Antitumor Effect of 5-Fluorouracil-Loaded Liposomes Containing n-3 Polyunsaturated Fatty Acids in Two Different Colorectal Cancer Cell Lines

Dupertuis, Y.M.; Boulens, Nathalie; Angibaud, E.; Briod, Anna-Sophia; Viglione, Alexandre; Allémann, Éric; Delié, Florence; Pichard, Claude

doi:10.1208/s12249-020-01897-5

Cited by 12 publications

(5 citation statements)

References 38 publications

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“…5-FU is an atypical cell cycle-specific drug, which, in addition to acting mainly in the S phase, also has effects on cells in other phases. On the one hand, it blocks DNA replication by inhibiting thymidine synthesis, leading to cell cycle arrest in S phase 50 . A study demonstrated that 5-Fu, an anticancer drug that primarily targets S phase, caused cell cycle arrest in S phase in HCT116 cells 51 .…”

Section: Discussionmentioning

confidence: 99%

Corilagin enhances the anti-tumor activity of 5-FU by downregulating the expression of GRP 78

Li,

Yang

et al. 2023

Sci Rep

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Colorectal cancer is one of the most common malignancies worldwide. Although initially effective, patients who receive chemotherapy ultimately experience various complications and develop chemo-resistance, leading to cancer recurrence. Therefore, we aimed to find a drug with good efficacy and low toxicity that could enhance the treatment with 5-Fluorouracil (a commonly used clinical drug) and reduce its dosing. Corilagin, an anti-tumor natural product, has received widespread attention. Glucose regulated protein 78 (GRP78) is overexpressed in colorectal cancer cells and plays a key role in the proliferation, migration and drug resistance of cancer cells. Importantly, GRP78 can affect the apoptosis induced by 5-fluorouracil in CRC cells. In the present study, we determined the synergistic anti-tumor activity of the combination treatment by cell proliferation assay, apoptosis assay, fluorescent staining, cell cycle analysis, WB and PCR assays. This synergistic effect was associated with S-phase blockade, intracellular reactive oxygen species production and downregulation of GRP78. Taken together, our results indicate that Corilagin acts as a potentiator of 5-fluorouracil and may have therapeutic potential for patients with CRC.

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Section: Discussionmentioning

confidence: 99%

Corilagin enhances the anti-tumor activity of 5-FU by downregulating the expression of GRP 78

Li,

Yang

et al. 2023

Sci Rep

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“…Based on these findings, combined enzyme treatment of N. oceanica may be an appropriate high-yield method to extract EPA-rich lipids for use as functional food ingredients or in nutraceuticals and pharmaceuticals. An EPA-rich diet may regulate human immunity [ 48 ], inhibit tumor-cell growth and metastasis [ 49 ], and reduce human triglyceride levels, thus reducing the risk of atherosclerosis [ 50 ].…”

Section: Discussionmentioning

confidence: 99%

Effects of Structural and Compositional Changes of Nanochloropsis oceania after Enzyme Treatment on EPA-Rich Lipids Extraction

et al. 2022

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Improved methods for the extraction of eicosapentaenoic acid (EPA), an essential and economically important polyunsaturated fatty acid, are urgently required. However, lipid extraction rates using food-grade solvents such as ethanol are usually low. To improve the ethanol-based extraction rate, and to elucidate the relevant mechanisms, we used cellulase and laccase to treat powdered Nannochloropsis, one of the most promising microalgal sources of EPA. Cellulase and laccase synergistically increased lipid yields by 69.31% and lipid EPA content by 42.63%, by degrading the amorphous hemicellulose and cellulose, improving crystallinity, and promoting the release and extraction of lysodiacylglyceryltrimethylhomoserine. Scanning electron microscopy showed that cell morphology was substantially altered, with cell-wall rupture, loss of cell boundaries, and the release of intracellular substances. In conclusion, Nannochloropsis lipid yields may be directly linked to cell-wall hemicellulose structure, and enzymatic treatment to alter this may improve lipid yields.

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“…Nanoparticles range in size from between 1 and 1000 nm [7]. Their composition includes phospholipids and other polymeric materials [8]. The size and design of nanoparticles increase the ease at which they permeate tumors, enhancing the deposition of a higher concentration of therapeutic agents in the tumors.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Anticancer Activity of Zhubech, a New 5-FU Analog Liposomal Formulation, against Pancreatic Cancer

Ndemazie

Bulusu

Xiao-lin

et al. 2023

IJMS

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Pancreatic cancer is projected to be the second leading cause of cancer-related death by 2030 in the US. The benefits of the most common systemic therapy for various pancreatic cancers have been masked by high drug toxicities, adverse reactions, and resistance. The use of nanocarriers such as liposomes to overcome these unwanted effects has become very popular. This study aims to formulate 1,3-bistertrahydrofuran-2yl-5FU (MFU)-loaded liposomal nanoparticles (Zhubech) and to evaluate itsstability, release kinetics, in vitro and in vivo anticancer activities, and biodistribution in different tissues. Particle size and zeta potential were determined using a particle size analyzer, while cellular uptake of rhodamine-entrapped liposomal nanoparticles (Rho-LnPs) was determined by confocal microscopy. Gadolinium hexanoate (Gd-Hex) was synthesized and entrapped into the liposomal nanoparticle (LnP) (Gd-Hex-LnP), as a model contrast agent, to evaluate gadolinium biodistribution and accumulation by LnPs in vivo using inductively coupled plasma mass spectrometry (ICP-MS). The mean hydrodynamic diameters of blank LnPs and Zhubech were 90.0 ± 0.65 nm and 124.9 ± 3.2 nm, respectively. The hydrodynamic diameter of Zhubech was found to be highly stable at 4 °C and 25 °C for 30 days in solution. In vitro drug release of MFU from Zhubech formulation exhibited the Higuchi model (R2 value = 0.95). Both Miapaca-2 and Panc-1 treated with Zhubech showed reduced viability, two- or four-fold lower than that of MFU-treated cells in 3D spheroid (IC50Zhubech = 3.4 ± 1.0 μM vs. IC50MFU = 6.8 ± 1.1 μM) and organoid (IC50Zhubech = 9.8 ± 1.4 μM vs. IC50MFU = 42.3 ± 1.0 μM) culture models. Confocal imaging confirmed a high uptake of rhodamine-entrapped LnP by Panc-1 cells in a time-dependent manner. Tumor-efficacy studies in a PDX bearing mouse model revealed a more than 9-fold decrease in mean tumor volumes in Zhubech-treated (108 ± 13.5 mm3) compared to 5-FU-treated (1107 ± 116.2 mm3) animals, respectively. This study demonstrates that Zhubech may be a potential candidate for delivering drugs for pancreatic cancer treatment.

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Antitumor Effect of 5-Fluorouracil-Loaded Liposomes Containing n-3 Polyunsaturated Fatty Acids in Two Different Colorectal Cancer Cell Lines

Cited by 12 publications

References 38 publications

Corilagin enhances the anti-tumor activity of 5-FU by downregulating the expression of GRP 78

Corilagin enhances the anti-tumor activity of 5-FU by downregulating the expression of GRP 78

Effects of Structural and Compositional Changes of Nanochloropsis oceania after Enzyme Treatment on EPA-Rich Lipids Extraction

Evaluation of Anticancer Activity of Zhubech, a New 5-FU Analog Liposomal Formulation, against Pancreatic Cancer

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