Costunolide and dehydrocostuslactone are well-known sesquiterpene lactones contained in many plants used as popular herbs, such as Saussurea lappa and Laurus novocanariensis, and have been considered as potential candidates for the treatment of various types of tumor. In the present work, a sensitive UPLC-MS/MS for the quantification of costunolide and dehydrocostuslactone in biological matrices has been developed. The method is based on protein precipitation with acetonitrile followed by isocratic ultraperformance liquid chromatographic separation using methanol-formic acid (0.1% in water; 70:30, v/v) mobile phase. Detection was performed by ESI mass spectrometry in MRM mode with the precursor-to-product ion transitions m/z 233-187 and m/z 231-185, respectively. The calibration curves of analytes showed good linearity within the established range 0.19-760 ng/mL for costunolide and 0.23-908 ng/mL for dehydrocostuslactone. The lower limits of quantification of costunolide and dehydrocostuslactone were found to be 0.19 and 0.23 ng/mL, respectively. The intra-day and inter-day presicions of this method for the entire validation were less than coefficient of variation of 7% and the accuracy was within ±8% (relative error). The mean extraction recoveries were 73.8 and 75.3%, respectively. The method was found to be precise, accurate and specific during the study, and was successfully used to analyze the pharmacokinetics of costunolide and dehydrocostuslactone.
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