Volume 2 • Issue 2 • 1000113
Neurochem Neuropharm Open Access journal
ISSN: 2469-9780
Research Article Open Access
Neurochemistry & Neuropharmacology
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ISSN: 2469-9780
Mohan et al., Neuropharm Open Access 2016, 2:2
DOI: 10.4172/2469-9780.1000113
Keywords: Heme; Protein kinase A; Inlammation; Neurons;
Morphine; Opioid receptor
Introduction
he toxicity of free heme has been documented in several disease
types. For example, in hemolytic anemias such as sickle cell disease and
thalassemia, release of heme from hemoglobin following lysis of red
blood cells is known to cause cell death [1,2]. In a critical care situation
such as hemorrhagic injury, neuronal cell death is caused by the
lysis of red blood cells, which release hemoglobin and its breakdown
product hemin [3-5]. Physiological levels of free heme in the blood
are maintained at low levels (0.1 -1 μM) by the high binding ainity
of proteins such as serum albumin, hemopexin and haptoglobin [6-
8]. When internalized, free heme is catabolized by heme oxygenases
(HO1 and HO2 isoforms) and therefore the amount of cellular damage
free heme produces is limited by the stress-responsive HO1 isoform
[9]. In addition to HO1 and HO2 isoform regulated cellular damage,
the oxidative state of iron (from Fe
2+
to Fe
3+
via the Fenton reaction)
within heme can produce harmful superoxide free radicals in the brain
that can lead to oxidative stress, initiation of lipid peroxidation and
neuronal death.
Pathological conditions can increase the level of heme and iron. For
example in acute conditions such as severe hemolytic crisis in sickle cell
disease, heme levels can increase up to 20 μM or to greater than 200
μM (supraphysiological levels) in thalassemia [10]. herefore, further
studies on the cross talk between neuroinlammatory mediators and
iron-containing hemoproteins such as hemin are warranted.
Morphine is a non-selective opioid receptor agonist and analgesic
agent used in clinical practice to manage pain. Morphine and
morphinans (class of compounds containing the basic morphine
structure) agents have been shown to be neuroprotective in various
models of inlammation and neurodegeneration. For example,
morphine pretreatment of purkinje cells and hippocampal slices
provided ischemic tolerance [11,12]. he same group also recently
discovered that morphine-mediated neuroprotection was not only
NMDA receptor mediated but also miR-134 dependent in primary
cortical neuronal cultures [13]. Besides it critical role in anti-
nociception, activation of the Mu-opioid receptor promotes cell
proliferation and also afects neuronal diferentiation both in vitro and
in vivo [14-16]. Studies have shown that morphine protects neurons
against microglia-mediated neuroinlammation and oxidative stress
[17]. More recently, activation of the Mu- receptor attenuated β-amyloid
peptide neurotoxicity through an mTOR-dependent mechanism
[18]. For a more comprehensive review of morphinans mediated
neuroprotection, Zhang et al. published a review in 2004 that discusses
the utility of opioids in neurodegerative disease. he role of opioid
Morphine-Mediated Cytoprotection against Hemin in SK-N-SH and A172
Cells
Shekher Mohan*, Tanner Robinson, Noah Allen, Lance Armstrong and Sarah Stevens
Department of Pharmaceutical Science and Research, School of Pharmacy, Marshall University, Huntington, WV, USA
Abstract
Study background: Heme and its catabolized form, hemin, are cytotoxic due to their ability to contribute
to the production of reactive oxygen species, increase intracellular calcium levels and stimulate glutamate
mediated-excitotoxicity. Previous work has shown that activation of the opioid receptors (i.e., mu, kappa and delta)
is neuroprotective against ischemia-induced neuronal death and neurotoxicity induced by Aβ oligomers in vitro.
However, the role of these opioid receptor in hemin toxicity remains unknown. Activation of the Mu-receptor results
in decreased 3, 5’-cyclic adenosine monophosphate (cAMP) and adenylyl cyclase activity, which then results in
reduced cAMP-dependent Ca
2+
inlux. Therefore, we hypothesized that the activation of the opioid receptors by
morphine may decrease hemin toxicity.
Methods: The human neuroblastoma SK-N-SH and human astroglia A172 cells were treated with hemin
(3.125, 6.25, 12.5, 25, 50 and 75 μM) for 18 h. In separate experiments, both cells types were pre- and co-treated
with opioid receptor agonist morphine (10 μM) and hemin (75 μM) or naltrexone (10 μM) alone and pre- and co-
treatment with hemin (75 μM) for 18 h. Cell viability was assessed using two assays, LDH and the number of live
cells measured using the Calcein-AM assay.
Results: In both SK-N-SH and A172 cells, hemin-dose dependently induced signiicant cell death compared to
the vehicle control. When pre-treated and co-treated with morphine, hemin toxicity in both cell types was signiicantly
attenuated. The protection mediated by morphine from hemin was blocked by opioid antagonist, naltrexone.
Conclusion: Together, the results suggest that activation of the opioid receptors my morphine is protective
against hemin toxicity in vitro and these indings suggest that cytoprotection may occur through the cAMP-AC
pathway. Therefore, activation of for example the Mu-receptor could be used to minimize neuronal and glial
damage following exposure to supraphysiological levels of hemin.
*Corresponding author: Shekher Mohan, Department of Pharmaceutical Science
and Research, School of Pharmacy, Marshall University, One John Marshall Drive,
Huntington, WV, 25755, USA, Tel: +13046967371; E-mail: mohans@marshall.edu
Received August 15, 2016; Accepted August 31, 2016; Published September 02,
2016
Citation: Mohan S, Robinson T, Allen N, Armstrong L, Stevens S (2016) Morphine-
Mediated Cytoprotection against Hemin in SK-N-SH and A172 Cells. Neurochem
Neuropharm Open Access 2: 113. doi: 10.4172/2469-9780.1000113
Copyright: © 2016 Mohan S, 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.