5-OH-HxMF

5-OH-HxMF is a hydroxylated polymethoxyflavone that has anti-inflammatory, anticancer, neurotrophic and neuroprotective activities^[1][2][3]. In Vitro:5-OH-HxMF (5-20 µM; 48 h) effectively induces PC12 neurite outgrowth accompanied with the expression of neuronal differentiation marker protein growth-associated protein-43(GAP-43)^[1].
5-OH-HxMF (20 µM; 0-120 min) causes the enhancement of cyclic AMP response element binding protein (CREB) phosphorylation, c-fos gene expression and CRE-mediated transcription^[1].
5-OH-HxMF significantly reduces the production of nitric oxide and prostaglandin E2 and downregulates inducible nitric oxide synthase (iNOS) and COX-2 expression in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. 5-OH-HxMF inhibits the release of pro-inflammatory cytokines, such as tumor necrosis factor-α and IL-1β, and decreases the transcriptional levels. 5-OH-HxMF significantly inhibits the LPS-induced NF-κB translocation from the cytosol to the nucleus, which is associated with the abrogation of inhibitory IκBα degradation and subsequent decreases in nuclear p65 levels^[2].
5-OH-HxMF inhibits cell growth and induces apoptosis in human leukemia cells^[3]. In Vivo:5-OH-HxMF (topically treated; twice a week; for 20 weeks; 1 and 3 μmol in 200 μL acetone) is an effective antitumor agent and its inhibitory effect is through the down-regulation of inflammatory iNOS and COX-2 gene expression in mouse skin^[3].