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Antiproliferative chromone derivatives induce K562 cell death through endogenous and exogenous pathways.
- Source :
- Journal of Enzyme Inhibition & Medicinal Chemistry; Dec2020, Vol. 35 Issue 1, p759-772, 14p
- Publication Year :
- 2020
-
Abstract
- A series of furoxan derivatives of chromone were prepared. The antiproliferative activities were tested against five cancer cell lines HepG2, MCF-7, HCT-116, B16, and K562, and two normal human cell lines L-02 and PBMCs. Among them, compound 15a exhibited the most potent antiproliferative activity. It was also found 15a produced more than 8 µM of NO at the peak time of 45 min by Griess assay. Generally, antiproliferative activity is positively related to NO release to some extent. Further in-depth studies on apoptosis-related mechanisms showed that 15a caused S-phase cell cycle arrest in a concentration-dependent manner and induced apoptosis significantly through mitochondria-related pathways. Human apoptosis protein array assay also demonstrated 15a increased the expression levels of pro-apoptotic Bax, Bad, HtrA2 and Trail R2/DR5. The expression of catalase and cell cycle blocker claspin were similarly up-regulated. In balance, 15a induced K562 cells death through both endogenous and exogenous pathways. [ABSTRACT FROM AUTHOR]
- Subjects :
- CELL death
CELL cycle
APOPTOSIS
PROTEIN microarrays
CANCER cells
CELL lines
Subjects
Details
- Language :
- English
- ISSN :
- 14756366
- Volume :
- 35
- Issue :
- 1
- Database :
- Complementary Index
- Journal :
- Journal of Enzyme Inhibition & Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 147176765
- Full Text :
- https://doi.org/10.1080/14756366.2020.1740696