Anti-proliferative, cytotoxic and NF-κB inhibitory properties of spiro(lactone-cyclohexanone) compounds in human leukemia

Mustapha M. Bouhenna; Barbora Orlikova; Oualid Talhi; Ben Schram; Diana C.G.A. Pinto; Nadia Taibi; Khaldoun Bachari; Marc Diederich; Artur M.S. Silva; Nabil Mameri

doi:10.21873/anticanres.11946

Anti-proliferative, cytotoxic and NF-κB inhibitory properties of spiro(lactone-cyclohexanone) compounds in human leukemia

Mustapha M. Bouhenna, Barbora Orlikova, Oualid Talhi, Ben Schram, Diana C.G.A. Pinto, Nadia Taibi, Khaldoun Bachari, Marc Diederich, Artur M.S. Silva, Nabil Mameri^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › Research › peer-review

9 Citations (Scopus)

Abstract

Background/Aim: NF-κB affects most aspects of cellular physiology. Deregulation of NF-κB signaling is associated with inflammatory diseases and cancer. In this study, we evaluated the cytotoxic and NF-κB inhibition potential of new spiro(lactone-cyclohexanone) compounds in two different human leukemia cell lines (U937 and K562). Materials and Methods: The anti-proliferative effects of the spiro(lactone-cyclohexanone) compounds on human K562 and U937 cell lines was evaluated by trypan blue staining, as well as their involvement in NF-kB regulation were analyzed by luciferase reporter gene assay, Caspase-3/7 activities were evaluated to analyze apoptosis induction. Results: Both spiro(coumarin-cyclohexanone) 4 and spiro(6-methyllactonecyclohexanone) 9 down-regulated cancer cell viability and proliferation. Compound 4 inhibited TNF-α-induced NF-κB activation in a dose-dependent manner and induced caspasedependent apoptosis in both leukemia cell lines. Conclusion: Results show that compound 4 and compound 9 have potential as anti-cancer agents. In addition, compound 4 exerted NFkB inhibition activity in leukemia cancer cells.

Original language	English
Pages (from-to)	5225-5233
Number of pages	9
Journal	Anticancer Research
Volume	37
Issue number	9
DOIs	https://doi.org/10.21873/anticanres.11946
Publication status	Published - Sept 2017
Externally published	Yes

Keywords

Anti-cancer
Anti-proliferation
Apoptosis
Cytotoxicity
Nuclear factor-κB
Spiro(lactone-cyclohexanones)

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10.21873/anticanres.11946

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@article{776a27f276b748c6a9e702843d98afde,

title = "Anti-proliferative, cytotoxic and NF-κB inhibitory properties of spiro(lactone-cyclohexanone) compounds in human leukemia",

abstract = "Background/Aim: NF-κB affects most aspects of cellular physiology. Deregulation of NF-κB signaling is associated with inflammatory diseases and cancer. In this study, we evaluated the cytotoxic and NF-κB inhibition potential of new spiro(lactone-cyclohexanone) compounds in two different human leukemia cell lines (U937 and K562). Materials and Methods: The anti-proliferative effects of the spiro(lactone-cyclohexanone) compounds on human K562 and U937 cell lines was evaluated by trypan blue staining, as well as their involvement in NF-kB regulation were analyzed by luciferase reporter gene assay, Caspase-3/7 activities were evaluated to analyze apoptosis induction. Results: Both spiro(coumarin-cyclohexanone) 4 and spiro(6-methyllactonecyclohexanone) 9 down-regulated cancer cell viability and proliferation. Compound 4 inhibited TNF-α-induced NF-κB activation in a dose-dependent manner and induced caspasedependent apoptosis in both leukemia cell lines. Conclusion: Results show that compound 4 and compound 9 have potential as anti-cancer agents. In addition, compound 4 exerted NFkB inhibition activity in leukemia cancer cells.",

keywords = "Anti-cancer, Anti-proliferation, Apoptosis, Cytotoxicity, Nuclear factor-κB, Spiro(lactone-cyclohexanones)",

author = "Bouhenna, {Mustapha M.} and Barbora Orlikova and Oualid Talhi and Ben Schram and Pinto, {Diana C.G.A.} and Nadia Taibi and Khaldoun Bachari and Marc Diederich and Silva, {Artur M.S.} and Nabil Mameri",

year = "2017",

month = sep,

doi = "10.21873/anticanres.11946",

language = "English",

volume = "37",

pages = "5225--5233",

journal = "Anticancer Research",

issn = "0250-7005",

publisher = "International Institute of Anticancer Research",

number = "9",

}

TY - JOUR

T1 - Anti-proliferative, cytotoxic and NF-κB inhibitory properties of spiro(lactone-cyclohexanone) compounds in human leukemia

AU - Bouhenna, Mustapha M.

AU - Orlikova, Barbora

AU - Talhi, Oualid

AU - Schram, Ben

AU - Pinto, Diana C.G.A.

AU - Taibi, Nadia

AU - Bachari, Khaldoun

AU - Diederich, Marc

AU - Silva, Artur M.S.

AU - Mameri, Nabil

PY - 2017/9

Y1 - 2017/9

N2 - Background/Aim: NF-κB affects most aspects of cellular physiology. Deregulation of NF-κB signaling is associated with inflammatory diseases and cancer. In this study, we evaluated the cytotoxic and NF-κB inhibition potential of new spiro(lactone-cyclohexanone) compounds in two different human leukemia cell lines (U937 and K562). Materials and Methods: The anti-proliferative effects of the spiro(lactone-cyclohexanone) compounds on human K562 and U937 cell lines was evaluated by trypan blue staining, as well as their involvement in NF-kB regulation were analyzed by luciferase reporter gene assay, Caspase-3/7 activities were evaluated to analyze apoptosis induction. Results: Both spiro(coumarin-cyclohexanone) 4 and spiro(6-methyllactonecyclohexanone) 9 down-regulated cancer cell viability and proliferation. Compound 4 inhibited TNF-α-induced NF-κB activation in a dose-dependent manner and induced caspasedependent apoptosis in both leukemia cell lines. Conclusion: Results show that compound 4 and compound 9 have potential as anti-cancer agents. In addition, compound 4 exerted NFkB inhibition activity in leukemia cancer cells.

AB - Background/Aim: NF-κB affects most aspects of cellular physiology. Deregulation of NF-κB signaling is associated with inflammatory diseases and cancer. In this study, we evaluated the cytotoxic and NF-κB inhibition potential of new spiro(lactone-cyclohexanone) compounds in two different human leukemia cell lines (U937 and K562). Materials and Methods: The anti-proliferative effects of the spiro(lactone-cyclohexanone) compounds on human K562 and U937 cell lines was evaluated by trypan blue staining, as well as their involvement in NF-kB regulation were analyzed by luciferase reporter gene assay, Caspase-3/7 activities were evaluated to analyze apoptosis induction. Results: Both spiro(coumarin-cyclohexanone) 4 and spiro(6-methyllactonecyclohexanone) 9 down-regulated cancer cell viability and proliferation. Compound 4 inhibited TNF-α-induced NF-κB activation in a dose-dependent manner and induced caspasedependent apoptosis in both leukemia cell lines. Conclusion: Results show that compound 4 and compound 9 have potential as anti-cancer agents. In addition, compound 4 exerted NFkB inhibition activity in leukemia cancer cells.

KW - Anti-cancer

KW - Anti-proliferation

KW - Apoptosis

KW - Cytotoxicity

KW - Nuclear factor-κB

KW - Spiro(lactone-cyclohexanones)

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DO - 10.21873/anticanres.11946

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SN - 0250-7005

VL - 37

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EP - 5233

JO - Anticancer Research

JF - Anticancer Research

IS - 9

ER -

Anti-proliferative, cytotoxic and NF-κB inhibitory properties of spiro(lactone-cyclohexanone) compounds in human leukemia

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