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In vivo metabolism of Talosin A, new isoflavonol glycoside from Kitasatospora kifunensis, in rats
Authors:Jong-Hwan Lim   In-Bae Song   Youn-Hwan Hwang   Myoung-Seok Kim   Jong-Woo Kim   Jin-Yong Kim   Joo Won Suh   Hyo-In Yun
Affiliation:1B&C Biopharm, Advanced Institutes of Convergence Technology, Suwon 443-270, Korea.;2Research Institute of Veterinary Science, Chungnam National University, Daejeon 305-764, Korea.;3Extract Collection of Useful Microorganism (ECUM), Myongji University, Yongin 449-728, Korea.
Abstract:The isoflavonol glycoside Talosin A, genistein (GT)-7-α-L-6-deoxy talopyranose (GT-Tal), was first isolated from the culture broth of Kitasatospora kifunensis MJM341. The aim of the present study was to evaluate the oral absorption and metabolism of the newly isolated isoflavonol glycoside, GT-Tal compared to genistin (GT-7-O-β-D-glucopyranoside; GT-Glu). Free GT-Glu and GT-Tal could not be detected prior to enzymatic hydrolysis of the corresponding conjugates in rat plasma. Following oral administration of GT-Tal (15 min), GT-Tal was rapidly absorbed through the gastrointestinal tract and metabolized into GT-Tal conjugates with a mean Cmax of 2.74 µg/mL. GT-Tal was further metabolized to its aglycone, free GT and conjugated GT. After oral administration, GT-Glu was absorbed after being convereted to its aglycone and then further metabolized into its conjugate metabolites (free GT with a mean Cmax of 0.24 mg/mL at 1.25 h; conjugated GT with a mean Cmax of 1.31 mg/mL at 2.00 h). Significant differences in absorption and metabolism of GT-Tal and GT-Glu were observed. GT-Tal was metabolized into its corresponding conjugates or underwent deglycosylation to form GT, whereas GT-Glu was metabolized into its aglycone, GT.
Keywords:genistin   isoflavonol   metabolism   pharmacokinetics   Talosin A
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