A series of novel steroidal pyrazoles was synthesized as substrates for bile acid transporters to explore their potential as drug carriers. The selected pyrazole fused bile acids were further conjugated with drugs and drug surrogates. Their in vitro transport activities were evaluated in human ileal bile acid transporter (hIBAT) and human liver bile acid transporter (hLBAT) expressing Chinese hamster ovary (CHO)-cells and Xenopus laevis oocytes. The results of synthetic efforts and transporter assays studies are described herein.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2004.10.027 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Aerobic exercise regulates gut microbiota profiles and metabolite in the early stage of Alzheimer's disease.
FASEB J
January 2025
Department of Neurology, Sichuan Academy of Medical Sciences & Sichuan Provincial People's Hospital, University of Electronic Science and Technology of China, Chengdu, China.
Aerobic exercise (AE) has been shown to offer significant benefits for Alzheimer's disease (AD), potentially influencing the gut microbiota. However, the impact of changes in intestinal flora in early Alzheimer's disease induced by aerobic exercise on metabolic pathways and metabolites is not well understood. In this study, 3-month-old APP/PS1 and C57BL/6 mice were divided into two groups each: a control group (ADC for APP/PS1 and WTC for C57BL/6) and an aerobic exercise group (ADE for APP/PS1 and WTE for C57BL/6).
View Article and Find Full Text PDFResearch progress on the synthesis process, detection method, pharmacological effects and application of glycocholic acid.
Front Pharmacol
January 2025
College of Pharmacy, Liaoning University of Traditional Chinese Medicine, Dalian, China.
Objective: This review aims to summarize the research progress of glycocholic acid to promote its broader development and application.
Methods: This article collects relevant literature from databases such as Science Direct, PubMed, Web of Science, Google Scholar and CNKI from the establishment to 2024, systematically organizing and analyzing aspects of glycocholic acid including its physicochemical properties, synthesis and extraction techniques, detection methods, pharmacological effects, mechanisms of action, clinical research, and application as an excipient.
Results: Glycocholic acid, as a key conjugated component in bile acids, exhibits various pharmacological effects such as anti-inflammatory and antioxidant activities.
Mechanism study on the enhancement of bile acid-binding capacity in corn by-product juice via HY127 fermentation.
Food Chem X
January 2025
School of Food and Health, Jinzhou Medical University, Jinzhou 121000, China.
Hyperlipidemia is a common endocrine metabolic disease in humans. Long-term medications often have adverse effects, making the search for safer and more effective treatments crucial. This study aimed to explore the impacts and mechanisms of HY127 fermentation on enhancing bile acid-binding capacity (BABC).
View Article and Find Full Text PDFUnlabelled: infections (CDI) cause almost 300,000 hospitalizations per year of which ∼15-30% are the result of recurring infections. The prevalence and persistence of CDI in hospital settings has resulted in an extensive collection of clinical isolates and their classification, typically by ribotype. While much of the current literature focuses on one or two prominent ribotypes ( .
View Article and Find Full Text PDFUnlabelled: Thiosulfate-citrate-bile salts-sucrose (TCBS) agar is a selective and differential media for the enrichment of pathogenic . We observed that an exonuclease VII ( ) mutant of failed to grow on TCBS agar, suggesting that DNA repair mutant strains may be hampered for growth in this selective media. Examination of the selective components of TCBS revealed that bile acids were primarily responsible for toxicity of the mutant.
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!