摘要
利用放射性核素示踪法研究抗病毒药半乳糖新糖白蛋白-无环鸟苷(NGA-ACV)的趋肝性及其机理,探讨其作为受体介导肝靶向抗病毒药的可能性。以哺乳动物肝细胞无唾液酸糖蛋白受体的特异性配体NGA为载体,通过丁二酰胺桥与抗病毒药ACV偶联,制备了肝靶向抗病毒药NGA-ACV。在用Ⅰ标记后,进行家兔和鸡显像及小鼠体内分布实验,并进行HPLC检测。结果表明:NGA-ACV有高度趋肝性和受体介导结合特性。肝摄取峰值>80%;并发现若保持一定的NGA-ACV糖密度,其药密度的高低对趋肝性无影响。因此,NGA-ACV有可能成为良好的受体介导肝靶向抗病毒药。
PURPOSE To assess livertaxis of antiviral drug galactosyl-neoglycoalbumin-(NGA)-acyclovir(ACV) and its mechanism using radioactive tracer technique. METHODS NGA was a synthetic ligand specific for asialoglyeoprotein receptor, which existed in the mammalian liver only. NGA as a carrier of hepatic targeting drugs was coupled with an antiviral drugs ACV via a butanediamide bridge to form a conjugator NGA-ACV. NGA-ACV was labelled with ^(131)I. The data of distribution in mice, animal (rabbit and chicken) and HPLC assay were obtained. RESULTS NGA-ACV had remarkable livertaxis and its uptake in liver was over 80% with the feature of receptor-mediated binding to hepatocytes in vivo. CONCLUSIONS NGA-ACV is a potential receptormediated hepatic targeting antiviral drug.
出处
《中华核医学杂志》
CAS
CSCD
北大核心
1996年第2期116-118,共3页
Chinese Journal of Nuclear Medicine
基金
国家自然科学基金
国家卫生部科研基金
