Background
Cancer is a condition in which abnormal cells in a particular
part of the body can proliferate in an unchecked way
and affect its surrounding healthy tissues. Inflammatory
pathways are some of the most important factors involved
in cancer and tumor formation (1). These pathways are
activated by various agents, which are responsible for
95% of cancers, including smoking, stress, food, obesity,
alcohol, infectious agents, environmental triggers, and
exposure to radiation (2). Inflammation is an immune
response to cellular or tissue injury or infection caused
by pathogens. Clinically, inflammation is determined by
features such as redness, warmth, swelling, and pain (3).
The mechanism of inflammatory pathways can be divided
into the arachidonic acid (AA)-dependent pathway and
the AA-independent pathway (4). Cyclooxygenase (COX),
lipoxygenase (LOX), and phospholipase A2 (PLA2) are
considered as AA-dependent pathways. On the other
hand, nitric oxide synthase (NOS) and NF-кB (i.e.,
nuclear factor kappa-light-chain-enhancer of activated B
cells) are AA-independent pathways (5). The products of
both pathways play an important role in the inflammation
process (6). In the past two decades, several molecules
involved in the inflammation have been identified,
including tumor necrosis factor (TNF), interleukin 1 (IL-
1), interleukin 6 (IL-6), COX -2, matrix metalloproteinase
(MMP) and vascular endothelial growth factor (VEGF).
The common feature of all these molecules is the fact that
they are regulated by the transcription factor NF-кB (7).
The NF-кB which is known as a transcription activator
is a heterodimer protein composed of two subunits
called p50 and RelA (p65). In the absence of stimulus,
the NF-кB is inhibited in the cytoplasm by an inhibitor
agent called IкBα; but in the presence of the stimulus, the
signaling pathway is activated. The protein IкB creates a
heterodimer nuclear translocation signal that prevents the
transferring of NF-кB into the nucleus. In these conditions,
the NF-кB is activated and enters into the nucleus which
will affect the expression of target genes (8). The NF-
кB connects cells that are involved in inflammation and
cancer (9). The expression of NF-кB is increased in the
majority of cancer tissues and is known as an inducer
of prostate cancer progression and tumor metastasis in
lymph nodes (10). Moreover, lung cancer progression
(11), breast cancer (12) and its response to chemotherapy
(13) are other NF-кB activities. Due to the large number
of cellular processes affected by NF-кB, modulators of
this pathway have received a considerable attention. For
Avicenna Journal of Medical Biochemistry
© 2021 The Author(s); Published by Hamadan University of Medical Sciences. This is an open-access article distributed under the terms of
the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0), which permits unrestricted use, distribution, and
reproduction in any medium, provided the original work is properly cited.
2021 December;9(2):48-53 doi:10.34172/ajmb.2021.09
Inhibition of NF-кB Expression in LPS-Induced RAW264.7
Macrophage Cells by a Thiazolidinone Derivative (TZD-
OCH
2
CH
3
)
Farahnaz Hasanzadeh
1
, Hossein Ghafouri
2,3*
ID
, Salman Ahmadi
2
, Sevda Zarei
2
ID
, Mahmoud Reza Aghamaali
2
, Asadollah
Mohammadi
4
1
Department of Biology, Faculty of Basic Sciences, University of Guilan, University Campus 2, Rasht, Iran
2
Department of Biology, Faculty of Basic Sciences, University of Guilan, Rasht, Iran
3
Department of Marine Sciences, The Caspian Sea Basin Research Center, University of Guilan, Rasht, Iran
4
Department of Chemistry, Faculty of Sciences, University of Guilan, Rasht, Iran
http://ajmb.umsha.ac.ir
Research Article
Abstract
To date, various derivatives of thiazolidinone in a variety of cell lines have been investigated. The present
study aimed to evaluate the toxicity and inhibitory effects of a thiazolidinone derivative called 5-(2,4-bis-
4-ethoxy-phenyl azo)-3-hydroxy-benzylidine)-2,4-thiazolidinone (TZD-OCH
2
CH
3
) on the expression of
NF-кB in LPS-induced RAW264.7 macrophage cell lines. Different concentrations of the MTT assay
(0-120 μg/mL) were performed to estimate the biological rate of the cells. The half-maximal inhibitory
concentration (IC
50
) of TZD-OCH
2
CH
3
-treated RAW264.7 cells was found to be 115 μg/mL. To determine
the inhibitory effect of the synthesized compound on the expression changes of NF-кB, the RAW264.7
cells were initially induced with LPS and then treated by 15, 30 and 60 µg/mL of TZD-OCH
2
CH
3
. Real-
time PCR results confirmed a strong inhibitory effect of TZD-OCH
2
CH
3
on the expression of NF-кB in
LPS-induced RAW264.7 cells (IC
50
= 48 μg/mL). Overall, these findings suggested that the derivative TZD-
OCH
2
CH
3
had a significant anti-inflammatory effect.
Keywords: Thiazolidinone, NF-кB, RAW264.7 cells, LPS- induced, Inflammatory pathways
Received: 13 July 2021
Revised: 22 August 2021
Accepted: 22 August 2021
ePublished: 29 December 2021
*Corresponding author:
Hossein Ghafouri,
Associate Professor in
Biochemistry, Department
of Biology, Faculty of Basic
Sciences, University of Guilan,
Rasht, Iran.
Tel: +981333333647;
Email: h.ghafoori@guilan.ac.ir