Abstract
Pinostrobin is a natural flavonoid found in various plants, well known for its wide range of pharmacological activities. However, there are few reports regarding the pharmacokinetics, tissue distribution, metabolism, and excretion of pinostrobin in rats after oral administration as a single compound. Therefore, we established a method using ultra-high-performance liquid chromatography coupled with linear trap quadrupole orbitrap mass spectrometry (UPLC-LTQ orbitrap-MS/MS) to determine pinostrobin and its metabolites in rat plasma, urine, feces, bile, and tissue homogenates. Pharmacokinetic parameters were measured. The large apparent volume of distribution implied that pinostrobin preferentially bound to tissues and preferably remained within the body. Based on previous pharmacological studies of its antiulcer, anti-HP, anti-inflammatory, and antioxidant activities, pinostrobin is mostly distributed in the gastrointestinal tract, indicating its potential as an effective component of traditional Chinese medicines for the treatment of peptic ulcers. Furthermore, 30 flavonoid metabolites were screened using UPLC-LTQ orbitrap-MS/MS. The metabolism pathways (mainly hydroxylation, demethylation, glucuronidation, and sulfation) of pinostrobin in rats have also been proposed. A small amount of pinostrobin in its parent form is excreted through the urine, feces, and bile, indicating that it is mainly metabolized in vivo. In this study, we systemically investigated the pharmacokinetics, tissue distribution, metabolism, and excretion of pinostrobin in rats. Our results provide a significant basis for the clinical development and application of pinostrobin as well as traditional Chinese medicines containing pinostrobin.
Highlights
Peptic ulcers are a common disease encountered in the clinic
Intra- and interday precisions for lower limit of quantification (LLOQ) were less than 20%, while those for low, middle, and high quality control (QC) were within 15%
Intra- and interday accuracies for LLOQ were within −13.0% to 15.3%, while those for low, middle, and high QC were within −13.2% to 10.4%
Summary
Peptic ulcers are a common disease encountered in the clinic. Epidemiology estimated the morbidity rate of peptic ulcer and its related disorders to be as high as 10%, especially in the past 10 years, and its incidence continues to increase (Lanas and Chan, 2017; Kuna et al, 2019). Pinostrobin content has been found to control the quality of Linderae Reflexae Radix. It is found more abundantly in roots than other secondary metabolites, such as pinocembrin and pinosylvin (Wang et al, 2016). Pinostrobin has a significant, dose-dependent protective effect on ethanolinduced gastric mucosal injury by scavenging free radicals produced by ethanol through the activation of cellular antioxidant defenses (Abdelwahab et al, 2011). It exhibits nontoxic and nongenotoxic effects (Charoensin et al, 2010). To the best of our knowledge, the pharmacokinetic processes of pinostrobin have not yet been explained clearly
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