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Anti-Inflammatory Activities of Biapigenin Mediated by Actions on p38 MAPK Pathway
Hum Nath Jnawali,박영근,전다솜,이은정,김양미 대한화학회 2015 Bulletin of the Korean Chemical Society Vol.36 No.9
Biapigenin is a naturally occurring biflavonoid found in Selaginella tamariscina. This study aimed to investigate the anti-inflammatory activity of biapigenin and its mechanisms of action, and to identify possible target proteins. Biapigenin suppressed nitric oxide (NO) production, as well as tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and macrophage inflammatory protein (MIP)-2 cytokine release. Moreover, biapigenin completely inhibited IL-1β, inducible nitric oxide synthases (iNOS), and MIP-2 mRNA expression and partially suppressed MIP-1 and TNF-α expression. Lipopolysaccharide (LPS)-induced upregulation of p38 mitogen-activated protein kinase (MAPK) phosphorylation was significantly reduced by biapigenin. Fluorescence titration experiment revealed that biapigenin bound to p38 with a high binding affinity of 2.57 × 106 M−1. These results suggest that biapigenin demonstrates anti-inflammatory activities by the regulation of phosphorylation of p38 MAPK pathway. Our results strongly suggest that biapigenin may be a potent biflavonoid inhibitor of p38 MAPK and have therapeutic applications in the treatment of inflammatory diseases.
Hum Nath Jnawali,전다솜,박영건,이은정,허용석,김양미 대한화학회 2015 Bulletin of the Korean Chemical Society Vol.36 No.8
Rhamnetin is a flavonoid found in cloves and vegetables. Previously, we found that rhamnetin showed anti-inflammatory activity in lipopolysaccharide-stimulated RAW264.7 cells, mediated by actions on mitogen-activated protein kinases pathways. Here, we investigated interactions between extracellular signal-regulated kinase 1 (ERK1) and rhamnetin. Based on docking study, we propose a binding model of rhamnetin and ERK1, where the 4′-hydroxyl groups of the B-ring and the 5-hydroxyl group of the A-ring of rhamnetin play key roles. In a fluorescence quenching experiment, rhamnetin exhibited high binding affinity to ERK1. We found that rhamnetin has an IC50 value similar to that of the ERK1 inhibitor U0126 in ERK1 kinase assays, as well as to that of the JNK1 inhibitor SP600125 in JNK1 kinase assays. These results imply that rhamnetin may be a candidate inhibitor of ERK1 and JNK1, with potent anti-inflammatory activity.
Jnawali, Hum Nath,Lee, Eunjung,Jeong, Ki-Woong,Shin, Areum,Heo, Yong-Seok,Kim, Yangmee American Chemical Society and American Society of 2014 Journal of natural products Vol.77 No.2
<P>Rhamnetin (<B>1</B>), a commonly occurring plant O-methylated flavonoid, possesses antioxidant properties. To address the potential therapeutic efficacy of <B>1</B>, its anti-inflammatory activity and mode of action in mouse macrophage-derived RAW264.7 cells stimulated with lipopolysaccharide (LPS) or interferon (IFN)-γ were investigated. Rhamnetin (<B>1</B>) suppressed mouse tumor necrosis factor (mTNF)-α, mouse macrophage inflammatory protein (mMIP)-1, and mMIP-2 cytokine production in LPS-stimulated macrophages. A nontoxic dose of <B>1</B> suppressed nitric oxide production. It was found that the anti-inflammatory effects of <B>1</B> are mediated by actions on the p38 mitogen-activated protein kinase (MAPK), extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK), and cyclooxygenase (COX)-2 pathways in LPS- or IFN-γ-stimulated RAW264.7 cells. It was determined that <B>1</B> binds to human JNK1 (9.7 × 10<SUP>8</SUP> M<SUP>–1</SUP>) and p38 MAPK (2.31 × 10<SUP>7</SUP> M<SUP>–1</SUP>) with good affinity. The binding model showed interactions with the 3′- and 4′-hydroxy groups of the B-ring and the 5-hydroxy group of the A-ring of <B>1</B>. Further, <B>1</B> exerted an anti-inflammatory effect, reducing the levels of pro-inflammatory cytokines and mediators.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/jnprdf/2014/jnprdf.2014.77.issue-2/np400803n/production/images/medium/np-2013-00803n_0008.gif'></P>
Jnawali, Hum Nath,Lee, Eunjung,Jeong, Ki-Woong,Heo, Yong-Seok,Kim, Yangmee Korean Chemical Society 2013 Bulletin of the Korean Chemical Society Vol.34 No.9
Fisetin is a naturally occurring flavonoid with some anti-cancer and anti-inflammation capabilities. In this study, we perform docking studies between human c-Jun N-terminal kinase 1 (JNK 1) and fisetin and proposed a binding model of fisetin and JNK 1, in which the hydroxyl groups of the B ring and oxygen at the 4-position of the C ring play key roles in binding interactions with JNK. Fluorescence quenching and saturation-transfer difference (STD) NMR experiments showed that fisetin exhibits good binding affinity to JNK, $1.32{\times}10^8M^{-1}$. The anti-inflammatory activity of fisetin was also investigated. Fisetin significantly suppressed tumor necrosis factor, the NO production, and macrophage inflammatory cytokine release in LPS-stimulated RAW264.7 mouse macrophages. We found that the anti-inflammatory cascade of fisetin was mediated through the JNK, and cyclooxygenase (COX)-2 pathways. Our findings suggest the potential of fisetin as an anti-inflammatory agent.