Edaravone is a free radical scavenger that protects against laser-induced choroidal neovascularization in mice and common marmosets
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Edaravone
Free radical scavenger
Increasing data suggest that oxygen free radical species play detrimental roles in ischemic diseases. A free radical scavenger capable of inhibiting oxidative injury is expected to become a new drug for the treatment of ischemic diseases such as cerebral ischemia. Edaravon (3-methyl-1-phenyl-2-pyrazolin-5-one), which has been developed as an neuroprotective agent for more than 15 years since its discovery, is approved for the treatment of acute cerebral infarction. In this paper, the pharmacologic characteristics and clinical effects of edaravone are reviewed. In early stage of investigation, edaravone was found to have promising activities as an antioxidative radical scavenger, quenching hydroxyl radical (•OH) and inhibiting both •OH-dependent and •OH-independent lipid peroxidation. Edaravone showed inhibitory effects on both water-soluble and lipid-soluble peroxyl radical-induced peroxidation systems, which are different from the inhibitory effects of vitamins C and E in each system, respectively. Oxidative injury to cultured endothelial cells caused by arachidonate (AA) peroxides is prevented in the existence of edaravone. To clarify the characteristics of this free radical scavenger, further investigation was carried out. Edaravone ameliorated exacerbation of cortical edema induced by a focal ischemia-reperfusion model in rats, suggesting inhibitory effects on oxidative injury to the blood-brain barrier (BBB). Additionally, edaravone also prevented rat cortical edema caused by intracortical AA infusion in which free radical production and subsequent oxidative injury to the BBB are involved. With advances in in vivo measurement technology of oxygen radicals, edaravone was shown to inhibit postischemic increases in •OH production and tissue injury in the penumbral or recirculated area in rat cerebral ischemia models. In clinical studies, edaravone improved the core neurologic deficits, activities of daily living, and functional outcome of stroke patients. Furthermore, a study using proton magnetic resonance spectroscopic techniques showed that edaravone preserved N-acetyl-aspartate in stroke patients, a promising neuronal marker in the brain. Further investigation is essential for a better understanding of free radical-mediated cerebral injury during ischemia followed by recirculation. We hope that edaravone represents a promising neuroprotectant for drug therapy in acute cerebral ischemia.
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Clinical Observation of the Early Treatment of Acute Cerebral Hemorrhage with Free Radical Scavenger
【Objective】To evaluate the clinical efficacy of free radical scavenger on the early treatment of acute cerebral hemorrhage.【Methods】Fifty nine cases of acute cerebral hemorrhage were divided into treatment group and control group randomly.The patients in treatment group were injected intravenously twice daily with 30 mg edaravone for 14 days.Meantime,routine treatment for acute cerebral hemorrhage was carried on.The same treatment except injection with edaravone was implemented in the control group.Neurological functional deficit scores were utilized for assessment before treatment.On the 14th day after treatment,the patients were assessed again and the efficacy was recorded.【Results】After 14 days treatment,the neurological functional deficit scores of treated group were 85.8±17.1,whereas those of the control group were 68.7±22.7.There was significant difference between two groups(P0.05).There were also significant differences between two groups in terms of apparent effect rate(33.3 % in treated group and 10.2 % in control group,P0.05) and improvement rate(66.7 % in treated group,44.7 % in control group,P0.05).【Conclusion】Free radical scavenger can accelerate the recovery of neural function after acute cerebral hemorrhage.
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Objective To explore the effect of free radical scavenger on the serum levels of endothelin-1 (ET-1) and interleukin-1 β (IL-1β) after the surgery and its meanings in the patients with cranial bases tumors.Methods Sixty-four patients with cranial bases tumors were randomly divided into both the routine treatment (not treated by free radical scavenger) and edaravone treatment groups.Thirty-two patients with cerebral convex lesions,who did not received free radical scavenger treatment,served as control group.Edaravone treatment included that the operated areas were irrigated with the fluid containing edaravone in the operation and the edaravone was injected into the peripheral veins after the operation.The serum levels of ET-1 and IL-1β were determined before and after the operation in all the patients.Results The serum levels of ET-1 and IL-1s levels were significantly higher in the routine treatment group than those in the control group after the operation (P0.05),they reached a peak 5～7 days after the operation,and then decreased gradually.The postoperative serum levels of ET-1 and IL-1β were significantly lower in edaravone treatment group than those in the routine treatment group (P0.05),but they were significantly higher than those in the control group (P0.05).Conclusions The increase in the serum levels of ET-1 and IL-1β after the operation may be decreased by free radical scavenger treatment in the patients with cranial bases tumors.It is suggested that the free radical scavenger may be of the protective effect on the cerebral vessels because the increase in the serum levels of ET-1 and IL-βmay be related to the cerebral vasospasm after the operation in the patients with cranial bases tumors.
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Edaravone is a free radical scavenger that was at first approved in the world. Edaravone has the therapeutic effect on ischemia reperfusion injury, nerve cells apoptosis, apomorphosis and so on by scavenging free radicals and preserving endoplasmic reticulum dysfunction, et al. Combining edaravone with other drugs to treat cerebral infarction, the effect is more effective. In addition, edaravone can protect the liver by scavenging free radicals and may have application values to many kinds of diseases. Edaravone is a free radical scavenger with a brilliantp erspectivei n clinic.
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Edaravone,a free radical scavenger,has been used for the treatment of acute cerebral ischemic stroke. Recent researches show that the pharmacological effect of edaravone may involve many organs and its clinical application is not limited to ischemic stroke. This article reviewed the pharmacological progress in the protective effects of edaravone on different organ injuries( brain,heart,liver,lung, etc.) in order to provide evidence for the novel clinical applications of edaravone in future.
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Objective To observe the clinical efficacy of free radical scavenger edaravone on cerebral hemorrhage.Methods Thirty-six cerebral hemorrhage patients were randomly selected and assigned to treatment group and control group.Edaravone was added to treat on the patients of treatment group respectively.ESS and ADL were adoped to evaluate the efficacy of edaravone on 1,2,4 week after treatment.Results There were significant differences between treatment group and control group on 1,2,4 weeks after treatment.Conclusion Free radical scavenger edaravone can advanced the recovery of neural function and activity of daily living.It is a effective and safe drug to the treatment of cerebral hemorrhage.
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Edaravone, a clinical drug used widely for the treatment of acute cerebral infarction, is reported to scavenge free radicals. In the present study, we investigated the radioprotective effect of edaravone on X-ray-induced apoptosis in MOLT-4 cells. Apoptosis was determined by the dye exclusion test, Annexin V binding assay, cleavage of caspase, and DNA fragmentation. We found that edaravone significantly suppressed the X-ray-induced apoptosis. The amount of intracellular ROS production was determined by the chloromethyl-2',7'-dichlorodihydro-fluorescein diacetate system. We found that the intracellular ROS production by X-irradiation was completely suppressed by the addition of edaravone. The accumulation and phosphorylation of p53 and the expression of p21WAF1, a target protein of p53, which were induced by X-irradiation, were also suppressed by adding edaravone. We conclude that the free radical scavenger edaravone suppresses X-ray-induced apoptosis in MOLT-4 cells by inhibiting p53.
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目的 探讨自由基清除剂依达拉奉对实验性脑出血的保护作用及其作用机制.方法 240只SD雄性大鼠随机分为4组:假手术组、手术模型组、依达拉奉术前给药(A)组和依达拉奉术后给药(B)组.参考Rosenberg的脑出血模型的制作方法建立大鼠脑出血模型,采用干重法评价脑水肿程度,Bederson评分法评价神经功能缺损,并观察依达拉奉对血肿周围脑组织中超氧化物歧化酶(SOD)活性和丙二醛(MDA)的影响.结果 手术模型组及依达拉奉A、B组脑组织中水的含量高于假手术组,而依达拉奉A、B组低于模型组,其差异有统计学意义(P＜0.01);依达拉奉A、B组大鼠肢体神经功能缺损的恢复明显快于模型组;与假手术组[(70.7±2.7)U/mg]相比,造模后20 min模型组及依达拉奉A、B组大鼠脑组织SOD活性即开始下降[分别为(62.5±2.5)、(65.2±5.3)、(61.6±4.2)U/mg],180 min时降至最低(P＜0.01),而与同时点模型组比较,依达拉奉各组SOD活性有不同程度升高,其差异有统计学意义(P＜0.01).与假手术组[(2.9±0.2)nmol/mg]相比,造模后20min模型组及依达拉奉A、B组大鼠脑组织MDA含量开始增加[分别为(3.4±0.2)、(3.1±0.2)、(3.2±0.5)nmol/mg],与同时点模型组比较,依达拉奉各组MDA含量有不同程度降低,80、110、180min时差异有统计学意义(P＜0.01).结论 依达拉奉可抑制大鼠实验性脑出血脑细胞的过氧化作用,减轻脑水肿,改善神经功能,具有脑保护作用。
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Edaravone, a novel potent free radical scavenger for acute ischemic stroke：From laboratory to clinic
Free radical plays a key role in the process of cerebral ischemic injury. It aggravates cell membrane damage through the peroxidation of unsaturated fatty acids, and then results in neuronal death and brain edema. Edaravone, a novel potent free radical scavenger, exerts its neuroprotective effect by inhibiting endothelial injury in cerebral ischemic areas and relieving neuronal damage. It also reduces thrombolytic therapy-induced brain edema and bleeding events after reperfusion. Clinical experiences suggest that the therapeutic time window of edaravone is very wide, and when it combines with thrombolytic therapy, it may reduce stroke mortality and promote the recovery of neurological deficit. This article reviews the course of development of edaravone from laboratory to clinical stage.
Key words:
edaravone; ischernic stroke; neuroprotection; antioxidant; free radical scavenger
Edaravone
Free radical scavenger
Stroke
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