氨基甲基萘醌(amnq1)对BALB/c小鼠急性毒性评价

Valéria Garrido, Caroline Barros, M. Tonelli, G. Teixeira, Patrícia Ocampo, G. Bezerra, Viveca A Giongo, I. Paixão
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引用次数: 2

摘要

我们报告了第一个临床前试验,表明氨基甲基萘醌- 3-[N-(正丁基)氨基-2,4-二氯苯基]-2-羟基-1,4-萘醌(amnq1)在体外Vero细胞中具有低细胞毒性和抗hsv -1活性。本研究的目的是评价amnq1对BALB/c小鼠的急性毒性。采用BALB/c雌性小鼠,分别以2000 mg/kg体重和550、175、55 mg/kg其他3种浓度评价AMNQ - 1的中位致死剂量(LD50)。我们将其与阿昔洛韦(ACV-50 mg/kg)和10%二甲基亚砜(10% DMSO)进行了为期14天的比较。BALB/c小鼠单次灌胃。两组小鼠均无死亡,临床体征无变化。血液学和生化分析显示一些变化恢复到参考水平,而不损害止血。组织学研究显示,amnq1治疗未引起器官的不良变化。体内实验结果表明,amnq1具有低毒性。综上所述,amnq1是安全的,在未来的研究中有可能作为抗hsv -1的药物。
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Acute toxicity evaluation of aminomethylnaphthoquinone (AMNQ 1) in BALB/c mice
We report the first preclinical tests showing that aminomethylnaphthoquinone - 3-[N-(n-butyl) amino-2,4-diclorobenzyl]-2-hydroxy-1,4-naphthoquinone (AMNQ 1) has low cytotoxicity and anti-HSV-1 activity in vitro in Vero cells. The aim of this study was to evaluate the acute toxicity of AMNQ 1 in BALB/c mice. We used BALB/c female mice to evaluate the median lethal dose (LD50) of AMNQ 1 with 2000 mg/kg body weight and other three concentrations using 550, 175 and 55 mg/kg. We compared this to acyclovir (ACV-50 mg/kg) and 10% dimethyl sulfoxide (10% DMSO) over a 14-day period. The BALB/c mice received a single oral dose by gavage. There were no deaths in either group and no change in the murine clinical signs. The hematological and biochemical analyses showed some changes that returned to reference levels without impairment of hemostasis. The AMNQ 1 treatment did not induce untoward changes in organs as shown by histological studies. The in vivo results showed that AMNQ 1 has low toxicity. In conclusion, AMNQ 1 is safe and can be potentially used as an anti-HSV-1 agent in future studies.
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