Chemical investigation of the 80% Me(2)CO extract from the seeds of Prunus tomentosa led to the isolation and identification of six flavonoids: kaempferol (1), kaempferol 3-O-alpha-L-rhamnopyranoside (2; afzelin), kaempferol 3-O-beta-D-(6-acetyl)-glucopyranosyl(1-->4)-alpha-L-rhamnopyranoside (3; multiflorin A), kaempferol 3-O-beta-D-glucopyranosyl(1-->4)-alpha-L-rhamnopyranoside (4; multiflorin B), quercetin 3-O-alpha-L-rhamnopyranoside (5; quercitrin), and quercetin 3-O-beta-D-glucopyranosyl (1-->4)-alpha-L-rhamnopyranoside (6; multinoside A). Anti-oxidative and inhibitory activities on nitric oxide (NO) and prostaglandin E(2) production in interferon-gamma (INF-gamma) and lipopolysaccharide (LPS)-activated RAW 264.7 cells in vitro (COX-2) of the isolated compounds were evaluated. Compounds 1, 5, and 6 exhibited potent anti-oxidative activity in the DPPH radical scavenging assay with IC(50) values of 57.2, 59.4, and 54.3 microg/mL respectively. The positive control, ascorbic acid, had an IC(50) of 55.5 mug/mL. Compounds 1, 5, and 6 also reduced COX-2 levels in a dose dependent manner with IC(50) values of 10.2, 8.7, and 9.6 microg/mL respectively, with the positive control, indomethacin, having an IC(50) of 5.1 microg/mL. All six compounds inhibited NO production in a dose dependent manner with IC(50) values of 35.1, 42.8, 40.0, 44.8, 43.7, and 43.9 microg/mL respectively, while the positive control, L-NMMA, had an IC(50) of 42.1 microg/mL.
Free radicals can cause oxidative damage by oxidizing biomolecules and this results in cell death and tissue damage as is observed in atherosclerosis, cancer, emphysema, cirrhosis, and arthritis. 1) Oxidative damage plays a critical pathological role in human diseases, and thus, anti-oxidative supplements are important because they reduce oxidative damage in the human body. 2)Inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) are known to contribute to inflammatory response via the production of nitric oxide (NO) and prostaglandins.3,4) These two enzymes, which mediated inflammatory events, are highly expressed by proinflammatory cytokines, such as, interferon-g (IFN-g) and tumor necrosis factor a (TNF-a), and by lipopolysaccharide (LPS), a component of the outer membranes of Gram-negative bacteria. 5)Thus, the screening of components that suppress these proteins and their mRNAs has proven to be a useful strategy for identifying therapeutics capable of combating inflammatory diseases. 6,7) As part of our on-going screening program to search antioxidative and anti-inflammatory natural products, 8) we examined the roots of Aconitum koreanum (RAK), which was traditionally used to treat pain, rheumatic arthralgia, epilepsia, furunculus, acne, vertigo, tetanus, and cardialgia.9,10) In addition, diterpene alkaloids, which have been shown to have anti-arrhythmic 11) and myorelaxant 12) effects, also have been isolated from this plant. Furthermore, RAK has been reported to possess analgesic and anti-inflammatory effects. 13)Thus, we undertook to search the components in RAK that scavenge 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radicals and inhibit NO production and the expression of iNOS and COX-2. MATERIALS AND METHODSGeneral Experiment TLC was carried out using precoated silica gel 60 F 254 plates (Merck, Darmstadt, Germany) and ethylacetate-water-acetic acid (10 : 9 : 1, volume ratio) or chloroform-methanol-water (6 : 4 : 1, volume ratio). The spots were detected using UV (254 nm) and by spraying with FeCl 3 and 10% H 2 SO 4 , followed by heating. Compounds were identified by 1 H-and Extraction, Isolation, and Identification The roots of Aconitum koreanum (3 kg) were extracted three times with 80% aqueous acetone at room temperature. After removing the acetone under vacuum, the residual aqueous solution was filtered. The filtrate was then concentrated (328 g) and applied to an Amberlite XAD-2 column (20-50 mesh, 2000 g, 10ϫ100 cm) (Fluka AG, Buchs, Switzerland) eluted with water containing increasing proportions of MeOH, to afford 6 sub-fractions. Repeated column chromatography of fraction 5, which showed anti-oxidative activity with an IC 50 value of 22.66Ϯ2.23 mg/ml compared with a positive control, L-ascorbic acid (IC 50 ϭ13.92Ϯ3.87 mg/ml) (data not shown) on a Sephadex LH-20 column (25-100 mm, 800 g, 6ϫ75 cm) (Pharmacia, Uppsala, Sweden) eluted with 60% MeOH resulted in two sub-fractions (5-1, 5-2). Sub-fraction 5-1 was further separated on a Sephadex LH-20 column (25-100 mm, 800 g, 6ϫ75 cm) el...
Increased levels of eosinphils, IgE, IL-4, 5, and 13 and pro-inflammatory factors (COX-2, iNOS) are observed in patients with atopic dermatitis (AD). Taxifolin 3-O-beta-D-glucopyranoside (TAX) from the roots of Rhododendron mucronulatum (RM) was examined to determine whether its immunomodulatory effect was applicable for treating atopic dermatitis.A total of 7 groups of NC/Nga mice with AD were treated by topical application or intraperitoneal injection of TAX for 4 weeks. Follow-up evaluations were done to assess the changes in clinical observations, eosinophil counts, and levels of IgE, cytokines, COX-2 and iNOS.In the clinical observation during the experimental period, TAX treatment significantly reduced the severity of AD-like lesions induced in NC/Nga mice. Eosinophil and IgE levels decreased after treatment of the animals with TAX. TAX may thus be associated with improvement of eosinophil-related allergic diseases. The expression of cytokines (IL-4, 5 and 13) was significantly inhibited in the TAX-treated group, suggesting that TAX might play an immunoregulatory role associated with AD. In RT-PCR, iNOS and COX-2 expression levels were reduced in the TAX-treated group. In western blotting, the expression levels of iNOS and COX-2 were also reduced in the TAX-treated group.These findings suggest that TAX is effective for the treatment of AD by preventing the production of inflammatory cytokines and by reducing skin inflammation.
The diarylheptanoid, oregonin (ORE), which was isolated from the bark of Alnus japonica Steudel that grows natively in Korea, has been known to exert antioxidative, anti-inflammatory, anti-cancer and immune response inhibitory effects. The antioxidative effect of ORE was observed on the superoxide and 1,1-diphenyl-2-picrylhydrazyl radical, as well as on the expression of inducible nitric oxide synthase and cyclooxygenase-2 in lipopolysaccharide-treated RAW264.7 macrophages. The statistically significant inhibitory action of ORE against production of cytokines induced by bacterial products or by interleukin (IL)-1beta, free radicals and nitrogen species, and a corresponding increase in cellular calcium concentration because of ORE were confirmed in bone marrow and spleen dendritic cells that are known to play important functions in the development and advancement of atopic dermatitis (AD). It was thus expected that ORE would exert a beneficial effect in the treatment of AD. A study on the pharmaceutical benefits of ORE against AD has not yet been conducted in vivo. We therefore used an in vivo AD animal model, namely the NC/Nga mice, and by applying ORE onto the animals through skin application as well as intraperitoneal injection, we attempted to evaluate the benefits of ORE in this system. Evaluation of ORE was conducted by following the SCORE method to score the effect, as well as by measuring the Th2 cytokines IL-4, IL-5 and IL-13 levels from serum and lymphocytes, and IgE and eosinophil levels from serum. Additionally, the expression of mRNA and protein levels was estimated using real-time polymerase chain reaction and Western blotting analysis. The following categories of clinical evaluation, Th2 cytokines IL-4, IL-5 and IL-13 values, serum IgE levels, serum eosinophil levels, and mRNA and protein expression levels of iNOS and COX-2, were evaluated from topical application and intraperitoneal injection groups of ORE. The effects of ORE on AD in NC/Nga mice were confirmed as being similar to the positive control group, while a significant difference with the negative control group was observed. The results presented in this report suggest that ORE might be beneficial in the treatment of AD.
The needles of Pinus densiflora Siebold et Zuccarini, a representative Pinus species that grows in Korea, have been used in oriental traditional medicine as remedies for rheumatitis, hemorrhage, cancer, etc. Phytochemical examination of the needles of Pinus densiflora Siebold et Zuccarini led to the isolation of four lignans, one flavan-3-ol, two flavonols and one organic acid. They were identified as icariside E(4) (1), cupressoside A (2), schizandriside (3), (+)-isolariciresinol (4), (+)-catechin (5), quercetin 3-O-β-D-glucopyranoside (6), 5,7,8,4'-tetrahydroxy-3-methoxy-6-methylflavone 8-O-β-D-glucopyranoside (7) and (-)-shikimic acid (8). In order to evaluate the anti-inflammatory effects of these compounds, their inhibitory activities against nitric oxide and prostaglandin E(2) production in IFN-γ- and lipopolysaccharide-stimulated RAW 264.7 cells were examined.
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