• Title/Summary/Keyword: In vitro cytotoxicity

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Secalonic acid D; A Cytotoxic Constituent from Marine Lichen-derived Fungus Gliocladium sp. T31

  • Ren, Hong;Tian, Li;Gu, Qianqun;Zhu, Weiming
    • Archives of Pharmacal Research
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    • v.29 no.1
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    • pp.59-63
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    • 2006
  • Secalonic acid D(SAD) was isolated as the major secondary metabolite of the marine lichen-derived fungus Gliocladium sp. T31. Its structure was established on the basic of physicochemical and spectroscopic data. This is the first report on the isolation of SAD from this fungus, as well as its inhibitory effect on K562 cell cycle and its cytotoxicity against several tumor cell lines in vitro.

Synthesis and Cytotoxic Properties of 3,4-dihydro-3-oxo-2H-1,2,4-benzothiadiazine-1,1-dioxides (3,4-디히드로-3-옥소-2H-1,2,4-벤조치아디아진-1,1-디옥사이드 유도체의 합성 및 세포 독성)

  • 박혜영;한윤정;이정옥
    • YAKHAK HOEJI
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    • v.39 no.6
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    • pp.631-635
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    • 1995
  • A series of 3, 4-dihydro-3-oxo-2H-1, 2, 4-benzothiadiazine-1, 1, dioxides with cytotoxic activity against human solid tumors is described. Synthesized compounds showed mild but broad spectrum cytotoxicity in vitro. The lipophilic substituents like alkyl, alkoxy and chloro on benzene ring increased the activity. Also hydrophobic group on 3 or 4 position of benzothiadiazine was important for the activity.

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Isolation and Biological Activity of Verbascoside, A Potent Inhibitor of Protein Kinase C from the Calyx of Campsis grandiflora (능소화의 꽃받침으로부터 Protein Kinase C 저해물질인 Verbascoside의 분리 및 그 생물활성)

  • 이현선;박문수;오원근;안순철;김보연;김환묵;오구택;민태익;안종석
    • YAKHAK HOEJI
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    • v.37 no.6
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    • pp.598-604
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    • 1993
  • The calyx extract of Campsis grandiflora displayed inhibitory activity against protein kinase C from the bovine brain. Separation guided by protein kinase C enzyme assay and bleb forming assay led to isolation of a potent protein kinase C inhibitor that was identified as a known phenylpropanoid glycoside, verbascoside. It suppressed completely bleb-formation of K562 cell surface induced by phorbol 12,13-dibutylate at the concentration of 60 $\mu\textrm{g}$/ml and IC$_{50}$ of the protein kinase C occured at 20 $\mu{M}$. This compound was tested for cytotoxic activity against ten human tumor cell lines in vitro. it exhibited moderate cytotoxic activity against skin tumor cell line M14 (IC$_{50}$ 2.2 $\mu\textrm{g}$/ml) and very weak cytotoxicity against other cell lines (IC$_{50}$>10 $\mu\textrm{g}$/ml)

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Synthesis and Evaluation of Cytotoxicity of Novel Arylsulfonylimidazolidinones Containing Sulfonylurea Pharmacophore

  • Jung, Sang-Hun;Song, Jae-Shin;Lee, Hui-Soon;Choi, Sang-Un;Lee, Chong-Ock
    • Archives of Pharmacal Research
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    • v.19 no.6
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    • pp.570-580
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    • 1996
  • Design and synthesis of novel 4-phenyl-1-arylsulfonylimidazolones 3 and 4-phenyl-3-arylsulfonylimidazolones 4 and evaluation of their cytotoxic activity against eleven human cancer cell lines and two murine leukemia cell lines in vitro were performed. As a result, a series of 4-phenyl-1(N)-arylsulfonylimidazolones (3) has been found to be the potential anticancer agent. Compounds 3b, 3c, and 3d exhibit strong activity as indicated by their $IC_{50}$ values 0.39, 3.19, $0.31{\mu}g/mL$ against A549 and 0.80, 0.48, $0.0007{\mu}g/mL$against SK-Mel-2, respectively. These compounds also possess much more potent activity (10-1000 times) than LY186641 against eleven other cell lines.

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Phytochemical Constituents of Artemisia stolonofera

  • Kwon, Hak-Cheol;Choi, Sang-Un;Lee, Kang-Ro
    • Archives of Pharmacal Research
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    • v.24 no.4
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    • pp.312-315
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    • 2001
  • Repeated column chromatographic separation of the $CH_{2}Cl_{2}$ extract of Artemisia stolonofera (Asteraceae) led to the isolation of a triterpene (I), a sesquiterpene (II), two aromatic compounds (III and IV) and a benzoquinone (V). Their structures were determined by spectroscopic means to be simiarenol (I), (1S,7S)-1 $\beta$-hydroxygermacra-4(15),5, 10(14)-triene (II), 3'-methoxy-4'-hydroxy-trans-cinnamaldehyde (III), vanillin(IV) and 2,6-dimethoxy-1,4-benzoquinone (V), respectively. Among these products, compound V showed significant cytotoxicity against five human tumor cell lines in vitro, A549 (non small cell lung adenocarcinoma), SK-OV-3 (ovarian), SK-MEL-2 (skin melanoma), XF498 (CNS) and HCT15 (colon) with ED_{50}$ values ranging from 1.33~4.22${\mu}g/ml$.

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A New Megastigmane Glucoside from the Aerial Parts of Erythronium japonicum

  • Lee, Seung-Young;Lee, Il-Kyun;Choi, Sang-Un;Lee, Kang-Ro
    • Natural Product Sciences
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    • v.18 no.3
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    • pp.166-170
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    • 2012
  • The purification of the MeOH extract from the aerial parts of Erythronium japonicum using column chromatography furnished a new megastigmane glucoside, erthrojaponiside (1), together with six known megastigmane derivatives (2 - 7). The structure of the new compound (1) was determined through 1D and 2D NMR spectral data analysis and chemical means. The isolated compounds (1 - 7) were tested for cytotoxicity against four human tumor cells in vitro using a Sulforhodamin B (SRB) bioassay.

In vitro cytotoxicity of Chloromethyl-2-dihydroxyphosphinyl-6, 7-dimethoxy-l,2,3,4-tetra hydroisoquinoline on HL60 cells and apoptotic effet

  • Kim, Kun-Jung;Ju, Sung-Min;Yeom, Kee-Bok;Kim, Dae-Geun;Lee, Chai-Ho;Kim, Won-Sin;Han, Dong-Min;Jeon, Byung-Hun
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2003.10b
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    • pp.115-115
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    • 2003
  • The chloromethyl-2-dihydroxyphosphinyl-6, 7-dimethoxy-1,2,3,4-tetrahydro isoquino- line (CDDT) is a newly synthesized agent which is derivated from 1,2,3,4- Tetrahydroiso- quinoline (TIQ). The TIQs include potent cytotoxic agents that display a range of antitumor activities, antimicrobial activity, and other biological properties. (omitted)

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Cytotoxic Alkaloids from Houttuynia cordata

  • Kim, Seong-Kie;Ryu, Shi-Yong;No, Jae-Sung;Choi, Sang-Un;Kim, Young-Sup
    • Archives of Pharmacal Research
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    • v.24 no.6
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    • pp.518-521
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    • 2001
  • Six bioactive alkaloids, aristolactam B(1), poperolactam A(2), aristolactam A(3), norcepharadione B(4), cepharadione B(5) and splendidine(6) were isolated by bioactivity-guided fractionalton of a methanolic extract of the aerial part of Houttuynia cordata. Several of them exhibited significant cytotoxicity against five human tumor cell lines (A-549,SK-OV-3,SK-MEL-2, XF-498 and HCT-15) in vitro.

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Crtotoxic Triterpenoides from Alismatis Rhizome

  • Lee, Sang-Myung;Kho, Yung-Hee;Min, Byung-Sun;Kim, Jin-Hee;Na, Min-Kyun;Kang, Shin-Jyung;Maeng, Hack-Young;Bae, Ki-Hwan
    • Archives of Pharmacal Research
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    • v.24 no.6
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    • pp.524-526
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    • 2001
  • Four prostate-type triterpenes were isolated from a methanol extract of Alismatis Rhizoma by bioassay-guided isolation using in vitro cytotoxic assay. The compounds were identified as alisol B 23-acetate (1), alisol C 23-acetate (2), alisol B (3), alisol A 24-acetate (4) by spectroscopic methods. Amongst the compounds, alisol B (3) showed significant cytotoxicity against SK-OV3, B16-F10, and HT1080 cancer cell lines with $ED_50$ values of 7.5, 7.5, $4.9\mu\textrm{g}/ml$, respectively.

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