Determination and pharmacokinetics of engeletin in rat plasma by ultra-high performance liquid chromatography with tandem mass spectrometry

Engeletin, a bioactive flavonoid, has attracted much attention recently by virtue of its multiple biological (anti-diabetic and anti-inflammatory) activities. Despite signifying many therapeutic applications researches indicating quantification or pharmacokinetics of engeletin in biological matrix are still lacking. Here, a simple, sensitive, accurate and reliable ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) approach for the quantification of engeletin in rat plasma was developed and fully validated for the first time. Plasma samples were processed with acetonitrile by a single step protein precipitation and the separation was achieved on a ZORBAX Eclipse Plus C18 Rapid Resolution High Definition column with a gradient acetonitrile-water mobile phase. Quantification of engeletin was carried out by electrospray ionization tandem mass spectrometry in multiple reaction monitoring (MRM) mode with negative ionization. Results revealed that the approach was linearity from 5 to 5000 ng/mL (r2 = 0.9937) and proved to be precise (better than 12.3%) and accurate (−3.3%-5.2%). The developed approach was successfully employed to pharmacokinetic study of engeletin following peroral and intravenous administration to rats. The results of pharmacokinetics demonstrated rapid engeletin absorption (Tmax of 15 min) after oral administration, extensive distribution after three different dosages and an absolute bioavailability of ∼1.53%. The developed method and pharmacokinetic data can provide a meaningful basis for further studies on engeletin.