Research Article
The R18 Polyarginine Peptide Is More Effective Than the
TAT-NR2B9c (NA-1) Peptide When Administered 60 Minutes
after Permanent Middle Cerebral Artery Occlusion in the Rat
D. Milani,
1,2,3
N. W. Knuckey,
2,3,4
R. S. Anderton,
1,2
J. L. Cross,
2,3,4
and B. P. Meloni
2,3,4
1
School of Health Sciences, Te University of Notre Dame Australia, Fremantle, WA 6160, Australia
2
Western Australian Neuroscience Research Institute, Nedlands, WA 6009, Australia
3
Department of Neurosurgery, Sir Charles Gairdner Hospital, QEII Medical Centre, Nedlands, WA 6009, Australia
4
Centre for Neuromuscular and Neurological Disorders, Te University of Western Australia, Nedlands, WA 6009, Australia
Correspondence should be addressed to D. Milani; diemilani@gmail.com
Received 24 February 2016; Accepted 11 April 2016
Academic Editor: David S. Liebeskind
Copyright © 2016 D. Milani et al. Tis is an open access article distributed under the Creative Commons Attribution License, which
permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
We examined the dose responsiveness of polyarginine R18 (100, 300, and 1000nmol/kg) when administered 60 minutes afer
permanent middle cerebral artery occlusion (MCAO). Te TAT-NR2B9c peptide, which is known to be neuroprotective in rodent
and nonhuman primate stroke models, served as a positive control. At 24 hours afer MCAO, there was reduced total infarct volume
in R18 treated animals at all doses, but this reduction only reached statistical signifcance at doses of 100 and 1000 nmol/kg. Te
TAT-NR2B9c peptide reduced infarct volume at doses of 300 and 1000nmol/kg, but not to a statistically signifcant extent, while
the 100 nmol/kg dose was inefective. Te reduction in infarct volume with R18 and TAT-NR2B9c peptide treatments was mirrored
by improvements in one or more functional outcomes (namely, neurological score, adhesive tape removal, and rota-rod), but not
to a statistically signifcant extent. Tese fndings further confrm the neuroprotective properties of polyarginine peptides and for
R18 extend its therapeutic time window and dose range, as well as demonstrating its greater efcacy compared to TAT-NR2B9c in
a severe stroke model. Te superior neuroprotective efcacy of R18 over TAT-NR2B9c highlights the potential of this polyarginine
peptide as a lead candidate for studies in human stroke.
1. Introduction
While the incidence of stroke is falling in developed coun-
tries, it remains a leading cause of death and disability
worldwide, with an increasing global disease burden due to
an aging population, as well as the ongoing epidemics of
diabetes, hypertension, and obesity [1]. In terms of acute
therapies, for ischaemic stroke, reperfusion therapy using
tPA (tissue plasminogen activator) alone or more recently in
combination with thrombectomy is by far the most efective
treatment intervention currently available [2–6]. However,
despite the success of tPA/thrombectomy therapy, the num-
ber of stroke patients that receive this treatment is relatively
small. Tis is due to a combination of factors including
the narrow therapeutic time window for tPA/thrombectomy
(3–4.5 h afer stroke), delays in patients obtaining medical
care, the requirement for a brain scan to exclude haemor-
ragic stroke, and the need for highly trained personnel and
specialised equipment to perform the intervention. Given
these limitations, the search continues for a neuroprotective
agent that can be safely administered early afer stroke
onset to limit the extent of brain injury afer stroke and
that can be used when reperfusion interventions cannot be
implemented. Additionally, any neuroprotective treatment
that improves the efcacy, safety, and therapeutic window for
tPA/thrombectomy would be of great clinical signifcance.
In terms of neuroprotective agents, our laboratory has
recently demonstrated that polyarginine and arginine-rich
peptides have potent neuroprotective properties in in vitro
injury models that mimic the efects of stroke [7–9]. More-
over, we have extended these in vitro fndings by demon-
strating that the polyarginine peptides R9, R12, and R18
Hindawi Publishing Corporation
Stroke Research and Treatment
Volume 2016, Article ID 2372710, 9 pages
http://dx.doi.org/10.1155/2016/2372710