• Title/Summary/Keyword: inhibitory compound

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Inhibitory Effect of Scopoletin Isolated from Sorbus commixta on TNF-α-Induced Inflammation in Human Vascular Endothelial EA.hy926 Cells through NF-κB Signaling Pathway Suppression (마가목 수피에서 분리한 scopoletin의 EA.hy926 혈관내피세포에서 NF-κB 신호전달을 통한 TNF-α로 유도된 혈관염증 저해 효과)

  • Kang, Hye Ryung;Kim, Hyo Jung;Kim, Bomi;Kim, Sun-Gun;So, Jai-Hyun;Cho, Soo Jeong;Kwon, Hyun Sook
    • Journal of Life Science
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    • v.30 no.4
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    • pp.343-351
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    • 2020
  • Sorbus commixta Hedl. has traditionally been used as a remedy for cough, asthma, and other bronchial disorders. In this study, three major triterpenoids-lupeol, β-sitosterol, and ursolic acid and a coumarin, scopoletin, were isolated from a CHCl3-soluble fragment of the bark of S. commixta. Their structures were identified by spectroscopic analyses, including mass spectrometry (MS), 1D-, and 2D- nuclear magnetic resonance spectroscopy (NMR), as well as by comparing the data with data reported in the literature. Scopoletin was isolated from this plant for the first time. It is a nutraceutical compound contained in many plants that has been reported to exert diverse biological activities, including anti-inflammatory effects. This study examined the inhibitory effect of scopoletin on TNF-α-induced vascular endothelial inflammation. Unlike the marginal impact of other compounds against low-density lipoprotein (LDL) oxidation and vascular endothelial inflammation, scopoletin showed remarkable activity on LDL oxidation (IC50 = 10.2 μM) and exerted vascular anti-inflammatory effects in EA.hy926 human endothelial cells activated by TNF-α. It suppressed the expression of adhesion molecules, such as ICAM-1, VCAM-1, and E-selectin, and blocked the adhesion between THP-1 monocytes and EA. hy926 endothelial cells. It also inhibited TNF-α-induced NF-κB translocation from the cytosol to the nucleus. Moreover, IκBα phosphorylation, which was increased by TNF-α treatment, was reduced after treatment with scopoletin. Thus, scopoletin inhibited TNF-α-induced vascular inflammation in endothelial cells by suppressing the NF-κB signaling pathway. These results demonstrate that owing to its anti-inflammatory activity in the vascular endothelium, scopoletin has the potential to inhibit atherosclerosis development.

The Inhibitory Effects of Pogostemon cablin Bentham Extract on Melanogenesis (광곽향 추출물의 멜라닌 생성 저해 효과)

  • Bae, Seong-Yun;Lee, Eung-Ji;Son, Rak-Ho;Lee, Yong-Hwa
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.35 no.1
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    • pp.33-39
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    • 2009
  • To develop a new natural whitening agent for cosmetics, we investigated the inhibitory effects of Pogostemon cablin Bentham extracts (PCE) and its active component on melanogenesis. PCE showed ROS scavenging activities in 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and xanthine/xanthine oxidase system with the $IC_{50}$ values of $24.2{\pm}2.85{\mu}g/mL$ and $IC_{50}=118{\pm}0.43{\mu}g/mL$, respectively. PCE reduced melanin contents of B16 melanoma cells in a dose-dependant manner and decreased to about 23 % at a concentration of $20{\mu}g/mL$ without cell cytotoxicity (below $100{\mu}g/mL$). And the PCE reduced intracellular tyrosinase activity about 18 % at concentration of $50{\mu}g/mL$. We purified one active compound from PCE and identified its structure. It was identified as patchouli alcohol, sesquiterpene family, by 1H-NMR, $13_C$-NMR, and Mass analysis. Patchouli alcohol also inhibited ROS scavenging activities in DPPH radical and xanthine/xanthine oxidase system with the $IC_{50}$ values of $3.14{\pm}0.12{\mu}g/mL$ and $49{\pm}3.24{\mu}g/mL$, respectively. Patchouli alcohol inhibited melanin synthesis in a dose dependent manner ($IC_{50}=3.9{\mu}g/mL$). And the patchouli alcohol reduced intracellular tyrosinase activity about 40 % at concentration of $10{\mu}g/mL$. Patchouli alcohol inhibited tyrosinase and TRP-2 expression at protein level. These results suggest that PCE and patchouli alcohol reduced melanin formation by the inhibited of tyrosinase activity and expression in B16 melanoma cells. Therefore, we suggest that PCE could be used as a useful whitening agent.

Studies on the Development of Natural Preservatives from Natural Products (전통식품 및 천연물에서 천연보존료 개발에 관한 연구)

  • Kim, Hee-Yun;Lee, Young-Ja;Hong, Ki-Hyoung;Kwon, Yong-Kwan;Lee, Ju-Yeun;Kim, So-Hee;Ha, Sang-Chunl;Cho, Hong-Yon;Chang, Ih-Seop;Lee, Chul-Won;Kim, Kil-Saeng
    • Korean Journal of Food Science and Technology
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    • v.31 no.6
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    • pp.1667-1678
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    • 1999
  • Certain parts of 190 kinds of medicinal herbs and 171 kinds of original materials of food were extracted by methanol. The extracts were tested their microbial inhibition activities against several food spoilage microorganisms, Micrococcus luteus, Bacillus subtilis, Bacillus cereus, Listeria monocytogenes, Pseudomonas aeruginosa, Salmonella typhimurium, Escherichia coli, Saccharomyces cerevisiae, Candida albicans, Penicillium citrinum, Aspergillus flavus and Aspergillus niger. The methanol extracts of Cornus officinalis, Evodia officinalis, Glycyrrhiza glabra, Salvia miltiorrhiza. Schizandrae fructus, Coptidis rhizoma, aroma hop and bitter hop were shown inhibitory effect on certain species of gram(+) bacteria. Aroma hop and bitter hop were shown inhibitory effect on certain species of gram(-) bacteria. The methanol extract of Salvia miltiorrhiza exhibited a strong antibacterial activities. It was purified by solvent fractionation, silicagel column chromatography, prep. TLC, prep. HPLC. The purified active substance was identified as cryptotanshinone by EIMS, $1^H-NMR,\;{13}^C-NMR$ and DEPT. Cryptotanshinone showed a strong antibacterial activity against gram positive bacteria $(MIC\;:\;3.91{\sim}62.50\;{\mu}g/mL)$. Especially, this compound was the most strong activity against Bacillus subtilis $(MIC\;:\;3.91\;{\mu}g/mL)$.

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Effect of gomchwi (Ligularia fischeri) extract against high glucose- and H2O2-induced oxidative stress in PC12 cells (PC12 신경세포에서 고당 및 과산화수소로 유도된 산화적 스트레스에 대한 곰취 추출물의 효과)

  • Park, Sang Hyun;Park, Seon Kyeong;Ha, Jeong Su;Lee, Du Sang;Kang, Jin Yong;Kim, Jong Min;Lee, Uk;Heo, Ho Jin
    • Korean Journal of Food Science and Technology
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    • v.48 no.5
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    • pp.508-514
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    • 2016
  • Effects of the ethyl acetate fraction from gomchwi (Ligularia fischeri) extract against high $glucose/H_2O_2-induced$ oxidative stress and in vitro neurodegeneration were investigated to confirm the physiological property of the extract. The ethyl acetate fraction of gomchwi extract showed the highest total phenolic contents than the other solvent fractions. An anti-hyperglycemic activity of the ethyl acetate fraction was evaluated using the ${\alpha}-glucosidase$ inhibitory assay, and the half maximal inhibitory concentration ($IC_{50}$) value for ${\alpha}-glucosidase$ was found to be $727.64{\mu}g/mL$. In addition, the ethyl acetate fraction showed excellent 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulfonic acid) diammonium salt radical scavenging activity, and inhibition of malondialdehyde production. The ethyl acetate fraction also decreased intracellular reactive oxygen species, whereas neuronal cell viability against high glucose/$H_2O_2$-induced cytotoxicity was found to be increased. Finally, 3,5-dicaffeoylquinic acid as a main phenolic compound in the ethyl acetate fraction was analyzed by high-performance liquid chromatography. These results suggest that gomchwi might be a good natural source of functional materials to prevent diabetic neurodegeneration.

Biological Activity of Extracts from Acanthopanax sessiliflorum Fruit (오가피(Acanthopanax sessiliflorum) 열매 추출물의 생리활성)

  • Jo, Bun-Sung;Cho, Young-Je
    • Food Science and Preservation
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    • v.19 no.4
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    • pp.586-593
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    • 2012
  • This study was carried out to determine the biological activity of Acanthopanax sessiliflorum fruit extracts. The phenolic compound contents of the extracts were 21.4 and 15.8 mg/g in hot water and 60% ethanol extracts. The total anti-oxidant activities of the water and the 60% ethanol extracts at a 200 ${\mu}g/mL$ phenolic concent ration were at $92.4{\pm}0.8$ and $89.2{\pm}1.1%$ in terms of the DPPH radical scavenging activity, $98.3{\pm}1.1$ and $96.5{\pm}3.5%$ in terms of the ABTS radical decolorization, $2.0{\pm}0.6$ and $1.2{\pm}2.8$ PF in terms of the anti-oxidant protection factor, and $66.3{\pm}0.8$ and $61.4{\pm}2.3%$ in terms of the TBARs inhibitory activity. The activities that inhibited the angiotensin-converting enzyme and xanthin oxidase were at $85.1{\pm}3.2$ and 0% in the water extracts and $59.3{\pm}1.5$ and $9.5{\pm}0.8%$ in the 60% ethanol extracts at the 200 ${\mu}g/mL$ phenolic concentration. The tyrosinase and elastase inhibitory activities were at $56.6{\pm}1.8$ and $53.1{\pm}1.1%$ in the water extracts and $33.7{\pm}2.2$ and $22.4{\pm}3.1%$ in the 60% ethanol extracts. The astringent effect of the water and the 60% ethanol extracts were at $50.5{\pm}0.9$ and $11.5{\pm}4.1%$.

Protective Effects of an Ethanol Extract of Elaeagnus umbellata Leaves on α-MSH-induced Melanin Production in B16-F0 Cells and UVB-induced Damage in CCD-986sk Cells (보리수나무 잎 에탄올 추출물이 α-MSH 유도 B16-F0 세포의 멜라닌 생성 및 UVB 유도성 CCD-986sk 세포 손상에 미치는 효과)

  • Park, Se-Ho;Jhee, Kwang-Hwan;Yang, Seun-Ah
    • Journal of Life Science
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    • v.29 no.5
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    • pp.555-563
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    • 2019
  • This study was undertaken to investigate the effect of an ethanol extract of Elaeagnus umbellata leaves (EUL-EE) on skin-related biological activities. Previously, we have reported that gallic acid was the major phenolic compound in EUL-EE through quantitative analysis and that EUL-EE had an inhibitory effect against the proliferation of liver cancer HepG2 cells. In the present study, the inhibitory effects of EUL-EE on melanin production and tyrosinase activity in ${\alpha}$-melanocyte-stimulated hormone-stimulated B16-F0 cells were determined to assess the effects of EUL-EE on skin whitening. The anti-wrinkle effect using UVB-irradiated CCD-986sk cells was examined by the expression of type I procollagen and metalloproteinase (MMP)-1 release. The EUL-EE significantly decreased intracellular melanin production (33.0% inhibition at $100{\mu}g/ml$) when compared with untreated B16-F0 cells. Tyrosinase activities in the stimulated B16-F0 cells were also decreased by EUL-EE (47.8% inhibition at $100{\mu}g/ml$). The EUL-EE also dose-dependently increased the production of type I procollagen (up to 1.74-fold at $250{\mu}g/ml$) in CCD-986sk cells when compared with UVB-irradiated controls. EUL-EE showed no cytotoxicity at concentrations up to $500{\mu}g/ml$. In addition, EUL-EE at $10-500{\mu}g/ml$ inhibited the release of MMP-1 to the medium from UVB-irradiated CCD-986sk cells. Taken together, these observations indicate that EUL-EE has high potential for use as inner beauty and cosmetic materials due to its whitening and anti-wrinkle effects.

Antioxidant activity and neuroprotective effect of ethanolic extract of Polygonum multiflorum (적하수오(Polygonum multiflorum) 에탄올 추출물의 항산화 활성 및 뇌 신경세포 보호효과)

  • Hye Ji Choi;Hyo Lim Lee;Min Ji Go;Ju Hui Kim;Han Su Lee;In Young Kim;Ho Jin Heo
    • Food Science and Preservation
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    • v.31 no.3
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    • pp.452-461
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    • 2024
  • This study evaluated the in vitro antioxidant activities of ethanolic Polygonum multiflorum (P. multiflorum) extracts and their cytoprotective effects on H2O2-induced HT22 and SK-N-MC cells. Among ethanolic extracts of P. multiflorum, the 40% ethanolic extract of P. multiflorum exhibited high total phenolics and flavonoid contents, with 105.68 mg of GAE/g and 28.92 mg of RE/g, respectively. The 40% ethanolic extract of P. multiflorum showed a high 2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) radical scavenging activity and malondialdehyde (MDA) inhibitory effect. The 40% ethanolic extract of P. multiflorum also showed efficient inhibitory activity against α-glucosidase and acetylcholinesterase. Moreover, the 40% ethanolic extract of P. multiflorum reduced oxidative stress and increased cell viability in H2O2-induced HT22 and SK-N-MC cells as determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetra-zoliumbromide (MTT) and 2',7'-dichlorodihydrofluorescein diacetate (DCF-DA) assay. High-performance liquid chromatography (HPLC) identified 2,3,5,4'-tetrahydroxystilbene-2-O-beta-D-glucoside (TSG) as the bioactive compound in the 40% ethanolic extract of P. multiflorum.

Effect of $Cd^{2+}$ on the Oocyte Maturation and Developmental Stages of Brown Frog Embryo, Rana dybowskii in vitro ($Cd^{2+}$이 북방산개구리의 난자성숙과 배아발달에 미치는 영향)

  • Ko Sun-Kun
    • Korean Journal of Environment and Ecology
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    • v.20 no.3
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    • pp.345-351
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    • 2006
  • This study investigates the toxic effects of $Cd^{2+}$on frog (Rana dybowskii) by the determination of oocyte maturation and development of embryo exposure to different concentrations of the toxicant. The results show that $Cd^{2+}$ concentration of 0.1ppm suppressed the maturation of the oocytes. To examine the reversibility of the inhibitory effects, the oocytes were exposed to the $Cd^{2+}$ only for 3 hours, and then transferred to plain medium and cultured further for 17 hours. The oocytes were recovered from the toxic effect of the $Cd^{2+}$ when they were exposed to 1ppm, but not to 2.5ppm of the $Cd^{2+}$. The development of 2 cell embryos to 32 cell was completely suppressed at 0.1ppm and the longer the embryos were exposed to the $Cd^{2+}$, the more damage appeared to the embryos and the cytolysis of the 32 cell was induced by $Cd^{2+}$ at 0.1ppm. On the other hand, the embryos of blastula stage were cultured 96 hours in presence of the $Cd^{2+}$ at various concentrations and were examined. The rates of mortality and malformed larvae were investigated by probit analysis. From the results of LC$_{50}$ of 0.1ppm and EC$_{50}$ of 0.08ppm, Tl of 5.0 was derived, which indicates $Cd^{2+}$ is to be considered a teratogenic compound. Such specific malformations occurred in 14.3% as spine deformations at the 0.05ppm, in 75.0% as tail deformations at the 0.1ppm, in 66.7% as abdominal deformations at the 0.01ppm and in 26.0% as profound deformations at the 0.1ppm of $Cd^{2+}$ concentration which living embryos were exposed to. $Cd^{2+}$ suppressed growth to head-tail length at 0.1ppm. In conclusion, The study results reveal that $Cd^{2+}$ must be considered highly toxic effect to oocyte maturation and embryonic development.

Inhibitory Effect of Steviol and Its Derivatives on Cell Migration via Regulation of Tight Junction-related Protein Claudin 8 (스테비올 및 그 유도체의 세포연접 관련 클라우딘 8 발현 조절을 통한 세포이동 저해효과)

  • Choi, Sun Kyung;Cho, Nam Joon;Cho, Uk Min;Shim, Joong Hyun;Kim, Kee K.;Hwang, Hyung Seo
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.42 no.4
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    • pp.403-412
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    • 2016
  • The tight junction, one of Intercellular junctions, performs a variety of biological functions by bonding adjacent cells, including the barrier function to control the movement of the electrolyte and water. Recent studies have revealed that unusual expression of tight junction-related genes have been shown to be related in cancer development and progression. Recently, there are many reports that control of tight junction proteins expression is closely related to the skin moisture. In this study, we are focusing on the regulating mechanism of tight junction-associated genes by the steviol and its derivatives. Steviol, used as a sweetner, is known to chemical compound isolated from stevia plant. The MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt) assay was carried out in HaCaT cells (human keratinocyte cell line) in order to determine the cytotoxicity. As a result, while steviol showing cytotoxicity from $250{\mu}M$, steviol derivatives are not cytotoxic more than $250{\mu}M$ concentration. We have observed a change in the tight junction protein via quantitative real-time PCR. Claudin 8 among tight junction proteins is only significantly reduced up to 30% in the presence of steviol. In addition, cell migration was inhibited by steviol, not by stevioside and rebaudioside. Finally, we could observe that steviol, not stevioside and rebaudioside, is able to increase the skin barrier permeability through the transepithelial electric resistance (TEER) measurements. These results suggest that the steviol and its derivatives are specifically acts on the tight junction related gene expression, but steviol derivatives are more suitable as a cosmetic material.

Antifungal and Antioxidant Activities of Extracts from Leaves and Flowers of Camellia japonica L. (동백나무 잎과 꽃 추출물의 항미생물 활성 및 항산화 효과)

  • Lee, Sook-Young;Hwang, Eun-Ju;Kim, Gi-Hae;Choi, Young-Bok;Lim, Chae-Young;Kim, Sun-Min
    • Korean Journal of Medicinal Crop Science
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    • v.13 no.3
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    • pp.93-100
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    • 2005
  • This research was performed to investigate the possibilities of industrial usage of camellia (Camellia japonica L.) by examining the antioxidant and antimicrobial effects of methanol extract with different sections. Content of total phenolics, DPPH radical scavenging activities and antibacterial activity of young leaf, mature leaf, flower bud, flower, bark, and seed of camellia were compared in vitro experimental models. Total phenolics was contained the higher in young leaf (74.62 mg), flower bud (65.02 mg) and flower (62.42 mg) but less than 20.95 mg per 100 g of dry weight in other parts of Camellia japonica L. And effects of antioxidant measured by DPPH radical scavenger activity ($RC_{50}$, reduce concentration 50%), was shown higher $7.16{\sim}18.14\;{\mu}g/m{\ell}$ in methanol extract of young leaf, flower bud and flower than $61.23\;{\mu}g/m{\ell}$ of BHT as a chemical oxidant. Also, the antimicrobial activity of Camellia japonica L. extracts determined using a paper disc method against food-borne pathogen and food spoilage bacteria, the young leaves extracts showed the most active antimicrobial activity against 7 kinds of harmful microorganisms. Flower bud extracts showed the highest antibacterial activity against P. aeruginosa and Enterobacter spp. C1036. In addition, the minimum inhibitory concentration (MIC) of young leaf extract against B. subtillis,S. fradiae,S. aureus,E. coli,P. aeruginosa, Enterobacter spp. C1036, and S. typhimurium were revealed 1 to 15 ${\mu}g/m{\ell}$. As a result, antimicrobial activity of camellia extracts was shown higher gram positive bacteria than gram negative bacteria.