A549 cells was 25.14%±3.31%, 28.40 0.5, respectively. After 24 hrs (hours) of treatment with 1 and 2 μM, NCI-H1299 cells were %±4.63%, 42.66%±1.30% and 27.99%±4.68%, 30.24%±3.61% and 38.51%±5.10%, respectively.

Cell cycle analysis [2]
Cell Types: HepaRG Cell
Tested Concentrations: 0 μ
Animal Protocol
Animal/Disease Models: A549 tumor xenografts were inoculated subcutaneously (sc) (sc) into the right flank of nude mice [1]
Doses: 2 mg/kg, 3 mg/kg, ) NLRP3 inflammasome is activated in nude mice with A549 tumors [3]. 4 mg/kg
Route of Administration: intraperitoneal (ip) injection
Experimental Results: After treatment with 2 mg/kg, 3 mg/kg and 4 mg/kg, the tumor volume was diminished to 25.63%, 41.71% and 40.41% respectively.

Animal/Disease Models: A549 tumor xenograft tumors were inoculated subcutaneously (sc) (sc) into the right flank of nude mice [3]
Doses: 2.5 mg/kg, 5 mg/kg, 10 mg/kg
Route of Administration: intraperitoneal (ip) injection
Experimental Results: NLRP3, NLRP3 The expression of caspase-1, IL-1β and GSDMD all demonstrated a dose-increasing trend.
References

[1]. Anti-lung Cancer Effects of Polyphyllin VI and VII Potentially Correlate with Apoptosis In Vitro and In Vivo. Phytother Res. 2015 Oct;29(10):1568-76.

[2]. Molecular Mechanisms of Apoptosis in HepaRG Cell Line Induced by Polyphyllin VI via the Fas Death Pathway and Mitochondrial-Dependent Pathway. Toxins (Basel). 2018 May 15;10(5). pii: E201.

[3]. Polyphyllin VI Induces Caspase-1-Mediated Pyroptosis via the Induction of ROS/NF-κB/NLRP3/GSDMD Signal Axis in Non-Small Cell Lung Cancer. Cancers (Basel). 2020 Jan 13;12(1):193.

Additional Infomation
Polyphyllin VI is a steroid saponin.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C39H62O13
Molecular Weight
738.9018
Exact Mass
738.419
CAS #
55916-51-3
Related CAS #
55916-51-3
PubChem CID
10417550
Appearance
White to off-white solid powder
Density
1.4±0.1 g/cm3
Boiling Point
871.2±65.0 °C at 760 mmHg
Flash Point
480.7±34.3 °C
Vapour Pressure
0.0±0.6 mmHg at 25°C
Index of Refraction
1.616
LogP
6.09
Hydrogen Bond Donor Count
7
Hydrogen Bond Acceptor Count
13
Rotatable Bond Count
5
Heavy Atom Count
52
Complexity
1370
Defined Atom Stereocenter Count
21
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)O)O[C@H]8[C@@H]([C@@H]([C@H]([C@@H](O8)C)O)O)O)C)C)O)C)OC1
InChi Key
WHWWQGPCTUQCMN-JDDKMXSSSA-N
InChi Code
InChI=1S/C39H62O13/c1-18-8-13-38(47-17-18)20(3)39(46)27(52-38)15-25-23-7-6-21-14-22(9-11-36(21,4)24(23)10-12-37(25,39)5)49-35-33(31(44)29(42)26(16-40)50-35)51-34-32(45)30(43)28(41)19(2)48-34/h6,18-20,22-35,40-46H,7-17H2,1-5H3/t18-,19+,20-,22+,23-,24+,25+,26-,27+,28+,29-,30-,31+,32-,33-,34+,35-,36+,37+,38-,39-/m1/s1
Chemical Name
(2S,3R,4R,5R,6S)-2-[(2R,3R,4S,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-2-[(1R,2S,4S,5'R,6R,7S,8S,9S,12S,13R,16S)-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
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~135.34 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 1 mg/mL (1.35 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (1.35 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 10.0 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.

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Solubility in Formulation 3: ≥ 1 mg/mL (1.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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
10 mM 0.1353 mL 0.6767 mL 1.3534 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.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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