4H-1-Benzopyran-4-one,5,6,7,8-tetramethoxy-2-(3,4,5-trimethoxyphenyl)-

5'-Methoxynobiletin is a potent and orally active antinociceptive and anti-inflammatory agent. 5'-Methoxynobiletin is a polymethoxyflavone, that can be isolated from A. conyzoides[1][2].

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

5'-Methoxynobiletin (5mg /kg, 腹腔注射) 可显著降低白细胞计数、中性粒细胞流入和渗出液中的蛋白质浓度，并降低几种促炎介质的水平[2]。< br/>5'-Methoxynobiletin (100 mg/kg，口服，一次) 显示出抗伤害和抗炎活性[2]。 5'-Methoxynobiletin (10 mg/kg，静脉注射；50 mg/kg，口服；一次) 在大鼠体内的口服生物利用度较低，约为 8-11%[2]。 Animal Model: Swiss mice (female)[2] Dosage: 100 mg/kg Administration: Orally Result: Significantly reduced both phases of formalin-induced nocifensive behavior after 15, 30 and 60 min of oral administration, when compared to control groups. In the neurogenic phase, inhibitions of 43±3%, 68±6% and 53±5% of the nociceptive response were observed, while for the infammatory phase inhibitions were 70±8%, 91±3% and 85±3% after 15, 30 and 60 min of the oral administration of 5'-Methoxynobiletin, respectively. Animal Model: Wistar rats (male)[2] Dosage: 10 mg/kg (IV), 50 mg/kg (oral) Administration: IV, oral, once (Pharmacokinetic Analysis) Result: Pharmacokinetic Parameters of 5'-Methoxynobiletin in male Wistar rats[1]. IV (10 mg/kg) IG (50 mg/kg) λ (h-1) 0.55±0.03 0.29±0.2 Tmax (h) 2.71±0.49 Cmax (mg/L) 0.62±0.21 AUC0-∞ (mg·h/L) 8.19±4.1 3.65±0.8 t1/2 elimination (h) 1.26±0.1 2.31±0.9 CL (L/h.kg) 1.22±0.26 13.68±0.29 Vd, ss (L/kg) 2.24±0.32 47.46±10.10 F (%) 8.67

[1]. Faqueti LG, et al. Antinociceptive and anti-inflammatory activities of standardized extract of polymethoxyflavones from Ageratum conyzoides. J Ethnopharmacol. 2016 Dec 24;194:369-377.  

[2]. Faqueti LG, et al. Preclinical Pharmacokinetic and Pharmacodynamic Investigation of 5'-Methoxynobiletin from Ageratum conyzoides: In vivo and In silico Approaches. Pharm Res. 2022 Sep;39(9):2135-2145.