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Developing a Novel Indolocarbazole as Histone Deacetylases Inhibitor against Leukemia Cell Lines.

Wang W, Lv M, Zhao X, Zhang J - J Anal Methods Chem (2015)

Bottom Line: ZW2-1 performed anti-population growth effect which was in a concentration-dependent manner (2-12 μM) by inducing both apoptosis and autophagy in cells.At relatively high concentration (8 μM), ZW2-1 significantly decreased intracellular histone deacetylase 1 level which was also observed.All the results indicated that ZW2-1 could be a novel antileukemia lead capable of simultaneously inducing apoptosis, autophagy, and differentiation.

View Article: PubMed Central - PubMed

Affiliation: Department of Blood Biopharmaceuticals and Viral Detection, Institute of Transfusion Medicine, The Academy of Military Medical Sciences, Beijing 100850, China.

ABSTRACT
A novel indolocarbazole (named as ZW2-1) possessing HDAC inhibition activity was synthesized and evaluated against human leukemia cell lines HL-60 and NB4. ZW2-1 performed anti-population growth effect which was in a concentration-dependent manner (2-12 μM) by inducing both apoptosis and autophagy in cells. The compound also caused differentiation of HL-60 and NB4 cells as shown by increasing expression of CD11b, CD14, and CD38 at moderate concentration (4 μM). At relatively high concentration (8 μM), ZW2-1 significantly decreased intracellular histone deacetylase 1 level which was also observed. All the results indicated that ZW2-1 could be a novel antileukemia lead capable of simultaneously inducing apoptosis, autophagy, and differentiation.

No MeSH data available.


Related in: MedlinePlus

Effects of ZW2-1 on apoptosis of HL-60 and NB4 cells. Annexin V and PI double staining for apoptosis of cells 48 h after incubation with ZW2-1 in comparison to the untreated control cells. All experiments are presented as mean ± SD of at least three independent experiments performed in replicates.
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fig2: Effects of ZW2-1 on apoptosis of HL-60 and NB4 cells. Annexin V and PI double staining for apoptosis of cells 48 h after incubation with ZW2-1 in comparison to the untreated control cells. All experiments are presented as mean ± SD of at least three independent experiments performed in replicates.

Mentions: To elucidate the possible mechanism(s) of inhibiting proliferation of HL-60 cells, we have tested the effects of ZW2-1 to induce apoptosis in HL-60 and NB4 cells by flow cytometric analysis of Annexin V/FITC and propidium iodide (PI) uptake. As shown in Figure 2, treatment with 8 μM ZW2-1 for 48 hr resulted in apoptotic cell death in HL-60 cells (49.2%) and NB4 cells (78.3%). The results indicated that cytotoxicity of ZW2-1 (8 μM, 48 hr) in HL-60 and NB4, at least partly, resulted from apoptosis.


Developing a Novel Indolocarbazole as Histone Deacetylases Inhibitor against Leukemia Cell Lines.

Wang W, Lv M, Zhao X, Zhang J - J Anal Methods Chem (2015)

Effects of ZW2-1 on apoptosis of HL-60 and NB4 cells. Annexin V and PI double staining for apoptosis of cells 48 h after incubation with ZW2-1 in comparison to the untreated control cells. All experiments are presented as mean ± SD of at least three independent experiments performed in replicates.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4663760&req=5

fig2: Effects of ZW2-1 on apoptosis of HL-60 and NB4 cells. Annexin V and PI double staining for apoptosis of cells 48 h after incubation with ZW2-1 in comparison to the untreated control cells. All experiments are presented as mean ± SD of at least three independent experiments performed in replicates.
Mentions: To elucidate the possible mechanism(s) of inhibiting proliferation of HL-60 cells, we have tested the effects of ZW2-1 to induce apoptosis in HL-60 and NB4 cells by flow cytometric analysis of Annexin V/FITC and propidium iodide (PI) uptake. As shown in Figure 2, treatment with 8 μM ZW2-1 for 48 hr resulted in apoptotic cell death in HL-60 cells (49.2%) and NB4 cells (78.3%). The results indicated that cytotoxicity of ZW2-1 (8 μM, 48 hr) in HL-60 and NB4, at least partly, resulted from apoptosis.

Bottom Line: ZW2-1 performed anti-population growth effect which was in a concentration-dependent manner (2-12 μM) by inducing both apoptosis and autophagy in cells.At relatively high concentration (8 μM), ZW2-1 significantly decreased intracellular histone deacetylase 1 level which was also observed.All the results indicated that ZW2-1 could be a novel antileukemia lead capable of simultaneously inducing apoptosis, autophagy, and differentiation.

View Article: PubMed Central - PubMed

Affiliation: Department of Blood Biopharmaceuticals and Viral Detection, Institute of Transfusion Medicine, The Academy of Military Medical Sciences, Beijing 100850, China.

ABSTRACT
A novel indolocarbazole (named as ZW2-1) possessing HDAC inhibition activity was synthesized and evaluated against human leukemia cell lines HL-60 and NB4. ZW2-1 performed anti-population growth effect which was in a concentration-dependent manner (2-12 μM) by inducing both apoptosis and autophagy in cells. The compound also caused differentiation of HL-60 and NB4 cells as shown by increasing expression of CD11b, CD14, and CD38 at moderate concentration (4 μM). At relatively high concentration (8 μM), ZW2-1 significantly decreased intracellular histone deacetylase 1 level which was also observed. All the results indicated that ZW2-1 could be a novel antileukemia lead capable of simultaneously inducing apoptosis, autophagy, and differentiation.

No MeSH data available.


Related in: MedlinePlus