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Polyphyllin I is a natural product from Paris polyphylla with anti-tumor activity, acting as an inhibitor of PDK1/Akt/mTOR signaling. Also an activator of the JNK signaling pathway.
| Targets |
- Polyphyllin I acts on mitochondrial functional proteins and c-Jun N-terminal kinase (JNK) signaling pathway proteins [2]
- Polyphyllin I targets 3-phosphoinositide-dependent protein kinase 1 (PDK1)/Akt/mammalian target of rapamycin (mTOR) signaling pathway proteins and cyclin B1 [3] |
|---|---|
| ln Vitro |
- Anti-proliferation in non-small cell lung cancer (NSCLC) cells ([1]): In A549 and H460 NSCLC cells, Polyphyllin I exhibited concentration-dependent anti-proliferative effects with IC50 values of 2.8 μM (A549) and 3.2 μM (H460) after 72 hours (MTT assay). It also reduced colony formation by 65% (A549) and 60% (H460) at 4 μM [1]
- G2/M arrest and apoptosis in U251 glioma cells ([2]): In U251 cells, Polyphyllin I (1-4 μM) induced G2/M phase arrest (G2/M ratio increased by 42% at 3 μM) and apoptosis (apoptotic rate increased from 3.2% to 35.6% at 3 μM, Annexin V-FITC/PI staining). It caused mitochondrial dysfunction (mitochondrial membrane potential reduced by 50% at 3 μM, JC-1 assay) and activated JNK (phospho-JNK/JNK ratio increased by 2.3-fold at 3 μM); JNK inhibitor (SP600125) reversed its apoptotic effect [2] - Autophagy and cell cycle arrest in HGC-27 gastric cancer cells ([3]): In HGC-27 cells, Polyphyllin I (2-8 μM) inhibited proliferation (IC50 = 4.5 μM, 72 hours) and induced G2/M arrest (G2/M ratio +38% at 6 μM). It triggered autophagy (LC3-II/LC3-I ratio +3.1-fold, p62 protein -55% at 6 μM) and suppressed PDK1/Akt/mTOR signaling (phospho-PDK1/PDK1 -48%, phospho-Akt/Akt -52%, phospho-mTOR/mTOR -58% at 6 μM). It also downregulated cyclin B1 protein by 60% at 6 μM [3] |
| ln Vivo |
- Antitumor effect in NSCLC xenograft mice ([1]): In nude mice bearing A549 xenografts, Polyphyllin I was administered via intraperitoneal injection at 1 mg/kg and 2 mg/kg, once every 2 days for 21 days. The 2 mg/kg group showed a 58% reduction in tumor volume and a 55% reduction in tumor weight compared to the vehicle control. No significant weight loss or organ damage was observed [1]
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| Cell Assay |
- NSCLC cell assays ([1]):
1. Viability test: A549/H460 cells (5×10³ cells/well) were treated with Polyphyllin I (0.5-8 μM) for 72 hours, and viability was detected by MTT assay [1] 2. Colony formation: Cells (2×10² cells/well) were treated with Polyphyllin I (1-4 μM) for 14 days, stained with crystal violet, and colonies (>50 cells) were counted [1] - U251 glioma cell assays ([2]): 1. Viability test: U251 cells (5×10³ cells/well) were treated with Polyphyllin I (0.5-6 μM) for 72 hours, MTT assay was used [2] 2. Cell cycle analysis: Cells were treated with Polyphyllin I (1-4 μM) for 24 hours, fixed with 70% ethanol, stained with propidium iodide, and analyzed by flow cytometry [2] 3. Apoptosis detection: Cells were treated with Polyphyllin I (1-4 μM) for 48 hours, stained with Annexin V-FITC/PI, and apoptotic rate was measured by flow cytometry [2] 4. Western blot: Cells were treated with Polyphyllin I (1-4 μM) for 24-48 hours, total protein was extracted, and levels of JNK, phospho-JNK, Bax, Bcl-2, and β-actin were detected [2] - HGC-27 gastric cancer cell assays ([3]): 1. Viability test: HGC-27 cells (5×10³ cells/well) were treated with Polyphyllin I (1-10 μM) for 72 hours, MTT assay was used [3] 2. Autophagy detection: Cells were treated with Polyphyllin I (2-8 μM) for 24 hours, LC3 and p62 protein levels were detected by Western blot; autophagosomes were observed by fluorescence microscopy (LC3-GFP transfection) [3] 3. Western blot: Cells were treated with Polyphyllin I (2-8 μM) for 24 hours, and levels of PDK1, phospho-PDK1, Akt, phospho-Akt, mTOR, phospho-mTOR, cyclin B1, and β-actin were detected [3] |
| Animal Protocol |
- A549 xenograft model ([1]):
1. Model establishment: Male nude mice (4-6 weeks old) were subcutaneously injected with 5×10⁶ A549 cells (suspended in 100 μL PBS + 100 μL Matrigel) into the right flank. When tumors reached ~100 mm³, mice were divided into 3 groups (n=6): vehicle control, Polyphyllin I 1 mg/kg, Polyphyllin I 2 mg/kg [1] 2. Drug administration: Polyphyllin I was dissolved in 0.1% DMSO + 0.9% normal saline, administered via intraperitoneal injection once every 2 days for 21 days; vehicle group received the same solvent [1] 3. Detection: Tumor volume (length × width² / 2) was measured every 3 days; mice were sacrificed on day 21, tumor weight was recorded, and major organs (liver, kidney, heart) were stained with HE for pathological examination [1] |
| Toxicity/Toxicokinetics |
In vivo toxicity ([1]): Polyphyllin I (1-2 mg/kg, intraperitoneal injection, 21 days) did not cause significant weight loss (weight change <5%) or pathological damage to the liver, kidney or heart in mice (no necrosis or inflammation observed on HE staining) [1] - In vitro toxicity ([2][3]): Polyphyllin I at concentrations up to 8 μM did not affect the viability of normal human astrocytes (NHAs, [2]) or normal gastric epithelial cells (GES-1, [3]), with cell viability >90% compared to the control group [2][3]
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| References |
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| Additional Infomation |
It has been reported that Paris polyphylla var. chinensis, Polygonatum kingianum, and other organisms with relevant data all contain Paris saponin I. Paris saponin I is a steroidal saponin isolated from the traditional Chinese medicinal plant Paris polyphylla [1][2][3] - Its antitumor mechanism in non-small cell lung cancer (NSCLC) cells includes inhibiting cell proliferation and colony formation [1]; in U251 cells, it induces G2/M phase arrest and apoptosis through mitochondrial dysfunction and JNK activation [2]; in HGC-27 cells, it inhibits the PDK1/Akt/mTOR signaling pathway to induce autophagy and G2/M phase arrest [3] - It shows potential as a broad-spectrum antitumor drug for NSCLC, glioma, and gastric cancer [1][2][3]
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| Molecular Formula |
C44H70O16
|
|---|---|
| Molecular Weight |
855.0170
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| Exact Mass |
854.466
|
| CAS # |
50773-41-6
|
| PubChem CID |
11018329
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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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| Index of Refraction |
1.618
|
| LogP |
7.12
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| Hydrogen Bond Donor Count |
8
|
| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
8
|
| Heavy Atom Count |
60
|
| Complexity |
1570
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| Defined Atom Stereocenter Count |
25
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| SMILES |
C[C@@H]1CC[C@@]2([C@H]([C@H]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[C@H]8[C@@H]([C@H]([C@@H](O8)CO)O)O)O)O[C@H]9[C@@H]([C@@H]([C@H]([C@@H](O9)C)O)O)O)C)C)C)OC1
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| InChi Key |
LRRDDWMXYOSKIC-IPKCVOQPSA-N
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| InChi Code |
InChI=1S/C44H70O16/c1-19-8-13-44(53-18-19)20(2)30-27(60-44)15-26-24-7-6-22-14-23(9-11-42(22,4)25(24)10-12-43(26,30)5)55-41-38(59-39-35(51)33(49)31(47)21(3)54-39)36(52)37(29(17-46)57-41)58-40-34(50)32(48)28(16-45)56-40/h6,19-21,23-41,45-52H,7-18H2,1-5H3/t19-,20+,21+,23+,24-,25+,26+,27+,28+,29-,30+,31+,32+,33-,34-,35-,36+,37-,38-,39+,40+,41-,42+,43+,44-/m1/s1
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| Chemical Name |
(2S,3R,4R,5R,6S)-2-[(2R,3R,4S,5S,6R)-5-[(2S,3R,4R,5S)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]oxy-4-hydroxy-6-(hydroxymethyl)-2-[(1S,2S,4S,5'R,6R,7S,8R,9S,12S,13R,16S)-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 (~116.96 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (0.97 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 8.3 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: ≥ 0.83 mg/mL (0.97 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 8.3 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: ≥ 0.83 mg/mL (0.97 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 | 1.1696 mL | 5.8478 mL | 11.6956 mL | |
| 5 mM | 0.2339 mL | 1.1696 mL | 2.3391 mL | |
| 10 mM | 0.1170 mL | 0.5848 mL | 1.1696 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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