Abstract
Isorhamnetin glycosides are representative compounds of Opuntia ficus-indica 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 O. ficus-indica 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(AP-BL)) of isorhamnetin was 2.6 to 4.6-fold higher than those obtained for its glycosides. Isorhamnetin diglycosides showed higher Papp(AP-BL) values than triglycosides. Sugar substituents affected the Papp(AP-BL) 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 O. ficus-indica extract was administered. These results suggest that isorhamnetin glycosides naturally found in O. ficus-indica could be a controlled delivery system to maintain a constant plasmatic concentration of this important flavonoid to exert its biological effects in vivo.
Highlights
The most abundant flavonoid in O. ficus-indica (L.) Mill is isorhamnetin and it is found as mono, di, and tri-glycosides [1,2,3,4,5]
The aim of this study was to compare the in vitro bioaccessibility and permeability of isorhamnetin and its glycosides extracted from O. ficus-indica after a simulated digestion using a Caco-2/HT-29 cell co-culture model
Four isorhamnetin glycosides (IGRR, IGRP, IGP, and IGR) were identified as the most abundant flavonols in the O. ficus-indica extract at 365 nm (Figure 1), as previously reported by Antunes-Ricardo et al [2] and Rodríguez-Rodríguez et al
Summary
The most abundant flavonoid in O. ficus-indica (L.) Mill is isorhamnetin and it is found as mono-, di-, and tri-glycosides [1,2,3,4,5]. Isorhamnetin and its glycosides possess effects in the adipogenesis inhibition, body weight reduction, ameliorate insulin resistance, and alleviate hepatic steatosis in diet-induced obese mice via the suppression of PPARγ activity [6,7,8,9,10,11]. These flavonoids have shown anti-inflammatory and chemopreventive activities [12,13,14,15]. Digestion allows the release of the compounds from the food matrix in the gastrointestinal lumen, making them available for absorption; this has been defined as bioaccessibility [20]
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