Evaluation of the Impact of Excipients on Albendazole Concentrations in Upper Small Intestine Using an In Vitro Biorelevant Gastrointestinal Transfer (BioGIT) System

Author(s):  
Maria Vertzoni
Keyword(s):  
2018 ◽  
Vol 6 (5) ◽  
Author(s):  
Vamoussa Coulibaly ◽  
N’dri Kouamé ◽  
Atolé Brice Kédi ◽  
Joseph Sei ◽  
Samuel Oyetola

In order to evaluate the impact of clay on the body during digestion, a study of the bioavailability of elements from clay minerals from Anyama and Bingerville (Abidjan district) was performed in vitro. A simulation of the destruction of a solid matrix in the human gastrointestinal tract was undertaken. The analysis of different juices after digestion revealed the presence of numerous inorganic elements essential for biological activity. Green clay of Anyama consisting of chlorite, illite and smectite, released more elements than those of Bingerville, the mineralogy of witch being dominated by kaolinite. The concentration of some ions (Al, Co, Ca, Cu, Fe, Zn, Pb, Si) decreased during the transition from the step of the stomach (pH = 2.5) to that of the small intestine (pH ≈ 7). The proportions of zinc and copper in spite of decrease during the small intestine step, remain superior to the others. To the contrary, an increase was observed for K, Ni and P. Iron and calcium in this series were distinguished by their disappearance during the stage of the small intestine.


Foods ◽  
2020 ◽  
Vol 9 (7) ◽  
pp. 913
Author(s):  
Carol González ◽  
Daniela González ◽  
Rommy N. Zúñiga ◽  
Humberto Estay ◽  
Elizabeth Troncoso

This work deepens our understanding of starch digestion and the consequent absorption of hydrolytic products generated in the human small intestine. Gelatinized starch dispersions were digested with α-amylase in an in vitro intestinal digestion system (i-IDS) based on a dialysis membrane process. This study innovates with respect to the existing literature, because it considers the impact of simultaneous digestion and absorption processes occurring during the intestinal digestion of starchy foods and adopts phenomenological models that deal in a more realistic manner with the behavior found in the small intestine. Operating the i-IDS at different flow/dialysate flow ratios resulted in distinct generation and transfer curves of reducing sugars mass. This indicates that the operating conditions affected the mass transfer by diffusion and convection. However, the transfer process was also affected by membrane fouling, a dynamic phenomenon that occurred in the i-IDS. The experimental results were extrapolated to the human small intestine, where the times reached to transfer the hydrolytic products ranged between 30 and 64 min, according to the flow ratio used. We consider that the i-IDS is a versatile system that can be used for assessing and/or comparing digestion and absorption behaviors of different starch-based food matrices as found in the human small intestine, but the formation and interpretation of membrane fouling requires further studies for a better understanding at physiological level. In addition, further studies with the i-IDS are required if food matrices based on fat, proteins or more complex carbohydrates are of interest for testing. Moreover, a next improvement step of the i-IDS must include the simulation of some physiological events (e.g., electrolytes addition, enzyme activities, bile, dilution and pH) occurring in the human small intestine, in order to improve the comparison with in vivo data.


2016 ◽  
Vol 105 (9) ◽  
pp. 2896-2903 ◽  
Author(s):  
Alexandros Kourentas ◽  
Maria Vertzoni ◽  
Ibrahim Khadra ◽  
Mira Symillides ◽  
Hugh Clark ◽  
...  
Keyword(s):  

2021 ◽  
pp. 1-18
Author(s):  
Prashanna Balaji Venkatasubramanian ◽  
Els Oosterink ◽  
Monic M. M. Tomassen ◽  
Maria Suarez-Diez ◽  
Jurriaan J. Mes ◽  
...  

BACKGROUND: Clostridium difficile Infection (CDI) can lead to diarrhea and fulminant colitis. C. difficile infects the host using toxins. Recent studies report prevalence of CDI in the small intestine. Berries are known to contain antioxidants and phenolic compounds that might mitigate bacterial infection. OBJECTIVE: We explored the impact of C. difficile toxins on the small intestine using an in vitro approach and used systems biology techniques together with data integration to identify food compounds that can reduce their cytopathic impact. METHODS: Differentiated Caco-2 cells were exposed to C. difficile toxins and the transcriptomic changes were studied. To identify foods with potential beneficial counteracting effects, the transcriptomic profiles were integrated with transcriptomics data from Caco-2 cells exposed to various food compounds and analyzed using multivariate analysis. RESULTS: Beneficial food candidates, selected by multivariate analysis, such as blackcurrant, strawberry and yellow onion were further examined for their potential to counteract the effect of the toxin-induced disruption of cell integrity and toxin translocation. Our results confirmed effects of food compounds, on the cytopathic effects of toxins in the small intestine. CONCLUSION: Blackcurrant, strawberry and yellow onion can counteract C. difficile toxins induced effects.


Author(s):  
A. J. Tousimis

The elemental composition of amino acids is similar to that of the major structural components of the epithelial cells of the small intestine and other tissues. Therefore, their subcellular localization and concentration measurements are not possible by x-ray microanalysis. Radioactive isotope labeling: I131-tyrosine, Se75-methionine and S35-methionine have been successfully employed in numerous absorption and transport studies. The latter two have been utilized both in vitro and vivo, with similar results in the hamster and human small intestine. Non-radioactive Selenomethionine, since its absorption/transport behavior is assumed to be the same as that of Se75- methionine and S75-methionine could serve as a compound tracer for this amino acid.


2020 ◽  
Vol 21 (7) ◽  
pp. 722-734
Author(s):  
Adele Soltani ◽  
Arefeh Jafarian ◽  
Abdolamir Allameh

micro (mi)-RNAs are vital regulators of multiple processes including insulin signaling pathways and glucose metabolism. Pancreatic β-cells function is dependent on some miRNAs and their target mRNA, which together form a complex regulative network. Several miRNAs are known to be directly involved in β-cells functions such as insulin expression and secretion. These small RNAs may also play significant roles in the fate of β-cells such as proliferation, differentiation, survival and apoptosis. Among the miRNAs, miR-7, miR-9, miR-375, miR-130 and miR-124 are of particular interest due to being highly expressed in these cells. Under diabetic conditions, although no specific miRNA profile has been noticed, the expression of some miRNAs and their target mRNAs are altered by posttranscriptional mechanisms, exerting diverse signs in the pathobiology of various diabetic complications. The aim of this review article is to discuss miRNAs involved in the process of stem cells differentiation into β-cells, resulting in enhanced β-cell functions with respect to diabetic disorders. This paper will also look into the impact of miRNA expression patterns on in vitro proliferation and differentiation of β-cells. The efficacy of the computational genomics and biochemical analysis to link the changes in miRNA expression profiles of stem cell-derived β-cells to therapeutically relevant outputs will be discussed as well.


2018 ◽  
Vol 16 (2) ◽  
pp. 127-137
Author(s):  
Paula Sofia Coutinho Medeiros ◽  
Ana Lúcia Marques Batista de Carvalho ◽  
Cristina Ruano ◽  
Juan Carlos Otero ◽  
Maria Paula Matos Marques

Background: The impact of the ubiquitous dietary phenolic compound p-coumaric acid on human breast cancer cells was assessed, through a multidisciplinary approach: Combined biological assays for cytotoxicity evaluation and biochemical profiling by Raman microspectroscopic analysis in cells. </P><P> Methods: Para-coumaric acid was shown to exert in vitro chemoprotective and antitumor activities, depending on the concentration and cell line probed: a significant anti-invasive ability was detected for the triple-negative MDA-MB-231 cells, while a high pro-oxidant effect was found for the estrogen- dependent MCF-7 cells. A striking cell selectivity was obtained, with a more noticeable outcome on the triple-negative MDA-MB-231 cell line. Results: The main impact on the cellular biochemical profile was verified to be on proteins and lipids, thus justifying the compound´s anti-invasive effect and chemoprotective ability. Conclusion: p-Coumaric acid was thus shown to be a promising chemoprotective/chemotherapeutic agent, particularly against the low prognosis triple-negative human breast adenocarcinoma.


2018 ◽  
Vol 18 (2) ◽  
pp. 255-262 ◽  
Author(s):  
Aikebaier Maimaiti ◽  
Amier Aili ◽  
Hureshitanmu Kuerban ◽  
Xuejun Li

Aims: Gallic acid (GA) is generally distributed in a variety of plants and foods, and possesses cell growth-inhibiting activities in cancer cell lines. In the present study, the impact of GA on cell viability, apoptosis induction and possible molecular mechanisms in cultured A549 lung carcinoma cells was investigated. Methods: In vitro experiments showed that treating A549 cells with various concentrations of GA inhibited cell viability and induced apoptosis in a dose-dependent manner. In order to understand the mechanism by which GA inhibits cell viability, comparative proteomic analysis was applied. The changed proteins were identified by Western blot and siRNA methods. Results: Two-dimensional electrophoresis revealed changes that occurred to the cells when treated with or without GA. Four up-regulated protein spots were clearly identified as malate dehydrogenase (MDH), voltagedependent, anion-selective channel protein 1(VDAC1), calreticulin (CRT) and brain acid soluble protein 1(BASP1). VDAC1 in A549 cells was reconfirmed by western blot. Transfection with VDAC1 siRNA significantly increased cell viability after the treatment of GA. Further investigation showed that GA down regulated PI3K/Akt signaling pathways. These data strongly suggest that up-regulation of VDAC1 by GA may play an important role in GA-induced, inhibitory effects on A549 cell viability.


2020 ◽  
Vol 10 ◽  
Author(s):  
Bianca Peterson ◽  
Henrico Heystek ◽  
Josias H. Hamman ◽  
Johan D. Steyn

Background:: Knowledge of the permeation characteristics of new chemical entities across biological membranes is essential to drug research and development. Transport medium composition may affect the absorption of compounds during in vitro drug transport testing. To preserve the predictive values of screening tests, the possible influence of transport media on the solubility of model drugs, and on the activities of tight junctions and efflux transporter proteins (e.g. P-glycoprotein) must be known. Objective:: The aim of this study was to compare the impact of different transport media on the bi-directional transport of standard compounds, selected from the four classes of the Biopharmaceutical Classification System (BCS), across excised pig intestinal tissue. Methods:: The Sweetana-Grass diffusion apparatus was used for the transport studies. Krebs-Ringer bicarbonate (KRB) buffer and simulated intestinal fluids in the fed (FeSSIF) and fasted (FaSSIF) states were used as the three transport media, while the chosen compounds were abacavir (BCS class 1), dapsone (BCS class 2), lamivudine (BCS class 3) and furosemide (BCS class 4). Results:: Abacavir exhibited lower permeability in both the simulated intestinal fluids than in the KRB buffer. Dapsone showed similar permeability in all media. Lamivudine exhibited lower permeability in FaSSIF than in the other two media. Furosemide exhibited improved transport with pronounced efflux in FaSSIF. Conclusion:: Different permeation behaviors were observed for the selected drugs in the respective media, which may have resulted from their different physico-chemical properties, as well as from the effects that dissimilar transport media components had on excised pig intestinal tissue.


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