Abstract
Purpose : To study the in vivo metabolism of kurarinone, a lavandulyl flavanone which is a major constituent of Kushen and a marker compound with many biological activities, using ultra-performance liquid chromatography coupled with linear ion trap Orbitrap mass spectrometry (UPLC-LTQ-Orbitrap-MS). Methods : Six male Sprague-Dawley rats were randomly divided into two groups. First, kurarinone was suspended in 0.5 % carboxymethylcellulose sodium (CMC-Na) aqueous solution, and was given to rats (n = 3, 2 mL for each rat) orally at 50 mg/kg. A 2 mL aliquot of 0.5 % CMC-Na aqueous solution was administered to the rats in the control group. Next, urine samples were collected over 0-24 h after the oral administrations and all urine samples were pretreated by a solid phase extraction (SPE) method. Finally, all samples were analyzed by a UPLC-LTQ-Orbitrap mass spectrometry coupled with an electrospray ionization source (ESI) that was operated in the negative ionization mode. Results : A total of 11 metabolites, including the parent drug and 10 phase II metabolites in rat urine, were first detected and interpreted based on accurate mass measurement, fragment ions, and chromatographic retention times. The results were based on the assumption that kurarinone glucuronidation was the dominant metabolite that was excreted in rat urine. Conclusion : The results from this work indicate that kurarinone in vivo is typically transformed to nontoxic glucuronidation metabolites, and these findings may help to characterize the metabolic profile of kurarinone. Keywords : Kurarinone, Metabolites, Sophora flavescens Ait., Glucuronidation metabolites
Highlights
Sophora flavescens Ait (Leguminosae) is a perennial shrub that is widely distributed in Asia, Oceania, and the Pacific Islands
The MSn fragmentation pattern of kurarinone was investigated to facilitate the structural identification of the metabolites
Our results indicated that in vivo the kurarinone is typically transformed to non - toxic glucuronidation metabolites by phase II drugmetabolizing enzymes
Summary
Sophora flavescens Ait (Leguminosae) is a perennial shrub that is widely distributed in Asia, Oceania, and the Pacific Islands. Phytochemical studies of Sophora flavescens described the isolation of quinolizidine alkaloids, flavonoids and triterpenoids. The alkaloids in Sophora flavescens mainly consist of oxymatrine and matrine, which have been used clinically in China for the treatment of chronic hepatitis. Several pharmacological products, such as injection oxymatrine and capsule matrine, are extensively used for the treatment of hepatitis and cancers in China. The flavonoids, which have been termed Kushen flavonoids, usually carry one or multiple prenyl units. Several studies have demonstrated that prenyl chains are crucial for the biological activity of flavonoids [1]. The pharmacology of Kushen prenylated flavonoids has become an area of increased research because of their anti-diabetic, anti-arthritic, anti-inflammation, and anti-bacterial activities
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