Asulacrine (ASL), an analogue of amsacrine, has shown higher anti-breast and anti-lung cancer activity. Hereby, a new sensitive and selective liquid chromatography-mass spectrometry (LC/MS) method was developed to determine intracellular asulacrine. The chromatographic separation was performed on an Agilent Zorbax Extend-C18 column (2.1 mm i.d. × 50 mm, 5 μm) using gradient elution with water (2 mmol/L ammonium acetate and 0.1% acetic acid) and acetonitrile as the mobile phase. The detection was achieved with selected ion monitoring mode using electrospray ionization in positive mode with target ions at m/z 465.3 and m/z 326.1 for asulacrine and midazolam, respectively. The standard curve showed a good linearity with the lower limit of quantification of 1 ng/mL, as a result of which, the trace concentration of ASL in cell suspension could be quantified. The intra- and inter-day accuracy ranged from -5.28 to 6.5% and from -6.32 to 1.05%, and the intra- and inter-day precisions were no more than 7.65% and 11.71%, respectively. Additionally, no degradation of asulacrine was observed during stability evaluation. The method was proved to be powerful and practical to determine and compare the intracellular distribution and kinetics of ASL under different formulations in MCF-7 breast cancer cells.

中文翻译：

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液相色谱-质谱法定量测定MCF-7乳腺癌细胞中胞内Asulacrine的含量及其在P188修饰脂质体细胞药代动力学研究中的应用。

Asamcrine的类似物Asulacrine（ASL）已显示出更高的抗乳腺癌和抗肺癌活性。因此，开发了一种新的灵敏和选择性的液相色谱-质谱（LC / MS）方法来确定细胞内芦荟碱。色谱分离是在Agilent Zorbax Extend-C18色谱柱（内径2.1 mm×50 mm，5μm）上进行的，使用水（2 mmol / L乙酸铵和0.1％乙酸）和乙腈作为流动相进行梯度洗脱。使用正离子模式电喷雾电离以选定的离子监测模式完成检测，目标离子分别为m / z 465.3和m / z 326.1，分别用于天竺葵和咪达唑仑。标准曲线显示出良好的线性，定量下限为1 ng / mL，因此，可以定量测定细胞悬浮液中ASL的痕量浓度。日内和日间精度的范围分别为-5.28至6.5％和-6.32至1.05％，日间和日间精度分别不超过7.65％和11.71％。另外，在稳定性评估过程中未观察到芥子碱的降解。实践证明，该方法对于测定和比较不同制剂在MCF-7乳腺癌细胞中ASL的细胞内分布和动力学是强大而实用的。