Iron-chelating Edaravone For Retinal Diseases

Discussion in 'Optometry Archives' started by ironjustice, Feb 11, 2009.

  1. ironjustice

    ironjustice Guest

    Edaravone, a free radical scavenger, protects against retinal damage
    in vitro and in vivo.
    J Pharmacol Exp Ther. 2009 Feb 6.
    Inokuchi Y, Imai S, Nakajima Y, Shimazawa M, Aihara M, Araie M, Hara
    Gifu Pharmaceutical University.

    Edaravone, a free radical scavenger, is used for the treatment of
    acute cerebral infarction.
    In this study, we investigated whether edaravone is neuroprotective
    against on retinal damage.
    In vitro, we employed a radical scavenging-capacity assay using
    reactive oxygen species (ROS)-sensitive probes to investigate the
    effects of edaravone on hydrogen peroxide (H2O2), superoxide anion (O2.
    (-)), and hydroxyl radical (.OH) production in a rat retinal ganglion
    cell-line (RGC-5). The effect of edaravone on oxygen-glucose
    deprivation (OGD)-induced RGC-5 damage was evaluated using a WST-8
    assay of cell viability.
    Edaravone significantly decreased radical-generation, and reduced the
    cell death induced by OGD-stress.
    In vivo, retinal damage was induced by intravitreous injection of N-
    methyl-D-aspartate (NMDA; 5 nmol), and was evaluated by examining
    ganglion cell layer (GCL) cell loss, TUNEL staining, and the
    expressions of two oxidant-stress markers [4-hydroxy-2-nonenal (4-HNE)
    and 8-hydroxy-2-deoxyguanosine (8-OHdG)].
    In addition, activations of MAPKs [extracellular signal regulated
    protein kinases (ERK), c-Jun N-terminal kinases (JNK), and p38 MAPK],
    as down stream signal pathways after NMDA-receptor activation, were
    measured using immunoblotting and immunostaining.
    Edaravone at 5 and 50 nmol (intravitreously) or at 1 and 3 mg/kg
    (i.v.) significantly protected against NMDA-induced retinal cell
    death. At 50 nmol (intravitreously) it : (a) decreased the retinal
    expressions of TUNEL-positive cells, 4-HNE, and 8-OHdG and (b) reduced
    the retinal expressions of NMDA-induced phosphorylated-JNK and
    phosphorylated-p38, but not that of phosphorylated-ERK.
    These findings suggest that oxidative stress plays a pivotal role in
    retinal damage and that edaravone may be a candidate for the effective
    treatment of retinal diseases.

    PMID: 19201991

    "Iron-chelating agents, N-acetyl-L-cysteine (NAC), apocynin,probucol,
    and edaravone, are useful in preventing cardiovascular injury and

    Recent Patents on Anti-Infective Drug Discovery, 2006, 1,
    17-31171574-891X/06 $100.00+.00(c) 2006 Bentham Science Publishers
    Ltd.Recent Progress in Pharmacological Research of Antioxidants
    inPathological Conditions: Cardiovascular Health


    Cardiovasc Ther. 2008 Summer;26(2):101-14.

    The novel antioxidant edaravone: from bench to bedside.

    Watanabe T, Tahara M, Todo S.

    Department of REDOX Medicinal Science, Graduate School of
    Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.

    Over the last decade, important advances have been made to support
    fact that reactive oxygen species (ROS) are generated and play a
    harmful role during the acute and late stages of cerebral ischemia.
    Several drugs, such as radical scavengers and antioxidants, have been
    evaluated in preclinical and clinical studies.
    Edaravone (3-methyl-1- phenyl-2-pyrazolin-5-one; Radicut((R)),
    Mitsubishi Tanabe Pharma Corporation) is a novel antioxidant that is
    currently used in Japan for the treatment of patients in the acute
    stage of cerebral infarction.
    Edaravone scavenges ROS and inhibits proinflammatory responses after
    brain ischemia in animals and humans.
    In particular, postischemic inflammation, leading to brain edema and
    infarction due to neuronal damage and endothelial cell death, can
    be ameliorated by edaravone.
    In addition to these antistroke effects, edaravone has also
    been shown to prevent oxidative damage to various extracerebral
    Therefore, in addition to its usefulness in the treatment of
    stroke, edaravone is expected to play an integral role in the
    treatment of many oxidative stress-related diseases.

    PMID: 18485133

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    ironjustice, Feb 11, 2009
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