Use of fluorescein isothiocyanate isomer I to study the mechanism of intestinal absorption of fucoidan sulfate <i>in vivo</i> and <i>in vitro</i>

Zhang, E; Chu, Fulong; Xu, Lixu; Liang, Hao; Song, Shuliang; Ji, Aiguo

doi:10.1002/bdd.2137

Cited by 25 publications

(13 citation statements)

References 25 publications

(18 reference statements)

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“…These results indicated that F-PM and F-PG entered Caco-2 cells via the macropinocytosis pathway and the clathrin and caveolae (or lipid raft)-mediated endocytosis pathway. This result was different from the transport mechanism of fucoidan that we reported previously, as the transport of fucoidan in the Caco-2 cell monolayers was almost completely blocked by chlorpromazine [11]. This confirmed that the absorption mechanism may be different for biomacromolecules with different structures.…”

Section: Effects Of Transport Inhibitors On the Transport Of F-pm Andcontrasting

confidence: 93%

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

Wang

Bai

et al. 2020

Pharmaceutics

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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.

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Section: Effects Of Transport Inhibitors On the Transport Of F-pm Andcontrasting

confidence: 93%

“…The fluorescently labeled products were verified by agarose gel electrophoresis and fluorescence spectrophotometry [11]. For agarose gel electrophoresis, gelatin was prepared using a sodium barbital solution containing 0.5% (m/v) agarose.…”

Section: Introductionmentioning

confidence: 99%

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

Wang

Bai

et al. 2020

Pharmaceutics

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“…Recent studies have shown that fucoidan can exert a wide range of pharmacological effects, including anti-inflammatory [6], antitumor [7], antioxidative [8], antiviral, and antithrombotic activity, as well as improving immune response and lipid metabolism [5,[9][10][11][12]. However, only a small number of studies addressed the mechanism of absorption and tissue distribution of this compound in vivo given their high molecular size [13][14][15][16]. Therefore, a detailed knowledge of its absorption mechanism is important for its biological activities.…”

Section: Introductionmentioning

confidence: 99%

Study on Absorption Mechanism and Tissue Distribution of Fucoidan

Bai

Zhang

et al. 2020

Molecules

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Fucoidan exhibits several pharmacological activities and is characterized by high safety and the absence of toxic side effects. However, the absorption of fucoidan is not well-characterized. In the present study, fucoidan were labeled with fluorescein isothiocyanate (FITC) and their ability to traverse a monolayer of Caco-2 cells was examined. The apparent permeability coefficients (Papp × 10−6) of FITC-labeled fucoidan (FITC-fucoidan) were 26.23, 20.15, 17.93, 16.11 cm/sec, respectively, at the concentration of 10 μg/mL at 0.5, 1, 1.5 and 2 h. The absorption of FITC-fucoidan was suppressed by inhibitors of clathrin-mediated endocytosis, chlorpromazine, NH4Cl, and Dynasore; the inhibition rates were 84.24%, 74.61%, and 63.94%, respectively. This finding suggested that clathrin-mediated endocytosis was involved in fucoidan transport. Finally, tissue distribution of FITC-fucoidan was studied in vivo after injection of 50 mg/kg body weight into the tail vein of mice. The results showed that FITC-fucoidan targeted kidney and liver, reaching concentrations of 1092.31 and 284.27 μg/g respectively after 0.5 h. In summary, the present work identified the mechanism of absorption of fucoidan and documented its tissue distribution, providing a theoretical basis for the future development of fucoidan applications.

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“…In addition, our analysis identified the process of endocytosis as a potential target for fucoidan. While cellular uptake of fucoidan might rely on clathrin-dependent endocytosis [22], previous studies reported that fucoidan can inhibit endocytosis in HeLa cells [23]. Fucoidan suppressed Ca 2+ -dependent endocytosis, potentially by inhibition of agonist-induced Ca 2+ responses [23].…”

Section: Discussionmentioning

confidence: 98%

Micro RNA Expression after Ingestion of Fucoidan; A Clinical Study

et al. 2020

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Fucoidans are a class of fucose-rich sulfated polysaccharides derived from brown macroalgae that exert a range of biological activities in vitro and in vivo. To generate an unbiased assessment of pathways and processes affected by fucoidan, a placebo-controlled double-blind pilot study was performed in healthy volunteers. Blood samples were taken immediately before and 24 h after ingestion of a single dose of 1 g of Undaria pinnatifida fucoidan (UPF) or placebo. Levels of isolated miRNAs were analyzed using Taqman Open Array Human MicroRNA panels. Out of 754 miRNAs screened, UPF affected a total of 53 miRNAs. Pathway analysis using the TALOS data analysis tool predicted 29 different pathways and processes that were largely grouped into cell surface receptor signaling, cancer-related pathways, the majority of which were previously associated with fucoidans. However, this analysis also identified nine pathways and processes that have not been associated with fucoidans before. Overall, this study illustrates that even a single dose of fucoidans has the potential to affect the expression of genes related to fundamental cellular processes. Moreover, it confirms previous data that fucoidans influence immunity, cancer cells, inflammation, and neurological function.

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Use of fluorescein isothiocyanate isomer I to study the mechanism of intestinal absorption of fucoidan sulfate in vivo and in vitro

Cited by 25 publications

References 25 publications

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

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

Study on Absorption Mechanism and Tissue Distribution of Fucoidan

Micro RNA Expression after Ingestion of Fucoidan; A Clinical Study

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