scholarly journals Methodology for evaluating inflammation induction potential of enteral absorption enhancers: Epithelial permeability enhancement via histamine receptors.

1998 ◽  
Vol 13 (2) ◽  
pp. 107-113 ◽  
Author(s):  
Masahiro Murakami ◽  
Tomomi Uchiyama ◽  
Hiroyuki Tatsumi ◽  
Yoshikatsu Majikawa ◽  
Hidenori Obata ◽  
...  
Keyword(s):  
Histamine Receptors ◽  
Epithelial Permeability ◽  
Absorption Enhancers ◽  
Enteral Absorption ◽  
Permeability Enhancement

Histamine receptors and pulmonary epithelial permeability

1987 ◽  
Vol 81 ◽  
pp. 260-267 ◽  
Author(s):  
T.B. Chan ◽  
Noemi Eiser ◽  
Diana Shelton ◽  
P.J. Rees
Keyword(s):  
Histamine Receptors ◽  
Epithelial Permeability ◽  
Pulmonary Epithelial Permeability

Total parenteral nutrition changes intestinal ion transport and increases epithelial permeability in a mouse model

2001 ◽  
Vol 120 (5) ◽  
pp. A675-A675
Author(s):  
H YANG ◽  
F ROBERT ◽  
Y FAN ◽  
D TEITELBAUM
Keyword(s):  
Mouse Model ◽  
Parenteral Nutrition ◽  
Ion Transport ◽  
Total Parenteral Nutrition ◽  
Epithelial Permeability ◽  
Intestinal Ion Transport

Gastrointestinal Region Specific Insulin Permeation Enhancement by Aloe vera Gel

2020 ◽  
Vol 10 (2) ◽  
pp. 117-122
Author(s):  
Elizca Pretorius ◽  
Clarissa Willers ◽  
Josias H. Hamman ◽  
Johan D. Steyn
Keyword(s):  
Gastrointestinal Tract ◽  
Ex Vivo ◽  
Aloe Vera ◽  
Diffusion Chamber ◽  
Proximal Jejunum ◽  
Absorption Enhancers ◽  
Permeation Enhancement ◽  
Insulin Transport ◽  
Aloe Vera Gel ◽  
Specific Insulin

Background: The oral administration route is still the most preferred by patients for drug treatment, but is unfortunately not suitable for all drug compounds. For example, protein and peptide drugs (e.g. insulin) are typically administered via injection seeing as they are unstable in the gastrointestinal luminal environment and have poor membrane permeation properties. To overcome this problem, functional excipients such as drug absorption enhancers can be co-administered. Although Aloe vera gel has the ability to improve the permeation of drugs across the intestinal epithelium, its drug permeation enhancing effect has not been investigated in the different regions of the gastrointestinal tract yet. Objective: The aim of this study was to investigate the insulin permeation enhancing effects of A. vera gel material across excised pig intestinal tissues from different regions of the gastrointestinal tract and to identify the gastrointestinal region where the highest insulin permeation enhancement was achieved. : Insulin transport across excised pig intestinal tissues from the duodenum, proximal jejunum, medial jejunum, distal jejunum, ileum and colon was measured in the absence and presence of A. vera gel (0.5% w/v) using both the Sweetana-Grass diffusion chamber and everted sac techniques. Results: The insulin permeation results obtained from both ex vivo techniques showed varied permeation enhancing effects of A. vera gel as a function of the different regions of the gastrointestinal tract. The colon was identified as the gastrointestinal region where A. vera gel was the most effective in terms of insulin permeation enhancement in the Sweetana-Grass diffusion chamber technique with a Papp value of 5.50 x 10-7 cm.s-1, whereas the ileum was the region where the highest permeation enhancement occurred in the everted sac technique with a Papp value of 5.45 x 10-7 cm.s-1. Conclusion: The gastrointestinal permeation enhancing effects of A. vera gel on insulin is region specific with the highest effect observed in the ileum and colon.

Multiple Effect of Thermal Treatment Approach on PVDF Membranes: Permeability Enhancement and Silver Nanoparticles Immobilization

2021 ◽  
pp. 105769
Author(s):  
Diyana Kamarudin ◽  
N. Awanis Hashim ◽  
Boon Hoong Ong ◽  
Yuriko Kakihana ◽  
Mitsuru Higa ◽  
...  
Keyword(s):  
Silver Nanoparticles ◽  
Thermal Treatment ◽  
Treatment Approach ◽  
Multiple Effect ◽  
Permeability Enhancement

scholarly journals Molecular Modeling of Histamine Receptors—Recent Advances in Drug Discovery

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1778
Author(s):  
Pakhuri Mehta ◽  
Przemysław Miszta ◽  
Sławomir Filipek
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Molecular Modeling ◽  
Molecular Targets ◽  
Histamine Receptors ◽  
Experimental Characterization ◽  
Complex Disorders ◽  
Theoretical Investigations ◽  
Recent Developments

The recent developments of fast reliable docking, virtual screening and other algorithms gave rise to discovery of many novel ligands of histamine receptors that could be used for treatment of allergic inflammatory disorders, central nervous system pathologies, pain, cancer and obesity. Furthermore, the pharmacological profiles of ligands clearly indicate that these receptors may be considered as targets not only for selective but also for multi-target drugs that could be used for treatment of complex disorders such as Alzheimer’s disease. Therefore, analysis of protein-ligand recognition in the binding site of histamine receptors and also other molecular targets has become a valuable tool in drug design toolkit. This review covers the period 2014–2020 in the field of theoretical investigations of histamine receptors mostly based on molecular modeling as well as the experimental characterization of novel ligands of these receptors.

Permeability enhancement and porosity change of coal by liquid carbon dioxide phase change fracturing

2021 ◽  
Vol 287 ◽  
pp. 106106
Author(s):  
Xianfeng Liu ◽  
Baisheng Nie ◽  
Kunyong Guo ◽  
Chengpeng Zhang ◽  
Zepeng Wang ◽  
...  
Keyword(s):  
Carbon Dioxide ◽  
Phase Change ◽  
Liquid Carbon ◽  
Liquid Carbon Dioxide ◽  
Porosity Change ◽  
Permeability Enhancement

GENETIC SUSCEPTIBILITY TO IBD OPERATES VIA CONTROL OF APICAL JUNCTIONAL COMPLEXES

2021 ◽  
Vol 27 (Supplement_1) ◽  
pp. S30-S30
Author(s):  
Isabelle Hébert-Milette ◽  
Chloé Lévesque ◽  
Guy Charron ◽  
John Rioux
Keyword(s):  
Tight Junction ◽  
Tight Junctions ◽  
Intestinal Inflammation ◽  
Protein Localization ◽  
Junctional Complex ◽  
Epithelial Permeability ◽  
3D Cultures ◽  
Apical Junctional Complex ◽  
Junction Protein ◽  
The Impact

Abstract Introduction Intestinal permeability is increased in unaffected 1st degree relatives of patients with inflammatory bowel disease (IBD), and is considered a risk factor for the development of IBD, likely increasing the interactions between intestinal microorganisms and the immune system. We recently reported that C1orf106, a gene located within a genomic region associated with IBD, regulates epithelial permeability. We further demonstrated that a rare coding variant within C1orf106 (p.Y333F) decreases protein stability and that lower levels of C1orf106 protein leads altered stability of adherens junctions (AJ) and to an increase in epithelial permeability. Hypothesis In addition to altering AJ, we believe that C1orf106 is also involved in the regulation of tight junction (TJ) formation, which also impacts epithelial permeability. Objectives The objectives of the project are to (a) validate the impact of C1orf106 on tight junctions and (b) verify the impact of C1orf106 IBD-associated variants on intestinal barrier integrity. Results We observed that knocking down the expression of C1orf106 in Caco-2 cells leads to a number of phenotypes in human epithelial monolayer (2D) and spheroid (3D) cultures that are associated with alterations in TJs. Specifically, when studying the dynamic reformation of TJ in 2D cultures after transient withdrawal of calcium, which is required for TJ stability, we observed that lower levels of C1orf106 resulted in (1) decreased recovery of barrier function as measured by transepithelial electrical resistance (TEER); (2) an alteration of tight junction protein localization; and (3) thickening of the circumferential actin belt. Moreover, in 3D cultures, we observed an altered spheroid formation associated with impaired epithelial polarization. In addition, our preliminary studies of human induced pluripotent stem cell (hiPSC)-derived epithelial cultures support that Y333F heterozygotes also have altered structure and function of their tight junctions. Conclusion Our observations indicate an important role of C1orf106 in apical junctional complex (AJC) formation likely mediated by a regulation of the circumferential actin belt. This can affect other functions of AJC, like the establishment of cell polarity. AJC formation is important for epithelial repair after an injury and its dysregulation impairs the formation of an impermeable epithelial barrier, which likely facilitates the passage of microorganisms and the induction and maintenance of intestinal inflammation.

Development of a homogeneous binding assay for histamine receptors

2004 ◽  
Vol 335 (1) ◽  
pp. 42-49 ◽  
Author(s):  
Kathy Crane ◽  
Daw-tsun Shih
Keyword(s):  
Binding Assay ◽  
Histamine Receptors

scholarly journals Enteral absorption and haemodynamic response of clonidine in infants post-cardiac surgery

2014 ◽  
Vol 113 (6) ◽  
pp. 964-969 ◽  
Author(s):  
S. Arenas-Lopez ◽  
H. Mulla ◽  
S. Manna ◽  
A. Durward ◽  
I.A. Murdoch ◽  
...  
Keyword(s):  
Cardiac Surgery ◽  
Haemodynamic Response ◽  
Enteral Absorption ◽  
Post Cardiac Surgery
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