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| Targets |
Asperulosidic acid targets inflammatory and oxidative stress pathways. It suppresses the production of pro-inflammatory cytokines (TNF-α, IL-6) and mediators via suppression of the NF-κB and mitogen-activated protein kinase (MAPK) signaling pathways. It has anticlastogenic activity, and its alpha-unsaturated carbonyl group is considered to play an important role in the anticlastogenicity.
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| ln Vitro |
When compared to the group treated with LPS alone, Asperulosidic Acid (ASPA) (40-160 μg/mL; first hour) dramatically down-regulated the mRNA levels of TNF-α and IL-6 in LPS-induced RAW 264.7 cells [1]. Asperulosidic Acid (ASPA) (40-160 μg/mL; first hour) had no effect on p-p38 but decreases Erk1/2 phosphorylation at all concentration levels and IκB-α phosphorylation in a concentration-dependent manner [1].
In vitro, asperulosidic acid has been shown to exhibit anti-inflammatory, antioxidant, antitumor, and antimicrobial activities. It suppresses the production of inflammatory cytokines (TNF-α, IL-6) via inhibition of the NF-κB and MAPK signaling pathways. It has been found to exhibit various biological activities. |
| ln Vivo |
In vivo, asperulosidic acid has potential therapeutic effects on various diseases, including cancer, inflammation, and diabetes. It has been used in Chinese medicine as a useful drug against some tumors. Its anti-inflammatory and antitumor activities have been demonstrated in animal models.
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| Enzyme Assay |
The activity of Asperulosidic acid can be assessed using cell-free assays to measure its antioxidant and anti-inflammatory properties. The DPPH radical scavenging assay and ABTS radical cation decolorization assay can be used to evaluate its antioxidant capacity. Its anti-inflammatory activity can be assessed by measuring the inhibition of inflammatory mediators such as NO, TNF-α, and IL-6 in cell-free systems.
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| Cell Assay |
RT-PCR[2]
Cell Types: RAW 264.7 Cell Tested Concentrations: 40 μg/mL, 80 μg/mL and 160 μg/mL Incubation Duration: 1 hour pretreatment Experimental Results: TNF-α and IL-6 mRNA expression diminished. Western Blot Analysis[2] Cell Types: RAW 264.7 Cell Tested Concentrations: 40 μg/mL, 80 μg/mL and 160 μg/mL Incubation Duration: 1 hour pretreatment Experimental Results: IκB-α phosphorylation and Erk1/2 phosphorylation were diminished. To evaluate the cellular effects of Asperulosidic acid, various cell lines are treated with the compound. The inhibition of NF-κB and MAPK signaling pathways is assessed by Western blotting. The production of inflammatory cytokines (TNF-α, IL-6) is measured by ELISA. Its cytoprotective effects are evaluated by treating cells with Asperulosidic acid prior to exposure to oxidative stress and measuring cell viability. |
| Animal Protocol |
In vivo studies with Asperulosidic acid typically involve administration to animal models via oral or intraperitoneal routes. In models of inflammation, the compound's anti-inflammatory effects are assessed. In models of cancer, its antitumor effects are evaluated. Its effects on oxidative stress markers are also assessed.
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| ADME/Pharmacokinetics |
Asperulosidic acid has a molecular formula of C18H24O12 and a molecular weight of 432.4 g/mol. Its CAS number is 25368-11-0. It is soluble in DMSO. It is an iridoid glycoside with a purity of ≥95%. It should be stored according to the manufacturer's instructions.
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| Toxicity/Toxicokinetics |
Specific toxicology data for Asperulosidic acid are not extensively detailed in the available literature. However, its potential side effects and toxicity should be considered. As with all research compounds, standard safety precautions should be taken when handling Asperulosidic acid.
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| References |
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| Additional Infomation |
Asperu glycoside is a glycoside and also an iridoid monoterpene. It has been reported to exist in Oldenlandia herbacea var. herbacea, Galium rivale, and other organisms with relevant data.
Asperulosidic acid is a natural iridoid glycoside with anti-tumor, anti-oxidant, and anti-inflammatory activities. It has been used in Chinese medicine against some tumors. It suppresses the production of inflammatory cytokines via inhibition of the NF-κB and MAPK signaling pathways. It is a research tool for studying inflammation, cancer, and oxidative stress. |
| Molecular Formula |
C18H24O12
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| Molecular Weight |
432.3760
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| Exact Mass |
432.127
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| CAS # |
25368-11-0
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| PubChem CID |
11968867
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| Appearance |
White to off-white solid powder
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| Density |
1.64±0.1 g/cm3
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| LogP |
-3.2
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
733
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| Defined Atom Stereocenter Count |
9
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| SMILES |
CC(=O)OCC1=C[C@@H]([C@H]2[C@@H]1[C@@H](OC=C2C(=O)O)O[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O)O
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| InChi Key |
DGDWCRWJRNMRKX-DILZHRMZSA-N
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| InChi Code |
InChI=1S/C18H24O12/c1-6(20)27-4-7-2-9(21)12-8(16(25)26)5-28-17(11(7)12)30-18-15(24)14(23)13(22)10(3-19)29-18/h2,5,9-15,17-19,21-24H,3-4H2,1H3,(H,25,26)/t9-,10+,11+,12-,13+,14-,15+,17-,18-/m0/s1
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| Chemical Name |
(1S,4aS,5S,7aS)-7-(acetyloxymethyl)-5-hydroxy-1-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-1,4a,5,7a-tetrahydrocyclopenta[c]pyran-4-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 |
| 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 (~231.28 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.78 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 (5.78 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 (5.78 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 | 2.3128 mL | 11.5639 mL | 23.1278 mL | |
| 5 mM | 0.4626 mL | 2.3128 mL | 4.6256 mL | |
| 10 mM | 0.2313 mL | 1.1564 mL | 2.3128 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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