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

J 2021

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

VESELY, O., P. MARSIK, V. JAROSOVA, I. DOSKOCIL, Karel ŠMEJKAL et. al.

Basic information

Original name

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

Authors

VESELY, O., P. MARSIK (guarantor), V. JAROSOVA, I. DOSKOCIL, Karel ŠMEJKAL (203 Czech Republic, belonging to the institution), P. KLOUCEK and J. HAVLIK

Edition

Foods, BASEL, MDPI, 2021, 2304-8158

Other information

Language

English

Type of outcome

Článek v odborném periodiku

Field of Study

30104 Pharmacology and pharmacy

Country of publisher

Switzerland

Confidentiality degree

není předmětem státního či obchodního tajemství

References:

URL

Impact factor

Impact factor: 5.561

RIV identification code

RIV/00216224:14160/21:00124273

Organization unit

Faculty of Pharmacy

DOI

http://dx.doi.org/10.3390/foods10112754

UT WoS

000723342700001

Keywords in English

moracin C; mulberrofuran G; mulberrofuran Y; permeability assay; Caco-2 cells; intestinal fermentation; LC-MS-Q-TOF

Abstract

V originále

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 (1), moracin C (2), and mulberrofuran G (3) 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 (1) and moracin C (2) were observed to be transformed into polar metabolites by conjugation. Among the test compounds, mulberrofuran Y (1) was mostly stable and accumulated in endothelial cells (85.3%) compared with mulberrofuran G (3) and moracin C (2) (14% and 8.2%, respectively). Thus, only a small amount of mulberrofuran Y (1) was conjugated. Moracin C (2) and mulberrofuran G (3) 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 (1) and moracin C (2) 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.

Links

MUNI/A/1688/2020, interní kód MU

Name: Izolace sekundárních metabolitů s potenciální biologickou aktivitou z rostlinných zdrojů (Acronym: Izolace sekundárních metabolitů)

Investor: Masaryk University

Citovat

VESELY, O., P. MARSIK, V. JAROSOVA, I. DOSKOCIL, Karel ŠMEJKAL, P. KLOUCEK and J. HAVLIK. Metabolism of Selected 2-Arylbenzofurans in a Colon In Vitro Model System. Foods. BASEL: MDPI, 2021, vol. 10, No 11, p. 1-11. ISSN 2304-8158. Available from: https://dx.doi.org/10.3390/foods10112754.

@article{1836641,
   author = {Vesely, O. and Marsik, P. and Jarosova, V. and Doskocil, I. and Šmejkal, Karel and Kloucek, P. and Havlik, J.},
   article_location = {BASEL},
   article_number = {11},
   doi = {http://dx.doi.org/10.3390/foods10112754},
   keywords = {moracin C; mulberrofuran G; mulberrofuran Y; permeability assay; Caco-2 cells; intestinal fermentation; LC-MS-Q-TOF},
   language = {eng},
   issn = {2304-8158},
   journal = {Foods},
   title = {Metabolism of Selected 2-Arylbenzofurans in a Colon In Vitro Model System},
   url = {https://www.mdpi.com/2304-8158/10/11/2754},
   volume = {10},
   year = {2021}
}

TY  - JOUR
ID  - 1836641
AU  - Vesely, O. - Marsik, P. - Jarosova, V. - Doskocil, I. - Šmejkal, Karel - Kloucek, P. - Havlik, J.
PY  - 2021
TI  - Metabolism of Selected 2-Arylbenzofurans in a Colon In Vitro Model System
JF  - Foods
VL  - 10
IS  - 11
SP  - 1-11
EP  - 1-11
PB  - MDPI
SN  - 23048158
KW  - moracin C
KW  - mulberrofuran G
KW  - mulberrofuran Y
KW  - permeability assay
KW  - Caco-2 cells
KW  - intestinal fermentation
KW  - LC-MS-Q-TOF
UR  - https://www.mdpi.com/2304-8158/10/11/2754
N2  - 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 (1), moracin C (2), and mulberrofuran G (3) 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 (1) and moracin C (2) were observed to be transformed into polar metabolites by conjugation. Among the test compounds, mulberrofuran Y (1) was mostly stable and accumulated in endothelial cells (85.3%) compared with mulberrofuran G (3) and moracin C (2) (14% and 8.2%, respectively). Thus, only a small amount of mulberrofuran Y (1) was conjugated. Moracin C (2) and mulberrofuran G (3) 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 (1) and moracin C (2) 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.
ER  -

VESELY, O., P. MARSIK, V. JAROSOVA, I. DOSKOCIL, Karel ŠMEJKAL, P. KLOUCEK and J. HAVLIK. Metabolism of Selected 2-Arylbenzofurans in a Colon In Vitro Model System. \textit{Foods}. BASEL: MDPI, 2021, vol.~10, No~11, p.~1-11. ISSN~2304-8158. Available from: https://dx.doi.org/10.3390/foods10112754.

Detailed Information on Publication Record