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In vivo metabolism of Talosin A, new isoflavonol glycoside from Kitasatospora kifunensis, in rats.

Lim JH, Song IB, Hwang YH, Kim MS, Kim JW, Kim JY, Suh JW, Yun HI - J. Vet. Sci. (2011)

Bottom Line: GT-Tal was further metabolized to its aglycone, free GT and conjugated GT.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.

View Article: PubMed Central - PubMed

Affiliation: B&C Biopharm, Advanced Institutes of Convergence Technology, Suwon 443-270, 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 C(max) 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 converted 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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Mean plasma concentration-time curves of GT-7-α-L-6-deoxy talopyranose (GT-Tal) and GT after an oral administration of 20 mg/kg GT-Tal in rats (n = 4). Filled circles (●): plasma conjugated GT-Tal, empty circles (○): plasma conjugated GT, filled triangles (▼): free plasma GT. Free GT-Tal was not detected in rat plasma samples after oral administration of GT-Tal. Data are expressed as mean ± SD.
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Figure 2: Mean plasma concentration-time curves of GT-7-α-L-6-deoxy talopyranose (GT-Tal) and GT after an oral administration of 20 mg/kg GT-Tal in rats (n = 4). Filled circles (●): plasma conjugated GT-Tal, empty circles (○): plasma conjugated GT, filled triangles (▼): free plasma GT. Free GT-Tal was not detected in rat plasma samples after oral administration of GT-Tal. Data are expressed as mean ± SD.

Mentions: The plasma concentration-time profiles of total GT-Glu and GT-Tal after oral administration of GT-Glu and GT-Tal are shown in Figs. 1 and 2. The pharmacokinetic parameters for GT-Glu and GT-Tal are summarized in Tables 1 and 2. Free GT-Glu or GT-Tal could not be detected prior to enzymatic hydrolysis of the conjugates after oral administration. GT-Glu was slowly absorbed compared to GT-Tal after being converted into its aglycone and conjugate metabolites (Free-GT, Cmax of 0.24 ± 0.08 µg/mL at 1.25 ± 0.05 h; Conjugated-GT, Cmax of 1.31 ± 0.45 µg/mL at 2.00 ± 0.00 h; Table 1). GT-Tal was rapidly absorbed through the gastrointestinal tract and metabolized into conjugates of GT-Tal with a Cmax of 2.74 ± 0.93 µg/mL at 0.25 ± 0.00 h (Table 2). It was further metabolized into its aglycone, Free-GT, with a Cmax of 0.24 ± 0.01 µg/mL at 1.00 ± 0.00 h and Conjugated-GT with a Cmax of 0.41 ± 0.25 µg/mL at 0.69 ± 0.38 h (Table 2).


In vivo metabolism of Talosin A, new isoflavonol glycoside from Kitasatospora kifunensis, in rats.

Lim JH, Song IB, Hwang YH, Kim MS, Kim JW, Kim JY, Suh JW, Yun HI - J. Vet. Sci. (2011)

Mean plasma concentration-time curves of GT-7-α-L-6-deoxy talopyranose (GT-Tal) and GT after an oral administration of 20 mg/kg GT-Tal in rats (n = 4). Filled circles (●): plasma conjugated GT-Tal, empty circles (○): plasma conjugated GT, filled triangles (▼): free plasma GT. Free GT-Tal was not detected in rat plasma samples after oral administration of GT-Tal. Data are expressed as mean ± SD.
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Related In: Results  -  Collection

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Figure 2: Mean plasma concentration-time curves of GT-7-α-L-6-deoxy talopyranose (GT-Tal) and GT after an oral administration of 20 mg/kg GT-Tal in rats (n = 4). Filled circles (●): plasma conjugated GT-Tal, empty circles (○): plasma conjugated GT, filled triangles (▼): free plasma GT. Free GT-Tal was not detected in rat plasma samples after oral administration of GT-Tal. Data are expressed as mean ± SD.
Mentions: The plasma concentration-time profiles of total GT-Glu and GT-Tal after oral administration of GT-Glu and GT-Tal are shown in Figs. 1 and 2. The pharmacokinetic parameters for GT-Glu and GT-Tal are summarized in Tables 1 and 2. Free GT-Glu or GT-Tal could not be detected prior to enzymatic hydrolysis of the conjugates after oral administration. GT-Glu was slowly absorbed compared to GT-Tal after being converted into its aglycone and conjugate metabolites (Free-GT, Cmax of 0.24 ± 0.08 µg/mL at 1.25 ± 0.05 h; Conjugated-GT, Cmax of 1.31 ± 0.45 µg/mL at 2.00 ± 0.00 h; Table 1). GT-Tal was rapidly absorbed through the gastrointestinal tract and metabolized into conjugates of GT-Tal with a Cmax of 2.74 ± 0.93 µg/mL at 0.25 ± 0.00 h (Table 2). It was further metabolized into its aglycone, Free-GT, with a Cmax of 0.24 ± 0.01 µg/mL at 1.00 ± 0.00 h and Conjugated-GT with a Cmax of 0.41 ± 0.25 µg/mL at 0.69 ± 0.38 h (Table 2).

Bottom Line: GT-Tal was further metabolized to its aglycone, free GT and conjugated GT.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.

View Article: PubMed Central - PubMed

Affiliation: B&C Biopharm, Advanced Institutes of Convergence Technology, Suwon 443-270, 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 C(max) 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 converted 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.

Show MeSH
Related in: MedlinePlus