Editorial
Kenkyu Journal of Medical Science & Clinical Research
Open Access
Citation: Obulesu M (2016) Iron Chelation Therapy. KJ Medscicr 1: 100101
Iron Chelation Therapy Obulesu M Materials Science, University of Tsukuba, Japan *
Corresponding Author: Obulesu M, Materials Science, University of Tsukuba, Japan, e-mail;
[email protected]
1. Introduction Iron plays a pivotal role in human physiology by
Biomedical field. Although a few nanoparticles used
serving multifarious functions such as cofactor in a
for metal overload diseases, studies on polymer
few enzymes, transport of hemoglobin etc. However,
conjugated iron chelator are significantly less [1,2].
its overload leads to dreadful diseases such as
Synthesized starch conjugated desferrioxamine which
Alzheimer’s
Hemochromatosis,
showed better chelation efficacy and entered phase 1b
Aceruloplasminemia, and Transfusional Siderosis.
clinical trials several years ago. However, it has been
Iron in free form provokes the production of reactive
found to induce urticarial reactions in patients and
oxygen species (ROS) via Fenton reaction. Therefore,
discouraged at a later date. In another study dendrimer
scavenging the excess metal is of considerable
conjugated
importance in biomedical field.
improvement in therapeutic properties by chelating
disease,
desferrioxamine
showed
significant
iron. In this study, initially hyperbranched glycerol
2. Chelation Therapy
scaffold was prepared and several molecules of
Currently, chelation therapy is widely used to
desferrioxamine were covalently conjugated to it.
overcome the iron intoxication.
Long systemic circulation of the dendrimer conjugated
A few Food and
Drug Administration (FDA) approved drugs currently
chelator
was
observed
resulting
in
enhanced
in use show better chelation.
Desferrioxamine,
therapeutic property. However, in HPG conjugated
Deferasirox and Deferiprone are some of the FDA
DFO study optimization and biodistribution of the
approved drugs to circumvent the iron overload.
molecules is yet to be determined.
Despite the interesting metal chelation activity exerted by these chelators, their systemic toxicity, rapid
Liu’s
study
of
elimination from systemic circulation greatly impede
nanoparticle showed some promise in reducing the
their success.
iron overload in brain tissue. They used 2-Methyl-N(2′-aminoethyl
To address the issues associated with low molecular weight compounds a potential polymer conjugated iron chelator, which successfully removes free iron
Volume 1, Issue 1 -KJMSCR-100101
or
iron
chelators
to
3′-aminopropyl)-3-hydroxyl-4-
pyridinone (MAEHP), 2-Methyl (or Ethyl)-N-(2′-
3. Nanotechnology for Chelators
from the cells, is of utmost importance in the
conjugating
hydroxyethoxy)
methyl-3-hydroxyl-4-pyridinone
(MHEMHP). Monodispersed polystyrene particles with carboxyl groups on the surface were used to conjugate MAEHP chelators, each of which contained
www.kenkyuonline.org
Received: February 24, 2016; Accepted: February, 2016; Published: February, 2016
Page 1
Editorial
Kenkyu Journal of Medical Science & Clinical Research
Open Access
Citation: Obulesu M (2016) Iron Chelation Therapy. KJ Medscicr 1: 100101
a free primary amino group available for the conjugation. These nanoparticles showed adsorption on lipoproteins such as low density lipoprotein (LDL). Since they mimic lipoproteins, they are first adsorbed on the low density lipoprotein receptors. Further they are uptaken by brain endothelial cells. Despite the better efficacy of the low molecular weight chelators and polymeric chelators, a few limitations impede their success. There has been an ambiguity whether polymeric chelators are mile stones in chelation therapy or a mirage.
4. Conclusion and Future Perspectives Although development of substantial iron chelators appears ambiguous, a few further studies may open a few novel avenues. In line with this, specific insights into conjugation of aminodiacetic acid ligands to biocompatible polymers such as poly (ethylene glycol) may significantly enhance systemic circulation, reduce toxicity and exhibit robust iron chelation.
Since
aminodiacetic acid containing compounds show better chelation efficacy, they can be used to develop potential armamentarium for iron overload diseases.
References: 1.
Philip E, Hallaway (1989) Proc Natl Acad. Sci. USA 86: 10108-10112.
2.
Obulesu (2016) Curr Drug Metab 17:142-149.
Copyright: © 2016 Obulesu M, This is an open-access article which is distributed under Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. Volume 1, Issue 1 -KJMSCR-100101
www.kenkyuonline.org
Received: February 24, 2016; Accepted: February, 2016; Published: February, 2016
Page 2
