Department of Bioengineering, Moores Cancer Center, University of California San Diego, 3855 Health Sciences Dr. # 0815, La Jolla, CA 92093-0815, USA.
J Mass Spectrom. 2013 Jul;48(7):768-73. doi: 10.1002/jms.3221.
The localized conversion of inactive doxorubicin prodrug chemotherapeutics to pharmacalogically active forms is difficult to quantify in mouse tumor models because it occurs only in small regions of tissue. The tumor tissue extraction protocol and LC-MS/MS analysis method described here were optimized to obtain a detection limit of 7.8 pg for the activated doxorubicin and 0.36 ng for the doxorubicin prodrug. This method can be useful for determining the biodistribution and activation efficiency for many different doxorubicin prodrugs. It can also be used for quantification of doxorubicin from tumor models that have poor vascularization resulting in low tissue accumulation.
由于仅在组织的小区域内发生,因此难以在小鼠肿瘤模型中定量测定无活性多柔比星前药化疗药物向药理活性形式的局部转化。本文中描述的肿瘤组织提取方案和 LC-MS/MS 分析方法经过优化,可将激活的多柔比星的检测限达到 7.8pg,多柔比星前药的检测限达到 0.36ng。该方法可用于测定许多不同多柔比星前药的生物分布和激活效率。它还可用于定量测定血管生成不良导致组织蓄积低的肿瘤模型中的多柔比星。