| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
Asperuloside acts by suppressing the NF-κB and MAPK signaling pathways, thereby inhibiting the expression of inflammatory mediators and cytokines. [1]
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| ln Vitro |
In RAW 264.7 cells, asperuloside (0-160 μg/mL, 1 hour) inhibits the production of NO, PGE2, TNF-α, and IL-6 induced by LPS [1]. In serum cell lines (U937, HL-60, AML), asperuloside (0–5 mM, 24 hours) suppresses cell viability and induces ER-dependent cellular reagents [1].
In LPS-induced RAW 264.7 macrophages, Asperuloside (40, 80, and 160 µg/mL) significantly decreased the production of nitric oxide (NO), prostaglandin E₂ (PGE₂), tumor necrosis factor-α (TNF-α), and interleukin-6 (IL-6). It also down-regulated the mRNA and protein expression of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), TNF-α, and IL-6. Furthermore, it inhibited the phosphorylation of IκB-α, p38, ERK1/2, and JNK, indicating suppression of NF-κB and MAPK pathways. [1] |
| ln Vivo |
On a high-fat diet (HFD), asperuloside (orally, 3 mg/day, 0.3% of the diet, daily, for 12 weeks) decreases food intake, body weight, and fat mass [2]. In a U937 xenograft mouse model, asperuloside (30 and 60 mg/kg, intraperitoneal injection, 30 days) suppresses the formation of tumors [3]. In BALB/c mice, asperuloside (20–80 mg/kg, i.p.) inhibits MAPK and NF-κB signaling.
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| Cell Assay |
Western Blot Analysis[3]
Cell Types: U937 cells Tested Concentrations: 0-5 mM Incubation Duration: 24 h Experimental Results: Increased release of cleaved Caspase-3, Caspase-9, PARP and Cyto-c in mitochondria. Induced expression of GRP78, p-PERK, p-eIF2α, CHOP, p-IRE1, XBP1, ATF6 and cleaved Caspase-12 Cell viability assay: RAW 264.7 cells were seeded in 96-well plates (1×10⁴ cells/well) and cultured for 24 h. Cells were treated with Asperuloside (0, 50, 100, 200 µg/mL) for 1 h, then induced with LPS (50 ng/mL) for 24 h. Cell viability was assessed using a Cell Counting Kit-8 (CCK-8) by measuring absorbance at 450 nm. [1] ELISA for inflammatory mediators: Cells were pretreated with Asperuloside (40, 80, 160 µg/mL) for 1 h, then stimulated with LPS (50 ng/mL) for 24 h. Supernatants were collected, and levels of NO, PGE₂, TNF-α, and IL-6 were measured using respective ELISA kits. [1] Real-time PCR: Cells were treated with Asperuloside (40, 80, 160 µg/mL) for 1 h, then induced with LPS for 24 h. Total RNA was extracted, reverse transcribed to cDNA, and mRNA levels of TNF-α, IL-6, iNOS, and COX-2 were quantified using SYBR Green-based real-time PCR. [1] Western blot: Cells were treated similarly, lysed, and proteins were separated by SDS-PAGE, transferred to PVDF membranes, and probed with antibodies against iNOS, COX-2, IκB-α, p-IκB-α, p38, p-p38, ERK1/2, p-ERK1/2, JNK, p-JNK, and β-actin. Signals were detected using chemiluminescence. [1] |
| Animal Protocol |
Animal/Disease Models: Rats eating high-fat diet (HFD) [2]
Doses: 3 mg/ Daily dosing: po, 0.3% in diet, daily, 12-week Experimental Results: weight loss, energy intake, adiposity, blood glucose, and plasma insulin. |
| Toxicity/Toxicokinetics |
In the presence of LPS, asperuloside at concentrations up to 200 µg/mL did not show significant cytotoxicity against RAW 264.7 cells. [1]
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| References |
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| Additional Infomation |
Asperuloside is an iridoid monoterpene glycoside isolated from Galium verum. It is a metabolite. It is an iridoid monoterpene, β-D-glucoside, monosaccharide derivative, acetate, and γ-lactone. Asperuloside has been reported in Oldenlandia herbacea var. herbacea, Psychotria rubra, and several other organisms with relevant data. See also: Whole plant (part) of Galium aparine. Asperuloside is an iridoid compound isolated from Hedyotis diffusa, a traditional Asian herb used to treat inflammation-related diseases. Its anti-inflammatory mechanism involves inhibiting the NF-κB and MAPK signaling pathways, thereby reducing the expression of inflammatory mediators and cytokines. It is considered a potentially bioactive compound that can be used for the quality control of Hedyotis diffusa and its related herbal preparations. [1]
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| Molecular Formula |
C18H22O11
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|---|---|
| Molecular Weight |
414.3607
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| Exact Mass |
414.116
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| CAS # |
14259-45-1
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| PubChem CID |
84298
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
704.2±60.0 °C at 760 mmHg
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| Melting Point |
131-132°
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| Flash Point |
254.1±26.4 °C
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| Vapour Pressure |
0.0±5.1 mmHg at 25°C
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| Index of Refraction |
1.635
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| LogP |
-3.28
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
746
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| Defined Atom Stereocenter Count |
9
|
| SMILES |
CC(=O)OCC1=C[C@H]2[C@H]3[C@@H]1[C@@H](OC=C3C(=O)O2)O[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O
|
| InChi Key |
IBIPGYWNOBGEMH-DILZHRMZSA-N
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| InChi Code |
InChI=1S/C18H22O11/c1-6(20)25-4-7-2-9-12-8(16(24)27-9)5-26-17(11(7)12)29-18-15(23)14(22)13(21)10(3-19)28-18/h2,5,9-15,17-19,21-23H,3-4H2,1H3/t9-,10+,11+,12-,13+,14-,15+,17-,18-/m0/s1
|
| Chemical Name |
[(4S,7S,8S,11S)-2-oxo-8-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-3,9-dioxatricyclo[5.3.1.04,11]undeca-1(10),5-dien-6-yl]methyl acetate
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| Synonyms |
Asperuloside
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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 (~241.34 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.03 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 (6.03 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 (6.03 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 | 2.4134 mL | 12.0668 mL | 24.1336 mL | |
| 5 mM | 0.4827 mL | 2.4134 mL | 4.8267 mL | |
| 10 mM | 0.2413 mL | 1.2067 mL | 2.4134 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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