• Title/Summary/Keyword: inhibitory compound

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Screening of Biologically Active Compound from Edible Plant Sources-IX. Isolation and Identification of Sesquiterpene Lactons Isolated from the Root of Ixeris dentata forma albiflora; Inhibition Effects on ACAT, DGAT and FPTase Activity (식용식물자원으로부터 활성물질의 탐색-IX. 흰씀바귀(Ixeris dentata forma albiflora)뿌리에서 Sesquiterpene Lactone 화합물의 분리 및 구조 동정; ACAT, DGAT 및 FPTase 효소 활성의 저해)

  • Bang, Myun-Ho;Jang, Tae-O;Song, Myoung-Chong;Kim, Dong-Hyun;Kwon, Byoung-Mog;Kim, Young-Kuk;Lee, Hyun-Sun;Chung, In-Sik;Kim, Dae-Keun;Kim, Sung-Hoon;Park, Mi-Hyun;Baek, Nam-In
    • Applied Biological Chemistry
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    • v.47 no.2
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    • pp.251-257
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    • 2004
  • The root of lxeris dentata forma albiflora was extracted with 80% aqueous MeOH and solvent fractionated with EtOAc, n-BuOH and water, successively. From the EtOAc and n-BuOH fractions, four sesquiterpene compounds were isolated through the repeated silica gel and ODS column chromatographies. The chemical structures were determined as zaluzanin C (1), $9{\alpha}-hydroxyguaian-4(l5),10(14),11(13)-triene-6,12-olide$ (2), $3{\beta}-O-{\beta}-D-glucopyranosyl-8{\alpha}-hydroxyguaian-4(15),10(14 )-diene-6,12-olide$ (3), and $3{\beta}-O-{\beta}- D-glucopyranosyl-8{\beta}hydroxyguaian-10(14)-ene-6,12-olide$ (4) through the interpretation of several spectral data including 2D-NMR. Some showed the inhibitory effects on DGAT (Diacylglycerol acyltransferase), ($IC_{50}$ values of 1, 2: 0.13, 0.10 mM), the catalyzing enzymes of the intracellular esterification of diacylglycerol and FPTase (Famesyl-protein transferase), ($IC_{50}$ values of 1, 2: 0.15, 0.18 mM), the farnesylation enzyme for Ras protein charge of cancer promotion.

Neuronal Cell Protective Effect of Dendropanax morbifera Extract against High Glucose-Induced Oxidative Stress (High Glucose로 유도된 산화 스트레스에 대한 황칠나무 잎 추출물의 뇌신경세포 보호 효과)

  • Kim, Jong Min;Park, Seon Kyeong;Guo, Tian Jiao;Kang, Jin Yong;Ha, Jeong Su;Lee, Du Sang;Kwon, O-Jun;Lee, Uk;Heo, Ho Jin
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.45 no.7
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    • pp.938-947
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    • 2016
  • Antioxidant activities and neuroprotective effects of ethyl acetate fraction from Dendropanax morbifera (EFDM) against high glucose-induced oxidative stress and neurotoxicity were investigated to confirm their physiological activities. An 80% ethanolic extract of D. morbifera showed the highest contents of total phenolic compounds as well as 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) and 1,1-diphenyl-2-picrylhydrazyl radical scavenging activities. The extract was fractionated using several solvents, and the ethyl acetate fraction showed the highest activities in ferric reducing/antioxidant power and malondialdehyde inhibitory assays. To evaluate the neuroprotective effect based on antioxidant activities, cell viability was assessed using PC12 and MC-IXC cells in $H_2O_2$- and high glucose-induced cytotoxic assays, respectively. EFDM evidently showed neuroprotective effects in all cells (neuron-like PC12 cells and human brain-originated neuroblastoma MC-IXC cells). Inhibitory effect of the extract on acetylcholinesterase (AChE) as an acetylcholine-hydrolyzing enzyme was performed to examine the effect on cognitive function. EFDM presented an AChE inhibitory effect. Finally, high-performance liquid chromatography analysis showed that the major phenolic compound of EFDM is probably a rutin.

Ameliorating effect of the ethyl acetate fraction of Pteridium aquilinum on glucose-induced neuronal apoptosis (포도당으로 유도된 신경세포 손상에 대한 고사리 아세트산에틸 분획물의 개선 효과)

  • Park, Seon Kyeong;Guo, Tian Jiao;Kim, Jong Min;Kang, Jin Yong;Park, Sang Hyun;Kang, Jeong Eun;Kwon, Bong Seok;Lee, Chang Jun;Lee, Uk;Heo, Ho Jin
    • Korean Journal of Food Science and Technology
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    • v.49 no.4
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    • pp.430-437
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    • 2017
  • The protective effect of Pteridium aquilinum on high glucose-induced cytotoxicity was examined in vitro to investigate the relationship between diabetic condition and neuronal dysfunction. The ethyl acetate fraction of P. aquilinum (EFPA), with total phenolic content of 265.08 mg gallic acid equivalent/g, showed higher 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid)/2,2-diphenyl-1-picrylhydrazyl radical scavenging activities and lipid peroxidation inhibitory effect than any other fraction. In addition, EFPA showed a significant reduction in the inhibitory effect on ${\alpha}$-glucosidase activity ($IC_{50}$ value=$205.26{\mu}g/mL$) compared to the acarbose positive control. The anti-oxidative effect in PC12 cells, protective effects on high glucose-induced oxidative stress in neuronal cells, and neurotoxicity were measured using 2',7'-dichlorofluorescin diacetate, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazoliumbromide, and lactate dehydrogenase assays, respectively. EFPA showed conspicuous inhibitory effect on cellular reactive oxygen species production and neuronal cell apoptosis. Finally, kaempferol-3-glucoside was identified as the main phenolic compound of EFPA using high performance liquid chromatography.

Healthy Functional Food Properties of Phenolic Compounds Isolated from Ulmus pumila (유근피(Ulmus pumila)로부터 분리한 phenol성 물질의 건강기능식품 활성)

  • Kim, Kyung-Bum;Jo, Bun-Sung;Park, Hye-Jin;Park, Ki-Tae;An, Bong-Jeun;Ahn, Dong-Hyun;Kim, Myung-Uk;Chae, Jung-Woo;Cho, Young-Je
    • Food Science and Preservation
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    • v.19 no.6
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    • pp.909-918
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    • 2012
  • The phenolic compounds which were extracted with 70% ethanol from Ulmus pumila for 12 hr were the highest as $17.9{\pm}1.0\;mg/g$. DPPH scavenging activity of 70% ethanol extracts was also the highest as $89.5{\pm}1.9%$ and it was confirmed to be high as 80% over in both of water and 70% ethanol extracts containing $50{\mu}g/mL$ over phenolic concentration. ABTS radical cation decolorization activities of water and 70% ethanol extracts were higher as $96.8{\pm}2.9%$, antioxidant protection factor (PF) was 2.0 PF in 70% ethanol and showed higher activities in both of water and 70% ethanol extracts containing $200{\mu}g/mL$ phenolic concentration as 2.5 PF than BHA. TBARs of 70% ethanol extracts was $86.5{\pm}4.6%$, it showed high anti-oxidative activity in $50{\sim}200{\mu}g/mL$ phenolic concentrations of water and 70% ethanol extracts as 80% over. The angiotensin converting enzyme (ACE) inhibitory activity of Ulmus pumila extracts against hypertension was 77.4% and 90.6% in water and 70% ethanol extracts of $200{\mu}g/mL$ phenolic concentration. Xanthine oxidase inhibitory activity of Ulmus pumila extracts for anti-gout effect was not observed in water extracts, but it showed 30% inhibitory activity in 70% ethanol extracts, and 48.1% at $200{\mu}g/mL$ phenolics concentration.

A Study of matrix metalloproteinase-9 inhibitor in root bark of ulmus davidiana planchon (유근피내의 Matrix Metalloproteinase-9 활성 억제제에 관한 연구)

  • Kong, Kwang-Hoon;Han, Kee-Jung;Lee, Kwang-Soo;Cho, Sung-Hye
    • Analytical Science and Technology
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    • v.18 no.2
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    • pp.104-111
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    • 2005
  • Several solvents were used to fractionate an extract obtained from the chapped root bark of Ulmus davidiana Planchon. The each fractionary part was condensed under reduced pressure and then examined to investigate the inhibitory effect on MMPs by modified gelatin zymography, where EA fraction showed the inhibition effect on the activity of MMPs. A compound showing inhibition effect on the MMPs was isolated and purified from EA fraction. Under IR, $^1H$- and $^{13}C$- NMR analyses it is very close to a catethin. This substance showed 48% inhibition effect on measurement of MMP-9 activity at 5 mM and 43% at 10 mM. To verify the effect of this substance on cells, human hepatoma, SK-Hep-1 cells as a cancer model, and Chang liver cells as a normal model were selected. MTT assay was performed to examine the cell viability by treatment of $1{\mu}L/mL$ of the purified substance on cells. The purified substance showed negligible toxicity on human liver cell line.

Purification and Identification of Apoptosis Modulator Pipernonaline from Piper longum Linn. against Prostate Cancer Cells (필발(Piper longum Linn.)로부터 전립선암 세포사멸물질 pipernonaline의 분리 및 동정)

  • Kim, Kwang-Youn;Kim, Yun-Jin;Lee, Wan;Yu, Sun-Nyoung;Cho, Hyo-Jin;Lee, Sun-Yi;Lee, Han-Seung;Sohn, Jae-Hak;Oh, Hyuncheol;Ahn, Soon-Cheol
    • Journal of Life Science
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    • v.19 no.5
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    • pp.671-675
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    • 2009
  • Prostate cancer has been a critical health problem due to an increase of prostate cancer-related deaths worldwide. Also, a frequent treatment option for prostate cancer is androgen ablation, but this treatment has a limited scope, especially for hormone-refractory cancer. There is an urgent need for the identification of alternative therapeutic strategies for prostate cancer. Previously, over one hundred species of dried-plant methanol extracts were tested for inhibitory effects on proliferation. One of them, Piper longum Linn. was selected based on its potent anti-proliferation effect. The dried root of P. longum Linn. was extracted with 100% methanol for 2-3 days and its extract was fractionated using chloroform. The chloroform layer was then subjected to column chromatography on silica gel, reverse phase-18 (RP-18) and Sephadex LH-20, in turn. Finally, the pure compound was obtained and identified as pipernonaline by NMR spectroscopic and physico-chemical analysis. In this study, anti-proliferation and cell cycle arrest effects of pipernonaline on human prostate cancer PC-3 cells were investigated using the MTT and PI staining, respectively. Our findings suggest that pipernonaline represents a dose-dependent growth inhibition pattern on PC-3 cells and, moreover, its growth inhibition is associated with sub-G1 and G0/G1 cell cycle accumulation in PC-3 cells. Also, these results provide an anticancer candidate for human prostate cancer.

Comparison of physiological activities and of useful compounds between new and waste bulbs of different lily (Lilium davidii) varieties

  • Yi, Tae Gyu;Park, Yeri;Yang, Su Jin;Lim, Jung Dae;Park, Sang Un;Park, Kyong Cheul;Park, Nam Il
    • Korean Journal of Agricultural Science
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    • v.43 no.5
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    • pp.734-741
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    • 2016
  • Lily (Lilium davidii) is a high-yielding flowering plant. Besides roses and chrysanthemums, lily bulbs have long been used as food and in oriental medicine. However, the usage and value of cut lily bulbs has not been recognized. A bulb whose yield has been decreased is called a waste bulb, and a large amount of such bulbs is discarded every year. In this study, the functionality of waste bulbs from cut lilies was investigated to explore their potential use as a value-added product. We divided lily bulbs into two groups, one group with six varieties of new bulbs (Medusa, Siberia, Woori Tower, Yelloween, Le Reve, and Morning Star) used for cultivation and the other group with six varieties of waste bulbs (Medusa, Siberia, Woori Tower, Yelloween, Sorbonne, and Sheila). Physiological activities (${\alpha},{\alpha}$-diphenyl-${\beta}$-picrylhydrazyl: DPPH) and 3-ethlbenzthiazolne-6-sulfonic acid (ABTS) radical scavenging capability and tyrosinase inhibiting activity), the amount of total as well as eight individual phenolic compounds (chlorogenic acid, epicatechin, rutin hydrate, p-coumaric acid, kaempferol 3-O-${\beta}$-rutinoside, phloridzin dihydrate, myricetin, and quercetin), and total flavonoid content were measured in the bulbs by high performance liquid chromatography. We detected high amounts of total phenol and total flavonoid as well as high DPPH and ABTS radical scavenging ability. More tyrosinase inhibiting activity was detected in the new bulbs than in the waste bulbs. However, both the new and waste bulbs showed a higher inhibitory activity than the standard (100 ppm ascorbic acid). Although the content of phenolic compounds differed among varieties, under the conditions of the experiment, the most abundant phenolics were epicatechins, followed by chlorogenic acid, and rutins. Overall, the waste bulbs had a higher content of these compounds than the new bulbs. Based on these results, we concluded that bulbs from cut lilies could be used as functional foods in the future and farmers could expect economic gain from the hitherto neglected waste bulbs.

Influences of PAHs and Ammonium on Growth of Duckweed (Lemna perpusilla Torr.) (좀개구리밥(Lemna perpusilla Torr.)의 생육에 대한 PAHs와 암모늄의 영향)

  • Park, Jin Hee;Shim, Sang In
    • Korean Journal of Environment and Ecology
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    • v.28 no.5
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    • pp.510-515
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    • 2014
  • Duckweed (Lemna perpusilla J. Torrey) is a typical floating aquatic macrophyte that has been used for evaluating phytotoxicity of toxicants. In this study, we evaluated the responses of duckweed to PAHs and ammonium as toxicants that frequently affect the growth of plants in polluted industrial and agricultural areas. As the duckweed is growing in aquatic environment, the PAHs and ammonium were incorporated into nutrient solution and the fronds were cultured hydroponically. Frond growth was responded differentially to the concentration and type of PAHs. The severe inhibition of frond growth was observed in the treatment of fluorene. Fluoranthene and pyrene, however, showed weak inhibition of frond growth. The latter PAHs that showed weak inhibition did not reduced frond number at the low concentration of 30 ppm. Pigment contents were also responded differentially. Phenanthrene and fluorene reduced chlorophyll content more strongly than fluoranthene and pyrene. Carotenoids, well-known antioxidative compound, was relatively increased at the low concentration of PAHs up to 30 ppm by the treatment of fluoranthene and pyrene, suggesting an increased antioxidative activity in fronds. Ammonium treatment showed higher inhibitory effect even low concentration of 3 mM.

Anti-invasive Effect of the Solvent-partitioned Fractions from Viticis Fructus in PMA-induced HT-1080 Cells (HT-1080 세포에서 만형자 용매 추출물의 암전이 억제효과)

  • Son, Jaemin;Kim, Hojun;Kong, Chang-Suk;Seo, Youngwan
    • Journal of Life Science
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    • v.28 no.3
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    • pp.293-299
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    • 2018
  • Viticis fructus (fruits of Vitex rotundifolia) is the dried fruit from Vitex rotundifolia; is a traditional medicine for treating inflammation, migraines, chronic bronchitis, headaches, eye pain, and gastrointestinal infections; and demonstrates various bioactivities, including anti-allergic, anti-cancer, and anti-inflammatory effects, which are partly due to its phenolic compound content. This study examines the inhibitory effects of viticis fructus (fruits of Vitex rotundifolia) on MMP-2 and MMP-9 expression using gelatin zymography and RT-PCR in phorbol-12-myristate-13-acetate (PMA)-induced HT-1080 fibro-sarcoma cells. Fruits of Vitex rotundifolia were extracted twice using dichloromethane ($CH_2Cl_2$) and methanol (MeOH). The combined crude extracts ($CH_2Cl_2$ and MeOH) significantly inhibited MMP-2 and MMP-9 activities in gelatin zymography. The combined extracts were fractionated into n-hexane, 85% aqueous methanol (85% aq. MeOH), n-butanol, and water, successively according to polarity. Among all solvent-partitioned fractions, 85% aq. MeOH fractions showed the strongest inhibition on the activation of MMP-2 and MMP-9 in gelatin zymography. In PMA-stimulated HT-1080 cells, the expression levels of MMP-2 and MMP-9 mRNA were also greatly inhibited by the 85% aq. MeOH fraction. These results suggest that viticis fructus can be used as an excellent source for anti-invasive agents.

Antimicrobial Activity of Ethanol Extracts from Medicinal Herbs and Its Active Compound against Plant Pathogens (한약재 주정추출물과 그 유효성분의 식물병원균에 대한 항균활성)

  • Yang, Ji-Yeon;Ryu, Song-Hee;Lim, Sung-Jin;Choi, Geun-Hyoung;Park, Byung-Jun
    • Korean Journal of Environmental Agriculture
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    • v.35 no.3
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    • pp.191-201
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    • 2016
  • BACKGROUND: The aim of this study was to investigate the antimicrobial effects of the ethanol extracts from various medicinal herbs against plant pathogens to understand the possible the crop protection agents.METHODS AND RESULTS: Among the tested medicinal herbs, Zizyphus jujuba ethanol extract had the potent antimicrobial activity against Phytophthora capsici, Erwinia carotovorum subsp. carotovora, Pseudomonas syringae pv. syringae and Ralstonia solanacearum. The major constituents of Z. jujuba were identified to eugenol(40.45%), dodecanoic acid(18.40%), β-caryophyllene (10.05%) and isoeugenol(9.85%) by GC/MS. Eugenol and isoeugenol had strong inhibitory activity on spore germination against P. capsici and growth against E. carotovorum subsp. carotovora, P. syringae pv. syringae and R. solanacearum.CONCLUSION: In this regard, eugenol and isoeugenol were found to be responsible for the antimicrobial activity of Z. jujuba ethanol extract against plant pathogens. In addition, Z. jujuba ethanol extract, eugenol and isoeugenol can be used the potent antimicrobial agents.