Anti-Inflammatory Effects of Flavonoids: Genistein, Kaempferol, Quercetin, and Daidzein Inhibit STAT-1 and NF-κB Activations, Whereas Flavone, Isorhamnetin, Naringenin, and Pelargonidin Inhibit only…
By M. Hämäläinen, R. Nieminen, P. Vuorela, M. Heinonen, E. Moilanen. Mediators of Inflammation, 2007
882 citations recorded by the source corpus.
In inflammation, bacterial products and proinflammatory cytokines induce the formation of large amounts of nitric oxide (NO) by inducible nitric oxide synthase (iNOS), and compounds that inhibit NO production have anti-inflammatory effects. In the present study, we systematically investigated the effects of 36 naturally occurring flavonoids and related compounds on NO production in macrophages exposed to an inflammatory stimulus (lipopolysaccharide, LPS), and evaluated the mechanisms of action of the effective compounds. Flavone, the isoflavones daidzein and genistein, the flavonols isorhamnetin, kaempferol and quercetin, the flavanone naringenin, and the anthocyanin pelargonidin inhibited iNOS protein and mRNA expression and also NO production in a dose-dependent manner. All eight active compounds inhibited the activation of nuclear factor-κB (NF-κB), which is a significant transcription factor for iNOS. Genistein, kaempferol, quercetin, and daidzein also inhibited the activation of the signal transducer and activator of transcription 1 (STAT-1), another important transcription factor for iNOS. The present study characterises the effects and mechanisms of naturally occurring phenolic compounds on iNOS expression and NO production in activated macrophages. The results partially explain the pharmacological efficacy of flavonoids as anti-inflammatory compounds.
Subfields: Biochemistry, Cancer Research, Pathology and Forensic Medicine
View Paper: https://www.semanticscholar.org/paper/83c975b099d90d73badd4d70924ebb04402411b3
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Citations in the corpus
- Flavonoids as anti-inflammatory agents: implications in cancer and cardiovascular disease (2009, background): “They identified eight compounds as being able to inhibit LPS-induced iNOS expression: flavones, daidzein, genistein, isorhamnetin, kaempferol, quercetin, naringenin and pelargonidin [101].”
- Flavonoids as Potential Anti-Inflammatory Molecules: A Review (2022, background): “Daidzein, genistein, kaempferol, and quercetin also inhibited the STAT-1 pathway [54].”
- Regulation of intestinal epithelial permeability by tight junctions (2012, background): “Recently, considerable attention has been given to the physiological effects of polyphenols, including their antioxidative, anti-inflammatory, and anti-carcinogenic effects [215, 216].”
- Bioactivity of dietary polyphenols: The role of metabolites (2020, background): “Both daidzein and genistein showed anti-inflammatory activity through inhibition of iNOS expression and nitric oxide production, and as well inhibition of iNOS STAT-1 and NF-jB transcription factors (H€am€al€ainen et al. 2007).”