黄芩苷对蓖麻毒素活性的抑制作用和机制研究

来源 :中国畜牧兽医学会兽医药理毒理学分会第十一届会员代表大会暨第十三次学术讨论会与中国毒理学会兽医毒理专业委员会第五次学术研讨 | 被引量 : 0次 | 上传用户:fly_wing
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  蓖麻毒素是从植物蓖麻种子中提取的最强的植物毒素之一,属于Ⅱ型核糖体失活蛋白家族,因其强毒性被美国疾病预防控制中心定义为Ⅱ类生物威胁毒素。真核动物细胞对蓖麻毒素敏感,在极低剂量下即可导致动物和人中毒甚至死亡。蓖麻毒素由AB两个亚基组成,其中A亚基具有N-糖苷酶活性,能从4324位腺嘌呤处切断真核细胞核糖体28S rRNA,导致蛋白质翻译停止而引起细胞死亡。蓖麻毒素提取工艺简单、毒性强等特性极易被用作生物恐怖武器,威胁公众的安全。因此亟待研究以抗蓖麻毒素为代表的抗Ⅱ型核糖体失活蛋白的小分子抑制剂和中和性抗体。尽管目前已研发出多种针对蓖麻毒素的中和性抗体,但由于其局限性严重限制了抗体在临床中的应用。因此,小分子抑制剂成为目前研发的热点。目前已报道的针对活性中心和毒素细胞内转运的小分子抑制剂在动物模型中仅具有预防作用,而其对于中毒后的治疗作用尚不明确。
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