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Anti-proliferative and Apoptotic Effects of the Derivatives from 4-aryl-4H-chromene Family on Human Leukemia K562 Cells
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  • Anti-proliferative and Apoptotic Effects of the Derivatives from 4-aryl-4H-chromene Family on Human Leukemia K562 Cells
  • Anti-proliferative and Apoptotic Effects of the Derivatives from 4-aryl-4H-chromene Family on Human Leukemia K562 Cells
저자명
Aryapour. Hassan,Mahdavi. Majid,Mohebbi. Seyed Reza,Zali. Mohammad Reza,Foroumadi. Alireza
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2012년|35권 9호|pp.1573-1582 (10 pages)
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대한약학회
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정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

Previous studies suggest that 4-aryl-4H-chromenes are potent apoptosis-inducing agents in various cancer cell lines. In this study, anti-proliferative and apoptotic effects of the derivatives from 4-aryl-4H-chromene family were investigated in the human leukemia K562 cells using [3-(4,5)-dimethyl-2-thiazolyl]-2,5-diphenyl-2H-tetrazolium bromide (MTT) growth inhibition assay. 3-NC was more active among these compounds with $IC_{50}$ of 65 nM and was selected for further studies. Apoptosis, as the mechanism of cell death, was investigated morphologically by Hoechst 33258 staining, cell surface expression assay of phosphatidylserine by Annexin V/PI technique, caspase-3 activation assay, as well as the formation of DNA ladder. The K562 cells underwent apoptosis upon a single dose (at $IC_{50}$ value) of the compound, and also increased caspase-3 activity by more than 2.3-fold, following a 72 h treatment. Caspase-9 was also activated which could be detected 48 hours post-treatment. Furthermore, Western blot analysis revealed that the treatment with the compound down-regulated the expression of certain IAP protein, including survivin. These data further suggest that these derivatives from 4-aryl-4H-chromene may provide a novel therapeutic approach for the treatment of leukemia.