• BMB Reports
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• v.35 no.5
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• pp.518-523
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• 2002

Nordihydroguaiaretic acid (NDGA), an inhibitor of lipoxygenase, inhibits the secretion of proteins and causes the redistribution of resident Golgi proteins into the endoplasmic reticulum (ER). In this study, the effect of NDGA on lipoprotein lipase (LPL) secretion was investigated in 3T3-L1 adipocytes, and compared with those of brefeldin A (BFA), a well-known fungal metabolite that exhibits similar ER-Golgi redistribution. Both BFA and NDGA blocked secretions of LPL. In the presence of BFA, the active and dimeric LPL was accumulated in adipocytes. After endoglycosidase H (endo H) digestion, the proportion of LPL subunits with partially endo H-sensitive oligosaccharide was significantly increased with BFA. However, in the presence of NDGA, the cellular LPL became inactive, and only the endo H-sensitive fraction of the LPL subunit was observed. An increase of the aggregated forms was observed in the fractions of the sucrose-density gradient ultracentrifugation. These properties of LPL in the NDGA-treated cells were similar to those of LPL that is retained in ER, and the effects of NDGA could not be reversed by BFA. These results indicate that the inhibitory mechanism of NDGA on the LPL secretion is functionally different from the ER-Golgi redistribution that is induced by BFA.

• Journal of Ginseng Research
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• v.14 no.2
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• pp.191-199
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• 1990

It has been well known that extended exposure to reactive oxygens causes severe damage to susceptible biomolecules. In this study, the effects of flavonoids including trifolin and kaempferol from Ginseng leaves on singlet oxygen induced photohemolysis of erythrocytes and free radical scavenging activities were investigated. Each flavonoid aglycone (5-50$\mu$M) such as kaempferol, quercetin or baicalein exhibited a high protective effect against the photohemolysis. They protected the cells by scavenging $^1O_2$ and free radicals Although the free radical scavenging activities of the flavonoid glycosides were not much lower than those of their corresponding aglycones, their insolubility into lipid bilayers of membrane made them less effective in preventing the photohemolysis induced by $^1O_2$. The $^1O_2$ and free radical scavenging activities of flavonoids were estimated by the decomposition of the flavonoid by $^1O_2$ and the bleaching of free radicals by the flavonoid, respectively. The solubilization of the flavonoid into micells or erythrocytes was deduced from spectrophotometric and microscopic observations. The cooperation of L-ascorbic acid and a flavonoid, and a possible involvement of lipoxygenase or cyclooxygenase in the photohemolysis mechanism were discussed.

• Korean Journal of Pharmacognosy
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• v.38 no.4
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• pp.363-371
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• 2007

Schizandrae Fruits has been used as a traditional Oriental medicine for treatment of many stress-induced diseases. In the present study, we investigated inhibitory activity of enzymatic hydrolysate of Schizandrae fructus (SC-EX) in growth of tested intestinal microorganism and activity of bowel inflammation related enzyme. SC-EX was added to the proteose peptone-yeast extract-fildes (PYF) media to investigation the effect on the growth of type culture of intestinal microorganism. The growth of lactic acid bacteria such as Bifidobacterium species and Lactobacillus species was accelerated by more than 3% concentration of SC-EX. But, growth of harmfulness bacteria such as E.coli, Clostridium sp. Staphylococcus sp. Streptococcus sp. was inhibited by more than 3% concentration of SC-EX. Also, SC-EX was exhibited a concentration-dependent inhibitory activity of the bowel inflammation related enzymes. The SC-EX was showed 76% and 92% inhibitory activity of 5-lipoxygenase and cyclooygenase at 5% additional concentration respectively. Our results indicated that SC-EX may possess improvement effect on the intestinal flora and Anti-inflammatory effect on the bowel.

• Natural Product Sciences
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• v.22 no.4
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• pp.225-230
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• 2016

Phytochemical investigation from the stem bark of Beilschmiedia pulverulenta resulted in the isolation of five lignans, (+)-yangambin (1), (+)-sesartemin (2), (+)-excelsin (3), (+)-sesamin (4), and (+)-syringaresinol (5), together with lupeol (6), lupenone (7), ${\beta}-sitosterol$ (8), and ${\beta}-sitostenone$ (9). Their structures were established by the analysis of their spectroscopic (1D and 2D NMR) and spectrometric (MS) data, as well as by comparison with those reported in the literature. The isolated lignans were tested for their anticholinesterase (AChE: acetylcholine esterase and BChE: butyryl cholineesterase) and anti-inflammatory (COX-2: cyclooxygenase-2 and LOX: lipoxygenase) activities. All the isolated lignans (1 - 5) exhibited significant inhibition activities in AChE/BChE and COX-2/LOX assays with $IC_{50}$ values ranging from $168.8-504.2{\mu}M$ and $21.0-59.4{\mu}M$, respectively.

• Environmental Analysis Health and Toxicology
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• v.14 no.3
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• pp.95-101
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• 1999

The scavenging effects of two hyaroxycinnamic acids such as caffeic acid and chlorogenic acid on paraquat induced pulmonary toxicity were investigated. The results are summerized as follows: 1. In the 5-lipoxygenase assay, caffeic acid and chlorogenic acid inhibited the enzyme activities whose inhibition concentration (IC$\_$50/) were 4.1 and 9.6 ${\mu}$M respectively. 2. To evaluate the antiinflammatory effects on mediator related to the mechanism of inflammation, ADP-induced platelet aggregation assay and histamine degranulation assay were used. Caffeic acid and chlorogenic acid inhibited on ADP-induced platelet aggregation and histamine release at a concentration dependent manners. 3. Arachidonic acid-induced ear edema were inhibited by administration of caffeic acid and chlorogenic acid. 4. Cytologicad analysis of branchoalveolar lavage fluid (BALF) which was the useful tool for detection of an inflammatory response in the lungs of animals intoxicated with chemicals were used. Alveolar macrophages and neutrophils in BALF, as well as the protein content and the LDH activity in BALF supernatant increased by intoxication of paraquat, but decreased by administration of caffeic acid and chlorogenic acid. Therefore, two hydroxyeinnamic acids tested were the useful candidates for scavenger and antiinflammatory agents on paraquat induced pulmonary toxicity.

• Environmental Analysis Health and Toxicology
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• v.10 no.3_4
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• pp.29-40
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• 1995

To investigate and evaluate the scavenging and antioxidative effects of various ftavonoids on paraquat induced pulmonary toxicity, in vivo and vitro tests of eight flavonoids(catechin, epicatechin, flayone, chrysin, apigenin, quercetin, morin and biochanin A) were carried out. In vitro test, inhibitory and antioxidative effects of lipoxygenase dependent lipidperoxidation, NADPH dependent cytochrome p-450 reductase to liver and lung microsome and superoxide anion production in rat peritoneal exudated macrophage were studied. In vivo test, biochemical parameters and cell population in bronchoalveolar lavage fluid(BALF) in mouse and rats after administration of paraquat and flavonoids were tested. The results are summerized as follows; 1. All flavonoids tested inhibited on NADPH dependent cytochrome p-450 reductase in liver and lung microsome. 2. All flavonoids tested showed the inhibitory effects on the superoxide anion production in rat peritoneal exudated macropharge. 3. Lactate dehydrogenase, acid phosphatase and total protein in BALF of mouse which increased by the administration of paraquat, decreased significantly by catechin, chrysin, morin and biochanin A. 4. Numbers of alveolar macropharge and PMN in BALF of rats which increased by the administration of paraquat decreased by all the tested flavonoids. Therefore, all flavonoids tested showed the useful compounds for scavenger and antioxidant on paraquat induced pulmonary toxicity.

• YAKHAK HOEJI
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• v.56 no.2
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• pp.80-85
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• 2012

Previously, we have reported that arachidonic acid (AA) appears to be involved in the induction of apoptosis in HepG2 human hepatoblastoma cells. In this study we investigated the possible role of the NADPH oxidase, a membranebound enzyme generating reactive oxygen species (ROS), in the mechanism of AA-induced apoptosis in HepG2 cells. Apoptotic cell death induced by AA was significantly suppressed by various inhibitors of the NADPH oxidase, diphenylene iodonium (DPI), apocynin (Apo) and neopterine (NP). In addition, these inhibitors of the NADPH oxidase completely blunted the AA-induced ROS elevation. Next, we investigated the implication of metabolic pathway of AA in these AA actions. Both apoptosis and ROS production induced by AA were not significantly altered by treatment with indomethacin (Indo) or nordihydroguaiaretic acid (NDGA), selective inhibitors of cyclooxygenase (COX) and lipoxygenase (LOX), respectively, suggesting that AA metabolites produced by COX or LOX may not have an essential role in the AA-induced apoptosis and ROS generation. Collectively, these results suggest that the NADPH oxidase may be a key player in the mechanism of AA-induced apoptosis in HepG2 cells. These results further suggest that NADPH oxidase may be a good target for the management of human hepatomas.

• BMB Reports
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• v.49 no.4
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• pp.232-237
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• 2016

Mulberry tree twigs (Ramulus mori) contain large amounts of oxyresveratrols and have traditionally been used as herbal medicines because of their anti-inflammatory properties. However, the signaling mechanism by which R. mori exerts its anti-inflammatory action remains to be elucidated. In this study, we observed that R. mori ethanol extracts (RME) exerted an inhibitory effect on the lipopolysaccharide (LPS)-induced production of the pro-inflammatory cytokine interleukin-6 (IL-6) in Raw264.7 macrophage cells. Additionally, RME inhibited IL-6 production by blocking the leukotriene B₄ receptor-2 (BLT2)-dependent-NADPH oxidase 1 (NOX1)-reactive oxygen species (ROS) cascade, leading to anti-inflammatory activity. Finally, RME suppressed the production of the BLT2 ligands LTB4 and 12(S)-HETE by inhibiting the p38 kinase-cytosolic phospholipase A₂-5-/12-lipoxygenase cascade in LPS-stimulated Raw264.7 cells. Overall, our results suggest that RME inhibits the 'BLT2 ligand-BLT2'-linked autocrine inflammatory axis, and that this BLT2-linked cascade is one of the targets of the anti-inflammatory action of R. mori.

• Nutritional Sciences
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• v.9 no.3
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• pp.152-158
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• 2006

Helicobacter pylori (H. pylori) infection rapidly stimulated either COX-2 or 5-LOX and released arachidonic acid metabolites that have been considered as pivotal mediators in H. pylori-induced inflammatory responses. To determine whether red ginseng extract (RGE) can suppress the biosynthesis of 5(S)-hydroxyeicosatetraenoic acids (HETE), a precursor metabolite of leukotrienes B4 (LTB4) in H. pylori-provoked inflammatory responses in gastric epithelial cells, the biosynthesis of monohydroxy fatty acids was measured using radioactive arachidonic acid and validated by RP-HPLC using non-radioactive AA as substrate in AGS cells cocultured with H. pylori (ATCC 43504) with or without pretreatment of RGE. Among three known major HETEs, H. pylori infection specifically induced the biosynthesis of $^{14}C-5(S)-HETE$ rather than the complex of $^{14}C-15S-/^{14}C-12(S)-HETE$ from $^{14}C-AA$, concomitantly obtained by HPLC(p<0.01). RGE, 1 to $100{\mu}g/ml$, selectively suppressed H. pylori-stimulated $^{14}C-5(S)-HETE$ production implying the attenuation of 5-lipoxygenase activity, of which was similar to known LOX inhibitor NDGA $(10{\mu}M)$ (p<0.01). However, the amount of 5(S)-HETE was significantly reduced by higher dose of RGE $(100{\mu}g/ml)$ (p<0.05). These results indicated that LOX pathway might be one of principle pathogenic mechanisms of H. pylori and red ginseng could be a nutraceutical against H. pylori infection through inhibiting action of LOX activity.

• Journal of the Korean Society of Food Science and Nutrition
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• v.26 no.3
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• pp.376-382
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• 1997

Antioxidative characteristics of doenjang(fermented soybeans paste) phenolics on the lipid oxidation systems were studied by the determination of the oxidative related activity including lipoxygenase (LOX) inhibition, metal chelating and free radical scavengning of doenjang phenolics. Manlikong variety containing the highest amounts of phenolic compounds among the soybean variety, was used for doenjang processing. Doenjang was prepared by the series of processes including soaking for overnight, cooking for 1hr at 12Lb, first fermentation (3 days at 30$\pm$2$^{\circ}C$) for the preparation of meju(soybean koji) after inoculation of Asp. oryzae, and further fermentation(60 days at 30$\pm$2$^{\circ}C$) for the ripening after addition of salt 13% to meju. In order to investigate the antioxidative activity of phenolics in doenjang, the doenjang phenolics was extracted with methanol form freeze dried defatted doenjang. Antioxidative effects of methanol extract on linoleic acid oxidation system were observed by the significantly decreased levels of peroxide and conjugated diene formation. In addition, methanol extract resulted in the inhibition of LOX activity. and also, metal(FeCl$_3$) chelation and free radical scavengning activities were increased with increasing concentration of methanol extract.