Quantitative determination of euphol in rat plasma by LC‐MS/MS and its application to a pharmacokinetic study

Abstract

Euphol is a potential pharmacologically active ingredient isolated from Euphorbia kansui. A simple, rapid, and sensitive method to determine euphol in rat plasma was developed based on liquid chromatography-tandem mass spectrometry (LC-MS/MS) for the first time. The analyte and internal standard (IS), oleanic acid, were extracted from plasma with methanol and chromatographied on a C18 short column eluted with a mobile phase of methanol–water–formic acid (95:5:0.1, v/v/v). Detection was performed by positive ion atmospheric pressure chemical ionization in selective reaction monitoring mode. This method monitored the transitions m/z 409.0 →109.2 and m/z 439.4 → 203.2 for euphol and IS, respectively. The assay was linear over the concentration range 27–9000 ng/mL, with a limit of quantitation of 27 ng/mL. The accuracy was between –7.04 and 4.11%, and the precision was <10.83%. This LC-MS/MS method was successfully applied to investigate the pharmacokinetic study of euphol in rats after intravenous (6 mg/kg) and oral (48 mg/kg) administration. Results showed that the absolute bioavailability of euphol was approximately 46.01%.

Pharmacokinetics, excretion and metabolites analysis of DL0410, a dual‑acting cholinesterase inhibitor and histamine‑3 receptor antagonist

“…The RE determined from all of the stability tests were within ±6.92% of each other (Table III). The results demonstrated that the accuracy, precision, recovery and stability tests met the criteria for quantitative determination in biological samples (28).…”

Terpenoids, Cannabimimetic Ligands, beyond the Cannabis Plant

“…Regarding the latest cited Euphorbia tirucalli, it is a common plant found in Brazil and by far the most studied species from the Euphorbia family in concern to its major compound: euphol. Studies on euphol chemical structure using x-ray crystallographic, Fourier transform-ion cyclotron resonance mass spectrometry, tandem mass spectrometry, and gas chromatography coupled mass spectrometry, as well as its quantitative determination in the rat plasma by liquid chromatography-tandem mass spectrometry allowed a better understanding of this compound chemical and biological behavior [222][223][224]. Importantly, ethnopharmacology evidences have lead and contributed to studies on the anticancer and anti-inflammatory effects of this triterpene compound, as by many years the plants from this family have been used as folk phytomedicine to treat tumors and inflammation states [221].…”