The aim of this study was to estimate in vivo permeability and bioavailability of epalrestat and newly synthesized compounds with possible therapeutic activity as aldose enzyme inhibitors (ARIs). For this purpose permeability in vitro using rat jejunum mounted in side-by-side diffusion cells was determined. Tested substances were found to be low and moderately permeable and some of them were also substrates for efflux transporters. It was shown, that the higher efflux for some derivatives was due to MRP-2, but not Pgp involvement. Tested ARIs do not share the same efflux transporter with epalrestat, the only ARI currently on the market in Japan. The most permeable compound, a 2,6-difluoro-4-pyrrol-1ylphenol derivative, is not a substrate for efflux transporters and would therefore be the most promising lead compound for further investigation of potent ARIs.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.ejps.2006.01.006 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Duodenal-jejunal bypass ameliorates MASLD in rats by regulating gut microbiota and bile acid metabolism through FXR pathways.
Hepatol Commun
February 2025
Department of Gastroenterology, The First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, Zhejiang, China.
Background: Although bariatric and metabolic surgical methods, including duodenal-jejunal bypass (DJB), were shown to improve metabolic dysfunction-associated steatotic liver disease (MASLD) in clinical trials and experimental rodent models, their underlying mechanisms remain unclear. The present study therefore evaluated the therapeutic effects and mechanisms of action of DJB in rats with MASLD.
Methods: Rats with MASLD were randomly assigned to undergo DJB or sham surgery.
Tea Saponins: a Novel Stabilizer for Enhancing the Oral Bioavailability of Albendazole Nanocrystals.
AAPS PharmSciTech
January 2025
School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, 211198, China.
Albendazole serves as a broad-spectrum anthelmintic medication for treating hydatid cysts and neurocysticercosis. However, its therapeutic effectiveness is limited by poor solubility. Nanocrystals offer a promising technology to address this limitation by enhancing drug solubility.
View Article and Find Full Text PDFEffects of BLa80 on fecal and mucosal flora and stem cell factor/c-kit signaling pathway in simulated microgravity rats.
World J Gastroenterol
January 2025
Department of Gastroenterology, The Air Force Medical Center, Beijing 100142, China.
Background: Simulated microgravity environment can lead to gastrointestinal motility disturbance. The pathogenesis of gastrointestinal motility disorders is closely related to the stem cell factor (SCF)/c-kit signaling pathway associated with intestinal flora and Cajal stromal cells. Moreover, intestinal flora can also affect the regulation of SCF/c-kit signaling pathway, thus affecting the expression of Cajal stromal cells.
View Article and Find Full Text PDFEvaluation of the anti-spasmodic activity of essential oils of fruits and its main chemical component "perillaldehyde" on intestinal smooth muscle contractions of rodents: and approaches.
Front Chem
December 2024
Laboratory of Bioresources, Biotechnology, Ethnopharmacology and Health, Faculty of Sciences, Mohammed First University, Oujda, Morocco.
Ethnopharmacological Relevance: In Moroccan traditional medicine, plants from the Apiaceae family are widely utilized in folk medicine to treat various diseases associated with the digestive system. plays an important role as an antispasmodic that has been traditionally used, especially to treat digestive tract diseases in children.
Aim Of The Study: The aim of this research was to verify the traditional use by assessing the relaxant and spasmolytic activities of essential oil (ALEO) and then comparing them to the effects and potency of the major constituent of ALEO, which is perillaldehyde.
Effects of Magnesium Forms on the Magnesium Balance and Jejunal Transporters in Healthy Rats.
Prev Nutr Food Sci
December 2024
Department of Biology, Faculty of Science, Firat University, Elazig 23100, Türkiye.
Magnesium (Mg) is a mineral necessary for many biological activities in mammals. Here, we compared the effect of two Mg compounds [Mg picolinate (MgPic) to Mg oxide (MgO)] on Mg bioavailability and intestinal Mg and calcium transporter protein levels. Three groups of 21 male Wistar-Albino rats were randomly allocated and fed a standard diet (control) or a 500 mg/kg Mg-supplemented (MgPic or MgO) diet for 8 weeks.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!