• Title/Summary/Keyword: $IC_{50}values$

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Effects of Herbal Medicines on Monoamine Oxidase Activity (수종의 천연물이 Monoamine Oxidase 활성에 미치는 영향 (제3보) : 황련, 계피, 지실의 활성 저해작용)

  • Lee, Sang Seon;Kim, Young Ho;Lee, Myung Koo
    • Korean Journal of Clinical Pharmacy
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    • v.8 no.2
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    • pp.139-142
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    • 1998
  • The effects of MeOH extracts from 28 herbal medicines on monoamine oxidase (MAO) activity were investigated. MAO was purified from mouse brain and its activity was determined by fluoro-photometry using kynuramine as a substrate. Three MeOH extracts, Coptis japonica, Cinnamomum cassia and Poncirus trifoliate from the herbal medicines showed a strong inhibitory effect with less than $100\;{\mu}g/ml$ in their inhibitory amounts of $50\%$ ($IC_{50}$ values) on MAO activity. Four MeOH extracts including Evodia officinalis exhibited a mild inhibition of MAO activity with $100-200\;{\mu}g/ml$ in their $IC_{50}$ values.

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Bioactive Constituents from the Leaves of Zanthoxylum schinifolium

  • Jeong, Su Yang;Nguyen, Phi Hung;Zhao, Bing Tian;Min, Byung Sun;Ma, Eun Sook;Woo, Mi Hee
    • Natural Product Sciences
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    • v.21 no.1
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    • pp.1-5
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    • 2015
  • Activity-guided separation of the methylene chloride-soluble fraction of the leaves of Zanthoxylum schinifolium, resulted in the isolation of four coumarinoids (1 - 4), two triterpenoids (5, 6) and three fatty acid derivatives (7 - 9) as active principles. Their chemical structures were identified as collinin (1), 8-methoxyanisocoumarin (2), 7-(6'R-hydroxy-3',7'-dimethylocta-2',7'-dienyloxy)-coumarin (3), (E)-4-methly-6-(coumarin-7'-yloxy) hex-4-enal (4), lupeol (5), epi-lupeol (6), phytol (7), hexadec-3-enoic acid (8) and palmitic acid (9), on the basis of spectroscopic (1D, 2D and MS) data analyses and comparing with the data published in the literatures. Compounds 1 and 7 showed potent cytotoxicity against Jurkat T cells with $IC_{50}$ values of 45.58 and $47.51{\mu}M$, respectively. The others showed moderate activity with $IC_{50}$ values ranging around 80.58 to $85.83{\mu}M$, while the positive control, auraptene, possessed an $IC_{50}$ value of $55.36{\mu}M$.

Anticancer Effects of Natural Medicinal Plant Extracts on Oral Carcinoma Cells (천연 약용식물 추출물의 구강상피세포암 세포주에 대한 항암효과)

  • 김정희;현진원;김여갑
    • Biomolecules & Therapeutics
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    • v.7 no.2
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    • pp.153-157
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    • 1999
  • The anticancer effect of medicinal plants against two oral carcinoma cells, A253 and SCC-25 were investigated in this study. Methanol extracts from 63 medicinal plants, which have anticancer activities against other cancers such as stomach, hepatocellular or colon carcinomas, were prepared and screened for their anti- oral cancer activity by using MTT assay. Thirty one samples showed anti-oral cancer activity against either cell line used, however, other 32 samples had no anti-oral cancer activity. Among these samples methanol extract of Caesalpinia sappan revealed the strongest anti-oral cancer activity. The $IC_{50}$/ values of this extract against A253 and SCC-25 cells were 16 and 25 $\mu$g/m1, respectively. Fractions of n-hexane, dichloromethane, ethylacetate, n-buthanol and water were prepared from methanol extracts of Caesalpinia sappan, Anthriscus sylvestris, Rhus japonica, Curcuma arowatica, Inula helenium, Sinoarnudinaria reticulata, and Polygonum cuspidatum, respectively. Among these 35 fractions the n-hexane fraction of Inula helenium showed the strongest anti-oral cancer activity, the $IC_{50}$/ value was 1.6$\pm$0.3 $\mu\textrm{g}$/ml. Ten other fractions showed $IC_{50}$/ values lower than 10 $\mu\textrm{g}$/ml.

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Bioactive Constituents from the n-Butanolic Fraction of Aruncus dioicus var. kamtschaticus

  • Vo, Quoc Hung;Nguyen, Phi Hung;Zhao, Bing Tian;Thi, Yen Nguyen;Nguyen, Duc Hung;Kim, Won Il;Seo, U Min;Min, Byung Sun;Woo, Mi Hee
    • Natural Product Sciences
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    • v.20 no.4
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    • pp.274-280
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    • 2014
  • Six compounds were isolated from the n-BuOH fraction of the aerial parts of Aruncus dioicus var. kamtschaticus including: sambunigrin (1), prunasin (2), aruncide A (3), aruncide C (4), 1-O-caffeoyl-${\beta}$-D-glucopyranose (5), and caffeic acid (6). Their structures were confirmed by comparing the spectral data with those reported in the literature. The isolated compounds (1 - 6) were then examined for their cytotoxic effects towards MCF-7, HL-60, and HeLa cancer cell lines, as well as their DPPH radical scavenging activity. The results indicated that compound 4 possessed the strongest inhibitory effect toward HeLa cell line with $IC_{50}$ value of $5.38{\pm}0.92{\mu}M$. Compound 3 possessed selective cytotoxic activity on HL-60 cells with $IC_{50}$ value of $6.27{\pm}0.17{\mu}M$, compound 5 was found as the best in inhibiting proliferation with $IC_{50}$ value of $2.25{\pm}0.09{\mu}M$, and the other compounds showed significant inhibition with $IC_{50}$ values ranging from 6.10 to $11.27{\mu}M$. Compound 5 also displayed the strongest cytotoxic effect toward MCF-7 cell line ($IC_{50}$ $4.32{\pm}0.15{\mu}M$). Both 5 and 6 demonstrated strong radical scavenging activity ($IC_{50}$ $6.87{\pm}0.03$ and $4.33{\pm}0.22{\mu}M$, respectively). Compounds 1 and 5 were isolated for the first time from this plant.

Enzymological Evaluation of Oral Inflammation inhibitory activity by Aloe vera peel extract (Aloe vera peel 추출물에 의한 구강염증 저해 효과의 효소학적 평가)

  • Pack, Chung-Sun;Ryu, Il-Hwan;Lee, Kap-Sang
    • Korean Journal of Food Science and Technology
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    • v.33 no.6
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    • pp.753-759
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    • 2001
  • To evaluate antiinflammation of Aloe vera peel, antiimflammation substances were extracted from Aloe vera peel and identified, and we investigated the effect of the its substance the inhibitory effect on the activity of hyaluoronidase, elastase, collagenase and prostaglandin endoperoxide synthase. The water extract from Aloe vera peel were successfully purified with solvent fractionation, silica gel column chromatography, preparative thin layer chromatography and UV spectrometer. Two purified active substances were identified as aloe-emodin and barbaloin by Mass Spectrometer, $^1H-NMR$ and FT-IR. Aloe-emodin and barbaloin. $IC_{50}$ values of aloe-emodin and barbaloin against hyaluronidase activity were 40 and $70\;{\mu}g/mL$, respectively. Leuckocyte elastase, which is related to the destruction of various tissue, $IC_{50}$ values of them were 50 and $60\;{\mu}g/mL$, respectively. $IC_{50}$ values of aloe-emodin and barbaloin against collagenase activity were 40 and $60\;{\mu}g/mL$, respectively. and $IC_{50}$ values of aloe-emodin and barbaloin aganist the prostaglandin endoperoxide synthase, which play an important role in inflammatory reactions, were 40 and $70\;{\mu}g/mL$, respectively. Inhibitory effects of aloe-emodin, barbaloin and aspirin against carrageenan paw edema were 74.9, 52.9 and 51.9% as inhibiton percentage, respectively, at dose of 100 mg/kg and that of indomethancin was 49.7 at dose of 10 mg/kg. Cell cytotoxicity of barbaloin against human gingival cells was lower than that of aloe-emodin. Aloe-emodin and barbaloin did not show cytotoxicity against human gingival cells at concentration of 1.0 and $5.0\;{\mu}g/mL$, However, aloe-emodin and barbaloin showed less cytotoxicity than chlorhexidine, which usually have been used as the agent of anticaries and antiinflammation. These results suggested that aloe-emodin and barbaloin from Aloe vera peel have the effect of anticaries and antiinflammation.

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Antioxidative Properties of Different Solvent Extracts from Persimmon (Diospyros kaki cv. Fuyu) Flower-Buds

  • You, Dong-Hyun;Lee, Seung-Cheol
    • Preventive Nutrition and Food Science
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    • v.16 no.4
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    • pp.328-332
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    • 2011
  • After preparation of acetone, ethanol, methanol, and water extracts (10 g/300 mL) of dried persimmon (Diospyros kaki cv. Fuyu) flower-buds, total phenolic contents (TPC), 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity (RSA), 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) RSA, reducing power (RP), and tyrosinase inhibitory activity of the extracts were evaluated. The methanol extracts produced the highest TPC (113.39 mg gallic acid equivalents/g), DPPH RSA ($IC_{50}=40.25\;{\mu}g/mL$), ABTS RSA ($IC_{50}=58.17\;{\mu}g/mL$) and RP ($IC_{50}=69.43\;{\mu}g/mL$) activities while the water extracts generated the lowest values. The ethanol extract showed the highest tyrosinase inhibitor activity (88.90%) at a concentration of 1 mg/mL. These results indicated that persimmon flower-buds may be a useful source of natural antioxidants.

DNA Strand-Nicking Principles of Mucuna birdwoodiana

  • Han, Ah-Reum;Mar, Woong-Chon;Seo, Eun-Kyoung
    • Natural Product Sciences
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    • v.9 no.2
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    • pp.105-108
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    • 2003
  • During our research program to find DNA strand-scission agents from higher plants, the MeOH extracts of the stems of Mucuna birdwoodiana Tutcher. (Leguminosae) exhibited the most potent activity with an $IC_{50}$ value of $4.9\;{\mu}g/ml$. Thus, detailed laboratory investigation was performed, and led to the isolation of known compounds, $({\pm})$-catechin (1) and (-)-epicatechin(2) as active principles. Compounds 1 and 2 showed significant activity of DNA strand-scission with $IC_{50}$ values of 10.8 and $7.5\;{\mu}g/ml$, respectively (positive control, bleomycin: $IC_{50}\;3.3\;{\mu}g/ml$.

Synthesis of New 6-(4-Fluorophenyl)-5-(2-substituted pyrimidin-4-yl)imidazo[2,1-b] thiazole Derivatives and their Antiproliferative Activity against Melanoma Cell Line

  • Park, Jin-Hun;Oh, Chang-Hyun
    • Bulletin of the Korean Chemical Society
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    • v.31 no.10
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    • pp.2854-2860
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    • 2010
  • Synthesis of a new series of pyrimidinyl-imidazo[2,1-b]thiazole derivatives is described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the pyrimidinyl ring side chain was investigated. The biological results indicated that most of the newly synthesized compounds showed moderate activity against A375, compared with Sorafenib. Among all of these derivatives, the cyclic sulfamide derivatives IIIa, IIIb, and IIIe showed the most potent antiproliferative activity against A375 human melanoma cell line. The IC50 values of compounds IIIa,b were in nanomolar scale. In addition, compound IIIe ($IC_{50}=1.9\;{\mu}M$) also demonstrated more potent antiproliferative activity compared with Sorafenib ($IC_{50}=5.6\;{\mu}M$).

Study on DPPH Free Radical Scavenging and Lipid Peroxidation Inhibitory Activities of Vietnamese Medicinal Plants

  • Phan, Thi Anh Dao;Nguyen, Xuan Hai;Nguyen, Trung Nhan;Tran, Le Quan;Nguyen, Thi Thanh Mai
    • Natural Product Sciences
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    • v.18 no.1
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    • pp.1-7
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    • 2012
  • Among 90 Vietnamese medicinal plant extracts investigated for their antioxidant activity by DPPH assay at various concentrations from $10-100{\mu}g/mL$, 67 showed an inhibition rate over 50% at $100{\mu}g/mL$; 47 had greater than 50% inhibition at $50{\mu}g/mL$; 17 showed over 50% inhibition at $25{\mu}g/mL$. 8 extracts which exhibited strong inhibitory activity more than 50% inhibition at $10{\mu}g/mL$ were further tested for lipid peroxidation inhibition by TBA assay. They displayed activity with $IC_{50}$ values from 30.6 to $158.9{\mu}g/mL$. Until now, this is the first report on antioxidant activity of the female flower of Borassus flabellifer, and the stem of Combretum latifolium, Embelia ribes, Spatholobus parviflorus, and Tetrastigma erubescens. Fractionations of the EtOAc extract prepared from S. parviflorus led to the isolation of protocatechuic acid (1), ferulic acid (2), epicatechin (3), and gallic acid (4). These compounds showed significant DPPH inhibitory activity with $IC_{50}$ values from 6.5 to $23.6{\mu}M$.

Cytotoxic and Antioxidant Compounds Isolated from the Cork of Euonymus alatus Sieb.

  • Jeong, Su Yang;Zhao, Bing Tian;Kim, Young Ho;Min, Byung Sun;Woo, Mi Hee
    • Natural Product Sciences
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    • v.19 no.4
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    • pp.366-371
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    • 2013
  • Seventeen compounds (1 - 17), ${\beta}$-sitosterone (1), lupenone (2), arborinone (3), ${\beta}$-sitosterol (4), lupeol (5), epi-lupeol (6), taraxerol (7), betulinic acid (8), 24R-methyllophenol (9), germanicol (10), hexatriacontane (11), nonacosan-1-ol (12), benzoic acid (13), tetradecyl(E)-ferulate (14), di(2-ethylhexyl) phthalate (15), trilinolein (16) and monopalmitin (17), were isolated from the methylene chloride-soluble fraction of the cork of Euonymus alatus Sieb. The structures of these compounds were elucidated on the basis of spectroscopic evidence. Compounds 6, 11, 13 and 14 were isolated for the first time from this plant. Compound 4 showed moderate cytotoxic activity with an $IC_{50}$ value of 6.22 ${\mu}M$ in HL-60 cell line. Compound 9 exhibited moderate cytotoxic activity with $IC_{50}$ values of 63.31, 15.45, 15.14 and 21.72 ${\mu}M$ in four kinds of human cancer cell lines, Jurkat T, HeLa, HL-60 and MCF-7, respectively. Compound 17 showed moderate cytotoxic activity with an $IC_{50}$ value of 70.71 ${\mu}M$ in Jurkat T cell line. In addition, compounds 2, 3, 14 and 16 exhibited weak antioxidant activity with $IC_{50}$ values of 151.76, 170.79, 137.46 and 139.37 ${\mu}M$, respectively.