Effects of baicalin, baicalein, and wogonin on interleukin-6 and interleukin-8 expression, and nuclear factor-κb binding activities induced by interleukin-1β in human retinal pigment epithelial cell line

Nakamura, Nobuo; Hayasaka, Seiji; Zhang, Xueyun; Nagaki, Yasunori; Matsumoto, Masayuki; Hayasaka, Yoriko; Terasawa, Katsutoshi

doi:10.1016/s0014-4835(03)00116-7

Cited by 77 publications

(49 citation statements)

References 28 publications

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“…Therefore, wogonin may be the first flavonoid inhibitor of COX-2 that does not affect COX-1 and LOX. A recent study also revealed that wogonin inhibited IL-6 and IL-8 production from IL-1b-treated human retinal pigment epithelial cell line (76). It was also observed that wogonin prevented TNF-a and IL-1b induction from LPS-treated RAW 264.7 cells (H.P.…”

Section: Wogonin As An Anti-inflammatory Agentmentioning

confidence: 91%

Anti-inflammatory Plant Flavonoids and Cellular Action Mechanisms

et al. 2004

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Abstract. Plant flavonoids show anti-inflammatory activity in vitro and in vivo. Although not fully understood, several action mechanisms are proposed to explain in vivo anti-inflammatory action. One of the important mechanisms is an inhibition of eicosanoid generating enzymes including phospholipase A 2 , cyclooxygenases, and lipoxygenases, thereby reducing the concentrations of prostanoids and leukotrienes. Recent studies have also shown that certain flavonoids, especially flavone derivatives, express their anti-inflammatory activity at least in part by modulation of proinflammatory gene expression such as cyclooxygenase-2, inducible nitric oxide synthase, and several pivotal cytokines. Due to these unique action mechanisms and significant in vivo activity, flavonoids are considered to be reasonable candidates for new anti-inflammatory drugs. To clearly establish the therapeutic value in inflammatory disorders, in vivo anti-inflammatory activity, and action mechanism of varieties of flavonoids need to be further elucidated. This review summarizes the effect of flavonoids on eicosanoid and nitric oxide generating enzymes and the effect on expression of proinflammatory genes. In vivo anti-inflammatory activity is also discussed. As natural modulators of proinflammatory gene expression, certain flavonoids have a potential for new anti-inflammatory agents.

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Section: Wogonin As An Anti-inflammatory Agentmentioning

confidence: 91%

Anti-inflammatory Plant Flavonoids and Cellular Action Mechanisms

et al. 2004

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“…Flavonoids refer to a series of naturally occurring, lowmolecular-weight plant products exhibiting a variety of biological activities such as antibacterial, antiviral, anti-inflammatory, antiallergic, and vasodilatory activities (Middleton et al, 2000;Nakamura et al, 2003;Suk et al, 2003). LYG-202 (5-hydroxy-8-methoxy-7-(4-(4-methylpiperazin-1-yl)butoxy)-2-phenyl-4H-chromen-4-one), a known synthesized flavonoid with a piperazine substitution (Fig.…”

Section: Introductionmentioning

confidence: 99%

LYG-202 Augments Tumor Necrosis Factor-α-Induced Apoptosis via Attenuating Casein Kinase 2-Dependent Nuclear Factor-κB Pathway in HepG2 Cells

Chen

Zhang

et al. 2012

Mol Pharmacol

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Tumor necrosis factor-␣ (TNF-␣) is being used as an antineoplastic agent in treatment regimens of patients with locally advanced solid tumors, but TNF-␣ alone is only marginally active. In clinical use, it is usually combined with other chemical agents to increase its tumor response rate. Our previous studies reported that LYG-202 (5-hydroxy-8-methoxy-7-(4-(4-methylpiperazin-1-yl)butoxy)-2-phenyl-4H-chromen-4-one), a synthesized flavonoid with a piperazine substitution, has antiproliferative, antiangiogenic, and proapoptotic activities in multiple cancer cell lines. Here we evaluated the antineoplastic effect of TNF-␣ and analyzed the mechanism underlying its combination with LYG-202. Our results indicated that LYG-202 significantly increased the cytostatic and proapoptotic activity of TNF-␣ in HepG2 cells and heightened the protein level of apoptosis-related genes including caspase-3, caspase-8/9, cleaved poly(ADPribose) polymerase, and Bid. The fact that LYG-202 had a fitness score similar to that of the casein kinase 2 (CK2) inhibitor naphthyridine-8-carboxylate (CX-4945) implied to us that it may serve as a potential candidate for CK2 inhibitor, and the kinase activity assay suggested that LYG-202 significantly inhibited CK2 activity. Moreover, the electrophoretic mobility shift assay and luciferase assay showed that LYG-202 blocked the TNF-␣-induced nuclear factor-B (NF-B) survival signaling pathway primarily by inactivating protein kinase CK2. In murine xenograft models, we also found that LYG-202 enhanced TNF-␣ antineoplastic activity and inhibited CK2 activity and NF-B-regulated antiapoptotic gene expression. All these results showed that LYG-202 enhanced TNF-␣-induced apoptosis by attenuating the CK2-dependent NF-B pathway and probably is a promising agent in combination with TNF-␣.

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“…It has been reported that baicalein inhibits NF-κB activation in various cell types such as RAW 264.7 cells, 26) human mast cells 27) and a retinal pigment epithelial cell line. 28) There are reports that 6-gingerol also inhibits NF-κB activation in mouse skin, 29) macrophages 14) and HuH-7 hepatoma cells. 30) Furthermore, it has been recently reported that 6-gingerol has protective effects against ischemia/ reperfusion-induced intestinal mucosa injury mediated by the NF-κB pathway.…”

Section: Discussionmentioning

confidence: 99%

Active Ingredients of Hange-shashin-to, Baicalelin and 6-Gingerol, Inhibit 5-Fluorouracil-Induced Upregulation of CXCL1 in the Colon to Attenuate Diarrhea Development

Sakai

Tabata

Kimura

et al. 2017

Biological & Pharmaceutical Bulletin

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5-Fluorouracil (5-FU)is widely used as an anti cancer drug and is known to cause severe diarrhea. Recently we suggested that levels of chemokine (C-X-C motif) ligand 1 (CXCL1) and neutrophil recruitment in the colonic mucosa were drastically increased by the 5-FU administration in mice. Hange-shashin-to (HST) is prescribed in Japan for treat gastritis, stomatitis, and inflammatory diarrhea. We therefore examined the effects of HST and its active ingredients on 5-FU-induced CXCL1 upregulation in cultured colon tissue, and also examined the effects of HST on 5-FU-induced diarrhea development in the mouse. The distal colon isolated from the mouse was incubated with 5-FU and HST. Mice were given 5-FU (50 mg/kg, intraperitoneally (i.p.)) daily for four days. HST (300 mg/kg, per os ( p.o.)) was administered 30 min before mice received 5-FU. mRNA levels of CXCL1 in the colon were examined using quantitative RT-PCR. 5-FU enhanced CXCL1 mRNA in the colon but the effect by 5-FU was markedly suppressed by application of HST and its active ingredients, baicalein and 6-gingerol. Nuclear factor kappa B (NF-κB) was activated by 5-FU treatment in cultured colon tissue, which was also suppressed by HST and the combination of baicalein and 6-gingerol. Furthermore, HST reduced 5-FU-induced diarrhea development. Under such experimental condition, CXCL1 gene, protein levels of neutrophil elastase and myeloperoxidase upregulation induced by 5-FU in the colon was attenuated by HST. These findings suggest that HST, especially baicalein and 6-gingerol, prevent the development of neutrophil recruitment and diarrhea by the inhibition of NF-κB activity.

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Effects of baicalin, baicalein, and wogonin on interleukin-6 and interleukin-8 expression, and nuclear factor-κb binding activities induced by interleukin-1β in human retinal pigment epithelial cell line

Cited by 77 publications

References 28 publications

Anti-inflammatory Plant Flavonoids and Cellular Action Mechanisms

Anti-inflammatory Plant Flavonoids and Cellular Action Mechanisms

LYG-202 Augments Tumor Necrosis Factor-α-Induced Apoptosis via Attenuating Casein Kinase 2-Dependent Nuclear Factor-κB Pathway in HepG2 Cells

Active Ingredients of Hange-shashin-to, Baicalelin and 6-Gingerol, Inhibit 5-Fluorouracil-Induced Upregulation of CXCL1 in the Colon to Attenuate Diarrhea Development

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