Bioaccessibility, Intestinal Permeability and Plasma Stability of Isorhamnetin Glycosides from Opuntia ficus-indica (L.)

• Published in: International journal of molecular sciences 2017-08, Vol.18 (8), p.1816
• Main Authors: Antunes-Ricardo, Marilena, Rodríguez-Rodríguez, César, Gutiérrez-Uribe, Janet A, Cepeda-Cañedo, Eduardo, Serna-Saldívar, Sergio O
• Format: Article
• Language: English
• Subjects: Animals; bioaccessibility; Bioavailability; Biological Availability; Biological effects; Cactus; Chromatography, High Pressure Liquid; Circulatory system; Digestion; Flavonoids; Glycosides; Glycosides - chemistry; Glycosides - pharmacokinetics; Glycosylation; Humans; Intestinal Mucosa - metabolism; Intestine; Intravenous administration; isorhamnetin; Molecular Structure; Opuntia - chemistry; Opuntia ficus-indica; Permeability; Plant Extracts - chemistry; Plant Extracts - pharmacokinetics; Plasma; Quercetin - analogs & derivatives; Quercetin - chemistry; Quercetin - pharmacokinetics; Rats; Reproducibility of Results; Stability analysis
• ISSN: 1422-0067; 1661-6596; 1422-0067
• DOI: 10.3390/ijms18081816

Isorhamnetin glycosides are representative compounds of that possess different biological activities. There is slight information about the changes in bioaccessibility induced by the glycosylation pattern of flavonoids, particularly for isorhamnetin. In this study, the bioaccessibility and permeability of isorhamnetin glycosides extracted from were contrasted with an isorhamnetin standard. Also, the plasma stability of these isorhamnetin glycosides after intravenous administration in rats was evaluated. Recoveries of isorhamnetin after oral and gastric digestion were lower than that observed for its glycosides. After intestinal digestion, isorhamnetin glycosides recoveries were reduced to less than 81.0%. The apparent permeability coefficient from apical (AP) to basolateral (BL) direction (Papp ) of isorhamnetin was 2.6 to 4.6-fold higher than those obtained for its glycosides. Isorhamnetin diglycosides showed higher Papp values than triglycosides. Sugar substituents affected the Papp of the triglycosides. Isorhamnetin glycosides were better retained in the circulatory system than the aglycone. After intravenous dose of the isorhamnetin standard, the elimination half-life was 0.64 h but increased to 1.08 h when the extract was administered. These results suggest that isorhamnetin glycosides naturally found in could be a controlled delivery system to maintain a constant plasmatic concentration of this important flavonoid to exert its biological effects in vivo.