Rifai N, Chao F F, Pham Q, Thiessen J, Soldin S J
Department of Laboratory Medicine, Children's Hospital, Boston, MA, USA.
Clin Biochem. 1996 Apr;29(2):149-55. doi: 10.1016/0009-9120(96)00001-x.
We wish to examine the role of lipoproteins in the transport and cellular uptake of cyclosporine (CsA) and tacrolimus.
The distribution of tritiated CsA and tacrolimus among lipoproteins was determined in normo- and hypertriglyceridemic sera. The uptake of these two drugs into HepG2 and JURKAT cell lines was assessed in the presence of various concentrations of low density lipoproteins. (LDL).
Our data showed that about 60% of these drugs were transported by high density lipoprotein in normolipidemic sera, while about 50-60% were carried by very low density lipoprotein in hypertriglyceridemic sera. Almost 80% of CsA and 70% of tacrolimus entered HepG2 and JURKAT cells within the first hour of incubation in lipoprotein free media. However, the uptake was decreased (CsA by 60% and tacrolimus by 40%) in the presence of LDL.
Lipoproteins play a major role in the transport of CsA and tacrolimus, but not in their cellular uptake.
我们希望研究脂蛋白在环孢素（CsA）和他克莫司的转运及细胞摄取中的作用。
在正常血脂和高甘油三酯血症血清中测定氚标记的CsA和他克莫司在脂蛋白中的分布。在存在不同浓度低密度脂蛋白（LDL）的情况下，评估这两种药物对HepG2和JURKAT细胞系的摄取情况。
我们的数据显示，在正常血脂血清中，约60%的这些药物由高密度脂蛋白转运，而在高甘油三酯血症血清中，约50 - 60%由极低密度脂蛋白携带。在无脂蛋白培养基中孵育的第一小时内，近80%的CsA和70%的他克莫司进入HepG2和JURKAT细胞。然而，在存在LDL的情况下，摄取量降低（CsA降低60%，他克莫司降低40%）。
脂蛋白在CsA和他克莫司的转运中起主要作用，但在它们的细胞摄取中不起作用。
