Embelin Derivatives and Their Anticancer Activity through Microtubule Disassembly
Biological activities of the 1,4-benzoquinone derivatives 5- O-ethylembelin ( 1) and 5- O-methylembelin ( 2) were investigated. Both of them showed antiproliferative activity against a panel of human tumor cell lines upon comparison to normal marsupial kidney cells (PtK2). They arrested HL-60 cells in the G 0/G 1 phase of the cell cycle in a dose- and time-dependent manner. In HeLa cells, exposure to 100 μM of 1 or 2 for 6 h induced a complete disassembly of the microtubule network and an increased number of cells blocked in mitotic stages. Treatment with 10 μM of 1 and 2 for 24 h induced apoptosis in HL-60 cells. This evidence suggests that both 1 and 2 are promising novel antimitotic and anticancer molecules targeting microtubular proteins. DMSO:dimethyl sulfoxide MTT:3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazo-lium bromide Pet. ether:petroleum ether SRB:sulphorhodamine B.
Medienart: |
E-Artikel |
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Erscheinungsjahr: |
2005 |
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Erschienen: |
Stuttgart: Georg Thieme Verlag ; 2005 |
Reproduktion: |
Thieme Zeitschriftenarchive 1980-2007 |
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Enthalten in: |
Zur Gesamtaufnahme - volume:71 |
Enthalten in: |
Planta medica - 71(2005), 10 vom: Okt., Seite 944-948 |
Sprache: |
Deutsch |
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Beteiligte Personen: |
Xu, Minjuan [VerfasserIn] |
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Links: |
dx.doi.org [Deutschlandweit zugänglich] |
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Themen: |
Aegiceras corniculatum |
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Umfang: |
5 |
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doi: |
10.1055/s-2005-871250 |
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funding: |
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Förderinstitution / Projekttitel: |
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PPN (Katalog-ID): |
NLEJ226233499 |
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520 | |a Biological activities of the 1,4-benzoquinone derivatives 5- O-ethylembelin ( 1) and 5- O-methylembelin ( 2) were investigated. Both of them showed antiproliferative activity against a panel of human tumor cell lines upon comparison to normal marsupial kidney cells (PtK2). They arrested HL-60 cells in the G 0/G 1 phase of the cell cycle in a dose- and time-dependent manner. In HeLa cells, exposure to 100 μM of 1 or 2 for 6 h induced a complete disassembly of the microtubule network and an increased number of cells blocked in mitotic stages. Treatment with 10 μM of 1 and 2 for 24 h induced apoptosis in HL-60 cells. This evidence suggests that both 1 and 2 are promising novel antimitotic and anticancer molecules targeting microtubular proteins. DMSO:dimethyl sulfoxide MTT:3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazo-lium bromide Pet. ether:petroleum ether SRB:sulphorhodamine B | ||
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