| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g | |||
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| Other Sizes |
Purity: ≥98%
| Targets |
Arctiin targets multiple cellular pathways. It is an inhibitor of NF-κB, a transcription factor that plays a critical role in inflammation and cancer. By inhibiting NF-κB, it suppresses the expression of pro-inflammatory mediators. Arctiin also inhibits adipogenesis in 3T3-L1 adipocytes through the inhibition of PPARγ and C/EBPα and the activation of AMPK signaling pathways. It suppresses cyclin D1 protein expression in human tumor cells.
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| ln Vitro |
In vitro, Arctiin has been reported to have anti-inflammatory, antioxidant, antibacterial, and antiviral effects. It inhibits adipogenesis in 3T3-L1 adipocytes through the inhibition of PPARγ and C/EBPα and the activation of AMPK signaling pathways. It suppresses cyclin D1 protein expression in multiple types of human tumor cells. Arctiin exerts anti-inflammatory effects by inhibiting pro-inflammatory mediators through the inactivation of NF-κB. It also reduces malondialdehyde and pro-inflammatory cytokine levels.
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| ln Vivo |
Male probasin/SV40 T antigen transgenic rats were fed diets containing 0.1%, 0.02%, or 0.004% Arctiin for 18 weeks. Histopathological evaluation showed that all rats developed adenocarcinoma in the dorsolateral prostate except two rats in the 0.1% group and one rat in the 0.02% group without carcinoma [1]. However, there were no definite treatment-related changes with statistical significance in any parameters for prostate carcinomas measured, including incidences of PIN and adenocarcinoma, and quantitative analysis of histological components in dorsolateral and anterior lobes [1]. Arctiin did not exert significant modifying effect (either promoting or chemopreventive) on prostate carcinogenesis in this model [1].
Small cell carcinomas were found in the dorsolateral prostate of four rats, with no group difference in distribution [1]. Two rats with extremely large prostates (each in the 0.02% arctiin and control groups) developed small cell carcinoma [1]. The average percentage of PIN, well-differentiated adenocarcinoma, and moderately differentiated adenocarcinoma in dorsolateral and anterior lobes showed no significant differences among groups [1]. In vivo, Arctiin is orally active. It has been shown to protect against UVB radiation exposure. Arctiin suppresses H9N2 avian influenza virus-mediated inflammation via activation of Nrf2/HO-1 signaling. It demonstrates potent antiviral activity against influenza A virus. These results demonstrate the diverse in vivo activities of Arctiin. |
| Enzyme Assay |
In vitro NF-κB inhibition assays for Arctiin involve measuring its ability to inhibit NF-κB activity in reporter gene assays. Cells are transfected with an NF-κB-responsive luciferase reporter and treated with Arctiin prior to stimulation with TNF-α or other NF-κB activators. Luciferase activity is measured to assess NF-κB inhibition. The effects on pro-inflammatory cytokine production are measured by ELISA.
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| Cell Assay |
In vitro cell-based assays for Arctiin are performed using various cell types, including cancer cell lines, adipocytes, and immune cells. Cells are cultured in appropriate media and treated with Arctiin at various concentrations. Cell viability is assessed by MTT assays. The expression of cyclin D1 and other target proteins is analyzed by Western blot. Adipogenesis is assessed by Oil Red O staining. Cytokine production is measured by ELISA.
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| Animal Protocol |
Heterozygous male SV40 T antigen transgenic rats (6 weeks old) were used [1]. Arctiin (purity >97%) was mixed into powdered soybean-free basal diet at concentrations of 0.1%, 0.02%, or 0.004% [1]. The control group received soybean-free basal diet alone [1]. Animals were housed 2 per cage on wood-chip bedding in an air-conditioned room at 23±2°C and 60±10% humidity, with diet and tap water available ad libitum [1]. The treatment duration was 18 weeks [1]. Body weight and food consumption were recorded biweekly [1]. At the end of week 18, all surviving rats were killed under ether anesthesia [1]. At autopsy, prostates were removed and fixed in 10% neutral buffered formalin; livers and kidneys were excised, weighed, and fixed [1]. After 48 hours of fixation, the dorsolateral and anterior lobes were carefully dissected, weighed, and 2-3 mm thick slices were made from each lobe, then embedded in paraffin for histopathological examination of hematoxylin and eosin stained sections [1]. Neoplastic lesions of the prostate were classified as prostatic intraepithelial neoplasia (PIN), well-differentiated adenocarcinoma, moderately differentiated adenocarcinoma, or poorly differentiated adenocarcinoma [1]. Each prostatic lobe was scored and the percentage area corresponding to each pathological stage was quantified using an image processor for analytical pathology [1].
In vivo animal studies for Arctiin have been conducted in models of inflammation, viral infection, and UVB radiation exposure. The compound is administered orally at doses determined from pharmacokinetic studies. In the UVB radiation model, skin damage is assessed histologically. In the influenza model, viral load and inflammatory markers are measured. In inflammation models, cytokine levels and tissue damage are assessed. |
| ADME/Pharmacokinetics |
Specific pharmacokinetic properties of Arctiin have been characterized as orally active. As a glycoside with a molecular weight of 534.55 g/mol, it is expected to be absorbed and metabolized to its aglycone, arctigenin, which is the active form. It is soluble in DMSO. The compound's pharmacokinetic profile supports oral administration in research studies.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for Arctiin are not widely available in public literature. As a natural product from a food source (burdock), it is generally considered to have a favorable safety profile. However, as with all research compounds, standard safety precautions should be followed. Arctiin is not intended for human therapeutic use.
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| References | |
| Additional Infomation |
Arctiin is a glycoside and lignan. Arctiin has been reported in Saussurea involucrata, Saussurea salsa, and other organisms for which data are available. See also: Lignans (subclasses of lignans); Burdock fruit (part); Burdock root (part).
Arctiin is a plant lignan belonging to the class of phytoestrogens, which are nonsteroidal substances with weak estrogenic activity [1]. Phytoestrogens are 1000-fold less potent than estradiol but have similar relative affinity for estrogen receptor, acting as ER partial antagonists [1]. Arctiin has been found to influence sex hormone metabolism, protein synthesis, and steroid biosynthesis [1]. It is converted by human intestinal bacteria to estrogenic and antiestrogenic substances [1]. Arctiin induces drug metabolism enzymes such as CYP1A2 in rat liver [1]. In the present study, Arctiin showed no definite effects on prostate carcinogenesis in SV40 T antigen transgenic rats, although a weak inhibitory tendency was observed in high dose groups [1]. Arctiin is the major active lignin in burdock (Arctium lappa) fruits. It is an orally active NF-κB inhibitor with anti-inflammatory, antioxidant, antibacterial, and antiviral effects. Arctiin suppresses cyclin D1 expression in multiple tumor cell types and inhibits adipogenesis. It has potential applications in cancer, inflammation, and metabolic disorders. This product is for research use only. |
| Molecular Formula |
C27H34O11
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|---|---|
| Molecular Weight |
534.5523
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| Exact Mass |
534.21
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| CAS # |
20362-31-6
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| PubChem CID |
100528
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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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| Boiling Point |
756.4±60.0 °C at 760 mmHg
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| Melting Point |
109 °C
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| Flash Point |
250.1±26.4 °C
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| Vapour Pressure |
0.0±2.7 mmHg at 25°C
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| Index of Refraction |
1.601
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| LogP |
0.23
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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 |
10
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| Heavy Atom Count |
38
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| Complexity |
753
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| Defined Atom Stereocenter Count |
7
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| SMILES |
COC1=C(C=C(C=C1)C[C@H]2COC(=O)[C@@H]2CC3=CC(=C(C=C3)O[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)OC)OC
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| InChi Key |
XOJVHLIYNSOZOO-SWOBOCGESA-N
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| InChi Code |
InChI=1S/C27H34O11/c1-33-18-6-4-14(10-20(18)34-2)8-16-13-36-26(32)17(16)9-15-5-7-19(21(11-15)35-3)37-27-25(31)24(30)23(29)22(12-28)38-27/h4-7,10-11,16-17,22-25,27-31H,8-9,12-13H2,1-3H3/t16-,17+,22+,23+,24-,25+,27+/m0/s1
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| Chemical Name |
(3R,4R)-4-[(3,4-dimethoxyphenyl)methyl]-3-{[3-methoxy-4-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyphenyl]methyl}oxolan-2-one
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| Synonyms |
Arctiin; Arctii; NSC 315527; NSC315527; NSC-315527; Arctigenin-4-glucoside
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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 : ~250 mg/mL (~467.68 mM)
H2O : ~10 mg/mL (~18.71 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.89 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 20.8 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: ≥ 2.08 mg/mL (3.89 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 20.8 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: ≥ 2.08 mg/mL (3.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10 mg/mL (18.71 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8707 mL | 9.3537 mL | 18.7073 mL | |
| 5 mM | 0.3741 mL | 1.8707 mL | 3.7415 mL | |
| 10 mM | 0.1871 mL | 0.9354 mL | 1.8707 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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