• 제목/요약/키워드: In vitro cytotoxicity

검색결과 1,117건 처리시간 0.025초

Novel Benzoylurea Derivatives as Potential Antitumor Agents; Synthesis, Activities and Structure-Activity Relationships

  • Hwang, Ki-Jun;Park, Kyung-Ho;Lee, Chong-Ock;Kim, Beom-Tae
    • Archives of Pharmacal Research
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    • 제25권6호
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    • pp.781-785
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    • 2002
  • A series of pyrazoloxyphenyl benzoyl urea derivatives was designed and synthesized for cytotoxic evaluation as potential antitumor agents. The synthetic compounds were evaluated for in vitro cytotoxicity against five human tumor cell lines, including A-549, SKOV-3, SK-MEL-2, XF-498 and HCT-15. Among others, compound 11 exhibited 50∼100 times greater antitumor activities than the commercial product, Cisplatin.

A New Sesquiterpene Hydroperoxide from the Aerial Parts of Aster oharai

  • Choi, Sang-Zin;Lee, Sung-Ok;Choi, Sang-Un;Lee, Kang-Ro
    • Archives of Pharmacal Research
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    • 제26권7호
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    • pp.521-525
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    • 2003
  • Phytochemical works on the aerial parts of Aster oharai (Compositae) led to the isolation of a new sesquiterpene hydroperoxide, 7$\alpha$-hydroperoxy-3, 11-eudesmadiene (2) and seven known compounds, teucdiol B (1), $\alpha$-spinasterol (3), oleanolic acid (4), $\alpha$-spinasterol 3-Ο-$\beta$-D-glucopyranoside (5), methyl 3,5-di-Ο-caffeoyl quinate (6), 3,5-di-Ο-caffeoylquinic acid (7), 3,4-di-Ο-caffeoylquinic acid (8). The chemical structures of 1-8 were established by chemical and spectroscopic methods. Compound 2 showed cytotoxicity against cultured human tumor cell lines in vitro, SK-OV-3 (ovarian), SK-MEL-2 (skin melanoma), and HCT15 (colon) with $ED_{50}$ values ranging from 3.86-17.21 $\mu$g/mL.

Cytotoxicity of T-2 Toxin on Primary Cultures of Rat Hepatocytes

  • Kim, Hwan-Mook;Kim, Byung-Sam;Choe, Suck-Young;Yang, Kyu-Hwan
    • Toxicological Research
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    • 제4권1호
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    • pp.37-45
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    • 1988
  • Primary cultures of adult rat hepatocytes were used to study in vitro cytotoxic effects of T-2 toxin on liver cells. When T-2 toxin was added to the culture, a significant depression of the hormonal induction of ${\alpha}$-aminoisobutyric acid (AIB) uptake and tyrosine aminotransferase (TAT) activity was observed. However, T-2 toxin did not affect the uptake of ouabain into hepatocytes. Protein synthesis was inhibited by T-2 toxin, but RNA synthesis was not severely affected. The inhibitory effects of T-2 toxin on protein synthesis was diminished rapidly with culture time and the hepatocytes culture maintained control level of protein synthesis within 24 hrs.

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Inhibition of Aminopeptidase N by 2-Hydroxy-3-amino-4-(p-nitrophenyl)butyryl Peptide Derivatives

  • Chung, Myung-Chul;Lee, Choong-Hwan;Lee, Ho-Jae;Chun, Hyo-Kon;Kho, Yung-Hee
    • Applied Biological Chemistry
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    • 제41권8호
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    • pp.608-610
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    • 1998
  • To investigate the inhibitory activity of 2-hydroxy-3-amino-4-phenylbutyrate-harboring aminopeptidase N inhibitors, p-nitro-AHPA-peptide derivatives (1 and 2) and an AHPA-peptide derivative (3) were synthesized by chain elongation from C-terminal end using DCC/HOBt as a coupling reagent. The peptides $1{\sim}3$ exerted strong inhibitory activities against aminopeptidase N with $IC_{50}$ values of 1.8, 7.3 and $24.0\;{\mu}g/ml$, respectively, and cytotoxicity on cancer cell lines in vitro.

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접시꽃뿌리의 페놀성 성분 (Phenolic Constituents of Althaea rosea Canival.)

  • 김도훈;양민철;이규하;김기현;이강노
    • 생약학회지
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    • 제38권3호통권150호
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    • pp.222-226
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    • 2007
  • Seven compounds, scopoletin (1), p-hydroxyphenethyl trans-ferulate (2), $1-({\alpha}-L-rhamnosyl(1\;{\rightarrow}\;6)-{\beta}-D-glucopyranosyloxy)-3,4,5-trimethoxybenzene$ (3), benzyl ${\alpha}-L-rhamnopyranosyl(1\;{\rightarrow}\;6)-{\beta}-D-glucopyranoside$ (4), suberic acid (5), sebacic acid (6) and scopolin (7) were isolated from the methanol extract of the roots of Althaea rosea Canival. Compounds $1\;{\sim}\;7$ were first isolated from this plant. The isolated compounds were tested for their cytotoxicity against human cancer cell lines using a SRB method in vitro.

지모(知母)의 항암활성성분에 관한 연구 (Antitumor Agent from the Rhizome of Anemarrhena asphodeloides)

  • 이승호;유시용;최상운;노재성;김성기;이정옥;안종웅
    • 생약학회지
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    • 제26권1호
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    • pp.47-50
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    • 1995
  • EtOAc soluble part of MeOH extract of Anemarrhena asphodeloides rhizome was evaluated for the cytotoxicity against the five kinds of human tumor cell lines (A-549, SK-OV-3, SK-MEL-2, XF498 and HCT15) in vitro. Bioassay-guided fractionation of EtOAc soluble part led to the isolation of active compound which was identified as timosaponin A-III showed potent cytotoxic activity, but its genin, sarsasapogenin, did not show cell growth inhibition.

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Lignans from the Roots of Berberis amurensis

  • Park, Hyun-Bong;Lee, Kyu-Ha;Kim, Ki-Hyun;Lee, Il-Kyun;Noh, Hyung-Jun;Choi, Sang-Un;Lee, Kang-Ro
    • Natural Product Sciences
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    • 제15권1호
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    • pp.17-21
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    • 2009
  • Column chromatographic separation of the alcoholic extract from the roots of Berberis amurensis yielded eight phenolic constituents including six lignans, hanultarin (1), (-)-secoisolariciresinol (3), (+)-lyoniresinol (5), (+)-syringaresinol (6), (+)-syringaresinol-O-$\beta$-D-glucopyranoside (7), liriodendrin (8), and two phenylpropanoids, 4-glucosyloxy-3-methoxyphenyl trans-propenoic ethyl ester (2), trans-ferulic acid (4). The structures were determined on the basis of NMR spectroscopic data. All isolated compounds(1-8) were reported for the first time from this source. Compound 1 exhibited moderate cytotoxicity against four human cancer cell lines in vitro using sulforhodamin B bioassay.

Phytochemical Constituents of Bletilla striata and Their Cytotoxic Activity

  • Woo, Kyeong Wan;Park, Jong Eel;Choi, Sang Un;Kim, Ki Hyun;Lee, Kang Ro
    • Natural Product Sciences
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    • 제20권2호
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    • pp.91-94
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    • 2014
  • Column chromatographic separation of the MeOH extract from the tubers of Bletilla striata yielded seven phenolic components including four phenanthrenes, 3,7-dihydroxy-2,4-dimethoxyphenanthrene (1), 3,7-dihydroxy-2,4,8-trimethoxyphenanthrene (2), 9,10-dihydro-4,7-dimethoxyphenanthrene-2,8-diol (3), and 9,10-dihydro-1-(4'-hydroxybenzyl)-4,7-dimethoxyphenanthrene-2,8-diol (4) and three stilbenes, gigantol (5), 3',4"-dihydroxy-5',3",5"-trimethoxybibenzyl (6), and batatasin III (7). Their structures were determined on the basis of NMR spectroscopic data. Among them, compound 2, 3, and 6 were reported for the first time from this plant. The isolated compounds (1-7) were tested for cytotoxicity against four human tumor cell lines in vitro using a Sulforhodamin B bioassay.

Triterpenes from Perilla frutescens var. acuta and Their Cytotoxic Activity

  • Woo, Kyeong Wan;Han, Ji Young;Choi, Sang Un;Kim, Ki Hyun;Lee, Kang Ro
    • Natural Product Sciences
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    • 제20권2호
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    • pp.71-75
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    • 2014
  • Nine triterpenes were isolated from the petroleum ether and MeOH extract of Perilla frutescens var. acuta leaves. Their structures were determined to be arjunic acid (1), maslinic acid (2), oleanolic acid (3), euscaphic acid (4), tormentic acid (5), 3-O-trans-p-coumaroyltormentic acid (6), 28-formyloxy-$3{\beta}$-hydroxy-urs-12-ene (7), ursolic acid (8), and corosolic acid (9) by spectroscopic methods. The compounds 1, 2, 4, 6, and 7 were isolated for the first time from this plant and the Genus Labiatae. The isolated compounds (1-9) were tested for cytotoxicity against four human tumor cell lines (A549, SK-OV-3, SK-MEL-2, and HCT-15) in vitro using a Sulforhodamin B bioassay.

Pytochemical Constituents of the Aerial Parts from Solidago virga-aurea var. gigantea

  • Choi, Sang-Zin;Choi, Sang-Un;Lee, Kang-Ro
    • Archives of Pharmacal Research
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    • 제27권2호
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    • pp.164-168
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    • 2004
  • The chromatographic separation of the MeOH extract of the aerial parts of Solidago virga-aurea var. gigantea $M_{IQ}$ . (Compositae) led to the isolation of six terpenoids and four phenolic compounds, trans-phytol (1), ent-germacra-4(15),5,10(14 )-trien-1$\alpha$-ol (2), $\beta$-amyrin acetate (3), ent-germacra-4(15),5,10(14)-trien-1$\beta$-ol (4), $\beta$-dictyopterol (5), oleanolic acid (6), kaempferol (7), kaempferol-3-O-rutinoside (8), methyl 3,5-di-O-caffeoyl quinate (9), and 3,5-di-O-caffeoyl quinic acid (10). Their structures were established by chemical and spectroscopic methods. Compounds 4, 5, and 10 showed moderate cytotoxicity against five cultured human tumor cell lines in vitro with its E $D_{50}$ values ranging from 1.52∼18.57 $\mu\textrm{g}$/mL.L.