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| Targets |
Polygalacin D targets multiple components of the PI3K/Akt signaling pathway. It inhibits the phosphorylation of GSK3β and Akt, and blocks the expression of PI3K, leading to the induction of apoptosis. It also inhibits the expression of IAP (inhibitor of apoptosis) protein family members. Additionally, Polygalacin D inhibits the expression of LPS-induced iNOS and COX-2 proteins, contributing to its anti-inflammatory activity.
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| ln Vitro |
Polygalacin D (0-40 µM; 48 hours) suppresses cell growth with an IC50 of 26.49 µM in A549 cells and 20.52 µM in H460 cells [1]. Polygala D (0-20 µM; 48 hours) increases the fraction of early and late apoptotic cells, and nuclear condensation is detected in A549 and H460 cells [1]. Polygala D (0-20 µM; 48 hours) may exert its apoptotic effects by affecting apoptotic proteins including the IAP protein family in A549 and H460 cells [1].
In vitro, Polygalacin D exhibits potent anti-proliferative and pro-apoptotic activity against various cancer cell lines. It induces apoptosis through the PI3K/Akt pathway. It also shows anti-inflammatory activity by inhibiting the expression of LPS-induced iNOS and COX-2 in RAW 264.7 macrophages without appreciable cytotoxicity. It suppresses the induction of pro-inflammatory cytokines like PGE2. |
| ln Vivo |
In vivo, Polygalacin D has been shown to protect mice from the lethal effects of LPS, reducing mortality from 89% to 60% and 50% when administered with LPS/galactosamine in combination with other saponins. Its anti-inflammatory and anticancer properties suggest potential therapeutic applications. However, specific in vivo data for Polygalacin D alone are limited.
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| Enzyme Assay |
In vitro non-cell enzyme assays for Polygalacin D are not standard. Its mechanism is primarily studied in cell-based systems. However, its effects on the PI3K/Akt pathway can be assessed by measuring the phosphorylation status of Akt and GSK3β using cell lysates in ELISA or western blot-based assays.
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: A549 and H460 Cancer cell lines Tested Concentrations: 10 µM, 20 µM, 40 µM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibition of proliferation of NSCLC cell lines. Apoptosis analysis [1] Cell Types: A549 and H460 cancer cell lines Tested Concentrations: 10 µM, 20 µM Incubation Duration: 48 hrs (hours) Experimental Results: Induction of apoptosis in NSCLC cell lines. Western Blot Analysis[1] Cell Types: A549 and H460 cancer cell lines Tested Concentrations: 10 µM, 20 µM Incubation Duration: 48 hrs (hours) Experimental Results: diminished expression of survivin, c-IAP-1 and c-IAP-2. In vitro cell-based assays for Polygalacin D use cancer cell lines and RAW 264.7 macrophages. Cells are treated with the compound, and apoptosis is assessed by Annexin V/PI staining, while PI3K/Akt pathway inhibition is confirmed by western blot for phospho-Akt and phospho-GSK3β. Anti-inflammatory activity is measured by LPS-induced NO production and PGE2 levels, as well as iNOS and COX-2 expression. |
| Animal Protocol |
In vivo animal studies for Polygalacin D employ mouse models of acute inflammation, such as LPS-induced lethality. The compound is administered to mice, and survival rates are monitored. Inflammatory markers in serum and tissues can also be measured to assess its anti-inflammatory effects. Tumor xenograft models could be used to study its anticancer efficacy.
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| ADME/Pharmacokinetics |
Polygalacin D has a molecular weight of 1209.32 g/mol and a molecular formula of C₅₇H₉₂O₂₇. It is a complex saponin with high molecular weight and is practically insoluble in water (6.8e-3 g/L). It is typically soluble in DMSO. For storage, it should be kept as a powder at -20°C for up to 3 years or at 4°C for up to 2 years.
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| Toxicity/Toxicokinetics |
The toxicity profile of Polygalacin D has not been fully characterized. In vitro studies show it has no appreciable cytotoxic effect on RAW 264.7 macrophages at active concentrations. However, as a potent apoptosis inducer, it may have significant biological effects that require careful evaluation. Comprehensive toxicological studies are needed.
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| References | |
| Additional Infomation |
[(2S,3R,4S,5S)-3-[(2S,3R,4S,5R,6S)-5-[(2S,3R,4S,5R)-4-[(2S,3R,4R)-3,4-dihydroxy-4-(hydroxymethyl)oxetane-2-yl]oxy-3,5-dihydroxyoxetane-2-yl]oxy-3,4-dihydroxy-6-methyloxetane-2-yl]oxy-4,5-dihydroxyoxetane-2-yl] has been reported in Platycodon grandiflorus. Grandiflorus contains (4aR,5R,6aR,6aS,6bR,8aR,9R,10R,11S,12aR,14bS)-5,11-dihydroxy-9-(hydroxymethyl)-2,2,6a,6b,9,12a-hexamethyl-10-[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxacyclohexane-2-yl]oxy-1,3,4,5,6,6a,7,8,8a,10,11,12,13,14b-tetradecanoylene-4a-carboxylic acid ester, and relevant data are available.
Polygalacin D is a bioactive triterpenoid saponin from Platycodon grandiflorum with significant anticancer and anti-proliferative properties. It induces apoptosis via the PI3K/Akt pathway and exhibits anti-inflammatory activity. It is a valuable research tool for studying cancer biology and drug development. Not approved for clinical use. |
| Molecular Formula |
C57H92O27
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|---|---|
| Molecular Weight |
1209.3242
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| Exact Mass |
1208.582
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| CAS # |
66663-91-0
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| PubChem CID |
53325780
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.652
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| LogP |
0.5
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| Hydrogen Bond Donor Count |
16
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| Hydrogen Bond Acceptor Count |
27
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
84
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| Complexity |
2370
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| Defined Atom Stereocenter Count |
32
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| SMILES |
C[C@H]1[C@@H]([C@H]([C@H]([C@@H](O1)O[C@@H]2[C@H]([C@H](CO[C@H]2OC(=O)[C@]34CCC(C[C@H]3C5=CC[C@H]6[C@]([C@@]5(C[C@H]4O)C)(CC[C@@H]7[C@@]6(C[C@@H]([C@@H]([C@]7(C)CO)O[C@H]8[C@@H]([C@H]([C@@H]([C@H](O8)CO)O)O)O)O)C)C)(C)C)O)O)O)O)O[C@H]9[C@@H]([C@H]([C@@H](CO9)O)O[C@H]1[C@@H]([C@](CO1)(CO)O)O)O
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| InChi Key |
BDCUGHMNUOTFKX-DDRWPPTGSA-N
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| InChi Code |
InChI=1S/C57H92O27/c1-23-40(80-45-39(71)41(28(63)19-75-45)81-49-43(72)56(74,21-60)22-77-49)36(68)38(70)46(78-23)82-42-33(65)27(62)18-76-48(42)84-50(73)57-13-12-51(2,3)14-25(57)24-8-9-31-52(4)15-26(61)44(83-47-37(69)35(67)34(66)29(17-58)79-47)53(5,20-59)30(52)10-11-54(31,6)55(24,7)16-32(57)64/h8,23,25-49,58-72,74H,9-22H2,1-7H3/t23-,25-,26-,27-,28+,29+,30+,31+,32+,33-,34+,35-,36-,37+,38+,39+,40-,41-,42+,43-,44-,45-,46-,47-,48-,49-,52-,53+,54+,55+,56+,57+/m0/s1
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| Chemical Name |
[(2S,3R,4S,5S)-3-[(2S,3R,4S,5R,6S)-5-[(2S,3R,4S,5R)-4-[(2S,3R,4R)-3,4-dihydroxy-4-(hydroxymethyl)oxolan-2-yl]oxy-3,5-dihydroxyoxan-2-yl]oxy-3,4-dihydroxy-6-methyloxan-2-yl]oxy-4,5-dihydroxyoxan-2-yl] (4aR,5R,6aR,6aS,6bR,8aR,9S,10R,11S,12aR,14bS)-5,11-dihydroxy-9-(hydroxymethyl)-2,2,6a,6b,9,12a-hexamethyl-10-[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-1,3,4,5,6,6a,7,8,8a,10,11,12,13,14b-tetradecahydropicene-4a-carboxylate
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~82.69 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.07 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.5 mg/mL (2.07 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 25.0 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: ≥ 2.5 mg/mL (2.07 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 | 0.8269 mL | 4.1346 mL | 8.2691 mL | |
| 5 mM | 0.1654 mL | 0.8269 mL | 1.6538 mL | |
| 10 mM | 0.0827 mL | 0.4135 mL | 0.8269 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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