5-OH-HxMF

5-OH-HxMF is a hydroxylated polymethoxyflavone that has anti-inflammatory, anticancer, neurotrophic and neuroprotective activities[1][2][3].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Research Areas >> Inflammation/Immunology

Research Areas >> Neurological Disease

5-OH-HxMF（5-20 µM；48 小时）有效诱导 PC12 神经突生长，并伴有神经元分化标记蛋白生长相关蛋白 43(GAP-43)的表达[1] 。 5-OH-HxMF（20 µM；0-120 分钟）导致环 AMP 反应元件结合蛋白 (CREB) 磷酸化、c-fos 基因表达和 CRE 介导的转录增强[1]。 5-OH-HxMF 显着减少一氧化氮和前列腺素 E2 的产生，并下调脂多糖 (LPS) 刺激的 RAW 264.7 细胞中的诱导型一氧化氮合酶 (iNOS) 和 COX-2 表达。5-OH-HxMF 抑制促炎细胞因子的释放，例如肿瘤坏死因子-α 和 IL-1β，并降低转录水平。5-OH-HxMF 显着抑制 LPS 诱导的 NF-κB 从细胞质向细胞核的易位，这与抑制性 IκBα 降解的消除和随后核 p65 水平的降低有关[2]。 5-OH-HxMF 在人白血病细胞中抑制细胞生长并诱导细胞凋亡[3]。PC12 cells10 µM, 20 µM24 hPromoted GAP-43 expression in PC12 cells.PC12 cells20 µM0 min, 30 min, 60 min or 120 minStimulated phosphorylation of CREB in PC12 cells. Cell Viability Assay[1] Cell Line: PC12 cells Concentration: 5 µM, 10 µM, 20 µM Incubation Time: 48 h Result: Significantly evoked a dose-dependent increase on neurite outgrowth. Western Blot Analysis[1] Cell Line: PC12 cells Concentration: 5 µM, 10 µM, 20 µM Incubation Time: 24 h Result: Promoted GAP-43 expression in PC12 cells. Western Blot Analysis[1] Cell Line: PC12 cells Concentration: 20 µM Incubation Time: 0 min, 30 min, 60 min or 120 min Result: Stimulated phosphorylation of CREB in PC12 cells.

5-OH-HxMF（局部处理；每周两次；20 周；200 μL 丙酮中 1 和 3 μmol）是一种有效的抗肿瘤剂，其抑制作用是通过下调炎症 iNOS 和 COX-2 基因表达在小鼠皮肤中[3]。 Animal Model: Female ICR mice treated with 12-O-tetradecanoylphorbol-13-acetate (TPA)[3]. Dosage: 1 and 3 μmol in 200 μL acetone Administration: Topically treated; twice a week; for 20 weeks Result: Significantly inhibited TPA-induced mouse skin inflammation by decreasing inflammatory parameters.

[1]. Hui-Chi Lai, et al. Neurotrophic effect of citrus 5-hydroxy-3,6,7,8,3',4'-hexamethoxyflavone: promotion of neurite outgrowth via cAMP/PKA/CREB pathway in PC12 cells. PLoS One. 2011;6(11):e28280.  

[2]. Min Jeong Kim, et al. Anti-inflammatory effects of 5-hydroxy-3,6,7,8,3',4'-hexamethoxyflavone via NF-κB inactivation in lipopolysaccharide-stimulated RAW 264.7 macrophage. Mol Med Rep. 2014 Apr;9(4):1197-203.  

[3]. Ching-Shu Lai, et al. Inhibitory effect of citrus 5-hydroxy-3,6,7,8,3',4'-hexamethoxyflavone on 12-O-tetradecanoylphorbol 13-acetate-induced skin inflammation and tumor promotion in mice. Carcinogenesis. 2007 Dec;28(12):2581-8.