Determination of bergamottin in human plasma after grapefruit juice ingestion by an UPLC/MS/MS method

Bergamottin was identified as a cause of pharmacokinetic interaction with grapefruit juice intake and as a physiologically active substance involved in lipolysis. However, the quantification method on concentrations of bergamottin in systemic circulation has not been well established. The aim of this study was to develop a simple, sensitive and high-throughput determination system for bergamottin in human plasma using an ultra performance liquid chromatography (UPLC)-MS-MS method. The UPLC system equipped with a UPLC BEH C18 column (2.1 x 50 mm, 1.7 microm) and an ESI prove was appropriate for detection of bergamottin. As a result, a primary product ion (m/z = 203) from precursor ion of bergamottin (m/z = 339) was observed. Plasma from a human volunteer who consumed grapefruit juice one hour before the time of blood sampling, was measured with the UPLC/MS/MS system. The determination of plasma-bergamottin was performed with the highest sensitivity presently available. In conclusion, we succeeded high performance bergamottin-determination in human plasma after grapefruit juice ingestion. The procedure can be usefulto clarify pharmacokinetic and pharmacodynamic characteristics of bergamottin.