Mankertz J, von Baeyer H, Rokos K, Nündel M, Pauli G, Riedel E
Freie Universität Berlin, Institut für Biochemie, Germany.
Int J Clin Pharmacol Ther. 1995 Feb;33(2):85-8.
Macrophages, besides helper T-lymphocytes, are target cells for the human immunodeficiency virus (HIV). We report on a mechanism to deliver selectively antiretroviral drugs to cells of the monocyte/macrophage lineage. These cells and cells of the endothelium express scavenger receptors which mediate the transport of modified low density lipoprotein (LDL). LDL modified by covalently bound azidothymidine (AZT), a potent inhibitor of HIV replication, is internalized via this pathway into human macrophages. Treatment of HIV-1 infected human macrophages with AZT-LDL showed in vitro efficient inhibition of viral replication. In contrast, HIV replication in T-lymphocytes (Molt 4/8), which do not express scavenger receptors, is not inhibited by AZT-LDL but by free AZT.
除辅助性T淋巴细胞外，巨噬细胞也是人类免疫缺陷病毒（HIV）的靶细胞。我们报告了一种将抗逆转录病毒药物选择性递送至单核细胞/巨噬细胞谱系细胞的机制。这些细胞和内皮细胞表达清道夫受体，该受体介导修饰的低密度脂蛋白（LDL）的转运。通过共价结合齐多夫定（AZT，一种有效的HIV复制抑制剂）修饰的LDL通过该途径被内化进入人类巨噬细胞。用AZT-LDL处理HIV-1感染的人类巨噬细胞在体外显示出对病毒复制的有效抑制。相比之下，不表达清道夫受体的T淋巴细胞（Molt 4/8）中的HIV复制不受AZT-LDL抑制，而是受游离AZT抑制。
