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| 1mg |
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| Targets |
Polygalacic acid targets multiple pathways involved in inflammation and neurodegeneration. It exhibits antioxidant activity by scavenging peroxyl and peroxynitrite radicals. It modulates inflammatory signaling pathways and can induce apoptosis in cancer cells. It may exert a significant neuroprotective effect on cognitive impairment, driven in part by the modulation of cholinergic activity and neuroinflammation.
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| ln Vitro |
The mRNA expression of MMP-3, MMP-9, MMP-13, and COX-2 was dramatically reduced by polygalic acid (0-100 μM; 24 hours), while these expressions were significantly raised in a dose-dependent manner by IL-1β [1]. IL-1β-induced production of phosphorylated p38, phosphorylated Erk, and phosphorylated Jnk is inhibited by polygalactonic acid (0-100 μM; 6 hours). Phosphorylated p65 expression is not decreased by polygalactonic acid [1].
In vitro, Polygalacic acid demonstrates a broad range of pharmacological effects, including anti-inflammatory, antioxidant, neuroprotective, and anticancer activities. It scavenges free radicals and modulates inflammatory signaling pathways. It can induce apoptosis in cancer cells. These activities make it a valuable compound for studying various diseases. |
| ln Vivo |
In vivo, Polygalacic acid has been shown to have neuroprotective effects in models of cognitive impairment. It has been used clinically to treat bronchitis, and to induce labor. Its anti-inflammatory and antioxidant properties suggest potential for treating neurodegenerative and inflammatory diseases. Further studies are needed to fully characterize its in vivo efficacy and safety.
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| Enzyme Assay |
For antioxidant assays, Polygalacic acid is tested for its ability to scavenge peroxyl and peroxynitrite radicals using in vitro methods. For anti-inflammatory assays, immune cells are stimulated with LPS in the presence or absence of the compound, and cytokine levels are measured by ELISA. For neuroprotection assays, neuronal cells are treated with the compound and then exposed to neurotoxic insults.
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| Cell Assay |
RT-PCR[1]
Cell Types: Chondrocytes Tested Concentrations: 50 μM; 100 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of IL-1β-induced COX-2, MMP3, MMP9 and MMP13 mRNA expression. Western Blot Analysis[1] Cell Types: Chondrocytes Tested Concentrations: 50 μM; 100 μM Incubation Duration: 6 hrs (hours) Experimental Results: Inhibition of IL-1β-induced MAPK pathway activation in chondrocytes. For cellular studies, neurons or cancer cells are cultured in appropriate medium. Polygalacic acid is dissolved in DMSO and diluted in culture medium. Cells are treated with the compound. Cell viability is assessed by MTT assay. Apoptosis is assessed by Annexin V/PI staining. Inflammatory markers and signaling proteins are analyzed by Western blot or ELISA. |
| Animal Protocol |
For in vivo efficacy studies, animal models of cognitive impairment, inflammation, or cancer could be used. Polygalacic acid would be formulated in vehicle and administered orally or intraperitoneally. Behavioral tests, inflammatory markers, and tumor growth would be assessed. For pharmacokinetic studies, blood and tissue samples would be collected for compound quantification.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Polygalacic acid are not extensively reported. As a triterpenoid saponin with a high molecular weight (504.71), it is expected to have low oral bioavailability. Its metabolism likely involves deglycosylation and hepatic clearance. A comprehensive PK study would be needed for any potential therapeutic development.
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| Toxicity/Toxicokinetics |
Toxicological data for Polygalacic acid are limited. No acute toxicity, organ-specific toxicity, or mutagenicity data have been reported. As with all research compounds, appropriate safety precautions should be taken during handling.
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| References |
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| Additional Infomation |
According to reports, daisies contain polygalactic acid, and relevant data is available for reference.
Polygalacic acid (CAS 22338-71-2) is a triterpenoid saponin with antioxidant and neuroprotective activities. It has the molecular formula C₃₀H₄₈O₆ and a molecular weight of 504.71. It exhibits anti-inflammatory, anticancer, and neuroprotective effects and is strictly for research use. |
| Molecular Formula |
C30H48O6
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|---|---|
| Molecular Weight |
504.6985
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| Exact Mass |
504.345
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| CAS # |
22338-71-2
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| PubChem CID |
12314427
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
638.1±55.0 °C at 760 mmHg
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| Melting Point |
315-318ºC
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| Flash Point |
353.7±28.0 °C
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| Vapour Pressure |
0.0±4.3 mmHg at 25°C
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| Index of Refraction |
1.593
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| LogP |
5.03
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
36
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| Complexity |
975
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| Defined Atom Stereocenter Count |
11
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| SMILES |
C[C@@]12CC[C@@H]3[C@@]([C@H]1CC=C4[C@]2(C[C@H]([C@@]5([C@H]4CC(CC5)(C)C)C(=O)O)O)C)(C[C@@H]([C@@H]([C@@]3(C)CO)O)O)C
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| InChi Key |
KGGGRGBDMBZXKF-PWFIOIGMSA-N
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| InChi Code |
InChI=1S/C30H48O6/c1-25(2)11-12-30(24(35)36)18(13-25)17-7-8-21-26(3)14-19(32)23(34)27(4,16-31)20(26)9-10-28(21,5)29(17,6)15-22(30)33/h7,18-23,31-34H,8-16H2,1-6H3,(H,35,36)/t18-,19-,20+,21+,22+,23-,26-,27-,28+,29+,30+/m0/s1
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| Chemical Name |
(4aR,5R,6aR,6aS,6bR,8aR,9R,10R,11S,12aR,14bS)-5,10,11-trihydroxy-9-(hydroxymethyl)-2,2,6a,6b,9,12a-hexamethyl-1,3,4,5,6,6a,7,8,8a,10,11,12,13,14b-tetradecahydropicene-4a-carboxylic acid
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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 : ~50 mg/mL (~99.07 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9814 mL | 9.9069 mL | 19.8138 mL | |
| 5 mM | 0.3963 mL | 1.9814 mL | 3.9628 mL | |
| 10 mM | 0.1981 mL | 0.9907 mL | 1.9814 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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