Antunes-Ricardo Marilena, Rodríguez-Rodríguez César, Gutiérrez-Uribe Janet A, Cepeda-Cañedo Eduardo, Serna-Saldívar Sergio O
Tecnologico de Monterrey, Centro de Biotecnología-FEMSA, Escuela de Ingeniería y Ciencias, Av. Eugenio Garza Sada 2501 Sur, Monterrey 64849, Mexico.
Int J Mol Sci. 2017 Aug 22;18(8):1816. 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.
异鼠李素苷是具有不同生物活性的代表性化合物。关于黄酮类化合物糖基化模式诱导的生物可及性变化的信息很少,尤其是对于异鼠李素。在本研究中,将从[具体来源未给出]中提取的异鼠李素苷的生物可及性和渗透性与异鼠李素标准品进行了对比。此外,还评估了这些异鼠李素苷在大鼠静脉给药后的血浆稳定性。口服和胃消化后异鼠李素的回收率低于其糖苷的回收率。肠道消化后,异鼠李素苷的回收率降至81.0%以下。异鼠李素从顶端(AP)到基底外侧(BL)方向的表观渗透系数(Papp)比其糖苷的表观渗透系数高2.6至4.6倍。异鼠李素二糖苷的Papp值高于三糖苷。糖取代基影响三糖苷的Papp。异鼠李素苷比苷元更好地保留在循环系统中。静脉注射异鼠李素标准品后,消除半衰期为0.64小时,但给予[具体提取物未给出]提取物时增加到1.08小时。这些结果表明,[具体来源未给出]中天然存在的异鼠李素苷可能是一种控释系统,以维持这种重要黄酮类化合物的恒定血浆浓度,从而在体内发挥其生物学作用。