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Antiproliferative effect of aaptamine on human chronic myeloid leukemia K562 cells.

Abstract
We previously isolated aaptamine, a benzonaphthyridine alkaloid, from marine sponge Aaptos suberitoids. In this study, we investigated the anti-proliferative effect of aaptamine on chronic myeloid leukemia (CML) K562 cells. Aaptamine inhibited growth of K562 with a GI50 as 10 μM, and arrested cell cycle at G2/M phase. Western blot analysis indicated that aaptamine induced p21 expression in K562 cells. Moreover, p21 promoter was activated by aaptamine treatment in p21 transfected K562 cells. Since K562 is p53 negative, aaptamine was demonstrated to be a p53-independent p21 inducer in CML cells.
AuthorsMeihua Jin, Wennan Zhao, Yanwen Zhang, Motomasa Kobayashi, Hongquan Duan, Dexin Kong
JournalInternational journal of molecular sciences (Int J Mol Sci) Vol. 12 Issue 11 Pg. 7352-9 ( 2011) ISSN: 1422-0067 [Electronic] Switzerland
PMID22174603 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents
  • Cyclin-Dependent Kinase Inhibitor p21
  • Naphthyridines
  • aaptamine
Topics
  • Antineoplastic Agents (pharmacology)
  • Cell Cycle Checkpoints (drug effects)
  • Cell Proliferation (drug effects)
  • Cyclin-Dependent Kinase Inhibitor p21 (genetics, metabolism)
  • Humans
  • K562 Cells
  • Leukemia, Myelogenous, Chronic, BCR-ABL Positive (metabolism)
  • Naphthyridines (pharmacology)
  • Promoter Regions, Genetic

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