The distribution of porphyrins with different tumour localising ability among human plasma proteins.
The distribution of porphyrins with different tumour localising ability among human plasma proteins.
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DOI：
10.1038/bjc.1989.38
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发表时间：
1989-02
影响因子：
8.8
通讯作者：
Brown, S B
中科院分区：
文献类型：
--
作者：
Kongshaug, M;Moan, J;Brown, S B
用超速离心法测定了几种具有不同肿瘤定位能力的卟啉在人血浆脂蛋白主要组分中的分布。一个主要的趋势是，随着染料的极性降低，与低密度脂蛋白(LDL)结合的染料的比例增加，而与HSA结合的比例减少。不对称的电荷分布，如在TPPS2a中，基于亲脂性，比预期更有利于低密度脂蛋白的结合。目前工作中测试的药物的已知肿瘤定位能力与它们对低密度脂蛋白的相对亲和力之间没有相关性。文献中报道的最好的肿瘤定位因子之一，TPPS4，几乎不能与低密度脂蛋白结合，而通常被认为是低效的肿瘤定位因子HP和PP对低密度脂蛋白有很大的亲和力。另一方面，药物的低密度脂蛋白结合能力被认为是细胞摄取的一个很好的指标。这样的指数并不一定意味着实际的摄取是通过低密度脂蛋白途径发生的。
The distribution among the main fractions of human plasma lipoproteins of a number of porphyrins with different tumour localising ability has been determined by means of ultracentrifugation. A main trend is that the fraction of the dyes that are bound to low density lipoprotein (LDL) increases, and the fraction bound to HSA decreases with decreasing polarity of the dyes. An asymmetric charge distribution, such as in TPPS2a, favours LDL-binding more than expected on the basis of lipophilicity. No correlation between the known tumour localising ability of the drugs tested in the present work and their relative affinity for LDL was found. One of the best tumour localisers reported in the literature, TPPS4, hardly binds to LDL, while Hp and Pp, which are commonly considered inefficient tumour localisers, do have a significant affinity for LDL. On the other hand, the LDL binding capacity for a drug is suggested to be a good index for cellular uptake. Such an index does not necessarily imply that the actual uptake occurs by the LDL pathway.