Abstract
Selaginella tamariscina (S. tamariscina) (Beauv.) Spring (Selaginellaceae) has been used in oriental medicine for the treatment of dysmenorrhea, chronic hepatitis, hyperglycemia, amenorrhea, hematuria, prolapse of the anus and metrorrhagia. In the present study, we isolated two strong anti-inflammatory compounds, the biflavonoids hinokiflavone (H) and 7′-O-methyl hinokiflavone (mH), from S. tamariscina and examined their anti-inflammatory activities in lipopolysaccharide (LPS)-mediated murine macrophages (RAW 264.7) and colon epithelial cells (HT-29). H and mH suppressed the production of the inflammatory mediators nitric oxide (NO), interleukin (IL)-6, IL-8, and tumor-necrosis factor (TNF)-α, which are most highly activated in inflammatory bowel disease (IBD). In addition, Western blot analysis revealed that H and mH suppressed the LPS-induced expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2, and the activation of nuclear factor-κB (NF-κB) and extracellular regulated kinases (ERK) 1/2. These results suggest that H and mH are compounds having potent anti-inflammatory effects that could be used to treat such diseases as IBD.
Highlights
Inflammation is part of our innate immunity, and is an important host defense response to injury, tissue ischemia, and autoimmune responses or pathogens, and consists of a complicated set of events regulated by various chemical mediators released by both resident and infiltrating cells [1,2].Inflammatory bowel diseases (IBDs)—principally, ulcerative colitis and Crohn0 s disease—are characterized by chronic inflammatory disease in the gastrointestinal tract due to the transmural infiltration of immune cells, leading to the disruption of the mucosa and, to ulceration
While searching for anti-inflammatory natural products targeting the treatment of IBD, we found that the methanolic extract of S. tamariscina has an inhibitory effect on nitric oxide (NO) production in LPS-induced macrophages
This methanolic extract was suspended in distilled water (DW) and successively partitioned with n-hexane, CHCl3, EtOAc, and n-butanol, and each fraction had no cytotoxicity at a range of ~50 μM (Figure 1A)
Summary
Inflammation is part of our innate immunity, and is an important host defense response to injury, tissue ischemia, and autoimmune responses or pathogens, and consists of a complicated set of events regulated by various chemical mediators released by both resident and infiltrating cells [1,2]. Inflammatory bowel diseases (IBDs)—principally, ulcerative colitis and Crohn0 s disease—are characterized by chronic inflammatory disease in the gastrointestinal tract due to the transmural infiltration of immune cells, leading to the disruption of the mucosa and, to ulceration. These diseases are caused by various environmental and genetic factors [3]. It was reported that amentoflavone and sumaflavone isolated from S. tamariscina have anti-inflammatory activities [20,21]. The potent anti-inflammatory molecular action of the biflavonoids H and mH, isolated from S. tamariscina, was investigated in LPS-induced murine macrophage and colon epithelial cells
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