In vivo metabolism of Talosin A, new isoflavonol glycoside from Kitasatospora kifunensis, in rats
2011
Lim, J.H., BnC Biopharm, Advanced Institutes of Convergence Technology, Suwon, Republic of Korea | Song, I.B., Chungnam National University, Daejeon, Republic of Korea | Hwang, Y.H., Chungnam National University, Daejeon, Republic of Korea | Kim, M.S., Chungnam National University, Daejeon, Republic of Korea | Kim, J.W., BnC Biopharm, Advanced Institutes of Convergence Technology, Suwon, Republic of Korea | Kim, J.Y., Myongji University, Yongin, Republic of Korea | Suh, J.W., Myongji University, Yongin, Republic of Korea | Yun, H.I., Chungnam National University, Daejeon, Republic of Korea
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 C∧max of 2.74 ㎍/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 C∧max of 0.24 mg/mL at 1.25 h; conjugated GT with a mean C∧max 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.
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