Abstract
Kuraridin is an active natural prenylated flavonoid ingredient originating from the well-known traditional Chinese medicine Sophora flavescens Ait., that possesses various bioactivities, such as antitumor activity, PLCγ1 inhibitory activity, glycosidase inhibitory activity, etc. However, there is no report on the plasma metabolic profile and pharmacokinetic study of kuraridin. The current study was designed to use an ultra-performance liquid chromatography/tandem mass spectrometry (UHPLC-MS/MS) method for the quantification and characterization metabolites in rat plasma after oral administration of kuraridin. A liquid-liquid extraction method with ethyl acetate-acetonitrile (1:3) was used to extract the kuraridin from rat plasma samples. The chromatographic separation was carried out on a Hypersil GOLD UHPLC C18 column equipped with a C18 guard cartridge using a gradient elution with organic solvent-water as mobile phase. Based on comparing the retention times with reference standards or on the basis of MS2 fragmentation behaviors, a total of 19 metabolites were identified or tentatively characterized from rat plasma. Under the optimized conditions, the method showed good linearity (r2 > 0.99) over the ranges of 1–500 ng/mL for kuraridin. The inter- and intra-day precisions were less than 8.95%, and the accuracy was in the range of −6.27–6.48%. The recovery of kuraridin ranged from 90.1% to 100.4%. The developed UHPLC-MS/MS method was thus successfully applied in the qualitative of metabolites and quantitative analysis of kuraridin in rat plasma.
Highlights
For thousands of years, the dried roots of Sophora flavescens Ait. (S. flavescens), named ‘Kushen’, have been traditionally used in East Asian countries as an herbal medicine for the treatment of eczema, fever, hepatitis, gastrointestinal hemorrhage and skin diseases [1]
Systematic there is no report on the plasma metabolic profileisand pharmacokinetic of kuraridin
The electro-spray ionization (ESI) sources bothresult positive and negative ionizationand were for getting a better response for kuraridin and IS,inthe indicated that kuraridin
Summary
The dried roots of Sophora flavescens Ait. (S. flavescens), named ‘Kushen’, have been traditionally used in East Asian countries as an herbal medicine for the treatment of eczema, fever, hepatitis, gastrointestinal hemorrhage and skin diseases [1]. Previous study have revealed that prenylated flavonoids from S. flavescens exhibit a variety of bioactivities. Kuraridin displays a variety of biological activities, such as antitumor activity [3,4], PLCγ 1 inhibitory activity [5], glycosidase inhibitory activity [6], SGLT inhibitory activity [7], tyrosinase inhibitory activity [8], antibacterial actions [9] and anti-reovirus activity [10], but as far as we know, Molecules 2018, 23, 132; doi:10.3390/molecules23020132 www.mdpi.com/journal/molecules. Molecules 2018, 23, 132 inhibitory activity [8], antibacterial actions [9] and anti-reovirus activity [10], but as far as we know, there is no report on the plasma metabolic profile and pharmacokinetic study of kuraridin. Systematic investigation of drug metabolism and clearance a critical part of drug study development
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