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

0532871 - BC 2021 RIV GB eng J - Journal Article
Heneberg, P. - Jegorov, Alexandr - Šimek, Petr
Peroral administration of beauverolides allows their transfer to the peripheral blood and urine.
CyTA-Journal of Food. Roč. 18, č. 1 (2020), s. 644-652. ISSN 1947-6337. E-ISSN 1947-6345
Grant - others:MZ(CZ) NV15-32432A
Institutional support: RVO:60077344
Keywords : biopesticide * gel capsule * fungal entomopathogen
OECD category: Endocrinology and metabolism (including diabetes, hormones)
Impact factor: 2.255, year: 2020
Method of publishing: Open access
https://www.tandfonline.com/doi/pdf/10.1080/19476337.2020.1809525?needAccess=true

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.
Permanent Link: http://hdl.handle.net/11104/0315250