GLPBio

Arctiin

Catalog No.: GN10387Purity:>98.00%Synonyms: Arctigenin4Glucoside, NSC 315527
COASDSData Sheet
Arctiin, a bioactive metabolite from Arctium lappa L. (A. lappa), is an orally active inhibitor of NF-κB.

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Arctiin
Cas No.: 20362-31-6
10mM (in 1mL DMSO)In Stock
$39.00
1
50mgIn Stock
$35.00
1
100mgIn Stock
$46.00
1
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    187(9):2288-2304 (2024)
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Description

Arctiin, a bioactive metabolite from Arctium lappa L. (A. lappa), is an orally active inhibitor of NF-κB [1]. Arctiin can inhibit the PI3K/AKT and JAK/STAT signaling pathways, reduce the expression of S100A4 protein, and hinder cell migration[2]. Arctiin has been widely used in various animal models to inhibit inflammation and combat viral infections[3].

In vitro, Arctiin treatment for 48 hours significantly inhibited the growth of SW480 cells with an IC50 value of 220.7µM [4]. Treatment with 2mg/ml Arctiin for 48 hours induced cell cycle arrest at G0/G1 phase and inhibited the proliferation of human retinal capillary endothelial cells (HRCECs) induced by high concentration (4.5mg/ml) glucose[5]. Treatment of U266 cells with 10µM Arctiin for 36 hours significantly hindered cell proliferation, arrested the cell cycle at G2/M phase, and induced cell apoptosis[6].

In vivo, Arctiin (80mg/kg) was administered orally once daily for 3 weeks to attenuate myocardial hypertrophy and inhibit myocardial fibrosis and collagen deposition in mice undergoing aortic banding[7]. Arctiin (25mg/kg) was intraperitoneally injected once a day for 16 consecutive days, which effectively alleviated 2,4-dinitrochlorobenzene (DNCB)-induced atopic dermatitis (AD)-like skin lesions in mice, reduced skin thickness, mast cell infiltration in skin tissue, and serum total IgE level[8].

References:
[1] Yang M, Peng G, Abudouwanli A, et al. Immunopharmacological potential of Arctium lappa L. in immune-mediated skin diseases: A critical review of experimental and clinical evidence[J]. Frontiers in Pharmacology, 2025, 16: 1660352.
[2] Chowdhury R, Bhuia M S, Wilairatana P, et al. An insight into the anticancer potentials of lignan arctiin: A comprehensive review of molecular mechanisms[J]. Heliyon, 2024, 10(12).
[3] Gao Q, Yang M, Zuo Z. Overview of the anti-inflammatory effects, pharmacokinetic properties and clinical efficacies of arctigenin and arctiin from Arctium lappa L[J]. Acta Pharmacologica Sinica, 2018, 39(5): 787-801.
[4] Yoo J H, Lee H J, Kang K, et al. Lignans inhibit cell growth via regulation of Wnt/β-catenin signaling[J]. Food and Chemical Toxicology, 2010, 48(8-9): 2247-2252.
[5] Zhou M, Li G, Zhu L, et al. Arctiin attenuates high glucose‐induced human retinal capillary endothelial cell proliferation by regulating ROCK1/PTEN/PI3K/Akt/VEGF pathway in vitro[J]. Journal of Cellular and Molecular Medicine, 2020, 24(10): 5695-5706.
[6] Lee J H, Kim C, Lee J, et al. Arctiin is a pharmacological inhibitor of STAT3 phosphorylation at tyrosine 705 residue and potentiates bortezomib-induced apoptotic and anti-angiogenic effects in human multiple myeloma cells[J]. Phytomedicine, 2019, 55: 282-292.
[7] Li J, Yuan Y P, Xu S C, et al. Arctiin protects against cardiac hypertrophy through inhibiting MAPKs and AKT signaling pathways[J]. Journal of Pharmacological Sciences, 2017, 135(3): 97-104.
[8] Li J, Du X, Mu Z, et al. Arctiin Alleviates Atopic Dermatitis Against Inflammation and Pyroptosis Through Suppressing TLR4/MyD88/NF-κB and NLRP3/Caspase-1/GSDMD Signaling Pathways[J]. Journal of Inflammation Research, 2024: 8009-8026.

Protocol

Cell experiment [1]:

Cell lines

SW480 cells

Preparation Method

SW480 cells were cultured in RPMI-1640 medium supplemented with 200mM HEPES, 10% (w/v) heat-inactivated fetal bovine serum (FBS), and 1% (w/v) penicillin-streptomycin. Cells were cultured in T-75 flasks and 100mm Petri dishes at 37°C in a humidified environment with 5% CO2 and sub-cultured twice a week with 0.25% trypsin containing 1mM EDTA. SW480 cells were seeded in 96-well flat bottom plates at a density of 6×103 cells/well. After incubation at 37°C for 24 hours, the medium was replaced, and Arctiin diluted to different concentrations (12.5, 100, 200, 300, 400µM) was added. Control cells were treated with DMSO at a final concentration of 1%. Cell proliferation was measured 48 hours later.

Reaction Conditions

12.5, 100, 200, 300, 400µM; 48h

Applications

Arctiin treatment reduced cell viability of SW480 cells in a dose-dependent manner.
Animal experiment [2]:

Animal models

Male C57/B6 mice

Preparation Method

Eighty adult male C57/B6 mice (8-10 weeks old; 23.5-27.5g) were housed in a standard sterile environment, and 40 of the mice underwent aortic banding (AB) one week after acclimatization to the laboratory environment. Subjects were randomly divided into four groups: sham+vehicle group (n=20), sham+Arctiin group (n=20), AB+vehicle group (n=20), and AB+Arctiin group (n=20). One week after AB, Arctiin was administered by regular daily gavage at a dose of 80mg/kg for 3 weeks. The control group was given the same volume of vehicle. All mice were anesthetized with 1.5% isoflurane and sacrificed by cervical dislocation. Heart samples were dissected and collected for analysis.

Dosage form

80mg/kg/day for 3 weeks; p.o.

Applications

Arctiin treatment attenuated cardiac hypertrophy induced by AB, and suppressed cardiac fibrosis and accumulation of collagen in mice.

References:
[1] Yoo J H, Lee H J, Kang K, et al. Lignans inhibit cell growth via regulation of Wnt/β-catenin signaling[J]. Food and Chemical Toxicology, 2010, 48(8-9): 2247-2252.
[2] Li J, Yuan Y P, Xu S C, et al. Arctiin protects against cardiac hypertrophy through inhibiting MAPKs and AKT signaling pathways[J]. Journal of Pharmacological Sciences, 2017, 135(3): 97-104.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
20362-31-6
Synonyms
Arctigenin4Glucoside, NSC 315527
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
SMILES
COC1=C(C=C(C=C1)CC2COC(=O)C2CC3=CC(=C(C=C3)OC4C(C(C(C(O4)CO)O)O)O)OC)OC
Molecular Formula
C27H34O11
Molecular Weight
534.55
Solubility
≥ 23.3mg/mL in DMSO
Storage
Store at -20°C, protect from light
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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