Luteolin 5-O-glucoside from Korean Milk Thistle,Cirsium maackii, Exhibits Anti-Inflammatory Activity via Activation of the Nrf2/HO-1 Pathway

Abstract

-Luteolin 5-O-glucoside is the major flavonoid from Korean thistle, Cirsium maackii. We previously reported the anti-inflammatory activities of luteolin 5-O-glucoside in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. In this study, we determined the anti-inflammatory mechanisms of luteolin 5-O-glucoside through the inhibition of nitric oxide (NO) production in vitro and in vivo. Results revealed that luteolin 5-O-glucoside dosedependently inhibited NO production and expression of iNOS and COX-2 in LPS-induced RAW 264.7 cells. Luteolin 5-O-glucoside also significantly inhibited the translocation of NF-κB, the activation of MAPKs, and ROS generation in LPS-induced RAW 264.7 cells. In addition, protein expressions of Nrf-2 and HO-1 were also upregulated by luteolin 5-O-glucoside treatment. Moreover, luteolin 5-O-glucoside inhibited λ-carrageenaninduced mouse paw edema by 65.34% and 48.31% at doses of 50 and 100 mg/kg body weight, respectively. These findings indicate potential anti-inflammatory effect of luteolin 5-O-glucoside particularly by downregulating NF-κB and upregulating HO-1/Nrf-2 pathway.

Heme Oxygenase 1-Mediated Anti-Inflammatory Effect of Extract from the Aerial Part of Heracleum moellendorffii Hance

“…MAPKs and NF-κB are crucial intracellular signaling molecules that mediate the synthesis and secretion of various inflammatory cytokines in LPS-treated macrophages [24]. NF-κB plays a pivotal role in regulating the expression of genes involved in inflammation.…”

Discovery of a Highly Potent Tyrosinase Inhibitor, Luteolin 5-O-β-d-Glucopyranoside, Isolated from Cirsium japonicum var. maackii (Maxim.) Matsum., Korean Thistle: Kinetics and Computational Molecular Docking Simulation

“…Furthermore, recent studies carried out on C. maackii have reported anti-inflammatory, , hepatoprotective, and anti-cancer effects. Additionally, it may have a preventive effect in diabetic complications through inhibition of advanced glycation end-product formation and aldose reductase. , Cirsium species show anti-tyrosinase inhibitory activity as well. , …”

“…Traditionally, it has been used in Chinese medicine as an anti-hepatitis, anti-hemorrhagic, anti-hypertensive, and a uretic agent. 7 Furthermore, recent studies carried out on C. maackii have reported anti-inflammatory, 8,9 hepatoprotective, 10 and anti-cancer 11 effects. Additionally, it may have a preventive effect in diabetic complications through inhibition of advanced glycation end-product formation 12 and aldose reductase.…”