利用热熔挤出技术制备雄黄新剂型及其对白血病K562细胞的作用研究

来源 :2013全国生物与医学纳米技术博士生学术论坛 | 被引量 : 0次 | 上传用户:pearljeejee
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  雄黄(Realgar)始载于《神农本草经》,是中医最早使用的矿物药物之一,主要成分为二硫化二砷(As2S2)。从20世纪六十年代开始,雄黄在临床上被用于治疗急性粒细胞性白血病(APL)和慢性粒细胞性白血病(CML),并取得了较好的疗效。已有的研究表明,雄黄治疗白血病作用机理是As2S2可以特异性的激活泛素连接酶E3,并最终通过E3家族中c-CBL作用将异常融合蛋白BCR-ABL或PML-RAR泛素化降解,从而抑制白血病细胞的增殖,并促进其凋亡或向正常细胞分化。但是,雄黄在临床应用中面临一个重要的挑战就是水溶性极低,导致其生物利用度难以提高。
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