Inhibition of DNA Topoisomerases I and II and Cytotoxicity of Compounds from Ulmus davidiana var. japonica

Title
Inhibition of DNA Topoisomerases I and II and Cytotoxicity of Compounds from Ulmus davidiana var. japonica
Author(s)
손종근정명선이연경이응황보경이종순김재룡이경선[이경선]장현욱
Keywords
PLANCH ULMACEAE; ANTITUMOR DRUGS; FATTY-ACIDS; INNER BARK; GLYCOSIDES; CONSTITUENTS; LEAVES; CELLS; LIGNAN; FRACTION
Issue Date
201009
Publisher
PHARMACEUTICAL SOC KOREA
Citation
ARCHIVES OF PHARMACAL RESEARCH, v.33, no.9, pp.1307 - 1315
Abstract
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 1,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).
URI
http://hdl.handle.net/YU.REPOSITORY/23694http://dx.doi.org/10.1007/s12272-010-0903-0
ISSN
0253-6269
Appears in Collections:
약학대학 > 약학부 > Articles
이과대학 > 화학생화학부 > Articles
의과대학 > 생화학.분자생물학교실 > Articles
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