The benzophenanthridine alkaloid sanguinarine perturbs microtubule assembly dynamics through tubulin binding
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Title |
The benzophenanthridine alkaloid sanguinarine perturbs microtubule assembly dynamics through tubulin binding
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Creator |
LOPUS, M
PANDA, D |
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Subject |
bimodal cell-death
nf-kappa-b polymerization mechanism apoptosis drugs suppression modulation inhibitor proteins cancer chemotherapy microtubules mitosis sanguinarine tubulin |
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Description |
Sanguinarine has been shown to inhibit proliferation of several types of human cancer cell including multidrug-resistant cells, whereas it has minimal cytotoxicity against normal cells such as neutrophils and keratinocytes. By analyzing the antiproliferative activity of sanguinarine in relation to its effects on mitosis and microtubule assembly, we found that it inhibits cancer cell proliferation by a novel mechanism. It inhibited HeLa cell proliferation with a half-maximal inhibitory concentration of 1.6 +/- 0.1 mu M. In its lower effective inhibitory concentration range, sanguinarine depolymerized microtubules of both interphase and mitotic cells and perturbed chromosome organization in mitotic HeLa cells. At concentrations of 2 mu M, it induced bundling of interphase microtubules and formation of granular tubulin aggregates. A brief exposure of HeLa cells to sanguinarine caused irreversible depolymerization of the microtubules, inhibited cell proliferation, and induced cell death. However, in contrast with several other microtubule-depolymerizing agents, sanguinarine did not arrest cell cycle progression at mitosis. In vitro, low concentrations of sanguinarine inhibited microtubule assembly. At higher concentrations (> 40 mu M), it altered polymer morphology. Further, it induced aggregation of tubulin in the presence of microtubule-associated proteins. The binding of sanguinarine to tubulin induces conformational changes in tubulin. Together, the results suggest that sanguinarine inhibits cell proliferation at least in part by perturbing microtubule assembly dynamics.
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Publisher |
BLACKWELL PUBLISHING
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Date |
2011-07-19T04:52:19Z
2011-12-26T12:51:00Z 2011-12-27T05:37:18Z 2011-07-19T04:52:19Z 2011-12-26T12:51:00Z 2011-12-27T05:37:18Z 2006 |
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Type |
Article
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Identifier |
FEBS JOURNAL, 273(10), 2139-2150
1742-464X http://dx.doi.org/10.1111/j.1742-4658.2006.05227.x http://dspace.library.iitb.ac.in/xmlui/handle/10054/5179 http://hdl.handle.net/10054/5179 |
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Language |
en
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