• Natural Product Sciences
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• 제14권1호
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• pp.16-20
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• 2008

Three flavonoids (1 - 3) and three phenolic compounds (4 - 6) were isolated from the whole plant of Geranium thunbergii Sieb. et Zucc (Geraniaceae). Their structures were determined by chemical and spectral analysis. These compounds were examined for the inhibitory activity of IL-6 production in $TNF-{\alpha}$ stimulated MG-63 cell. Among the isolated compounds, gallic acid (4) and gallic acid methyl ester (6) showed potent inhibitory activity.

• Natural Product Sciences
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• 제25권3호
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• pp.268-274
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• 2019

Morus alba L., known as white mulberry, is a medicinal plant belongs to family Moraceae. It has long been used commonly in Ayurvedic for the treatment of lung-heat, cough, asthma, hematemesis, dropsy and hypertension. In the present study, seven prenylated flavonoids, along with four benzofuran compounds were isolated by means of repeated column chromatography. The structures of the known compounds were identified as kuwanon G (1), kuwanon E (2), kuwanon T (3), morusin (4), sanggenon A (5), sanggenon M (6), sanggenol A (7), moracin R (8), mulberofuran G (9), mulberofuran A (10) and mulberofuran B (11), by comparing their spectroscopic data with those reported in the literature. For these isolates, containing trace compounds, the inhibitory activity against IL-6 production in $TNF-{\alpha}$ stimulated MG-63 cells was examined. All isolated compounds (1 - 11) showed excellent inhibitory activity against IL-6 production in $TNF-{\alpha}$ stimulated MG-63 cells. Especially this study is first time to report that sanggenon A (5), sanggenon M (6), sanggenol A (7), mulberofuran G (9), mulberofuran A (10) and mulberofuran B (11) showed the inhibitory activity of IL-6 production. Our study suggested the possibility of anti-inflammatory regulation by compounds (1 - 11) isolated from M. alba.

• 한국작물학회:학술대회논문집
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• 한국작물학회 2022년도 추계학술대회
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• pp.312-312
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• 2022

Peanut hull as by-product has been discarded during peanut processing. However, peanut hull contains plenty of polyphenols that shows various physiological activities. The objectives of this study were to investigate anti-inflammatory and enzyme inhibitory activities of polyphenols from 'Sinpalkwang' peanut (Arachis hypogaea L.) hull. Compounds were isolated from methanol extracts of peanut hull by preparative-high performance liquid chromatography after identifying and quantifying polyphenols using Ultra performance liquid chromatography (UPLC) and UPLC-Quadrupole time-of-flight-mass spectrometry profiling. The structures of compounds were elucidated by one-dimensional [¹H, ¹³C] nuclear magnetic resonance (NMR) and two-dimensional NMR (correlated spectroscopy, heteronuclear single quantum coherence and heteronuclear multiple bond correlation). Three compounds were identified as 5,7-dihydroxy-4H-chromen-4-one (peak 2), luteolin (peak 4) and eriodictyol (peak 5). Significant differences in inflammatory mediator such as nitric oxide (NO), interleukin-6 (IL-6) and interleukin-1β (IL-lβ) in lipopolysaccharide stimulated Raw 264.7 macrophages and in enzyme (xanthine oxidase [XO] and α-glucosidase [AG]) inhibitory activities were observed between three compounds (p < 0.05). Peak 5 treated Raw 264.7 macrophages showed lower content of NO (16.4 uM), IL-6 (7.0 ng/mL), and IL-1β (60.6 pg/mL) than peak 2 (NO: 28.3 uM, IL-6: 11.3 ng/mL, IL-1β: 66.9 pg/mL) and peak 4 (NO: 24.7 uM, IL-6: 9.3 ng/mL, IL-1β: 62.6 pg/mL). Peak 5 showed higher XO inhibitory activity (84.7%) and higher AG inhibitory activity (52.4%) than peak 2 (XO inhibitory activity: 45.4%, AG inhibitory activity: 21.6%) and peak 4 (XO inhibitory activity: 37.9%, AG inhibitory activity: 37.5%) at concentration of 0.5mg/mL. This study suggests that peanut hull could be a potential source of anti-inflammatory and physiological materials while creating new use of discarded peanut hull as by-products concomitantly.

• Molecules and Cells
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• 제20권1호
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• pp.105-111
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• 2005

Mannasantin B, a dilignan structurally related to manssantin A, is an inhibitor of NF-${\kappa}B$ transactivation. In the present study, we found that it inhibited PMA-induced expression of IL-$1{\beta}$, IL-$1{\beta}$ mRNA, and IL-$1{\beta}$ promoter activity in U937 cells with $IC_{50}$ values of about 50 nM. It also inhibited NF-IL6- and NF-${\kappa}B$-induced activation of IL-$1{\beta}$, with $IC_{50}$ values of 78 nM and $1.6{\mu}M$, respectively, revealing a potent inhibitory effect on NF-IL6. Electrophoretic mobility shift assays showed that manassantin B had an inhibitory effect on DNA binding by NF-IL6, but not by NF-${\kappa}B$. Further analysis revealed that transactivation by NF-IL6 was also inhibited. Our results indicate that manassantin B suppresses expression of IL-$1{\beta}$ in promonocytic cells by inhibiting not only NF-${\kappa}B$ but also NF-IL6 activity. Furthermore, our observations suggest that manassantin B may be clinically useful as a potent inhibitor of NF-IL6 activity.

• 한방안이비인후피부과학회지
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• 제17권2호
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• pp.12-30
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• 2004

This study was carried out to investigate the effects of SMG on the in vitro and in vivo inflammatory reactions. In experiment I, in vitro tests, ethanol extract of SMG showed potent radical scavenging activity tested by DPPH(I,1-diphenyl-2-picryl-hyrazyl) method and inhibited the lipopolysaccharide-induced gene expressions of interleukin-1${\beta}$, interleukin-6 and tumor necrosis factor-${\alpha}$ (above 50$\%$ at a concentration of 50㎍／㎖) by the macrophage RAW 246.7 cells. Among the herbal ingredients of SMG, ethanol extracts of Scutellaria baicalensis, Paeonia lactiflora, Glycyrrhiza glabra showed potent radical scavenging activity. And Glycyrrhiza glabra and Scutellaria baicalensis showed potent inhibitory activity of nitric oxide production. Especially, ethanol extract of Scutellaria baicalensis inhibited the gene expression of IL-1${\beta}$, IL-6 and TNF-${\alpha}$. In cyclooxygenase-2 assay, Scutellaria baicalensis and Glycyrrhiza glabra showed the potent inhibition of prostaglandin E2 generation. In experiment 2, in vivo tests, SMG showed inhibitory effects on vascular permeability (28.7$\%$) and leukocyte migration (11.5$\%$). These results mean that SMG has a anti-inflammatory effects by it's inhibitory effects of leukocyte migration and vascular permeability as well as it's inhibitory effects of lipopolysaccharide-induced gene expression of IL-1${\beta}$, IL-6 and TNF-${\alpha}$, and radical scavenging activity. Therefore, I expect that SMG may be used as a effective drug for treatment on inflammation.

• 생약학회지
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• 제40권2호
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• pp.123-127
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• 2009

In an ongoing investigation into anti-oxidative compounds from natural products, the EtOAc soluble fraction of Aster tataricus L. (Compositae) showed significant anti-oxidative activity on the NBT superoxide scavenging assay. By means of an activity-guided purification, three flavonoids, kaempferol (1), quercetin (2), astragalin (3) and one monoterpene glycoside, shionoside A (4) were isolated. Their structures were determined spectral analyses. Compounds 2 and 3 showed potent antioxidative activity, while, compounds 1 and 4 were inactive $IC_{50}$>120${\mu}g/mL$. In addition, these compounds were examined for the effect of interleukin-6 (IL-6) production in TNF-${\alpha}$ stimulated MG-63 cell. Compounds 1-3 showed negligible inhibitory activity against IL-6 production in $TNF-{\alpha}$ stimulated $MG-6{\beta}$ cell, and compound 4 was inactive.

• Natural Product Sciences
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• 제12권2호
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• pp.113-117
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• 2006

Quercitrin gallate was previously isolated from Persicaria lapathifolia (Polygonaceae) as an inhibitor of superoxide production. In the present study, quercitrin gallate was found to inhibit interleukin (IL)-6 production in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7 with an $IC_{50}$ value of $63\;{\mu}M$. Furthermore, quercitrin gallate attenuated LPS-induced synthesis of IL-6 transcript but also inhibited LPS-induced IL-6 promoter activity, indicating that the compound could down-regulate IL-6 expression at the transcription level. Since nuclear factor (NF)-kB has been shown to play a key role in LPS-inducible IL-6 expression, an effect of quercitrin gallate on LPS-induced NF-kB activation was further analyzed. Quercitrin gallate exhibited a dosedependent inhibitory effect on LPS-induced nuclear translocation of NF-kB without affecting inhibitory kB (IkB) degradation, and subsequently inhibited LPS-induced NF-kB transcriptional activity in macrophages RAW 264.7. Taken together, quercitrin gallate down-regulated LPS-induced IL-6 expression by inhibiting NF-kB activation, which could provide a pharmacological potential of the compound in IL-6-related immune and inflammatory diseases.

• Archives of Pharmacal Research
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• 제22권1호
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• pp.25-29
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• 1999

Psammaplin A, a natural bromotyrosine derivative from an associated form of two sponges (Poecillastra sp. and jaspis sp.) was found to possess the antimicrobial effect on the Gram-positive bacteria, especially on methicillin-resistant Staphylococcus aureus (MRSA). The minimal inhibitory concentration of psammaplin A against twenty one MRSAs ranged from 0.781 to 6.25 ${\mu}g/ml$, which that of ciprofloxacin was 0.391~3.125${\mu}g/ml$. Psammaplin A could not bind to penicillin binding protein, but inhibited the DNA synthesis and the DNA gyrase activity with the respective 50% (DNA synthesis) and 100% (DNA gyrase) inhibitory concentration 2.83 and 100 ${\mu}g/ml$. These results indicate that psammaplin A has a considerable antibacterial activity, although restricted to a somewhat narrow range of bacteria, probably by inhibiting DNA gyrase.

• 동의생리병리학회지
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• 제18권1호
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• pp.137-147
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• 2004

In order to evaluate the antitumor activity and immunomodulatory effects of Seoleosojong-tang(SST), studies were done. We measured the cytotoxic activity for various kinds of cancer cells, inhibitory effect on activity of DNA topoisomerase I, cell adhesion to complex extracellular matrix, survival time in ICR bearing S-180, pulmonary colonization and histological changes of lung in C57BL/6 injected i.v. with B16-F10, CAM assay, expression of CD4/sup +/, CD8/sup +/, B220/sup +/, cytokine gene in spleen cell. The results were obtained as follows: 1. In cytotoxicity against A549, HT1080, 816-F10, NCL-H661 was showed cytotoxicity as compared with control. 2. The inhibitory effect on adhesion of A549, 816-F10 to complex extracellular matrix was over 40% at 100 ㎍/㎖ of SST. 3. In DNA topoisomerase I assay, SST has inhibitory effect. 4. The T/C% was 120.8 in SST treated group in S-180 bearing ICR mice. 5. In pulmonary colonization assay, a number of colonies were decreased significantly and histological changes were showed that infiltration area of cancer cells were inhibited effectively in SST treated group. 6. In CAM Assay, SST has antiangiogenic effect. 7. On the expression of positive cell to CD4/sup +/, CD8/sup +/ and 8220/sup +/ in spleen cells, CD4/sup +/ cells were increased significantly in SST treated group. 8. Effect of SST on IL-1β gene expression in splenic cell was significantly increased as function of whole concentration. 9. The gene expression of IL-4, IL-6, IL-10, IL-12, IFN-γ, TNF-α were increased in SST treated group. From above results SST could be usefully applied for antitumor activity and immunomodulatory effects, but further research of SST should be required.

• Applied Biological Chemistry
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• 제48권4호
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• pp.315-321
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• 2005

유색미 겨 추출물이 염증반응에 미치는 효과를 호중구 세포주 및 비만세포가 분비하는 염증매개물질인 histamine과 ${\beta}-hexosaminidase$의 분비 및 염증 cytokine 생성에 대한 억제활성을 측정하여 평가하였다. 호중구 세포주인 RBL-2H3 세포와 rat에서 분리 추출한 복강 비만세포(RPMC, peritoneal mast cell)를 이용하여 histamine과 ${\beta}-hexosaminidase$ 분비에 대한 억제활성을 조사한 결과, 일반미 겨 추출물은 RBL-2H3 세포에서 염증매개물질들의 분비량을 증가시킨 반면, 유색미 겨 추출물은 이들의 분비를 억제하였다(histamine 10.19% 억제, ${\beta}-hexosaminidase$ 110.03% 억제). RPMC에서는 유색미가 histamine과 ${\beta}-hexosaminidase$의 분비를 일반미보다 각각 8배와 3배나 높게 억제하는 것으로 나타났다. 염증관련 cytokine으로서 $IL-1{\beta},\;TNF-{\alpha}$ 및 IL-6의 발현을 RT-PCR로 측정한 결과, 유색미가 일반미 보다 $TNF-{\alpha},\;IL-1{\beta}$ 및 IL-6의 발현을 억제하는 효과가 우수하였다. ELISA를 이용하여 cytokine의 분비량을 측정한 실험에서도 유색미가 일반미보다 $TNF-{\alpha},\;IL-1{\beta}$ 및 IL-6의 분비를 효과적으로 억제하였다. 이상의 결과는 유색미가 염증반응의 원인 물질인 histamine과 ${\beta}-hexosaminidase$의 분비에 대한 억제효과 뿐 아니라, 염증 cytokine의 발현을 저해하는 효과도 일반미보다 우수하다는 사실을 보여주었다.