Intestinal Saturated Long-Chain Fatty Acid, Glucose and Fructose Transporters and Their Inhibition by Natural Plant Extracts in Caco-2 Cells

Schreck, Katharina; Melzig, Matthias F.

doi:10.3390/molecules23102544

Cited by 26 publications

(22 citation statements)

References 168 publications

(244 reference statements)

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“…Screening a few ratios of CPT:PTX showed 5.22:1 to be most effective in cytotoxicity assays in vitro . We performed these assays using Caco-2 cells, which are heterogeneous human epithelial colorectal adenocarcinoma cells (Schreck and Melzig, 2018) used most often as a confluent monolayer rather than individual cells (Ellens et al, 2018); the monolayer can, under certain conditions, form a polarized epithelial cell monolayer (Gibaud and Attivi, 2012). Therefore Caco-2 was used here to mimic normal colorectal epithelial cells (Beloqui et al, 2016).…”

Section: Discussionmentioning

confidence: 99%

Characterization of an Amphiphilic Phosphonated Calixarene Carrier Loaded With Carboplatin and Paclitaxel: A Preliminary Study to Treat Colon Cancer in vitro and in vivo

Mao

Chen

et al. 2019

Front. Bioeng. Biotechnol.

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The inadequacy of available detection methods and a naturally aggressive progression have made colon cancer the third most common type of cancer, accounting for ~10% of all cancer cases. The heterogeneity and genomic instability of colon cancer tumors make current treatments unsatisfactory. This study evaluated a novel nanoscale delivery platform comprising phosphonated calixarenes (P4C6) co-loaded with paclitaxel (PTX) and carboplatin (CPT). The nanoparticles showed average hydrodynamic sizes of 84 ± 8 nm for empty P4C6 nanoparticle and 119 ± 13 nm for PTX-CPT-P4C6. The corresponding zeta potentials were −40.8 ± 8.8 and −35.4 ± 4.2 mV. The optimal CPT:PTX ratio was 5.22:1, and PTX-CPT-P4C6 with this ratio was more cytotoxic against HT-29 cells than against Caco-2 cells (IC50, 0.4 ± 0.02 vs. 2.1 ± 0.3 μM), and it induced higher apoptosis in HT-29 cells (56.6 ± 4.5 vs. 44.9 ± 3.44%). PTX-CPT-P4C6 inhibited the invasion and migration of HT-29 cells more strongly than the free drugs. It also inhibited the growth of HT-29 tumors in mice to the greatest extent of all formulations, with negligible side effects. This research demonstrates the potential of P4C6 to deliver two chemotherapeutic agents to colon cancer tumors to provide synergistic efficacy than single drug administration.

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Section: Discussionmentioning

confidence: 99%

Characterization of an Amphiphilic Phosphonated Calixarene Carrier Loaded With Carboplatin and Paclitaxel: A Preliminary Study to Treat Colon Cancer in vitro and in vivo

Mao

Chen

et al. 2019

Front. Bioeng. Biotechnol.

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“…Since polyphenols obtained from dietary sources gain high concentration in gut lumen, they are able to regulate biological activities of the cells in the intestine. Recent data proved that polyphenols are able to influence intestinal processes of glucose and FFA absorption, not only via inhibition of digestive enzymes, but also by attenuation of their uptake [10,11,12]. Some investigations suggested that polyphenolic compounds lower glucose absorption via influence on the sodium-dependent glucose transporter 1 (SGLT1), however, their stronger inhibition potential was identified in the case of the sodium-free glucose transporter known as GLUT2 [13].…”

Section: Introductionmentioning

confidence: 99%

Viburnum opulus Fruit Phenolic Compounds as Cytoprotective Agents Able to Decrease Free Fatty Acids and Glucose Uptake by Caco-2 Cells

et al. 2019

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In recent years, there has been increasing interest in studying food-originated phytocompounds with beneficial influences for humans. Amongst the most active natural substances are polyphenols, for which high content has been identified in the Viburnum opulus berry, and which are unused in Western Europe. Due to its strong antioxidant activity we explored the potential of V. opulus as a preventive agent against diet-related chronic diseases, such as obesity and type 2 diabetes. Among the causes of these ailments is oxidative stress, as well as impaired glucose and free fatty acids (FFA) uptake. Thus, the purpose of this study was to determine biological activity of V. opulus phenolic extracts as cytoprotective agents able to decrease induced oxidative stress, lower lipid accumulation and attenuate glucose and FFA uptake by Caco-2 cells via GLUT2 and CD36/FAT transporters. To determine the source of the most biologically active phenolic compounds, we obtained four phenolic compounds extracts as crude juice, phenolics isolated from juice and two preparations of phenolics obtained with different extraction agents from fruit pomace. Among the studied extracts, the phenolic rich fraction obtained from fruit juice revealed the strongest activity to decrease uptake of glucose, FFA and accumulation of lipid droplets in Caco-2 cells without affecting their viability (IC0 50 μg/mL). Observed uptake attenuation was followed by decrease of the CD36/FAT gene expression, without influence on the GLUT2 and PPARα levels. We suspect that V. opulus phenolics were able to modulate the cellular membrane dynamic, although that hypothesis requires further, more detailed studies. Extracts revealed strong chemo-preventive activity against oxidative stress induced chemically by tert-butylhydroperoxide (t-BOOH), as well as against DNA damage through the induction of DNA repair after cell exposition to methylnitronitrosoguanidine (MNNG) and H2O2. Our findings suggest Viburnum opulus fruit as a dietary source of phytocompounds, which could be considered as a tailored design food supplement components for the prevention and treatment of postprandial elevation of glucose and fatty acids through delaying the rate of glucose and fatty acid absorption by intestinal cells.

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“…In this respect, literature data showed the ability of a large variety of classes of dietary polyphenols, including rutin, quercetin, myricetin, ellagic acid [ 30 ], and avicularin [ 38 ], all present in our extract, to affect glucose transport in Caco-2 cells via both facilitated transport proteins (GLUT 1 and 2) and sodium-dependent glucose transporter 1 (SGLT1). Several natural extracts, usually rich in these molecules, were also found to inhibit glucose uptake in Caco-2 cells through these mechanisms [ 38 , 71 ]. Being the main cellular energetic source, glucose plays a key role also in cancer cell growth [ 72 ].…”

Section: Discussionmentioning

confidence: 99%

Antimicrobial, Antioxidant, and Cytotoxic Activities of Juglans regia L. Pellicle Extract

et al. 2021

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The difficulty to treat resistant strains-related hospital-acquired infections (HAIs) promoted the study of phytoextracts, known sources of bioactive molecules. Accordingly, in the present study, the pharmacological activities of Juglans regia (L.) pellicle extract (WPE) were investigated. The antiviral effect was tested against Herpes simplex virus type 1 and 2, Poliovirus 1, Adenovirus 2, Echovirus 9, Coxsackievirus B1 through the plaque reduction assay. The antibacterial and antifungal activities were evaluated against medically important strains, by the microdilution method. DPPH and superoxide dismutase (SOD)s-like activity assays were used to determine the antioxidant effect. Besides, the extract was screened for cytotoxicity on Caco-2, MCF-7, and HFF1 cell lines by the 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) assay. The total phenolic and flavonoid contents were also evaluated. Interestingly, WPE inhibited Herpes simplex viruses (HSVs) replication, bacterial and fungal growth. WPE showed free radical scavenging capacity and inhibited superoxide anion formation in a dose-dependent manner. These effects could be attributed to the high content of phenols and flavonoids, which were 0.377 ± 0.01 mg GE/g and 0.292 ± 0.08 mg CE/g, respectively. Moreover, WPE was able to reduce Caco-2 cell viability, at both 48 h and 72 h. The promising results encourage further studies aimed to better elucidate the role of WPE in the prevention of human infectious diseases.

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Intestinal Saturated Long-Chain Fatty Acid, Glucose and Fructose Transporters and Their Inhibition by Natural Plant Extracts in Caco-2 Cells

Cited by 26 publications

References 168 publications

Characterization of an Amphiphilic Phosphonated Calixarene Carrier Loaded With Carboplatin and Paclitaxel: A Preliminary Study to Treat Colon Cancer in vitro and in vivo

Characterization of an Amphiphilic Phosphonated Calixarene Carrier Loaded With Carboplatin and Paclitaxel: A Preliminary Study to Treat Colon Cancer in vitro and in vivo

Viburnum opulus Fruit Phenolic Compounds as Cytoprotective Agents Able to Decrease Free Fatty Acids and Glucose Uptake by Caco-2 Cells

Antimicrobial, Antioxidant, and Cytotoxic Activities of Juglans regia L. Pellicle Extract

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