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.

Základní údaje

Originální název

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

Autoři

VESELY, O., P. MARSIK (garant), V. JAROSOVA, I. DOSKOCIL, Karel ŠMEJKAL (203 Česká republika, domácí), P. KLOUCEK a J. HAVLIK

Vydání

Foods, BASEL, MDPI, 2021, 2304-8158

Další údaje

Jazyk

angličtina

Typ výsledku

Článek v odborném periodiku

Obor

30104 Pharmacology and pharmacy

Stát vydavatele

Švýcarsko

Utajení

není předmětem státního či obchodního tajemství

Odkazy

URL

Impakt faktor

Impact factor: 5.561

Kód RIV

RIV/00216224:14160/21:00124273

Organizační jednotka

Farmaceutická fakulta

DOI

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

UT WoS

000723342700001

Klíčová slova anglicky

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

Štítky

rivok, ÚPL

Příznaky

Mezinárodní význam, Recenzováno

Změněno: 23. 2. 2022 16:22, JUDr. Sabina Krejčiříková

Anotace

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.

Návaznosti

MUNI/A/1688/2020, interní kód MU

Název: Izolace sekundárních metabolitů s potenciální biologickou aktivitou z rostlinných zdrojů (Akronym: Izolace sekundárních metabolitů)

Investor: Masarykova univerzita, Izolace sekundárních metabolitů s potenciální biologickou aktivitou z rostlinných zdrojů

Citovat

VESELY, O., P. MARSIK, V. JAROSOVA, I. DOSKOCIL, Karel ŠMEJKAL, P. KLOUCEK a J. HAVLIK. Metabolism of Selected 2-Arylbenzofurans in a Colon In Vitro Model System. Foods. BASEL: MDPI, 2021, roč. 10, č. 11, s. 1-11. ISSN 2304-8158. Dostupné z: 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 a J. HAVLIK. Metabolism of Selected 2-Arylbenzofurans in a Colon In Vitro Model System. \textit{Foods}. BASEL: MDPI, 2021, roč.~10, č.~11, s.~1-11. ISSN~2304-8158. Dostupné z: https://dx.doi.org/10.3390/foods10112754.

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