Search results for "cholic acid"
showing 10 items of 97 documents
Synthesis and Structure-Activity Relationships of Amino Acid Conjugates of Cholanic Acid as Antagonists of the EphA2 Receptor
2013
The Eph–ephrin system plays a critical role in tumor growth and vascular functions during carcinogenesis. We had previously identified cholanic acid as a competitive and reversible EphA2 antagonist able to disrupt EphA2-ephrinA1 interaction and to inhibit EphA2 activation in prostate cancer cells. Herein, we report the synthesis and biological evaluation of a set of cholanic acid derivatives obtained by conjugation of its carboxyl group with a panel of naturally occurring amino acids with the aim to improve EphA2 receptor inhibition. Structure-activity relationships indicate that conjugation of cholanic acid with linear amino acids of small size leads to effective EphA2 antagonists whereas …
13C NMR spectral assignments of 3α,3′α-bis(arylcarboxy)-5β-cholan-24-oic acid ethane-1,2-diol diesters: new lithocholic acid-based molecular clefts
1999
3α,3′α-Bis(arylcarboxy)-5β-cholan-24-oic acid ethane-1,2-diol diesters (1–3) were synthesized by the reaction of an aroyl chloride (aroyl=2,6-dichlorobenzoyl, 2-naphthoyl and 1-pyrenoyl) with lithocholic acid (3α-hydroxy-5β-cholan-24-oic acid) ethane-1,2-diol diester. The 13C NMR chemical shift assignments of the formed molecular clefts 1–3, pyrene-1-carboxylic acid methyl ester (4) (used as model compound) and 1-pyrenoyl chloride (5) are based on literature data and 13C DEPT-135, 1H,13C HMQC and 1H,13C HMBC experiments. The molecular weights of 1–3 were determined by matrix-assisted laser desorption/ionization time-of-flight mass spectrometry. Copyright © 1999 John Wiley & Sons, Ltd.
Modelling phase transition kinetics of chenodeoxycholic acid with the Runge–Kutta method
2009
Abstract The phase transition kinetics of two chenodeoxycholic acid polymorphic modifications— form I (stable at high temperature), form III (stable at low temperature) and the amorphous phase has been examined under various conditions of temperature and relative humidity. Form III conversion to form I was examined at high temperature conditions and was found to be non-spontaneous, requiring seed crystals for initiation. The formation kinetic model of form I was created incorporating the three-dimensional seed crystal growth, the phase transition rate proportion to the surface area of form I crystals, and the influence of the amorphous phase surface area changes with an empirical stage poin…
Evaluation of Safe and Effectiveness of an Injectable Solution Acid Deoxycholic Based for Reduction of Localized Adiposities
2018
Background:. The use of deoxycholic acid to reduce localized fat deposits is a procedure that has been in use for about 30 years. Its effectiveness as treatment is due to emulsification of phospholipids and therefore, solubilization of the biological membranes with resulting fat necrosis. The purpose of the study was to assess the effectiveness and the safety of an injectable solution containing sodium deoxycholtate 1.25% (DB125), used as intralipotherapy. Methods:. The effectiveness and safety of DB125 solution have been assessed with a multicentre observational prospective study carried out between February and October 2017. The 221 selected patients presented with various forms and degre…
Predictors of serious adverse events and non-response in cirrhotic patients with primary biliary cholangitis treated with obeticholic acid
2022
Background & Aims Obeticholic acid (OCA) has recently been restricted in patients with primary biliary cholangitis (PBC) with "advanced cirrhosis" because of its narrow therapeutic index. We aimed to better define the predicting factors of hepatic serious adverse events (SAEs) and non-response in cirrhotic patients undergoing OCA therapy. Methods Safety and efficacy of treatment were evaluated in a cohort of consecutive PBC cirrhotic patients started with OCA. OCA response was evaluated according to the Poise criteria. Risk factors for hepatic SAEs and non-response were reported as risk ratios (RR) with 95% confidence intervals (CIs). Results One hundred PBC cirrhotics were included, 97…
Ursodeoxycholic acid protects against secondary biliary cirrhosis in rats by preventing mitochondrial oxidative stress
2004
Ursodeoxycholic acid (UDCA) improves clinical and biochemical indices in primary biliary cirrhosis and prolongs survival free of liver transplantation. Recently, it was suggested that the cytoprotective mechanisms of UDCA may be mediated by protection against oxidative stress, which is involved in the development of cirrhosis induced by chronic cholestasis. The aims of the current study were 1) to identify the mechanisms involved in glutathione depletion, oxidative stress, and mitochondrial impairment during biliary cirrhosis induced by chronic cholestasis in rats; and 2) to determine the mechanisms associated with the protective effects of UDCA against secondary biliary cirrhosis. The find…
AISF position paper on liver disease and pregnancy.
2016
Abstract The relationship between liver disease and pregnancy is of great clinical impact. Severe liver disease in pregnancy is rare; however, pregnancy-related liver disease is the most frequent cause of liver dysfunction during pregnancy and represents a severe threat to foetal and maternal survival. A rapid differential diagnosis between liver disease related or unrelated to pregnancy is required in women who present with liver dysfunction during pregnancy. This report summarizes the recommendation of an expert panel established by the Italian Association for the Study of the Liver (AISF) on the management of liver disease during pregnancy. The article provides an overview of liver disea…
Tauroursodeoxycholic acid in the treatment of patients with amyotrophic lateral sclerosis
2015
Background and purpose: Tauroursodeoxycholic acid (TUDCA) is a hydrophilic bile acid that is produced in the liver and used for treatment of chronic cholestatic liver diseases. Experimental studies suggest that TUDCA may have cytoprotective and anti-apoptotic action, with potential neuroprotective activity. A proof of principle approach was adopted to provide preliminary data regarding the efficacy and tolerability of TUDCA in a series of patients with amyotrophic lateral sclerosis (ALS). Methods: As a proof of principle, using a double-blind placebo controlled design, 34 ALS patients under treatment with riluzole who were randomized to placebo or TUDCA (1 g twice daily for 54 weeks) were e…
Primary biliary cirrhosis and hereditary hemorrhagic telangiectasia: When two rare diseases coexist
2013
Primary biliary cirrhosis is a slowly progressive cholestatic autoimmune liver disease that mainly affects middle- aged women with an estimated prevalence ranging from 6.7 to 402 cases per million. Hereditary hemorrhagic telangiectasia, or Rendu-Osler-Weber disease, is an autosomal dominant disorder characterized by angiodysplastic lesions (telangiectases and arteriovenous malformations) that can affect many organs, including liver, with a prevalence of 1-2 cases per 10000. We describe the coexistence, for the first time to our knowledge, of these two rare diseases in a 50-year old Caucasian woman. In this setting, the relevance of an accurate medical history, the role of liver histology an…
Sterols and Steroids
1994
Sterols and steroids, like the terpenes and carotinoids, are isoprene derivatives. The sterols are components of the membranes of all eukaryotic cells and they bind and condense the phospholipid bilayer. The outer cell membrane is particularly rich in sterols, with a molar ratio of sterols to phospholipids of 0.8–0.1, compared with the usual value of 0.1–0.3 for intracellular membranes. The parent substance of all sterols is cholesterol (Fig. 16.1). The sterols are classified with the steroid hormones and bile salts as steroids because they also have the gonan (formerly steran) four-ring system and have their biosynthetic origin in cholesterol. Steroids with hormonal functions are known fro…