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.
Arctiin是Arctium lappa L. (A. lappa) 的一种生物活性代谢物，是一种口服有效的NF-κB抑制剂[1]。Arctiin能够抑制PI3K/AKT和JAK/STAT信号通路，降低S100A4蛋白的表达，并阻碍细胞迁移[2]。Arctiin已被广泛用于多种动物模型以抑制炎症和抗病毒感染[3]。
在体外，Arctiin处理48小时显著抑制了SW480细胞的生长，IC50值为220.7µM[4]。使用2mg/ml的Arctiin处理48小时，可诱导细胞周期阻滞在G0/G1期，并抑制高浓度（4.5mg/ml）葡萄糖诱导的人视网膜毛细血管内皮细胞（HRCECs）增殖[5]。用10µM的Arctiin处理U266细胞36小时，显著阻碍细胞增殖，将细胞周期阻滞在G2/M期，并诱导细胞凋亡[6]。
在体内，每日口服给予Arctiin（80mg/kg）一次，持续3周，可减轻主动脉弓缩窄小鼠的心肌肥大，并抑制心肌纤维化和胶原沉积[7]。连续16天每日腹腔注射Arctiin（25mg/kg），有效缓解了2,4-dinitrochlorobenzene（DNCB）诱导的小鼠特应性皮炎（AD）样皮肤损伤，减轻了皮肤厚度、皮肤组织中的肥大细胞浸润以及血清总IgE水平[8]。