Identification and Quantification of Both Methylation and Demethylation Biotransformation Metabolites of 5-Demethylsinensetin in Rats.
J Agric Food Chem
; 70(10): 3162-3171, 2022 Mar 16.
Article
en En
| MEDLINE
| ID: mdl-35230106
5-Demethylated polymethoxyflavones (5-OH PMFs) are the most unique monodemethylated PMFs with relatively low polarities and are proved to possess better anticancer and anti-inflammatory effects than their respective permethoxylated ones. However, their detailed in vivo metabolic fates have not been fully studied. 5-Demethylsinensetin (5-OH Sin), being one of the 5-demethylated citrus PMFs, was used in the present research to investigate its biotransformation in pharmacokinetics and excretion in rats. The results showed that 5-OH Sin was mostly accumulated in the large intestine, indicating its poor absorption in the small intestine. In addition, 5,3'-didemethylsinensetin and 5,4'-didemethylsinensetin were identified as two dominated metabolites of 5-OH Sin, and the C-3' position of 5-OH Sin was more facile to be demethylated in systemic circulation. Moreover, other than demethylation reactions, the methylation transformation of 5-OH Sin and its metabolites were also observed and quantified, suggesting that the bidirectional biotransformation between 5-OH Sin and its parent compound, Sin, occurred under in vivo conditions.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Citrus
/
Flavonas
Tipo de estudio:
Diagnostic_studies
Límite:
Animals
Idioma:
En
Revista:
J Agric Food Chem
Año:
2022
Tipo del documento:
Article
País de afiliación:
Estados Unidos
Pais de publicación:
Estados Unidos