Liu Huaming, Zhang Dandan, Tang Zhidan, Sun Mengjie, Azietaku John Teye, Ouyang Huizi, Chang Yanxu, Wang Meng, He Jun, Gao Xiumei
Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, China.
First Teaching Hospital of Tianjin University of Traditional Chinese Medicine, Tianjin, China.
Biomed Chromatogr. 2018 Oct;32(10):e4302. doi: 10.1002/bmc.4302. Epub 2018 Jun 26.
Periplocin is a cardiac glycoside and has been used widely in the clinic for its cardiotonic, anti-inflammatory and anti-tumor effects. Although it is taken frequently by oral administration in the clinic, there have been no reports demonstrating that periplocin could be detected in vivo after an oral administration, so there is an urgen need to determine the characteristics of periplocin in vivo after oral administration. In this study, a sensitive and reliable liquid chromatography-tandem mass spectrometry method was developed and validated to identify and quantify periplocin and its two metabolites in rat tissue after a single dosage of perplocin at 50 mg/kg. The results demonstrated that periplocin and its two metabolites were detected in all of the selected tissues; periplocin could reach peak concentration quickly after administration, while periplocymarin and periplogenin reached maximum concentration > 4.83 h after administration. The tissue distribution of analytes tended to be mostly in the liver, and higher analyte concentrations were found in the heart, liver, spleen, lung and kidney, but a small amount of chemical constituents was distributed into the brain. The consequences obtained using this method might provide a meaningful insight for clinical investigations and applications.
杠柳毒苷是一种强心苷，因其强心、抗炎和抗肿瘤作用而在临床上被广泛应用。尽管临床上常采用口服给药方式，但尚无报告表明口服后能在体内检测到杠柳毒苷，因此迫切需要确定口服后杠柳毒苷在体内的特征。在本研究中，建立并验证了一种灵敏可靠的液相色谱 - 串联质谱法，用于在大鼠单次给予50 mg/kg杠柳毒苷后，鉴定和定量大鼠组织中的杠柳毒苷及其两种代谢产物。结果表明，在所有选定组织中均检测到了杠柳毒苷及其两种代谢产物；给药后杠柳毒苷能迅速达到峰值浓度，而杠柳次苷和杠柳苷元在给药后>4.83小时达到最大浓度。分析物的组织分布倾向于主要在肝脏，在心脏、肝脏、脾脏、肺和肾脏中发现较高的分析物浓度，但少量化学成分分布到大脑中。使用该方法获得的结果可能为临床研究和应用提供有意义的见解。
