Abstract
Linarin, a flavone glycoside, is considered to be a promising natural product due to its diverse pharmacological activities. Recently, it has been brought into focus for its potential to treat liver failure. In this study, a rapid and sensitive liquid chromatography electrospray-ionization tandem mass spectrometry (LC–MS/MS) method was developed and validated for the simultaneous determination of linarin and its three metabolites (acacetin, apigenin, and p-hydroxy benzaldehyde) in plasma and liver tissue samples of normal rats and rats with d-galactosamine (d-GalN)-induced liver injury. After liquid–liquid extraction (LLE) with ethyl acetate, chromatographic separation of the four analytes was achieved using an ACQUITY UPLC BEH-C18 (1.7 μm, 2.1 × 50 mm) with a mobile phase of 0.01% formic acid in methanol and 0.01% formic acid at a flow rate of 0.3 mL/min. The detection was accomplished on a tandem mass spectrometer via an electrospray ionization (ESI) source by multiple reaction monitoring (MRM) in the negative ionization mode. The method had a good linearity over the concentration range of 1.00–200 ng/mL for linarin and its metabolites. The validated method was successfully applied to the pharmacokinetic and liver tissue distribution study of linarin and its metabolites after a single oral administration of linarin (90 mg/kg) to rats.
Highlights
A recent research carried out by Kim et al [9] demonstrated the protective effect of linarin against severe hepatic failure in mice induced by d-galactosamine (d-GalN)/lipopolysaccharide (LPS), which suggested the potential of linarin in clinical applications for the treatment of liver injury
Apigenin, and p-hydroxy benzaldehyde (Figure 1) have been identified as the metabolites of linarin [12]. We found that these three metabolites showed a protective effect against severe d-GalN-induced hepatic failure in rats
88.1–107.9%, and the matrix effect of internal standard (IS) was 108.4%. These results reveal that no significant matrix effect was observed, and the liquid–liquid extraction (LLE) efficiency was acceptable in the current conditions
Summary
Linarin (acacetin-7-O-β-d-rutinoside) (Figure 1) is an active flavonoid glycoside isolated from. As the main active component of Chrysanthemum indicum L, linarin retains the main antipyretic, analgesic, and anti-inflammatory effects of Chrysanthemum indicum L [1], and exhibits a variety of pharmacological activities, such as sedative, neuroprotective, anti-apoptotic, and acetylcholinesterase and aldose reductase inhibitory activities [2,3,4,5,6,7]. The hepatoprotective effect of linarin has been investigated by increasingly more researchers [8,9,10]. Studies have shown that linarin can exert an hepatoprotective effect by inhibiting inflammatory reaction and cell apoptosis [3]. A recent research carried out by Kim et al [9] demonstrated the protective effect of linarin against severe hepatic failure in mice induced by d-galactosamine (d-GalN)/lipopolysaccharide (LPS), which suggested the potential of linarin in clinical applications for the treatment of liver injury.
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