Fiume L, Mattioli A, Spinosa G
Cancer Drug Deliv. 1987 Spring;4(1):11-6. doi: 10.1089/cdd.1987.4.11.
9-beta-D-Arabinofuranosyladenine 5'-monophosphate (ara-AMP) coupled to lactosaminated human albumin (L-HSA), injected i.v. into rats, selectively enters the liver. The conjugate concentration in parenchymal and sinusoidal hepatic cells, isolated by collagenase perfusion, was found to be practically equal in both cell types. This indicates that the high uptake of L-HSA-ara-AMP complex by the whole liver also corresponds to a high conjugate concentration in hepatocytes where ara-AMP should be targeted in order to increase its chemotherapeutic index in chronic hepatitis B treatment.
与乳糖胺化人白蛋白(L-HSA)偶联的9-β-D-阿拉伯呋喃糖基腺嘌呤5'-单磷酸酯(ara-AMP)经静脉注射到大鼠体内后,会选择性地进入肝脏。通过胶原酶灌注分离得到的肝实质细胞和肝血窦细胞中的缀合物浓度,在两种细胞类型中实际上是相等的。这表明整个肝脏对L-HSA-ara-AMP复合物的高摄取也对应着肝细胞中高浓度的缀合物,在慢性乙型肝炎治疗中,ara-AMP应靶向肝细胞以提高其化疗指数。