| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
Polyphyllin VI targets apoptosis, pyroptosis, and cell cycle pathways. It induces G2/M cell cycle arrest. The compound induces caspase-1-mediated pyroptosis via the ROS/NF-κB/NLRP3/GSDMD signaling axis. It activates the NLRP3 inflammasome and exerts anti-proliferative effects. Polyphyllin VI has anti-cancer activities against non-small cell lung cancer. Its diverse bioactivities include hemostasis, bacteriostasis, and anti-pregnancy effects.
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| 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]
In vitro, Polyphyllin VI induces G2/M cell cycle arrest and triggers apoptosis in cancer cells. It induces caspase-1-mediated pyroptosis via the ROS/NF-κB/NLRP3/GSDMD signal axis in non-small cell lung cancer. The compound activates the NLRP3 inflammasome. It exerts strong inhibitory effects on lung cancer cell growth in vitro. Its anti-cancer activities have been characterized in various cell-based assays. |
| 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
In vivo, Polyphyllin VI possesses anti-cancer activities and exhibits strong inhibitory effects on lung cancer cell growth. It induces G2/M cell cycle arrest and triggers apoptosis in tumor tissues. The compound has been studied in animal models of cancer for its anti-tumor efficacy. Its hemostasis, expectorant, and bacteriostasis effects have been demonstrated in preclinical studies. Further in vivo studies are ongoing to fully characterize its therapeutic potential. |
| Enzyme Assay |
Polyphyllin VI enzyme assays involve measuring its effects on apoptosis, pyroptosis, and cell cycle pathways. Caspase-1 activity is assessed using fluorogenic substrates. ROS levels are measured using fluorescent probes. NF-κB activation is assessed by measuring nuclear translocation or DNA binding. NLRP3 inflammasome activation is assessed by measuring ASC oligomerization or IL-1β release. Cell cycle analysis is performed by flow cytometry. Apoptosis is evaluated by Annexin V/PI staining and caspase activity assays. Assays are performed in appropriate buffer systems with positive controls such as known apoptosis inducers.
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| 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 Polyphyllin VI cell-based assays are conducted in non-small cell lung cancer cells and other cancer cell lines. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with Polyphyllin VI at varying concentrations. Cell viability is assessed by MTT or CCK-8 assays. Cell cycle analysis is performed by flow cytometry. Apoptosis is evaluated by Annexin V/PI staining and caspase activity assays. Pyroptosis is assessed by measuring caspase-1 activity, IL-1β release, and GSDMD cleavage. ROS levels are measured using fluorescent probes. NF-κB and NLRP3 pathway activation are assessed by Western blot. Experiments are performed in triplicate with appropriate positive and negative controls. |
| 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. Polyphyllin VI in vivo studies are conducted in mouse models of non-small cell lung cancer. Tumor-bearing mice are treated with Polyphyllin VI via oral administration or injection. Tumor growth is monitored by caliper measurements. Apoptosis and pyroptosis in tumor tissues are assessed by TUNEL assay, immunohistochemistry for cleaved caspase-3, and Western blot for GSDMD cleavage. Cell cycle analysis is performed on tumor tissue. ROS levels and NF-κB activation are assessed. Animals are monitored for clinical signs. Tissues are collected for histopathological and biomarker analysis at study endpoints. Studies are conducted in accordance with institutional animal care guidelines. |
| ADME/Pharmacokinetics |
Polyphyllin VI (MW 738.90 g/mol, C39H62O13) is an active saponin. It is a natural product derived from the rhizomes of Paris yunnanensis Franch. The compound is a white powder with ≥98% purity. It is soluble in DMSO and other organic solvents. It is stable as a powder at -20°C for up to 3 years and at 4°C for 2 years; in solvent, it is stable at -80°C for 2 years and at -20°C for 1 year. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution would be determined in species-specific studies.
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| Toxicity/Toxicokinetics |
Polyphyllin VI is generally well-tolerated in preclinical studies at therapeutic doses. The compound is a natural saponin with anti-cancer activities. Its anti-cancer effects have been demonstrated with acceptable safety profiles. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
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| References |
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| Additional Infomation |
Multileaf saponin VI is a steroidal saponin.
Polyphyllin VI is an active saponin with anti-cancer activities that induces G2/M cell cycle arrest and triggers apoptosis. It induces caspase-1-mediated pyroptosis via the ROS/NF-κB/NLRP3/GSDMD signal axis in non-small cell lung cancer. The compound also has hemostasis, expectorant, bacteriostasis, anti-pregnancy, and sperm-killing effects. Its molecular formula is C39H62O13 with a molecular weight of 738.90 g/mol. All applications are limited to non-human research use. |
| Molecular Formula |
C39H62O13
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| Molecular Weight |
738.9018
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| Exact Mass |
738.419
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| CAS # |
55916-51-3
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| Related CAS # |
55916-51-3
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| PubChem CID |
10417550
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
871.2±65.0 °C at 760 mmHg
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| Flash Point |
480.7±34.3 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.616
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| LogP |
6.09
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
52
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| Complexity |
1370
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| Defined Atom Stereocenter Count |
21
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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)O)O[C@H]8[C@@H]([C@@H]([C@H]([C@@H](O8)C)O)O)O)C)C)O)C)OC1
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| InChi Key |
WHWWQGPCTUQCMN-JDDKMXSSSA-N
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| 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
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| 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
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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 (~135.34 mM)
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| 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. View More
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. |
| 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.
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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