Biotransformation and Quantification of Sinensetin and Its Metabolites in Plasma, Urine, and Feces of Rats

As one of the major polymethoxyflavones in citrus peels, sinensetin (Sin) has been reported to possess numerous bioactivities. However, its detailed in vivo metabolic fate has not been uncovered yet. In the present study, the possible metabolites of Sin were synthesized, and all five mono-demethylat...

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Bibliographic Details
Published in:Journal of agricultural and food chemistry 2021-12, Vol.69 (47), p.14143-14150
Main Authors: Wang, Xiaoqi, Li, Dongli, Cao, Yong, Ho, Chi-Tang, Huang, Qingrong
Format: Article
Language:English
Subjects:
Animals
Bioactive Constituents, Metabolites, and Functions
Biotransformation
Chromatography, High Pressure Liquid
Chromatography, Liquid
Feces
Flavonoids
Rats
Tandem Mass Spectrometry
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Summary:As one of the major polymethoxyflavones in citrus peels, sinensetin (Sin) has been reported to possess numerous bioactivities. However, its detailed in vivo metabolic fate has not been uncovered yet. In the present study, the possible metabolites of Sin were synthesized, and all five mono-demethylated metabolites were successfully identified via ultraperformance liquid chromatography–tandem mass spectrometry (UPLC–MS/MS) analysis in rats fed with 100 mg/(kg·bw) Sin. The excretion and pharmacokinetic studies were then carried out to quantitatively investigate their variation in content with time in urine, feces, and plasma samples. Results showed that 4′-demethylsinensetin, 6-demethylsinensetin, and 3′-demethylsinensetin were the three most abundant metabolites generated in the above-mentioned biological samples. In addition, the total amount of Sin with its metabolites showed a significantly higher content in urine than in feces, indicating that Sin may be easily absorbed in the small intestine.
ISSN:0021-8561
1520-5118
DOI:10.1021/acs.jafc.1c05024