https://scholars.lib.ntu.edu.tw/handle/123456789/564863
標題: | Denbinobin-mediated anticancer effect in human K562 leukemia cells: Role in tubulin polymerization and Bcr-Abl activity | 作者: | Huang Y.-C. JIH-HWA GUH Teng C.-M. |
公開日期: | 2005 | 卷: | 12 | 期: | 1 | 起(迄)頁: | 113-121 | 來源出版物: | Journal of Biomedical Science | 摘要: | Denbinobin (5-hydroxy-3,7-dimethoxy-1,4-phenanthraquinone) has been reported to exhibit anti-tumor and anti-inflammatory activity. Nevertheless, the anti-tumor mechanism of denbinobin remains unclear. In the present study, we evaluated the anticancer activity of denbinobin in human myelogenous K562 leukemia cells. In accordance with the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide (MTT) assay, we demonstrated that denbinobin inhibited cell viability in a concentration-dependent manner with an IC50 value of 1.84μM. Cell cycle analysis illustrated that exposure of denbinobin caused a G2/M phase accumulation in a time-dependent manner. Tubulin polymerization in cells was apparently enhanced by denbinobin, implying that denbinobin might have a regulatory role in tubulin/microtubule. Furthermore, denbinobin significantly suppressed the expression of Bcr-Abl and phosphorylation of CrkL, a crucial tyrosine kinase and an adaptor protein in chronic myeloid leukemia, respectively. Denbinobin also markedly enhanced CD11b expression after a long-term treatment, suggesting that denbinobin might play a role in facilitating differentiation in K562 cells. In summary, we have demonstrated that denbinobin displays anticancer effects in K562 cells through the increase of levels of tubulin polymerization and deregulation of Bcr-Abl signaling. Our data demonstrate that denbinobin could be a potential anticancer lead compound for further development. ? 2005 National Science Council. |
URI: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-17744393624&doi=10.1007%2fs11373-004-8171-y&partnerID=40&md5=cacb401f3448f8df52eef824c346aca4 https://scholars.lib.ntu.edu.tw/handle/123456789/564863 |
ISSN: | 10217770 | DOI: | 10.1007/s11373-004-8171-y | SDG/關鍵字: | adaptor protein; antineoplastic agent; BCR ABL protein; CD11b antigen; denbinobin; protein tyrosine kinase; unclassified drug; antineoplastic activity; article; assay; cell cycle; cell cycle G2 phase; cell differentiation; cell strain K 562; cell viability; chronic myeloid leukemia; concentration response; controlled study; exposure; human; human cell; microtubule assembly; priority journal; protein expression; Anthraquinones; Antigens, CD11b; Antineoplastic Agents; Apoptosis; Cell Cycle; Cell Proliferation; Humans; K562 Cells; Medicine, Chinese Traditional; Molecular Structure; Phenanthrenes; Plant Extracts; Polymers; Protein-Tyrosine Kinases; Tubulin |
顯示於: | 藥學系 |
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