A novel bioanalytical method based on UHPLC‐HRMS/MS for the quantification of oleuropein in human serum. Application to a pharmacokinetic study

Abstract

A highly sensitive, rapid and specific ultrahigh-performance liquid chromatography, coupled to negative electrospray ionization high-resolution tandem mass spectrometry, method was developed and validated in order to investigate the absorption of dietary oleuropein (OE) in human subjects. Serum samples were collected at predefined time points, after oral administration of an olive leaf extract enriched in OE (204.4 mg OE per capsule) to two subjects. Subsequently, samples were analyzed by the developed method after a simple solid-phase extraction step. Chromatographic separation was operated with aqueous formic acid, 0.1% (v/v), and acetonitrile following a gradient program at a flow rate of 0.45 mL/min in an RP-C (50 × 2.1 mm, 1.9 μm) column with a total run time of 2.7 min. The method was validated and successfully applied to the determination of OE in human serum, with the pharmacokinetic analysis of the data revealing a biphasic response.

Oleuropein, a Bioactive Compound from Olea europaea L., as a Potential Preventive and Therapeutic Agent in Non-Communicable Diseases

“…However, the data on the metabolism of oleuropein from EVOO or olive leaves in humans are poor, and often the results on the level and the form found in plasma, and/or excreted in urine, are conflicting [173][174][175]. This discrepancy may be explained by the fact that oleuropein bioavailability is influenced by several factors, such as the route of administration, genotype, age, sex, interaction with food, and by the different extraction processes and analytical methods used [176]. A recent human trial showed that oral Ole ingestion is resistant to the acidic conditions of the stomach, and it is rapidly absorbed (55-60%) in the intestinal tract, reaching a maximum plasma concentration (23-30 min, depending on the preparation, liquid vs. capsule) earlier than conjugated metabolites of HT, glucuronidated and sulfated (at 64-93 min), that made up 96-99% of the Ole phenolic metabolites detected in plasma and urine after intake [177].…”

Soft-MS and Computational Mapping of Oleuropein

“…Enhancement of bioactives in olive oil and table olives is a growing area of interest in nutrigenomics with requiring doses of antioxidants like hydroxytyrosol and tyrosol [23,24,25]. Therefore, oleuropein has been thoroughly evaluated and quantified as precursor of its hydrolytic bioactives [26,27,28]. Biomolecular approaches exploiting complex hyphenated high performance liquid chromatography electron spray ionization mass spectrometry (HPLC-ESI-MS) were used for these natural bioactive assessments [29].…”

Pencil graphite electrodes for improved electrochemical detection of oleuropein by the combination of Natural Deep Eutectic Solvents and graphene oxide

“…The developed methodology has demonstrated to be better in terms of cost, simplicity and sample throughput compared with traditional methodologies for determination of OLE like HPLC and comparable in terms of sensitivity and robustness. Finally, Table lists the main analytical features obtained in the selected related works found in the literature involving the electrochemical sensing of OLE .…”

“…Reliable, sensitive and robust methodologies for the rapid determination of OLE in olive leaves, olive oil industry by‐products, functional foods and pharmaceuticals are needed. OLE has been determined by classical approaches, including liquid chromatography and electrochemical techniques .…”