Peroral administration of beauverolides allows their transfer to the peripheral blood and urine

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60077344%3A_____%2F20%3A00532871" target="_blank" >RIV/60077344:_____/20:00532871 - isvavai.cz</a>

Výsledek na webu

<a href="https://www.tandfonline.com/doi/pdf/10.1080/19476337.2020.1809525?needAccess=true" target="_blank" >https://www.tandfonline.com/doi/pdf/10.1080/19476337.2020.1809525?needAccess=true</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1080/19476337.2020.1809525" target="_blank" >10.1080/19476337.2020.1809525</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Peroral administration of beauverolides allows their transfer to the peripheral blood and urine

Popis výsledku v původním jazyce

Beauverolides are hydrophobic cyclodepsipeptides that inhibit sterol O-acyltransferases and calmodulin, thereby reducing senile plaques in Alzheimer’s disease and preventing foam cell formation in atherosclerosis. Other sterol O-acyltransferase inhibitors suffer from low bioavailability, and evidence of the distribution of beauverolides in bodily fluids is lacking. We aimed to determine the optimal formulation of beauverolides for administration to experimental animals and to determine if the orally administered beauverolides could cross the gastrointestinal barrier and be secreted in urine. We found that beauverolides formed gels in aqueous solutions and we developed a formula for their peroral administration. Administration of the beauverolide gel pellets to experimental mice revealed that beauverolides cross the gastrointestinal barrier, circulate untouched in the blood, and are excreted in the urine. Using liquid chromatography-mass spectrometry analyses, we show that the administered beauverolides circulate in mouse blood and are excreted from the body 24 h after their administration.

Název v anglickém jazyce

Peroral administration of beauverolides allows their transfer to the peripheral blood and urine

Popis výsledku anglicky

Beauverolides are hydrophobic cyclodepsipeptides that inhibit sterol O-acyltransferases and calmodulin, thereby reducing senile plaques in Alzheimer’s disease and preventing foam cell formation in atherosclerosis. Other sterol O-acyltransferase inhibitors suffer from low bioavailability, and evidence of the distribution of beauverolides in bodily fluids is lacking. We aimed to determine the optimal formulation of beauverolides for administration to experimental animals and to determine if the orally administered beauverolides could cross the gastrointestinal barrier and be secreted in urine. We found that beauverolides formed gels in aqueous solutions and we developed a formula for their peroral administration. Administration of the beauverolide gel pellets to experimental mice revealed that beauverolides cross the gastrointestinal barrier, circulate untouched in the blood, and are excreted in the urine. Using liquid chromatography-mass spectrometry analyses, we show that the administered beauverolides circulate in mouse blood and are excreted from the body 24 h after their administration.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

30202 - Endocrinology and metabolism (including diabetes, hormones)

Projekt

—

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2020

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

CyTA-Journal of Food

ISSN

1947-6337

e-ISSN

—

Svazek periodika

18

Číslo periodika v rámci svazku

1

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

9

Strana od-do

644-652

Kód UT WoS článku

000575190800001

EID výsledku v databázi Scopus

2-s2.0-85091986033