Volume 5 • Issue 4 • 1000159
Transl Med
ISSN: 2161-1025 TM, an open access journal
Sanyal et al., Transl Med (Sunnyvale) 2015, 5:4
DOI: 10.4172/2161-1025.1000159
Translational Medicine
Research Article Open Access
the COX-2 inhibitors mediated cancer cell killings. Tree COX-2
inhibitors used on comparable basis are 1) Celecoxib, a methylphenyl
trifuoromethyl pyrazolyl benzene sulphonamide, 2) Etoricoxib, a
chloromethyl methylsulfonyl phenyl bipyridine and 3) Diclofenac, a
dichloro anilinophenyl acetic acid.
Materials and Methods
Chemicals
1, 2-Dimethylhydrazine (DMH) and Bradford reagent have been
purchased from Sigma Aldrich (St. Louis, MO, USA). Celecoxib
and Diclofenac were a generous gif from Ranbaxy Phamaceuticals
(Gurgaon, India). Te primary antibody against Bcl-2, Bax, Bad, Apaf-
1, Cyt c, Caspase-9, Caspase-3, SK-1 and β-actin was purchased from
Santa Cruz Biotechnology, Inc., CA (USA). Alkaline phosphatase
conjugated secondary antibodies and BCIP-NBT were purchased from
Genei, Bangalore, India. All other chemicals and reagents used in the
present study were of analytical grade and purchased from the reputed
Indian manufacturers.
Animal Procurement
Female Sprague-Dawley rats of body weight between 100-150g
were obtained from the inbred population of the Central Animal
House, Panjab University, Chandigarh. Te animals were acclimatized
for at least 1 week and given normal diet (rodent chow) and water ad
libitum. Tey were maintained as per the principles and guidelines of
the Ethics Committee of Animal Care of Panjab University and in general,
followed the NIH guidelines (Rule No. 23-85, as revised in 1985). Tey
Abstract
Bcl-2 family of proteins is implicated in the malignant tumors including colorectal cancer. Activation of Bcl-2 inhibits
the pro-apoptotic proteins (Bax and Bad) and regulates many biological processes such as apoptosis, cell proliferation
and cell growth. As the mitochondrial enzymes are involved in sphingolipid metabolism, it can regulate ceramide
formation and in turn mitochondria play a central role for the regulation of ceramide induced apoptosis. Bcl-2/ Bcl-
xL activates sphingosine kinases (SKs), resulting in the accumulation of S1P (sphingosine-1-phosphate), thereby
reducing apoptosis. In the present study, the anti-neoplastic effects have been observed of Etoricoxib and Celecoxib,
two COX-2 selective non-steroidal anti-infammatory drugs (NSAIDs), and Diclofenac, a preferential COX-2 inhibitory
NSAIDs, in the early stage of colon cancer in rats. These NSAIDs regress the expressions of Bcl-2 and SK-1 and
promote apoptosis. Gross morphological analysis revealed the occurrence of raised mucosal lesions called MPL or
multiple plaque lesions, which were maximum in the 1, 2-Dimethylhydrazine (DMH) treated group and their number
regressed with the co-administration of the NSAIDs. An abnormal histo-architecture like hyperplasia and dysplasia
were evident in the carcinogenic group, which were reduced with NSAIDs co-administration.
Activation of Mitochondrial Apoptosis and Regulation of Ceramide
Signalling by COX-2 Inhibitors in Colon Cancer
SN Sanyal
*
, Shelly Jain, Preety Ghanghas and Chandan Rana
Department of Biophysics, Panjab University, Chandigarh, India 160014
*Corresponding author: Sanyal SN, Department of Biophysics, Panjab University,
Chandigarh- 160014, India, Tel: +911722534122; E-mail: sanyalpu@gmail.com
Received September 21, 2015; Accepted October 21, 2015; Published
November 02, 2015
Citation: Sanyal SN, Jain S, Ghanghas P, Rana C (2015) Activation of Mitochondrial
Apoptosis and Regulation of Ceramide Signalling by COX-2 Inhibitors in Colon
Cancer. Transl Med 5: 159. doi:10.4172/2161-1025.1000159
Copyright: © 2015 Sanyal SN, et al., This is an open-access article distributed
under the terms of the Creative Commons Attribution License, which permits
unrestricted use, distribution, and reproduction in any medium, provided the
original author and source are credited.
Keywords: Apoptosis; Bcl-2; Colorectal cancer; DMH; NSAIDs; SK-1
Introduction
Cells die in response to various stimuli and during apoptosis or
programmed cell death this happens in a controlled way to maintain
homeostasis in constantly replicating tissues such as the colon [1]. Te
pro-apoptotic Bax and Bad protein form important components of Bcl-2
family which is one of the dominant member in the mitochondrion form
of apoptosis [2, 3]. It also involves down-modulation of Bax-antagonists
such as Bcl-2 [4]. Translocation of pro-apoptotic Bax and Bak from the
cytoplasm to the mitochondria is a crucial event in apoptosis cascades
and therefore Bax has been recognized as an important mediator of
anticancer drug-induced cell death [5]. Cytochrome c interacts with
Apaf-1 and triggers the formation of apoptosome protein complex in
the cytosol and in the presence of ATP and Apaf-1 then becomes an
allosteric activator of the caspase cascade and the proteolytic demolition
of the cell [6, 7]. Caspases are the family of endoproteases, it provides
critical links in cellular regulatory networks to control infammation
and cell death. Activation of apoptotic caspases results in either the
inactivation or activation of the substrates, and the production of a
cascade of signalling events permitting to the controlled demolition
of cellular components [8]. Stimulation of infammatory caspases
promotes the production of active pro-infammatory cytokines and
promotes apoptosis. Caspases are critical links as their dysregulation
underlies human diseases which includes infammatory disorders and
cancer [9].
Cell signalling pathway mediated by ceramide has been shown
to contribute to terminal cell diferentiation, cell cycle arrest and
apoptosis [10] as well as to cell proliferation [11]. Ceramide may
modify the relationship between pro-apoptotic (i.e., Bax and Bad) and
anti-apoptotic (i.e., Bcl-2 and Bcl-XL) members of the Bcl-2 family
of proteins. Key components of the sphingolipid metabolic pathway,
are the ceramide and its metabolites, which includes sphingosine and
sphingosine-1-phosphate (S1P). S1P has been exhibited to stimulate cell
growth and prevent apoptosis [12]. Sphingosine kinase (SK) catalyse
the phosphorylation of sphingosine that results in the synthesis of S1P.
Sphingosine kinase (SK1) can be stimulated by a variety of growth
factors, cytokines and mitogens [13].
Presently, in an experimental colorectal cancer (CRC) in rodents,
apoptotic proteins and sphingosine kinase have been targeted in
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ISSN: 2161-1025