• Toxicological Research
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• v.27 no.2
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• pp.71-76
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• 2011

We demonstrate that baicalein, a bioactive flavonoid originally isolated from Scutellaria baicalensis, inhibits LPS-induced expression of iNOS gene in RAW 264.7 cells. Treatment of peritoneal macrophages and RAW 264.7 cells with baicalein inhibited LPS-stimulated nitric oxide production in a dose-related manner. Immunohistochemical staining of iNOS and RT-PCR analysis showed that the decrease of NO was due to the inhibition of iNOS gene expression in RAW 264.7 cells. Immunostaining of p65, EMSA, and reporter gene assay showed that baicalein inhibited NF-${\kappa}$B nuclear translocation, DNA binding, and transcriptional activation, respectively. Collectively, these series of experiments indicate that baicalein inhibits iNOS gene expression by blocking NF-${\kappa}$B nuclear translocation. Due to the critical role that NO release plays in mediating inflammatory responses, the inhibitory effects of baicalein on iNOS suggest that baicalein may represent a useful anti-inflammatory agent.

• Food Science and Biotechnology
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• v.15 no.4
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• pp.559-563
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• 2006

The growth responses of six bacterial strains exposed to materials extracted from turmeric (Curcuma longa) rhizomes were examined using impregnated paper disk agar diffusion. Methanol extracts of turmeric rhizomes exhibited strong inhibitory activity against Clostridium perfringens and weak inhibitory activity toward Escherichia coli at 5 mg/disk. However, in tests conducted with Bifidobacterium adolescentis, B. bifidum, B. longum, and Lactobacillus casei, the methanol extract showed no inhibitory response. The biologically active constituent isolated from the turmeric rhizomes extracts was characterized as ar-turmerone using various spectroscopic analyses including EI-MS and NMR. The responses varied according to the dosage, chemicals, and bacterial strain tested. At 2 and 1 mg/disk, ar-turmerone strongly inhibited the growth of C. perfringens and moderately inhibited the growth of E. coli without any adverse effects on the growth of four lactic acid-bacteria. Of the commercially available compounds originating from turmeric rhizomes, curcumin exhibited strong and moderate growth inhibition against C. perfringens at 2 and 1 mg/disk, respectively, and weak growth inhibition against E. coli at 1 mg/disk. However, little or no activity was observed for borneol, 1,8-cineole, and sabinene against all six bacteria strains tested. The observed inhibitory activity of the turmeric rhizome-derived curcumin and ar-turmerone against C. perfringens and E. coli demonstrate one of the important pharmacological activities of turmeric rhizomes.

• Journal of Life Science
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• v.21 no.5
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• pp.678-683
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• 2011

The objective of this study was to evaluate the skin inflammation effects of three herb mixture extracts, Ligularia fischeri, Solidago virga-aurea and Aruncus dioicus, which are from Ullung island in Korea. Regulatory mechanisms of cytokines and nitric oxide (NO) are involved in the immunological activity of Raw 264.7 cells. Tested cells were pretreated with 70% acetone extracts of Ligularia fischeri, Solidago virga-aurea and Aruncus dioicus (LSA-A) and further cultured for an appropriated time after lipopolyssacharide (LPS) addition. During the entire experimental period, 1, 10, and 100 ${\mu}g/ml$ of LSA-A had no cytotoxicity. In these concentrations, LSA-A inhibited the production of NO and prostaglandin $E_2$ ($PGE_2$), tumor necorsis factor-a (TNF-a), interleukin-1${\beta}$ (IL-1${\beta}$), interleukin-6 (IL-6) expression of inducible NO synthase (iNOS), and cyclooxygenase-2 (COX-2). LSA-A showed a 60% $PGE_2$ inhibition rate at 100 ${\mu}g/ml$. iNOS and COX-2 inhibition activities were 54%, and 65% at 100 ${\mu}g/ml$, respectively. In addition, LSA-A extract reduced the release of inflammatory cytokines including TNF-a, IL-1${\beta}$ and IL-6. These results suggest that LSA-A may have significant effects on inflammatory factors, and may be a potential anti-inflammatory therapeutic agent.

• YAKHAK HOEJI
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• v.38 no.2
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• pp.114-122
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• 1994

A study on the absorption mechanism of cefixime(CF), an oral ${\alpha}-amino$ group deficient cephalosporin antibiotic, has been undertaken through the rat jejunum and nasal cavity using an in situ simultaneous perfusion technique developed in our laboratory. CF was well absorbed in the jejunum and nasal cavity of rats at pH 5.0, but not at pH 7.0. CF absorption was studied over four orders of magnitude in concentration to determine saturability. Disappearance of CF in the perfusate followed first-order kinetics at all tested concentrations. The apparent first-order absorption rate constant was found to be dependent on the concentration over the range of $0.1\;mM{\sim}3\;mM$ in the jejunum and nasal cavity of rats. Inhibitors were added to determine the competitive inhibition of CF absorption. The presence of L-tyrosine, L-phenylalanine, alanine-alanine, glycine-glycine and cefadroxil produced the significant inhibition of CF absorption in the nasal cavity and jejunum. However, there was no evidence of the inhibition in the presence of cefazolin. In addition, The CF absorption in the nasal cavity and jejunum was inhibited significantly by ouabain and 2,4-dinitrophenol(DNP). This study suggested that CF is absorbed across the rat nasal cavity and jejunum by carrier-mediated transport mechanism and energy consuming system.

• The Korean Journal of Physiology and Pharmacology
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• v.22 no.5
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• pp.597-605
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• 2018

In this study, we demonstrated the inhibitory effect of the Class Ic antiarrhythmic agent propafenone on voltage-dependent $K^+$ (Kv) channels using freshly isolated coronary artery smooth muscle cells from rabbits. The Kv current amplitude was progressively inhibited by propafenone in a dose-dependent manner, with an apparent $IC_{50}$ value of $5.04{\pm}1.05{\mu}M$ and a Hill coefficient of $0.78{\pm}0.06$. The application of propafenone had no significant effect on the steady-state activation and inactivation curves, indicating that propafenone did not affect the voltage-sensitivity of Kv channels. The application of train pulses at frequencies of 1 or 2 Hz progressively increased the propafenone-induced inhibition of the Kv current. Furthermore, the inactivation recovery time constant was increased after the application of propafenone, suggesting that the inhibitory action of propafenone on Kv current is partially use-dependent. Pretreatment with Kv1.5, Kv2.1 or Kv7 inhibitor did not change the inhibitory effect of propafenone on the Kv current. Together, these results suggest that propafenone inhibits the vascular Kv channels in a dose- and use-dependent manner, regardless of $Na^+$ channel inhibition.

• Mycobiology
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• v.31 no.4
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• pp.251-254
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• 2003

To select active bacterial strains to control plant diseases, 57 bacterial strains were isolated from the rhizosphere of the plants growing in various areas such as coast, middle and top of Halla Mountain in Jeju Island. Anti-fungal effect of isolated bactrial strains was tested in vitro by incubating in potato dextrose agar with isolates of four fungal plant pathogens Rhizoctonia solani, Fusarium oxysporum, Colletotrichum gloeosporioides and C. orbiculare, respectively. Thirty-four bacterial strains inhibited the hyphal growth of the plant pathogens, from which 17 strains inhibited one of the tested fungi, 10 strains two fungi, six strains three and a strain TRL2-3 inhibited all of the tested fungi. Some bacterial strains could inhibit weakly the hyphal growth of the plant pathogens, whereas some did very strongly with apparent inhibition zone between the plant pathogens and bacterial strains indicating the unfavorable condition for hyphal growth. Although there was no apparent inhibition zone, some bacterial strains showed a strong suppression of hyphal growth of plant pathogens. Especially, the inhibition by TRL2-3 was remarkably strong in all cases of the tested plant pathogens in this study that could be a possible candidate for biological control of various plant diseases.

• Journal of Ginseng Research
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• v.20 no.3
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• pp.219-225
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• 1996

This study was performed to investigate the inhibition mechanism of cancer cell proof iferation caused by the petroleum-ether extract of ginseng against human rectum (HRT-18), colon (HT-29), llepatoma (Hep G2) and prostate (LNCaP) cancer cells and monkey kidney cells (Vero 76). Cells were treated with the petroleum-ether extract of ginseng (50 to 200 $\mu\textrm{g}$/ml) in G1 or S phase of the cell cycle, and proliferation and protein kinase C activity were measured. The petroleum-eth or extract of ginseng inhibited proliferation of HRT-18, HT-29, Hep G2 and LNCaP when treated in Gl phase, but not in S phase. This result shows that the ginseng extract arrests the cell cycle in G1 phase, resulting in the inhibition of cell proliferation. At the same concentrations, treatment of the ginseng extract in G1 phase decreased protein kinase C activity, while the treatment in S phase had no effect. This reault suggests that protein kinase C might be involved in the inhibition of the cell cycle and proliferation of cancer cells caused by the petroleum-ether extract of ginseng.

• Journal of Microbiology and Biotechnology
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• v.30 no.9
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• pp.1387-1394
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• 2020

Clam worms (Marphysa sanguinea) are a rich source of bioactive components such as the antibacterial peptide, perinerin. In the present study, we explored the physiological activities of a novel NCWPFQGVPLGFQAPP peptide (NCW peptide), which was purified from clam worm extract through high-performance liquid chromatography. Tandem mass spectrometry (MS/MS) revealed that NCW was a new peptide with a molecular weight of 1757.86 kDa. Moreover, NCW peptide exhibited significant antioxidant effects, causing a 50% inhibition of DPPH radical at a concentration of 20 μM without showing any cytotoxicity. These were associated with a reduction in the activity of catalase (CAT), superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), and malondialdehyde (MDA) in LPS-stimulated RAW264. 7 cells. Furthermore, NCW peptide exhibited anti-inflammatory effects in LPS-stimulated RAW264.7 macrophages via inhibition of the abnormal production of pro-inflammatory cytokines including nitric oxide (NO), inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2). These anti-inflammatory effects of NCW peptide were associated with the inhibition of interleukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α). Our results therefore suggest that this novel NCW peptide with antioxidant and anti-inflammatory effects could be a good therapeutic agent against inflammation-related diseases.

• Archives of Pharmacal Research
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• v.22 no.2
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• pp.143-150
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• 1999

melatonin (MLT), N-acetyl-5-methoxytryptamine, is mainly secreted by the pineal gland. The ultraviolet (UV), infrared (IR) and 1H-NMR spectra of irradiated and non-irradiated MLT were measured, and phototoxicity tests of MLT, anthracence (positive control) and sodium lauryl sulfate (SLS, negative control) were performed. The methods employed include both in vitro test such as MTS assay using the human fibroblast cell and yeast growth inhibition assay using Candida albicans and in vivo method using the skin of guinea pig. UV absorption spectra and 1H-NMR spectra of MLT were changed by UVA (365 nm, 15 J/$\textrm{cm}^2$), but IR spectra of MLT were not changed. The fifty percent inhibitory concentration (IC50) ratio (UV-/UV+) of MLT was 10. The inhibition zone of irradiated-paper disks treated with MLT was not observed. According to the results of histophathological examination, no pathologic lesion was observed in the non-irradiated group, but slight degeneration of keratinocytes in the epidermis, homorrhage and vasodilation in dermis were observed in the irradiated group. These results indicated that the molecular structure of MLT is altered by UVA to unidentified photoproducts and a moderate phototoxicity of MLT is predicted.

• Journal of Physiology & Pathology in Korean Medicine
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• v.20 no.5
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• pp.1295-1302
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• 2006

Our preliminary aim is to elucidate the pharmacokinetic features of the PNS(Panax notoginseng Buck F.H. Chen. (Arialiaceae) root). First, we assessed the prevention of neurtrophil functions. A Panax notoginseng inhibited neutrophil functions, including degranulation, superoxide generation, and leukotriene B4 production, without any effect on 5-lipoxygenase activity. This Panax notoginseng reduced nitric oxide (NO) and prostaglandin E2 production in mouse peritoneal macrophages stimulated with lipopolysaccharide, whereas no influence on the activity of inducible NO synthase, cyclo-oxygenase-2 or cyclo-oxygenase-1 was observed. Panax notoginseng significantly reduced mouse paw oedema induced by carrageenan. The results indicate that Panax notoginseng exerts anti-inflammatory effects related to the inhibition of neutrophil functions and of NO and prostaglandin E2 production, which could be due to a decreased expression of inducible NO synthase and cyclo-oxygenase-2.