Bile sequestration potential of an edible mineral (clinoptilolite) under simulated digestion of a high-fat meal: an in vitro investigation

2015 ◽  
Vol 6 (12) ◽  
pp. 3818-3827 ◽  
Author(s):  
Aleksandra S. Kristo ◽  
Garyfallia Tzanidaki ◽  
Andreas Lygeros ◽  
Angelos K. Sikalidis
Keyword(s):  
Molecular Docking ◽  
Bile Acids ◽  
Cholic Acid ◽  
High Fat ◽  
Simulated Digestion ◽  
Sequestration Potential ◽  
In Vitro Investigation ◽  
Fat Meal

Bile was sequestered with clinoptilolite under simulated digestion of a high-fat meal. Molecular docking modeling indicates the most electronegative parts of the bile acids (here: cholic acid) docking at an electropositive region of the clinoptilolite matrix.

Effect of intestinal resection on bile salt absorption in dogs

1965 ◽  
Vol 208 (2) ◽  
pp. 363-369 ◽  
Author(s):  
M. R. Playoust ◽  
Leon Lack ◽  
I. M. Weiner
Keyword(s):  
Bile Salt ◽  
Bile Salts ◽  
Enterohepatic Circulation ◽  
Sodium Taurocholate ◽  
Intestinal Resection ◽  
High Fat ◽  
Salt Absorption ◽  
Complete Failure ◽  
Fat Meal

The efficiency of intestinal absorption of bile salts was evaluated by studying the rate of disappearance of radioactivity from the bile of dogs after the intravenous administration of sodium taurocholate-24-C14. Bile was sampled through an indwelling tube in the gall bladder. One day after a high-fat meal normal dogs retained 48% of the radioactivity; dogs with resection of the jejunum retained 48%, whereas those with resection of the ileum retained only 3% in the bile. This is consistent with previous observations that the ileum is the site of bile salt absorption in vitro and in anesthetized animals. Animals with resection of the ileum exhibited significant steatorrhea; however, three-fourths of the ingested fat was absorbed in spite of almost complete failure to absorb bile salts. This indicates that fat and bile salts are not normally absorbed together. Elimination of enterohepatic circulation of bile salts by resection of the ileum contributes to the observed steatorrhea.

scholarly journals Synthesis, Characterization, Biological Screening, ADME and Molecular Docking Studies of 2-Phenyl Quinoline-4-Carboxamide Derivatives

2020 ◽  
Vol 32 (5) ◽  
pp. 1151-1157 ◽  
Author(s):  
P. Raghurama Shetty ◽  
G. Shivaraja ◽  
G. Krishnaswamy ◽  
K. Pruthviraj ◽  
Vivek Chandra Mohan ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Molecular Docking ◽  
Anticancer Activity ◽  
In Silico ◽  
Active Sites ◽  
Docking Studies ◽  
Spectrometric Analysis ◽  
Molecular Docking Studies ◽  
In Vitro Investigation

In this work, some 2-phenyl quinoline-4-carboxamide derivatives (5a-j) were synthesized via base catalyzed Pfitzinger reaction of isatin and acetophenone followed by C-N coupling reaction using POCl3 and assessed them for their in vitro antimicrobial and anticancer activity. The structure of newly synthesized compound were established by FT-IR, 1H & 13C NMR and Mass spectrometric analysis. The synthesized carboxamides were subjected to preliminary in vitro antibacterial activity as well as for antifungal activity. Results of antibacterial activity were compared with standard antibacterial (ciprofloxocin) and antifungal (fluconozole). Among the tested compounds, 5d, 5f and 5h exhibited promising activity with zone of inhibition ranging from 10 to 25 mm. Further, the anticancer activity determined using MTT assay against two cancer cell lines. Compounds 5b, 5d, 5f and 5h showed good anticancer activity among all the other derivatives. In order to correlate the in vitro results, in silico ADME and Molecular docking studies were carried out for (5a-j). ADME properties results showed that all the compounds obey rule of Five rule except 5a, 5e and 5g compound. Molecular docking studies of the synthesized compounds showed good binding affinity through hydrogen bond interactions with key residues on active sites as well as neighboring residues within the active site of chosen target proteins viz. antibacterial, antifungal and anticancer. Comparison of both results of in silico as well as in vitro investigation suggests that the synthesized compounds may act as potential antimicrobial as well as anticancer agents.

scholarly journals Microbiological degradation of bile acids. Ring a cleavage and 7α,12α-dehydroxylation of cholic acid by Arthrobacter simplex

1969 ◽  
Vol 115 (2) ◽  
pp. 249-256 ◽  
Author(s):  
Shohei Hayakawa ◽  
Yoshiko Kanematsu ◽  
Takashi Fujiwara
Keyword(s):  
Bile Acids ◽  
Cholic Acid ◽  
Valeric Acid ◽  
Hydroxyl Groups ◽  
Partial Synthesis ◽  
Arthrobacter Simplex ◽  
Degradative Pathway ◽  
Acid Degradation

The metabolism of cholic acid by Arthrobacter simplex was investigated. This organism effected both ring a cleavage and elimination of the hydroxyl groups at C-7 and C-12 and gave a new metabolite, (4R)-4-[4α-(2-carboxyethyl)-3aα-hexahydro-7aβ-methyl-5-oxoindan-1β-yl]valeric acid, which was isolated and identified through its partial synthesis. A degradative pathway of cholic acid into this metabolite is tentatively proposed, and the possibility that the proposed pathway could be extended to the cholic acid degradation by other microorganisms besides A. simplex is discussed. The possibility that the observed reactions in vitro could occur during the metabolism of bile acids in vivo is considered.

scholarly journals A novel mechanism for gut barrier dysfunction by dietary fat: epithelial disruption by hydrophobic bile acids

2013 ◽  
Vol 304 (3) ◽  
pp. G227-G234 ◽  
Author(s):  
Lotta K. Stenman ◽  
Reetta Holma ◽  
Ariane Eggert ◽  
Riitta Korpela
Keyword(s):  
Bile Acids ◽  
Dietary Fat ◽  
Barrier Function ◽  
High Fat Diet ◽  
High Fat ◽  
Barrier Dysfunction ◽  
Gut Barrier ◽  
Epithelial Integrity

Impairment of gut barrier is associated with a fat-rich diet, but mechanisms are unknown. We have earlier shown that dietary fat modifies fecal bile acids in mice, decreasing the proportion of ursodeoxycholic acid (UDCA) vs. deoxycholic acid (DCA). To clarify the potential role of bile acids in fat-induced barrier dysfunction, we here investigated how physiological concentrations of DCA and UDCA affect barrier function in mouse intestinal tissue. Bile acid experiments were conducted in vitro in Ussing chambers using 4- and 20-kDa FITC-labeled dextrans. Epithelial integrity and inflammation were assayed by histology and Western blot analysis for cyclooxygenase-2. LPS was studied in DCA-induced barrier dysfunction. Finally, we investigated in a 10-wk in vivo feeding trial in mice the barrier-disrupting effect of a diet containing 0.1% DCA. DCA disrupted epithelial integrity dose dependently at 1–3 mM, which correspond to physiological concentrations on a high-fat diet. Low-fat diet-related concentrations of DCA had no effect. In vivo, the DCA-containing diet increased intestinal permeability 1.5-fold compared with control ( P = 0.016). Hematoxylin-eosin staining showed a clear disruption of the epithelial barrier by 3 mM DCA in vitro. A short-term treatment by DCA did not increase cyclooxygenase-2 content in colon preparations. UDCA did not affect barrier function itself, but it ameliorated DCA-induced barrier disruption at a 0.6 mM concentration. LPS had no significant effect on barrier function at 0.5–4.5 μg/ml concentrations. We suggest a novel mechanism for barrier dysfunction on a high-fat diet involving the effect of hydrophobic luminal bile acids.

scholarly journals Influence of bile acids on the adsorption of lidocaine and verapamil in an in vitro experiment

2010 ◽  
Vol 75 (4) ◽  
pp. 433-440 ◽  
Author(s):  
Mihalj Posa ◽  
Ksenija Kuhajda
Keyword(s):  
Hydrogen Bonds ◽  
Aqueous Medium ◽  
Bile Acids ◽  
Membrane Transport ◽  
Cholic Acid ◽  
Aqueous Phase ◽  
Vitro Experiment ◽  
In Vitro Experiment

The work is concerned with the influence of the structure of bile acids (cholic, deoxycholic, chenodeoxycholic, and their keto derivatives) on the in vitro adsorption of lidocaine and verapamil from an aqueous phase to rat's intestine membrane. Transport of lidocaine from an aqueous medium to the rat's intestine membrane was significantly increased (p < 0.05) only by 7-monoketocholic acid, whereas an analogous increase in verapamil transport was produced only by cholic acid. It appeared that, of all the tested bile acids, these two acids form the most stable complexes (by hydrogen bonds) with the respective drug.

In vitro investigation of the interaction between the hepatitis C virus drug sofosbuvir and human serum albumin through 1H NMR, molecular docking, and spectroscopic analyses

2016 ◽  
Vol 40 (3) ◽  
pp. 2530-2540 ◽  
Author(s):  
Hongqin Yang ◽  
Yanmei Huang ◽  
Di Wu ◽  
Jin Yan ◽  
Jiawei He ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Hepatitis C Virus ◽  
Hepatitis C ◽  
Human Serum Albumin ◽  
Binding Mechanism ◽  
Quantitative Investigation ◽  
Qualitative And Quantitative ◽  
Spectroscopic Analyses ◽  
In Vitro Investigation

The qualitative and quantitative investigation of sofosbuvir and HSA interaction provides a convictive explanation for its binding mechanism.

In vitro investigation of domain specific interactions of phenothiazine dye with serum proteins by spectroscopic and molecular docking approaches

RSC Advances ◽  
2014 ◽  
Vol 4 (68) ◽  
pp. 36267-36281 ◽  
Author(s):  
Arumugam Selva Sharma ◽  
Shanmugam Anandakumar ◽  
Malaichamy Ilanchelian
Keyword(s):  
Molecular Docking ◽  
Human Serum Albumin ◽  
Bovine Serum Albumin ◽  
Serum Albumin ◽  
Serum Proteins ◽  
Chemotherapeutic Agent ◽  
Specific Interactions ◽  
Domain Specific ◽  
In Vitro Investigation

In the present study the interaction of the chemotherapeutic agent, Azure A (AZA) with Human Serum Albumin (HSA) and Bovine Serum Albumin (BSA) was investigated by multi spectroscopic and molecular docking methods.

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