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Inhibition of DNA Topoisomerases I and II and Cytotoxicity of Compounds from Ulmus davidiana var. japonica
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  • Inhibition of DNA Topoisomerases I and II and Cytotoxicity of Compounds from Ulmus davidiana var. japonica
  • Inhibition of DNA Topoisomerases I and II and Cytotoxicity of Compounds from Ulmus davidiana var. japonica
저자명
Zheng. Ming-Shan,Lee. Yeun-Kyung,Li. Ying,HwangBo. Kyoung,Lee. Chong-Soon,Kim. Jae-Ryong,Lee. Sunny Kyung-Seon,Chang. Hyun-Wook,
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2010년|33권 9호|pp.1307-1315 (9 pages)
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대한약학회
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정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

Twenty five compounds including ten triterpenes (1-3, 5-11), six flavonoids (12-15, 24, 25), five lignans (17, 18, 21-23), two butenyl clohexnone glycosides (19-20), one fructofuranoside (16) and one fatty acid (4) were isolated from the roots of Ulmus davidiana var. japonica. The structures of those compounds were identified by comparing their physicochemical and spectral data with those of published in literatures. All the compounds were evaluated for DNA topoisomerase inhibitory activities and cytotoxicities. Among the purified compounds, 4 and 19 showed more potent inhibitory acitivities ($IC_{50}$: 39 and 19 ${mu}M$, respectively) than camptothecin, as the positive control ($IC_{50}$: 46 ${mu}M$) against topoisomerase I. Compounds, 4, 10, 12, 19, 24 and 25 showed strong inhibitory activities toward DNA topoisomerase II ($IC_{50}$: 0.1, 0.52, 0.47, 0.42, 0.17 ${mu}M$ and 17 nM, respectively), which were more potent than that of etoposide as positive control ($IC_{50}$: 20 ${mu}M$). In A549 cell line, 5 and 6 showed cytotoxicities ($IC_{50}$: 4 ${mu}M$ and 3 ${mu}M$, respectively, with $IC_{50}$ of camptothecin as positive control: 10.3 ${mu}M$). In the HepG2 cell line, 3, 5 and 7 showed cytotoxicity ($IC_{50}$: 4, 3 and 4 ${mu}M$, respectively, with $IC_{50}$ of camptothecin: 0.3 ${mu}M$). Compounds 6, 12 and 23 showed cytotoxicities in the HT-29 cell line ($IC_{50}$: 19, 19 and 15 ${mu}M$, respectively, with $IC_{50}$ of camptothecin: 2 ${mu}M$).