• Biomolecules & Therapeutics
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• v.18 no.2
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• pp.197-204
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• 2010

To establish the anti-inflammatory activity of the total flavonoid fraction of the root barks of Broussonetia papyrifera (EBP) and a new formula, the ethanol extract of the root barks of B. papyrifera was fractionated with ethylacetate, yielding the hydrophobic prenylated flavonoid-enriched fraction. EBP and the ethanol extract of the whole Lonicera japonica (ELJ) plant were then mixed at a ratio of 1:1 (w/w) to give a new preparation (BL) in the hope of obtaining an optimal formula with a higher anti-inflammatory activity. Evaluation of the effects of these preparations on A23187-treated rat basophilic leukemia (RBL-1) cells revealed that EBP potently inhibited 5-lipoxygenase (5-LOX), while ELJ showed weak inhibition. Additionally, the mixture (BL) clearly showed stronger inhibitory effects against 5-LOX than either preparation alone. These preparations also inhibited cyclooxygenase-2-catalyzed $PGE_2$ and inducible nitric oxide (NO) synthase-catalyzed NO production by lipopolysaccharide-treated RAW 264.7 cells. When tested against arachidonic acid-induced mouse ear edema, EBP showed strong inhibitory activity at doses of 5-200 mg/kg when administered orally, but BL had obviously stronger inhibitory effects. When tested against ${\lambda}$-carrageenan-induced paw edema in mice, BL showed a potent and synergistic anti-inflammatory effect. In addition, in the acetic acid-induced writhing test, BL was found to have strong analgesic activity at 50-400 mg/kg. Taken together, these results indicate that each of these preparations exert anti-inflammatory activity in vitro and in vivo. In particular, BL showed stronger anti-inflammatory activity than EBP, and these anti-inflammatory effects were partially related to the inhibition of eicosanoid and NO production. BL may be useful for the treatment of human inflammatory disorders.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.37 no.1
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• pp.29-41
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• 2024

Objectives : The purpose of this study is to confirm the anti-inflammatory, antioxidant and anti-aging efficacy of Pyeonggangaeuljihyeol-tang(PGJT) extract. Methods : In order to confirm the anti-inflammatory activity of PGJT extract, the inhibitory effect on NO PGE₂ production were evaluated and the expression level of iNOS, COX-2 and IL-6 mRNA were measured through qRT-PCR, Antioxidant activity was evaluated for radical scavenging activity using DPPH and ABTS, anti-aging activity was evaulated for collagenase, elastase, tyrosinase and L-DOPA oxidation inhibitory activity. Results : PGJT extract shows anti-inflammatory effect by inhibiting the production of NO and PGE₂ by reducing the expression level of iNOS, COX-2 and IL-6 mRNA, antioxidant effect by increasing DPPH and ABTS scavenging abillity in a concentration dependent manner. In addition, the anti-aging effect was confirmed by inhibiting collagenase, elastase, tyrosinase production and L-DOPA oxidation. Conclusion : This suggests that PGJT showed an overall excellent anti-inflammatory effect and an inhibitory effect on the activity of antioxidant and anti-aging related enzymes.

• Journal of Periodontal and Implant Science
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• v.23 no.1
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• pp.145-158
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• 1993

The oral microbiota such as P. gingivalis, P. intermedia and A. actinomycetemcomitans play a primary role in the initiation and progression of the periodontal disease. The purpose of this study was to evaluate the antimicrobial effects and inhibitory effects of honokiol and magnolol on the bacterial collagenase activity, cytotoxicity and cytokine production of periodontopathic microorganisms. The antimicrobial activities of honokiol and magnolol was evaluted with minimum inhibition concentration. Honokiol was more active than magnolol, but less than chlorhexidine on antimicrobial activity. The inhibitory effects of magnolol and honokiol on the collagenolytic activity and cytotoxicity were evaluated using a Collagenokit CLN-100 and rapid colorimetric assay (MTT method) for cellular growth and survival of gingival fibroblast and periodontalligament cell and $[^3H]-thymidine$ incorporation for the gingival epithelial cell. The inhibitory effects on the collagenolytic activity was the highest in chlorhexidine, and the lowest in magnolol. Magnolol had the lowest cytotoxic effect and chlorhexidine had the highest. The inhibitory effects on cytokine production was evaluated using $interleukin-1{\beta}$ ELISA kit (Cistron Biotech.), IL-6, $TNF-{\alpha}$ ELISA kit (Genzyme) and inhibitory effects were higher than bacterial LPS and there is no difference among the honokiol, magnolol and chlorhexidine. From these results, the antimicrobial and antienzymatic activities of honokiol and magnolol were seemed to inhibit bacterial growth and enzyme activities with lesser cytotoxic activities. Therefore, it was suggested that honokiol and magnolol are very effective antimicrobial agents on periodontal pathogens.

• Journal of Life Science
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• v.34 no.1
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• pp.28-36
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• 2024

We evaluated the efficacy of Geranium thunbergii (GT), which has so far been understudied as a cosmetic material, and conducted anti-inflammatory-related activity studies. We measured the electron donation ability and ABTS⁺ radical scavenging ability to confirm the antioxidant ability of GT and found values of 91% and 94% at a concentration of 50 ㎍/ml, respectively, confirming that GT had excellent antioxidant ability. Tyrosinase inhibitory activity was measured to evaluate whitening activity, and it was found that inhibitory activity was 24.8% at the highest concentration of 1,000 ㎍/ml. Elastase and collagenase inhibitory activity were measured to determine the wrinkle improvement activity of the GT; 30.6% and 90% inhibitory activity were shown at the highest concentration of 1,000 ㎍/ml, respectively. Excellent inhibitory activity was confirmed through the measurement of collagenase inhibitory activity. Before the cell experiments were conducted, the survival rate of the macrophages Raw 264.7 according to GT treatment was determined based on the MTT assay, and the cell survival rate was greater than 83.6% at a concentration of 100 ㎍/ml. Subsequent cell-related experiments were conducted at concentrations of 100 ㎍/ml or less. The NO production inhibitory activity according to the GT treatment by NO assay was measured, and a 74.9% inhibitory rate was confirmed at a concentration of 100 ㎍/ml. Western blotting was performed to determine protein expression inhibition, and both COX-2 and iNOS factors were concentration-dependently inhibited in GT. Based on these results, GT is considered to have potential as an anti-inflammatory functional cosmetic material.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.41 no.2
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• pp.151-157
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• 2015

In this study, we prepared Eriobotrya japonica leaf extracts by several extraction processes and then evaluated their biological activities for their potential application as a new raw material of functional cosmetic. Their whitening effects were measured by tyrosinase inhibitory activities, and anti-inflammatory effects were determined by inhibitory activities of nitric oxide (NO) production. Among the several extracts obtained from E. japonica leaf, supercritical fluid extract showed tyrosinase inhibitory activities at the concentration of 10%. Inhibitory activity on NO production effect related to anti-inflammatory efficacy was in the order: supercritical fluid extract > ethanol extract > hot water extract. According to the results of MTT assay, cell cytotoxicity was not observed at all concentrations except for a 5% concentration of the 70% ethanol extract. For whitening effects, 30% ethanol and 70% ethanol extract showed mushroom tyrosinase inhibitory activity at the concentration of 5%. These results indicated that E. japonica leaf extracts could have the functional effects when they are added as ingredients in cosmetics.

• Journal of Plant Biology
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• v.38 no.3
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• pp.235-242
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• 1995

Effects of methyl jasmonate (MeJA) on ethylene production in tomato(Lycopersicon esculentum Mill.) hypocotyl segments and fruits were studied. Ethylene production in tomato hypocotyl segments was inhibited by the increasing concentratons of MeJA, and 450 $\mu$M of MeJA showed 50% inhibitory effect. Time course data indicate that this inhibitory effect of MeJA appeared after 3 h of incubation period and continued until 24 h. Inhibition of ethylene producton by MeJA was due to the decrease in 1-aminocyclopropane-1-carboxylic acid(ACC) synthase activity. However, MeJA treatment had no effect on ACC oxidase activity and the accumulaton of ACC oxidase mRNAs. MeJA also inhibited auxin-induced ethylene production by decreasing in ACC synthase activity. In contrast, MeJA stimulated ethylene production in tomato fruits. When 30 $\mu$L/mL MeJA was treated in a gaseous state, ethylene production doubled and this stimulating effect continued until 4 days. To investigate the mechanisms of MeJA on ethylene production, ACC synthase and ACC oxidase activities were examined after MeJA treatment. MeJA increased the activities of both ACC synthase and ACC oxidase, and induced ACC oxidase mRNA accumulation. These data suggest that MeJA plays distinct roles in the ethylene production in different tomato tissues. It is possible that MeJA affects differently the mechanisms of signal transuction leading to the ethylene biosynthesis.

• Bulletin of the Korean Chemical Society
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• v.31 no.1
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• pp.27-30
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• 2010

A series of thioureas were synthesized as inhibitors of NO production in lipopolysaccharide-activated macrophages. We investigated the effect of lipophilic moiety and N-substituents of the thioureas on the activity. Phenoxazine and carbazole-containing derivatives revealed higher activity than indole-containing thioureas. The appropriate spacer between lipophilic tail and thiourea head and methyl substituent at N3 position of thiourea brought beneficial effect on the inhibition of NO production. Among prepared compounds, phenoxazine-containing derivative 2a was the most potent with $2.32 {\mu}M$ of $IC_{50}$ value. RT-PCR analysis suggested that the prepared thioureas inhibited NO production through the suppression of iNOS mRNA expression.

• Journal of Plant Biology
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• v.37 no.4
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• pp.445-452
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• 1994

Effects of methyl jasmonate (MeJA) on ethylene production in mungbean (Phaseolus radiatus L.) hypocotyl and leaf segments were studied. Ethylene production in mungbean hypocotyl segments was decreased in proportion to MeJA concentrations and $450\;\mu\textrm{M}$ of MeJA showed 50% inhibitory effect. This inhibitory effect appeared after 3 h of incubation period and continued for 24 h. Inhibition of ethylene production by MeJA was due to the decrease in 1-aminocyclopropane-1-carboxylic acid (ACC) oxidase activity. However, MeJA treatment had no effect on ACC content and ACC synthase activity. MeJA also inhibited auxin-induced ethylene production in hypocotyls. To investigate the mechanisms of the inhibitory effect of MeJA on the auxin-induced ethylene production, ACC synthase and ACC oxidase activity were examined after MeJA treatment. MeJA decreased the ACC content and ACC synthase activity as weD as ACC oxidase activity in the auxin-treated tissue. These results suggest that the inhibition of MeJA on auxin-induced ethylene production is not due to the direct inhibitory effect of MeJA on the ACC synthase, but to the inhibition of the ability of IAA to promote the synthesis of ACC synthase. In contrast, ethylene production from the detached mungbean leaves was stimulated by MeJA. The rate of ethylene production increased approximately 65% over the control after 12 h of incubation period by $4.5\;\mu\textrm{M}$ MeJA. When MeJA was applied to detached leaves along with IAA, the effect of MeJA appeared to be additive. In an effort to elucidate mechanisms of MeJA action on auxin-induced ethylene production in the leaf tissue, enzyme activities of ACC synthase and ACC oxidase were examined. MeJA stimulated ACC oxidase activity but did not affect ACC synthase activity in leaf tissue. Together, these results suggest that MeJA plays different roles in the ethylene production in the different mungbean tissues.issues.

• Natural Product Sciences
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• v.28 no.1
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• pp.33-39
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• 2022

Eight lignans (1-8) and two macrolides (9-10) were isolated from the CHCl₃-soluble fraction of Houttuynia cordata Thumb (Saururaceae). Structures of isolates were elucidated by extensive spectroscopic methods. Fatty acid-derived macrolides (9-10) have rarely been reported from nature. All the isolates were tested for their inhibitory activities against NO production in RAW 264.7 cells stimulated by LPS. It was found that compounds 3 and 9 remarkably down-regulated LPS-induced NO production with IC₅₀ values, 5.4 and 40.3 μM, respectively, without cytotoxicity.

• Korean Journal of Pharmacognosy
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• v.30 no.4
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• pp.413-416
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• 1999

During the screening for inhibitors on nitric oxide (NO) production in LPS-activated murine macrophage, RAW 264.7 cells, two coumarins were isolated from chloroform extract of Ponciri Fructus. They were identified as imperatorin (10), phellopterin (11) on the basis of spectroscopic methods. The $IC_{50}$ values for NO formatiom were about $5.4\;{\um}M$ and $35.0\;{\um}M$, respectively, and then eleven coumarins were tested for the inhibitory effects on NO production in activated macrophages. All the test coumarins inhibited NO production in concentration-dependent manner and furanocoumarins (6-11) showed much more potent inhibitory effect than simple coumarins. Among the compounds examined xanthotoxin (8) was the most potent inhibitors of NO production $(IC_{50}=1.4\;{\mu}M)$. Analysis of the structure-activity relationship among these coumarins led to the conclusion that the substitution of C-5 position in furanocoumarins reduces greatly their inhibitory potency although the substitution of C-8 does not almost affect it.