Metabolism of Selected 2-Arylbenzofurans in a Colon In Vitro Model System

2-arylbenzofurans represent a small group of bioactive compounds found in the plant family Moraceae. As it has not been investigated whether these substances are stable during passage through the gastrointestinal tract, their biological effects may be altered by the metabolism of intestinal microbio...

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Autores principales:	Ondrej Vesely, Petr Marsik, Veronika Jarosova, Ivo Doskocil, Karel Smejkal, Pavel Kloucek, Jaroslav Havlik
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	moracin C mulberrofuran G mulberrofuran Y permeability assay Caco-2 cells intestinal fermentation Chemical technology TP1-1185
Acceso en línea:	https://doaj.org/article/f4ca026d48844cb2ac1d365fba1e5b54
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spelling	oai:doaj.org-article:f4ca026d48844cb2ac1d365fba1e5b542021-11-25T17:35:16ZMetabolism of Selected 2-Arylbenzofurans in a Colon In Vitro Model System10.3390/foods101127542304-8158https://doaj.org/article/f4ca026d48844cb2ac1d365fba1e5b542021-11-01T00:00:00Zhttps://www.mdpi.com/2304-8158/10/11/2754https://doaj.org/toc/2304-81582-arylbenzofurans represent a small group of bioactive compounds found in the plant family Moraceae. As it has not been investigated whether these substances are stable during passage through the gastrointestinal tract, their biological effects may be altered by the metabolism of intestinal microbiota or cells. The aim of the present study was to investigate and compare mulberrofuran Y (<b>1</b>), moracin C (<b>2</b>), and mulberrofuran G (<b>3</b>) in an in vitro model of human intestinal bacterial fermentation and in an epithelial model using the Caco-2 cell line. The analysis of compounds by LC-MS-Q-TOF showed sufficient stability in the fermentation model, with no bacterial metabolites detected. However, great differences in the quantity of permeation were observed in the permeability assay. Moreover, mulberrofuran Y (<b>1</b>) and moracin C (<b>2</b>) were observed to be transformed into polar metabolites by conjugation. Among the test compounds, mulberrofuran Y (<b>1</b>) was mostly stable and accumulated in endothelial cells (85.3%) compared with mulberrofuran G (<b>3</b>) and moracin C (<b>2</b>) (14% and 8.2%, respectively). Thus, only a small amount of mulberrofuran Y (<b>1</b>) was conjugated. Moracin C (<b>2</b>) and mulberrofuran G (<b>3</b>) were metabolized almost completely, with only traces of the unchanged molecule being found on the apical and cellular sides of the system. Only conjugates of mulberrofuran Y (<b>1</b>) and moracin C (<b>2</b>) were able to reach the basolateral side. Our results provide the basic description of bioavailability of these three compounds, which is a necessary characteristic for final evaluation of bio-efficacy.Ondrej VeselyPetr MarsikVeronika JarosovaIvo DoskocilKarel SmejkalPavel KloucekJaroslav HavlikMDPI AGarticlemoracin Cmulberrofuran Gmulberrofuran Ypermeability assayCaco-2 cellsintestinal fermentationChemical technologyTP1-1185ENFoods, Vol 10, Iss 2754, p 2754 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	moracin C mulberrofuran G mulberrofuran Y permeability assay Caco-2 cells intestinal fermentation Chemical technology TP1-1185
spellingShingle	moracin C mulberrofuran G mulberrofuran Y permeability assay Caco-2 cells intestinal fermentation Chemical technology TP1-1185 Ondrej Vesely Petr Marsik Veronika Jarosova Ivo Doskocil Karel Smejkal Pavel Kloucek Jaroslav Havlik Metabolism of Selected 2-Arylbenzofurans in a Colon In Vitro Model System
description	2-arylbenzofurans represent a small group of bioactive compounds found in the plant family Moraceae. As it has not been investigated whether these substances are stable during passage through the gastrointestinal tract, their biological effects may be altered by the metabolism of intestinal microbiota or cells. The aim of the present study was to investigate and compare mulberrofuran Y (<b>1</b>), moracin C (<b>2</b>), and mulberrofuran G (<b>3</b>) in an in vitro model of human intestinal bacterial fermentation and in an epithelial model using the Caco-2 cell line. The analysis of compounds by LC-MS-Q-TOF showed sufficient stability in the fermentation model, with no bacterial metabolites detected. However, great differences in the quantity of permeation were observed in the permeability assay. Moreover, mulberrofuran Y (<b>1</b>) and moracin C (<b>2</b>) were observed to be transformed into polar metabolites by conjugation. Among the test compounds, mulberrofuran Y (<b>1</b>) was mostly stable and accumulated in endothelial cells (85.3%) compared with mulberrofuran G (<b>3</b>) and moracin C (<b>2</b>) (14% and 8.2%, respectively). Thus, only a small amount of mulberrofuran Y (<b>1</b>) was conjugated. Moracin C (<b>2</b>) and mulberrofuran G (<b>3</b>) were metabolized almost completely, with only traces of the unchanged molecule being found on the apical and cellular sides of the system. Only conjugates of mulberrofuran Y (<b>1</b>) and moracin C (<b>2</b>) were able to reach the basolateral side. Our results provide the basic description of bioavailability of these three compounds, which is a necessary characteristic for final evaluation of bio-efficacy.
format	article
author	Ondrej Vesely Petr Marsik Veronika Jarosova Ivo Doskocil Karel Smejkal Pavel Kloucek Jaroslav Havlik
author_facet	Ondrej Vesely Petr Marsik Veronika Jarosova Ivo Doskocil Karel Smejkal Pavel Kloucek Jaroslav Havlik
author_sort	Ondrej Vesely
title	Metabolism of Selected 2-Arylbenzofurans in a Colon In Vitro Model System
title_short	Metabolism of Selected 2-Arylbenzofurans in a Colon In Vitro Model System
title_full	Metabolism of Selected 2-Arylbenzofurans in a Colon In Vitro Model System
title_fullStr	Metabolism of Selected 2-Arylbenzofurans in a Colon In Vitro Model System
title_full_unstemmed	Metabolism of Selected 2-Arylbenzofurans in a Colon In Vitro Model System
title_sort	metabolism of selected 2-arylbenzofurans in a colon in vitro model system
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/f4ca026d48844cb2ac1d365fba1e5b54
work_keys_str_mv	AT ondrejvesely metabolismofselected2arylbenzofuransinacoloninvitromodelsystem AT petrmarsik metabolismofselected2arylbenzofuransinacoloninvitromodelsystem AT veronikajarosova metabolismofselected2arylbenzofuransinacoloninvitromodelsystem AT ivodoskocil metabolismofselected2arylbenzofuransinacoloninvitromodelsystem AT karelsmejkal metabolismofselected2arylbenzofuransinacoloninvitromodelsystem AT pavelkloucek metabolismofselected2arylbenzofuransinacoloninvitromodelsystem AT jaroslavhavlik metabolismofselected2arylbenzofuransinacoloninvitromodelsystem
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Metabolism of Selected 2-Arylbenzofurans in a Colon In Vitro Model System

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