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

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Cytotoxicity and DNA Topoisomerases Inhibitory Activity of Constituents from the Sclerotium of Poria cocos

  • Li, Gao;Xu, Ming-Lu;Lee, Chong-Soon;Woo, Mi-Hee;Chang, Hyun-Wook;Son, Jong-Keun
    • Archives of Pharmacal Research
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    • v.27 no.8
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    • pp.829-833
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    • 2004
  • The bioactivity-guided fractionation of the methylene chloride extract of the sclerotium of Poria cocos led to the isolation of (S)-(+)-turmerone (1), ergosterol peroxide (2), polyporenic acid C (3), dehydropachymic acid (4), pachymic acid (5), and tumulosic acid (6). Compounds 4-6 exhibited moderate cytotoxicities, with $IC_{50}$ values of 20.5, 29.1, and $10.4{\;}\mu\textrm{m}$, respectively, against a human colon carcinoma cell line. However, 3-6 not only showed inhibitory activities as potent as etoposide used as a positive control on DNA topoisomerase II (36.1, 36.2, 43.9 and 66.7% inhibition at a concentration of $20{\;}\mu\textrm{m}$, respectively), but also inhibition of DNA topoisomerase I (55.8, 60.7, 43.5, and 83.3% inhibition at a concentration of $100{\;}\mu\textrm{m}$, respec-tively).

Topoisomerase I and II Inhibitory Activities and Cytotoxic Constituents from the Barks of Tilia amurnesis

  • Piao, Dong Gen;Lee, You-Jeong;Seo, Chang-Seob;Lee, Chong-Soon;Kim, Jae-Ryong;Chang, Hyun-Wook;Son, Jong-Keun
    • Natural Product Sciences
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    • v.17 no.3
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    • pp.245-249
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    • 2011
  • Eight compounds, squalene (1), friedelin (2), ${\beta}$-sitosterol (3), ${\beta}$-sitosterol-3-O-glucoside (4), ${\alpha}$-tocopherol (5), betulinic acid (6), trilinolein (7) and 1-O-(9Z,12Z-Octadecadienoyl)-3-nonadecanoyl glycerol (8), were isolated from the barks of Tilia amurensis. Their chemical structures were identified by comparing their physicochemical and spectral data with those published in the literature. These isolated compounds were examined for their inhibitory activities against topoisomerase I and II. Compound 7 showed significant inhibition of DNA topoisomerase I and II activities, with percent decreases in activity of 87 and 95%, respectively at a concentration of $100\;{\mu}M$. Compound 6 exhibited cytotoxicity against the human colon adenocarcinoma cell line (HT-29), the human breast adenocarcinoma cell line (MCF-7) and the human liver hepatoblastoma cell line (HepG-2), with $IC_{50}$ values of 20, 59 and $16\;{\mu}M$, respectively.

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).