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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

Structure of ZW2-1 and its effects on cell proliferation. (a) Chemical structure of ZW2-1. (b) Effects of ZW2-1 on cell proliferation of human leukemia cell line HL-60, NB4, and immortal human keratinocyte cell line Haca T. The values are represented as mean ± SD of three independent experiments with five replicates in each.
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fig1: Structure of ZW2-1 and its effects on cell proliferation. (a) Chemical structure of ZW2-1. (b) Effects of ZW2-1 on cell proliferation of human leukemia cell line HL-60, NB4, and immortal human keratinocyte cell line Haca T. The values are represented as mean ± SD of three independent experiments with five replicates in each.

Mentions: In this paper a novel antileukemia agent, 4-(5,7-dihydroindolo[2,3-b]carbazol-6-yl)phenol (named as ZW2-1, Figure 1(a)), possessing potential HDAC inhibition activity was reported. ZW2-1 was prepared via the chemical synthesis method described in Supporting Information in Supplementary Material available online at http://dx.doi.org/10.1155/2015/675053. The synthesized product was purified by HPLC with a purity of 98.9% and analyzed using NMR and MS, and data were also provided in Supporting Information.


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)

Structure of ZW2-1 and its effects on cell proliferation. (a) Chemical structure of ZW2-1. (b) Effects of ZW2-1 on cell proliferation of human leukemia cell line HL-60, NB4, and immortal human keratinocyte cell line Haca T. The values are represented as mean ± SD of three independent experiments with five replicates in each.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

fig1: Structure of ZW2-1 and its effects on cell proliferation. (a) Chemical structure of ZW2-1. (b) Effects of ZW2-1 on cell proliferation of human leukemia cell line HL-60, NB4, and immortal human keratinocyte cell line Haca T. The values are represented as mean ± SD of three independent experiments with five replicates in each.
Mentions: In this paper a novel antileukemia agent, 4-(5,7-dihydroindolo[2,3-b]carbazol-6-yl)phenol (named as ZW2-1, Figure 1(a)), possessing potential HDAC inhibition activity was reported. ZW2-1 was prepared via the chemical synthesis method described in Supporting Information in Supplementary Material available online at http://dx.doi.org/10.1155/2015/675053. The synthesized product was purified by HPLC with a purity of 98.9% and analyzed using NMR and MS, and data were also provided in Supporting Information.

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