• Korean Journal of Pharmacognosy
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• v.34 no.1 s.132
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• pp.100-108
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• 2003

The regulation of plasma lipid level, particularly LDL cholesterol, represents the focus of current therapy for atherosclerosis. And $Lp-PLA_2$ is able to hydrolyse oxidized phosphatidylcholine within LDL into lyso-PC and oxidized fatty acids. $Lp-PLA_2$ is a potential biomarker of coronary heart disease and plays an important proinflammatory role in the progression of atherosclerosis. We investigated the inhibitory effects of methanol extracts of 224 natural plants on $Lp-PLA_2$ activity. Seven kinds of methanol extracts of tested plants showed above 50% inhibitory effect with the concentration of $100\;{\mu}g/ml$. The concentrated aqueous suspensions of each methanol extract were partitioned with n-hexane, $CHCl_3$, and EtOAc. Among them, EtOAc extracts of Astilbe chinensis var. davidii (root) and Pourthiaea villosa var. brunnea (leaf) significantly inhibited $Lp-PLA_2$ activity at the same concentration.

• Bulletin of the Korean Chemical Society
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• v.35 no.1
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• pp.250-252
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• 2014

Lipoprotein-associated phospholipase A2 (Lp-$PLA_2$) is a crucial enzyme in atherosclerosis as a potential drug target. The most remarkable Lp-$PLA_2$ inhibitory drug is Darapladib. We determined the binding pose of Darapladib to Lp-$PLA_2$ through docking study. Darapladib formed two hydrogen bonding interactions with the side chain of Tyr160 and Gln352 and several pi-pi interactions with aromatic and aliphatic hydrophobic residues of Lp-$PLA_2$. It is known that the dietylpropan-amine moiety of Darapladib has influence on the improvement of its oral bioavailability and we supposed this in our docking results.

• Food Science and Preservation
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• v.16 no.4
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• pp.512-517
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• 2009

Total phenolic content and the antioxidative activity (DPPH radical-scavenging capacity) of 29 fruits and vegetables were determined. The total phenolic contents of plum (1.06 mg GAE/g fresh weight) and cherry (0.95 mg GAE/g fresh weight) were high, whereas those of banana, carrot, and cucumber (each at 0.07 mg GAE/g fresh weight) were low. In the DPPH radical-scavenging assay, apple mango extract showed the highest value(92.8%) among the 29 ethanol extracts tested, followed by paprika (75.4%), beet (75.3%), and cherry (75.1%). In the $Lp-PLA_2$ inhibition assay, cherry (34.95% inhibition) and grape (31.03%) showed the highest $Lp-PLA_2$ activities among the 29 fruits and vegetables examined.

• Journal of Radiation Industry
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• v.3 no.1
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• pp.25-29
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• 2009

Microarrays can be used to screen thousands of binding events in a parallel and high throughput fashion and are of major importance in disease diagnosis and drug discovery. The use of radioisotope is conventionally regarded as one of the most sensitive detection methods. Atherosclerosis is a common disorder affecting arterial blood vessels. It happens when fat, cholesterol, and other substances made in the arterial blood vessels form a hard substances called plaque. Lipoprotein-associated phospholipase $A_2$ ($Lp-PLA_2$), a phospholipase $A_2$ enzyme, is used as a marker for cardiac disease. The detection of $Lp-PLA_2$ was accomplished by using radioactive [$^3H-acetyl$] PAF as a substrate and a feasibility study on RI biochip application to detection of $Lp-PLA_2$, a risk factors of atherosclerosis was performed. Inhibitive activity of a native plant extract was also determined by using the RI biochip. It was found to be applicable to a high-throughput screening of inhibitors for developing atherosclerosis therapeutic agents.

• Korean Journal of Pharmacognosy
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• v.35 no.3 s.138
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• pp.233-238
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• 2004

Lipoprotein-associated phospholipase $A_2\;(Lp-PLA_2)$ is a potential biomarker of coronary heart disease and plays an important proinflammatory role in the progression of atherosclerosis. Also acyl-CoA: cholesterol acyltransferase (ACAT) and oxidized low-density lipoprotein (LDL) playa key role in atherosclerosis, respectively. And so, the inhibitory activities of the methanol extracts of 42 insect resources were examined on $Lp-PLA_2$, ACAT, and LDL oxidation for screening of anti-atherogenic substances. Among them, the methanol extracts of Eurydema rugosa significantly inhibited all of upper three activities. Several kinds of tested insects having high inhibitory effect with the methanol extracts were extracted with n-hexane, ethyl acetate, and acetone, and their inhibitory activities were tested.

• Journal of Society of Preventive Korean Medicine
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• v.12 no.3
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• pp.91-98
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• 2008

80% MeOH extract of black rices fractionated with n-hexane, EtOAc, and n-BuOH. Copper-induced LDL oxidation inhibition assay and ACAT inhibition assay examined with fractions. n-Hexane and EtOAc fractions showed high inhibition activity. We divided n-hexane fraction into three sub-layers(H1 - H3) and EtOAc into eight sub-layers(E1 - E8). H1, H2, E6, and E7 are showed higher inhibition activity than standard in Lp-PLA2 inhibition assay and H1 and E6 are showed higher ACAT inhibition activity than standard.

• Archives of Pharmacal Research
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• v.28 no.5
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• pp.541-545
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• 2005

Flowers of Erigeron annuus L. were extracted with 80% aqueous MeOH, and the concentrated extract was partitioned with EtOAc, n-BuOH, and H$_2$O. Repeated silica gel and OD S column chromatography of the EtOAc fraction led to the isolation of a sterol, through activityguided fractionation, using ACAT inhibitory activity measurements. From the physico-chemical data, including NMR, MS, and IR, the chemical structure of the compound was determined to be an ergosterol peroxide (1), which has been isolated for the first time from this plant. This compound exhibited hACAT-1 and Lp-PLA$_2$ inhibitory effects, with inhibitory values of 51.6 ${\pm}$ 0.9 and 51 .7 ${\pm}$ 1.2%, at a treatment concentration of 0.23 mM.

• Korean Journal of Food Science and Technology
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• v.50 no.6
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• pp.671-679
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• 2018

Glasswort has attracted an attention because of its interesting physiological actions. In this study, the effects of glasswort on inflammatory events including nitric oxide (NO) synthesis and arachidonic acid metabolism in cultured RAW264.7 macrophages were investigated. A series of solvent fractions, including fractions of hexane (Fr.H), ethyl ether (Fr.E), ethyl acetate, butanol, and water, were prepared from a 70% methanol extract of glasswort. Among the fractions, Fr.E showed the strongest inhibition of NO synthesis and inducible NO synthase (iNOS) expression in lipopolysaccharide (LPS)-stimulated macrophages. At a concentration of $80{\mu}g/mL$, Fr.E decreased the NO and iNOS levels by 73 and 77%, respectively, after 24 h. Fr.E showed the most potent inhibitory effects on the expressions of cytosolic phospholipase $A_2$ and cyclooxygenase-2 with $IC_{50}$ values of 33.4 and $27.9{\mu}g/mL$, respectively. Fr.H and Fr.E also significantly inhibited 5-lipoxygenase expression in LPS-stimulated macrophages. These results suggest that the hydrophobic fractions of glasswort possess anti-inflammatory activities through modulating the arachidonic acid metabolism and NO synthesis.

• Journal of Acupuncture Research
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• v.22 no.3
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• pp.155-167
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• 2005

Objectives : The purpose of this study was to investigate the anti-inflammatory effect of Cobrotoxin on binding affinity of cobrotoxin with P50, $IKK{\alpa}$ and $IKK{\beta}$, activities of NF-${\kappa}B$, Cell viability of astrocyte, expressions of protein molecules of NF-${\kappa}B$ such as P50, P-$1{kappa}B$, $1{\kappa}B$ and iflammation related genes such as Cox-2, iNOS, cPLA2 in the SNP or LPS induced Inflammatory pathway of Rats' astrocytes. Methods : In this study, The expression of cytosolic phospholipase A2, Nitric oxcide, Cyclooxygenase-2 and inducible nitrogen oxide synthase was determined by western blotting with corresponding antibodies, and the generation of NF-${\kappa}B$ was assayed by EMSA method in astrocytes of rats. The Cell viability of astrocytes was determined by MTT assay, and Binding affinity of Cobrotoxin with P50, $IKK{\alpha}$ and $IKK{\beta}$ was assayed by Surface plasmon resonance analysis, and NF-${\kappa}B$ dependent luciferase activity was determined by luciferase analysis, and Uptake of cobrotoxin in astrocytes was identified by Confocal laser scanning microscope Results : 1. Compared with control, LPS-induced NF-${\kappa}B$ DNA binding activity was decreased significantly by 0.1, $0.5{\mu}g/m{\ell}$ of Cobrotoxin in Astrocyte. 2. Compared with control, LPS-induced NF-kB dependent luciferase expression was decreased significantly by 0.1, 0.5 and $1{\mu}g/m{\ell}$ of Cobrotoxin in Astrocyte. 3. Compared with control, SNP induced P50, $I{\kappa}B$ expressions in astrocyte were decreased significantly by 0.1, 0.5 and $1{\mu}g/m{\ell}$ of Cobrotoxin and P-$1{\kappa}B$ expression was decreased significantly by 0.5 and $1{\mu}g/m{\ell}$ of Cobrotoxin. 4. Compared with control, LPS induced P50, $1{\kappa}B$ expressions in astrocyte were decreased significantly by 0.5 and $1{\mu}g/m{\ell}$ of Cobrotoxin. 5. Compared with control, SNP induced Cox-2, iNOS, CPLA2 expressions in astrocyte were decreased significantly by $1{\mu}g/m{\ell}$ of Cobrotoxin. 6. Compared with control, LPS induced Cox-2, cPLA2 expressions in astrocyte were decreased significantly by 0.1, 0.5, $1{\mu}g/m{\ell}$ of Cobrotoxin and iNOS expression was decreased significantly by 0.5, $1{\mu}g/m{\ell}$ of Cobrotoxin. 7. Compared with $0.5{\mu}g/m{\ell}$ of Cobrotoxin, SNP-induced NF-${\kappa}B$ DNA bindins activity in astrocyte was increased significantly by Cobrotoxin $0.5{\mu}g/m{\ell}$ with DTT 1mM and Cobrotoxin $0.5{\mu}g/m{\ell}$ with DTT 5mM. 8. Compared with $0.5{\mu}g/m{\ell}$ of Cobrotoxin, LPS-induced NF-${\kappa}B$ DNA binding activity in astrocyte was increased significantly by Cobrotoxin $0.5{\mu}g/m{\ell}$ with DTT 1mM, Cobrotoxin $0.5{\mu}g/m{\ell}$ with DTT 5mM, Cobrotoxin $0.5{\mu}g/m{\ell}$with GSH 1mM and Cobrotoxin $0.5{\mu}g/m{\ell}$ with GSH 5mM 9. Compared with $0.1{\mu}g/m{\ell}$ of cobrotoxin, SNP induced P50 expressions in astrocyte were increased significantly by Cobrotoxin $0.5{\mu}g/m{\ell}$ with DTT 1mM, Cobrotoxin $0.5{\mu}g/m{\ell}$ with DTT 5mM Cobrotoxin $0.5{\mu}g/m{\ell}$ with GSH 1mM and Cobrotoxin $0.5{\mu}g/m{\ell}$ with GSH 5mM. 10. The uptake of the labeled cobrotoxin into the cells was shown under a confocal laser scanning microscope. cobrotoxin was uptaken into the membrane and nucleus of astrocytes. Conclusions : In summary, the present results demonstrate that cobrotoxin directly binds to sulfhydryl group of p50 and IKKS resulting In the reduction of translocation of p50 and IkB release, thereby inhibits activation of NF-${\kappa}B$, and suggest that pico to nanomolar range of cobrotoxin could inhibit the expression of genes in the NF-${\kappa}B$ signal pathway.

• Korean Journal of Food Science and Technology
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• v.48 no.4
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• pp.378-383
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• 2016

The glasswort is an edible halophyte demonstrating various physiological effects including anti-inflammatory activity. In the present study, the effects of glasswort extracts on inflammatory events and interactions of THP-1 monocytes with intestinal epithelial cells were investigated. Five solvent fractions, including the ethylether fraction (Fr.E), were prepared from a 70% methanol extract of glasswort. THP-1 monocytes underwent differentiation by phorbol 12-myristate 13-acetate treatment and were then activated by lipopolysaccharide (LPS), which induced cyclooxygenase (COX)-2 expression. None of the glasswort fractions tested alone induced COX-2 in differentiated THP-1 cells. Fr.E, however, enhanced LPS-induced COX-2 expression in differentiated THP-1 cells. Culture media of THP-1 cells treated with each fraction stimulated the growth of normal intestinal INT-407 cells more prominently than that of HT-29 colon cancer cells. COX-2 expression in HT-29 cells was inhibited when the cells were exposed to the THP-1 culture medium treated with Fr.E. Thus, glasswort could modulate the interaction between immune cells and intestinal cells.