• Title/Summary/Keyword: DNA topoisomerases I and II inhibitors

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DNA Topoisomerases I and II Inhibitory Activity of Constituents Isolated from Juglans mandshurica

  • Li, Gao;Lee, Sun-Young;Lee, Kyeung-Seon;Lee, Sung-Won;Kim, Sang-Hyun;Lee, Seung-Ho;Lee, Chong-Soon;Woo, Mi-Hee;Son, Jong-Keun
    • Archives of Pharmacal Research
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    • v.26 no.6
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    • pp.466-470
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    • 2003
  • Nine diarylheptanoids (1-9), one triterpene (10), one sesquiterpenoid (11), one naphthoquinone (12), four tetralones (13-16), one naphthalene carboxylic acid glucoside (17) and six naphthalenyl glycosides (18-23) were isolated from the roots of Juglans mandshurica Maximowicz (Juglandaceae), and their structures determined from the chemical and spectral data. Here, we report the inhibitory effects, on the DNA topoisomerases I and II activities, of all these compounds. Compounds 10 and 23 showed more potent inhibitory effects, on the DNA topoisomerases I and II (94.0 and 86.0% inhibitions at the concentration of 5 $\mu$ g/mL, respectively), than the positive control compounds, camptothecin and etoposide.

Computer-based screening for novel inhibitors of human topoisomerase I with FlexiDock docking protocol

  • Choi, In-Hee;Kim, Choon-Mi
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.315.1-315.1
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    • 2002
  • DNA topoisomerases I (topo I) and II are essential enzymes that relax DNA supercoiling and relieve torsional strain during DNA processing. including replication. transcription. and repair. Topo I relaxes DNA by cleaving one strand of DNA by attacking a backbone phosphale with a catalytic lyrosine (Tyr723. human topo I). This enzyme has recently been investigated as a new target for antineoplastic drugs. Inhibitors to the enzyme intercalate between the DNA base pairs. interfering religation of cleaved DNA, therefore inhibit the activity of topo I. (omitted)

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Cytotoxicity and DNA Topoisomerase Inhibitory Activity of Constituents Isolated from the Fruits of Evodia officinalis

  • Xu, Ming-Lu;Li, Gao;Moon, Dong-Cheol;Lee, Chong-Soon;Woo, Mi-Hee;Lee, Eung-Seok;Jahng, Yurng-Dong;Chang, Hyeun-Wook;Lee, Seung-Ho;Son, Jong-Keun
    • Archives of Pharmacal Research
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    • v.29 no.7
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    • pp.541-547
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    • 2006
  • Four alkaloids (1-4), three quinolone alkaloids (5-7), and three flavanoid glucosides (8-10) were isolated from the fruits of Evodia officinalis Dode, and their structures were determined from chemical and spectral data. Compounds, 3, 8, 9 and 10 were isolated from this plant for the first time. Of these compounds, 1-3 and 5-7 exhibited moderate cytotoxicities against cultured human colon carcinoma (HT-29), human breast carcinoma (MCF-7), and human hepatoblastoma (HepG-2). Compound 8 showed strong inhibitory effects on DNA topoisomerases I and II (70 and 96% inhibition at a concentration of $20\;{\mu}M$, respectively).