Transepithelial transport mechanisms of 7,8-dihydroxyflavone, a small molecular TrkB receptor agonist, in human intestinal Caco-2 cells

2019 ◽  
Vol 10 (8) ◽  
pp. 5215-5227 ◽  
Author(s):  
Yufeng Chen ◽  
Fan Xue ◽  
Guobin Xia ◽  
Zhenlei Zhao ◽  
Chun Chen ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Transepithelial Transport ◽  
Efflux Transporters ◽  
Transport Mechanisms ◽  
Passive Transport ◽  
Cell Monolayers ◽  
Trkb Receptor

7,8-DHF was transported across Caco-2 cell monolayers by passive transport with carrier-mediated influx and efflux transporters.

scholarly journals Transepithelial Transport and Metabolism of Boronated Dipeptides Across Caco-2 and HCT-8 Cell Monolayers

1996 ◽  
Vol 3 (6) ◽  
pp. 277-286
Author(s):  
Amy L. Elkins ◽  
John G. Eley ◽  
Merrill C. Miller III ◽  
Iris H. Hall ◽  
Anup Sood ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Cell Monolayer ◽  
Therapeutic Agents ◽  
Transepithelial Transport ◽  
Passive Transport ◽  
Cell Monolayers ◽  
Proteins And Peptides

Oral delivery of proteins and peptides as therapeutic agents is problematic due to their low bioavailability. This study examined the effect of boronation on the transepithelial transport and metabolism of three glycine-phenylalanine dipeptides in Caco-2 and HCT-8 cell monolayers. The three dipeptides exhibited passive transport characteristics in the monolayer systems. However, metabolism of the boronated dipeptides did occur, but to a lesser extent than the non-boronated glycine-phenylalanine dipeptide. The same metabolic scheme was seen in both cell monolayer system, but greater metabolism was seen in the HCT-8 cell monolayers.

scholarly journals Enhanced Transepithelial Permeation of Gallic Acid and (−)-Epigallocatechin Gallate across Human Intestinal Caco-2 Cells Using Electrospun Xanthan Nanofibers

Pharmaceutics ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 155 ◽  
Author(s):  
Adele Faralli ◽  
Elhamalsadat Shekarforoush ◽  
Ana Mendes ◽  
Ioannis Chronakis
Keyword(s):  
Gallic Acid ◽  
Epigallocatechin Gallate ◽  
Electrospun Nanofibers ◽  
Transepithelial Transport ◽  
Efflux Transporters ◽  
Polyphenol Compounds ◽  
Cell Monolayers ◽  
Permeability Enhancement ◽  
Release Studies

Electrospun xanthan polysaccharide nanofibers (X) were developed as an encapsulation and delivery system of the poorly absorbed polyphenol compounds, gallic acid (GA) and (−)-epigallocatechin gallate (EGCG). Scanning electron microscopy was used to characterize the electrospun nanofibers, and controlled release studies were performed at pH 6.5 and 7.4 in saline buffer, suggesting that the release of polyphenols from xanthan nanofibers follows a non Fickian mechanism. Furthermore, the X-GA and X-EGCG nanofibers were incubated with Caco-2 cells, and the cell viability, transepithelial transport, and permeability properties across cell monolayers were investigated. An increase of GA and EGCG permeability was observed when the polyphenols were loaded into xanthan nanofibers, compared to the free compounds. The observed in vitro permeability enhancement of GA and EGCG was induced by the presence of the polysaccharide nanofibers, which successfully inhibited efflux transporters, as well as by tight junctions opening.

Mitochondriomics reveals the underlying neuroprotective mechanism of TrkB receptor agonist R13 in the 5×FAD mice

2021 ◽  
pp. 108899
Author(s):  
Ting Li ◽  
Xiao Li ◽  
Xi Huang ◽  
Hao Yu ◽  
Shupeng Li ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Trkb Receptor

scholarly journals Transport Mechanisms of Polymannuronic Acid and Polyguluronic Acid Across Caco-2 Cell Monolayers

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 167
Author(s):  
Yu Wang ◽  
Xu Bai ◽  
Bo Hu ◽  
Maochen Xing ◽  
Qi Cao ◽  
...  
Keyword(s):  
Epithelial Cells ◽  
Biological Activities ◽  
Intestinal Transport ◽  
Fluorescein Isothiocyanate ◽  
Endocytic Pathway ◽  
Detailed Knowledge ◽  
Intestinal Epithelial ◽  
Transport Mechanisms ◽  
Apparent Permeability ◽  
Cell Monolayers

Detailed knowledge of the intestinal transport of polymannuronic acid (PM) and polyguluronic acid (PG) is critical for understanding their biological activities. To investigate the transport in the gastrointestinal tract, PM and PG were chemically modified with tyramine and conjugated with fluorescein isothiocyanate (FITC) to synthesize FITC-PM (F-PM) and FITC-PG (F-PG) successfully. The transport mechanisms of F-PM and F-PG across the intestinal epithelial cell monolayers (Caco-2 cell monolayers) were then investigated. The results demonstrated that the transport of F-PM and F-PG into epithelial cells was time- and energy-dependent, which was mediated by the macropinocytosis pathway and the clathrin- and caveolae (or lipid raft)-mediated endocytic pathway. The transport process of F-PM and F-PG in Caco-2 cells depended on the acidification of endosomes and involved lysosomes. Tubulin mediated the transport of F-PM, but not of F-PG. Moreover, the absorption enhancer chitosan (CS) promoted the transport of F-PM and F-PG, increasing the apparent permeability coefficient (Papp) by 1.9-fold and 2.6-fold, respectively, by reversibly opening the tight junction (TJ). In summary, this study provided a comprehensive understanding of the transport of PM and PG in the small intestinal epithelial cells, which will provide a theoretical basis for the development of PM and PG with good intestinal absorption.

LMDS-1, a potential TrkB receptor agonist provides a safe and neurotrophic effect for early-phase Alzheimer’s disease

2020 ◽  
Vol 237 (10) ◽  
pp. 3173-3190
Author(s):  
Chia-Hao Fan ◽  
Chia-Wei Lin ◽  
Hei-Jen Huang ◽  
Guey-Jen Lee-Chen ◽  
Ying-Chieh Sun ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Early Phase ◽  
Receptor Agonist ◽  
Trkb Receptor ◽  
Neurotrophic Effect

Transepithelial transport of Cerulenin across Caco-2 cell monolayers

2009 ◽  
Vol 34 (2) ◽  
pp. 67-72 ◽  
Author(s):  
Da-Hua Fu ◽  
Zhi-Li Liu ◽  
Jun-Shi Liu ◽  
Yun Luo ◽  
Yong Shu ◽  
...  
Keyword(s):  
Transepithelial Transport ◽  
Cell Monolayers
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