In vitro studies of bioaccessibility, intestinal transportation and phases I, II and III metabolism of pentacyclic triterpenes from cultivars of Malus domestica Borkh

• Grant number: 14/17479-0
• Support Opportunities: Scholarships abroad - Research
• Start date: April 01, 2015
• End date: September 30, 2015
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Principal Investigator: Niege Araçari Jacometti Cardoso Furtado
• Grantee: Niege Araçari Jacometti Cardoso Furtado
• Host Investigator: Yvan Larondelle
• Host Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil
• Institution abroad: Universitè Catolique de Louvain (UCL), Belgium

Abstract

Pentacyclic triterpenes are widespread in the plant kingdom and they have been known for their remarkable bioactivities and health-promoting properties. Triterpenes occur largely in apple cultivars, which are among the most highly consumed fruits worldwide. Cultivars of Malus domestica Borkh possess different triterpene pattern, which could reflect in bioavailability and health-promoting properties. Only scarce information is available concerning the bioavailability of pentacyclic triterpenes in different databases and there is no complete information about the fate of these compounds that are constituents of medicinal and edible plants. Poor bioavailability reported for isolated triterpenes could be due to low gastrointestinal absorption, extensive metabolic degradation, efficient uptake by other tissues, and/or rapid excretion. The plant extract matrix could also play an important role in triterpene bioaccessibility and absorption. According to the type of transport involved, competition between triterpene constituents of an extract may also take place. The present project aims at carrying out bioaccessibility studies on isolated pentacyclic triterpenes and apple triterpene extracts from different cultivars of Malus domestica Borkh assessing the influence of the conditions of the upper gastrointestinal digestion through the use of an in vitro model developed by the group of Dr. Larondelle. The transport of the digested triterpene solutions across the human intestinal epithelium will then be studied using the Caco-2/TC-7 cell monolayer as a model in the presence and absence of transporters. In vitro assessment of phase I, II and III metabolism of pure triterpenes and extracts will be investigated using the same Caco-2/TC-7 enterocytes, as well as commercial rat and human liver microsomes. The identification of triterpenes and their metabolites will be carried out by using high performance liquid chromatography/high resolution tandem mass spectrometry (Orbitrap-LC-MS/MS). (AU)

Scientific publications

(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)

FURTADO, NIEGE A. J. C.; PIRSON, LAETITIA; EDELBERG, HELENE; MIRANDA, LISA M.; LOIRA-PASTORIZA, CRISTINA; PREAT, VERONIQUE; LARONDELLE, YVAN; ANDRE, CHRISTELLE M.. Pentacyclic Triterpene Bioavailability: An Overview of In Vitro and In Vivo Studies. Molecules, v. 22, n. 3, MAR 2017. (14/17479-0)