Extensive and saturable accumulation of paclitaxel by the human platelet.
Extensive and saturable accumulation of paclitaxel by the human platelet.
复制标题
人血小板对紫杉醇的广泛且可饱和的积累。
DOI：
10.1007/bf00685730
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发表时间：
1995
影响因子：
3
通讯作者：
Walle,T
中科院分区：
文献类型：
--
作者：
Wild,MD;Walle,UK;Walle,T
关于紫杉醇在人体内的细胞分布知之甚少。在本研究中，我们研究了[3 H]-紫杉醇在人体血液中的分布。当1 μ M紫杉醇与新鲜血液在37°C下孵育时，血小板/血浆浓度比为240±17（平均值±SEM），而红细胞（RBC）/血浆浓度比仅为0.59±0.05。在使用富血小板血浆的动力学实验中，我们观察到紫杉醇的血小板蓄积具有高度的温度和浓度依赖性。Scatchard分析37°C摄取数据表明解离常数（Kapp）为0.80±0.10 μ M，最大结合容量为672±102 pmol/109个血小板。有人提出，紫杉醇的血小板蓄积反映了结合微管，并可能作为一个有用的模型结合到较难访问的细胞网站。
Little is known about the cellular distribution of paclitaxel in humans. In the present study we examined the distribution of [3H]-paclitaxel in human blood. When 1 μMpaclitaxel was incubated with fresh blood at 37°C, the platelet/plasma concentration ratio was 240±17 (mean±SEM), whereas the red blood cell (RBC)/plasma concentration ratio was only 0.59±0.05. In kinetics experiments using platelet-rich plasma, we observed that the platelet accumulation of paclitaxel was highly temperature- and concentration-dependent. Scatchard analysis of the 37°C uptake data demonstrated a dissociation constant (Kapp) of 0.80±0.10 μMand a maximal binding capacity of 672±102 pmol/109platelets. It is proposed that the platelet accumulation of paclitaxel reflects binding to microtubules and may serve as a useful model for binding to less accessible cellular sites.