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Fenretinide

Fenretinide is a synthetic retinoid compound that has been investigated for its potential applications in cancer prevention and treatment.
It is structurally similar to vitamin A and has been shown to have antiproliferative and pro-apoptotic effects in a variety of cancer cell lines.
Fenretinide has been studied for its ability to induce cell cycle arrest and apoptosis, as well as its potential to inhibit angiogenesis and metastaesis.
Additionally, fenretinide has been explored for its ability to modulate the immune system and enhance the efficacy of other antineoplastic agents.
Reserach on fenretinide is ongoing, with studies examining its pharmacokinetics, toxicology, and optimal dosing regimens to maximize its therapeutic potential whiel minimizing adverse effects.

Most cited protocols related to «Fenretinide»

Human SH-SY5Y neuroblastoma and A375 and SK-MEL110 melanoma cells were cultured in DMEM containing 4.5 g l−1 glucose and supplemented with 10% foetal bovine serum as described previously for SH-SY5Y cells (Lovat et al, 2004 (link)). Fenretinide (Janssen-Cilag Ltd, Basserdorf, Switzerland), temozolomide (OSI Pharmaceuticals), vincristine, velcade (Janssen Pharmaceutica) or thapsigargin (Sigma Chemical Co., St Louis, MO, USA) were added in ethanol (fenretinide and vincristine) or DMSO (Lovat et al, 2004 (link)), with an equal volume of vehicle used to treat control cells. The SH-SY5Y cells were treated with fenretinide at a concentration of 3 μM, vincristine at 10 nM, velcade at 5 nM or thapsigargin at 1.5 μM. The melanoma cell lines were more resistant to drug-induced apoptosis, and for these cells, fenretinide was used at final concentrations of 10 or 15 μM, as specified in the results, temozolomide was used at 1 mM, velcade at 30 nM and thapsigargin at 7.5 μM. In these experiments, thapsigargin was used as a reference positive control for ER stress responses and vincristine and temozolomide as negative controls. Velcade was also used in some experiments as a comparator for fenretinide responses. The concentrations of fenretinide used were within the range of IC50 values described previously for a sample of 10 human melanoma cell lines (Montaldo et al, 1999a (link)). Vitamin C was added to cells to a final concentration of 100 μM as described previously (Lovat et al, 2000 (link)). Flow cytometry of fixed and propidium iodide-stained cells was used to estimate the level of cell death or apoptosis, expressed as the percentage of cells which were hypodiploid (Lovat et al, 2000 (link)). The generation of ROS was detected by staining cells after trypsinization with 10 μM 5-(and –6)-chloromethyl-2′,7′-dihydrodichlorofluorescein diacetate (CM-H2DCFDA) or 1 μM dihydroethidine (DHE) for 20 min at 37°C in the dark and evaluated by flow cytometry as previously described (Lovat et al, 2000 (link), 2002 (link)).
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Publication 2007
2',7'-dichlorodihydrofluorescein diacetate Apoptosis Ascorbic Acid Cell Death Cell Lines Cells dihydroethidine Ethanol Fenretinide Fetal Bovine Serum Flow Cytometry Glucose Homo sapiens Melanoma Neuroblastoma Pharmaceutical Preparations Propidium Iodide Sulfoxide, Dimethyl Temozolomide Thapsigargin Velcade Vincristine
Flasks of fenretinide-treated and control cells were twice washed in 1 x Dulbecco’s phosphate-buffered saline (2.7 mM KCl, 1.47 mM KH2PO4, 8.1 mM NaCl and 50.5 mM Na2HPO4 - PAA Laboratories Ltd., Yeovil, UK). TRIzol reagent (Invitrogen) was added to the flasks and cells lysed by trituration. RNA was isolated with chloroform induced phase separation and precipitated using isopropanol as instructed by the manufacturers. The RNA was treated with RQ1-RNase-free DNase (Promega, Southampton, UK) to remove any contaminating DNA. First-strand cDNA synthesis was performed on 3 μg of total RNA, using Superscript III Reverse Transcriptase with an oligo-(dT)20 primer (Invitrogen) at 50 °C, according to the manufacturer’s protocol. A reaction containing no reverse transcriptase was also prepared for each RNA sample as a control (-RT). Following cDNA synthesis all reactions were treated with RNase H (Invitrogen) to degrade the RNA template. PCR was performed on the first-strand cDNA synthesis reaction products, using GoTaq polymerase (Promega) according to the manufacturer’s protocol with gene-specific primers (synthesized by Eurofins MWG Operon, Ebersberg, Germany) described in Table 1. The PCR cycling parameters consisted of an initial denaturation step at 95 °C for 2 min, followed by 35 cycles of denaturation at 95 °C for 30 s, annealing at primer melting temperature minus 3 °C for 30 s and extension at 72 °C for 30 s, followed by a final extension step at 72 °C for 5 min. PCR products were separated on a 2% agarose gel and visualized using ethidium bromide. A no template water PCR control was included for each primer set.
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Publication 2011
Anabolism Cells Chloroform Deoxyribonucleases DNA, Complementary Endoribonucleases Ethidium Bromide Fenretinide Genes Isopropyl Alcohol Oligonucleotide Primers Oligonucleotides Operon Phosphates Ribonuclease H RNA-Directed DNA Polymerase Saline Solution Sepharose Sodium Chloride trizol
Solution X-ray scattering data were collected on a samples of EI (5 mg/ml corresponding to ∼40 μM dimer), EI-HPr complex (5 mg/ml EI and 4.4 mg/ml HPr, corresponding to ∼40 μM EI dimer and 0.49 mM HPr) and HPr (4.4. mg/ml) in 20 mM Tris buffer, pH 7.4, 100 mM NaCl, 10 mM DTT, 4 mM MgCl2, 1 mM EDTA, and 1 tablet of protease inhibitor cocktail (SigmaFAST S8830). Solution X-ray scattering data were acquired at the Beam Line 12-IDC at the Advanced Light Source (Argonne National Laboratory, Argonne, IL). Data collection was done using a Gold CCD detector positioned at two distances, 4 m and 36 cm, from the sample capillary. Incident radiation with an energy of 20 keV was used resulting in observable q-ranges of 0.014 - 0.23 A-1 (SAXS) for the 4 m sample-detector distance and 0.10 - 2.5 A-1 (WAXS) for the 36 cm distance. Q-axis mapping for both geometries was done using scattering from a silver behenate standard sample. A total of 20 sequential data frames with exposure times of 0.25 seconds was recorded with the samples kept at 25°C throughout the measurement. To prevent radiation damage, volumes of 150 μL of samples and buffers were oscillated during data collection using a flow-though setup. Individual data frames were masked, corrected for the detector sensitivity, radially integrated and normalized by the corresponding incident beam intensities. The final 1D scattering profiles and their uncertainties were calculated as means and standard deviations over the 20 individual frames. The buffer data were then subtracted from the scattering profiles. In the case of the SAXS profile obtained for the EI/HPr sample, the contribution from unbound HPr (present in the sample in excess) was also subtracted, based on the experimental SAXS/WAXS profile of free HPr and the concentration of unbound HPr in the EI/HPr sample calculated from the Kdiss determined by isothermal titration calorimetry. To evaluate the magnitude of a possible structure factor, data were collected at protein concentrations of 5.0 and 2.5 mg/ml for EI and HPr samples. The data at these concentrations were indistinguishable at q > 0.015 A-1.
Publication 2010
Buffers Calorimetry Capillaries Edetic Acid Epistropheus factor A Fenretinide Gold Hypersensitivity Light Magnesium Chloride Neoplasm Metastasis Proteins Radiation Radiography Reading Frames SERPINA1 protein, human Silver Sodium Chloride Tablet Titrimetry Tromethamine
Cell growth inhibition assay was performed as described previously [28 (link)]. For cell growth experiment, cells were treated with the RRs for 6 days. MTT assay was performed at the end of the experiment. Calculations of combination indices were done using the Calcusyn program (Biosoft, Cambridge, United Kingdom). For colony formation assay, cells were plated 1000 per well in complete media in six-well plates and allowed to adhere for 24 h. The next day cells were treated with (VN/14-1, ATRA, CGP57380, cercosporamide and 4-HPR) and RRs (10 μmol/L). After 24 h compound containing media were removed, and cells were allowed to form colonies in complete media. Approximately 2–3 weeks later the colonies were fixed, stained with 0.5% crystal violet (sigma) for 30 min and counted manually. Results represent the mean ± standard deviation of three independent experiments.
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Publication 2014
4-(1H-imidazol-1-yl)retinoic acid Biological Assay Cells cercosporamide CGP 57380 Fenretinide Psychological Inhibition Tretinoin Violet, Gentian
Each cell line was studied in growth inhibition experiments using 96-well microtiter plates. Twenty-four hours after cell plating, cell lines were exposed to CEP-701, 13cRA, 4HPR or their combination for 72 h (three replicates per experiment). Cells were then washed in the appropriate media and grown for an additional 72 h. To ensure that a complete sigmoidal survival-concentration curve could be observed, the following drug concentrations were studied: CEP-701 (0.01–0.5 μM), 13cRA (0.001–200 μM), and 4HPR (0.1–10 μM). Experiments were repeated at least twice.
Survival-concentration curves were generated using the SRB assay [15 (link), 27 (link)]. Following 72-hour drug exposure and subsequent 72-hour growth, 50 μl of cold 50% trichloroacetic acid (TCA) (4°C) was added to the wells at the liquid air interface of each well to produce a final TCA concentration of 10%. The cell culture plates were incubated for 30 min at 4°C and then washed three times with distilled water. Once plates were air dried, 100 μl of 0.4% SRB stain containing 1% acetic acid was added to each well. The plates were then incubated for 30 min at room temperature and washed with 1% acetic acid. Once the stained plates were air dried, 100 μl of 10 mM Tris Base was added to each well and plates were gently agitated for 5 min. The optical density was then read using a Molecular Devices VERSAmax (Sunnyvale, CA) microplate reader at 520 nm. The background signal from media-alone controls was subtracted and data were normalized to untreated cells. The 50% growth inhibitory concentration (IC50) was determined by fitting a four parameter logistic equation to the data: %survival=[(EmaxEmin)(1+(XEC50)slope)]+Emin where X is the drug concentration, Emax and Emin are the concentrations at which maximum and minimum cytotoxicity are observed, respectively, and EC50 is the concentration at which 50% of the maximum cytotoxicity is attained (Emin + Emax)/2. The IC50 was then calculated using the fitted parameters and solving for X with survival set to 50%.
Publication 2011
Acetic Acid Biological Assay Cell Culture Techniques Cell Lines Cells CEP-701 Cold Temperature Cytotoxin Fenretinide Medical Devices Pharmaceutical Preparations Psychological Inhibition Trichloroacetic Acid Tromethamine Vision

Most recents protocols related to «Fenretinide»

All animal procedures were performed under a project licence (PPL P94B395E0) approved by the U.K. Home Office under the Animals (Scientific Procedures) Act 1986 and the University of Aberdeen ethics review board. Studies were performed following the recommendations in the ARRIVE guidelines under guidance by the Veterinary Surgeon and Animal Care and Welfare Officers of the institutional animal research facility. Thus, all methods were performed in accordance with the relevant guidelines and regulations. Male LDLR−/− mice, aged 4–6 weeks, were purchased from The Jackson Laboratory (supplied by Charles River UK Ltd), male and female ApoE−/− mice were bred in-house (University of Aberdeen). All mice were fed chow diet until 12 weeks of age then placed into three groups and fed the following diets (all Research Diets Inc.) to induce atherogenesis and NAFLD for 14 weeks: control (10% kCal fat D14121001) or high-fat/high-cholesterol diet (HFD, 40% kCal fat from cocoa butter and soybean oil, 34.5% kcal and 5.5% kcal respectively, plus 1.25% cholesterol, Clinton/Cybulsky D12108C) + /- 0.04% Fenretinide (FEN-HFD, D18061502,16 (link),27 (link)–29 (link)). Mice were maintained at 22–24 °C on 12-h light/dark cycle with free access to food/water. At week 14, mice were fasted for 5 h and injected intraperitoneally with either saline or insulin (10 mU/g body weight) for 10 min prior to CO2-induced anaesthesia followed by cervical dislocation. Heart and aortic tissues were collected for histological analysis. Peripheral metabolic tissues (liver, muscle and white adipose tissue (WAT)) were frozen in liquid nitrogen and stored at − 80 °C until subsequent analysis.
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Publication 2023
Anesthesia Animals Aorta Apolipoproteins E Atherogenesis Body Weight Cholesterol cocoa butter Diet Diet, High-Fat Females Fenretinide Food Freezing Heart Insulin Joint Dislocations LDLR protein, human Liver Males Mice, House Muscle Tissue Neck Nitrogen Non-alcoholic Fatty Liver Disease Rivers Saline Solution Soybean oil Surgeons Therapy, Diet Tissues White Adipose Tissue
The data sets generated and analyzed during the current study are available from the corresponding author upon reasonable request including RNA-Seq data referred to briefly here in the discussion, previously17 (link) and manuscript in preparation. Fenretinide used in the current study is available from the corresponding author upon reasonable request and for non-commercial purposes17 (link).
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Publication 2023
Fenretinide RNA-Seq
To evaluate the effect of Nanofenretinide, Nanospermidine, and naxitamab on cell viability, the cells were treated with the single components or with Nanofenretinide or Nanospermidine in combination with naxitamab, and MTT assays were performed. Treatments were conducted at Nanofenretinide and Nanospermidine concentrations ranging from 0.025 to 0.20 mg/mL corresponding to fenretinide concentrations ranging from 5 to 40 μM or spermidine concentrations ranging 22 to 173 μM, respectively. The empty nanomicelles were also tested at the same concentrations as the loaded ones. Naxitamab was evaluated at 5, 10, and 20 μg/mL as a single component and in combination with 0.05 mg/mL Nanofenretinide or Nanospermidine. Cell proliferation and viability were detected by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) tetrazolium salt assay. This assay is based on MTT reduction to the insoluble formazan salt by cellular dehydrogenase. The amount of formazan produced is indicative of the number of viable cells in the sample [26 (link),27 (link)]. To perform the MTT assay, the cells were seeded at 10 × 103 cell/cm2 in 96 multiwell plates, and, after 24 h, they were treated with Nanofenretinide, Nanospermidine, or the empty nanomicelles for 24 h, otherwise they were treated with naxitamab alone or in combination with Nanofenretinide or Nanospermidine for 24 or 72 h. Subsequently, 10 µL of MTT solution 5 mg/mL was added to each well to a final concentration of 0.5 mg/mL. After 4 h at 37 °C in the dark, 100 µL of sodium dodecylsulfate (SDS) 10% (w/v) in HCl 0.01 mM was added to each well to dissolve the purple formazan crystals and left overnight on a shaker. The absorbance was read for each well on a TECAN plate reader (Männedorf, Switzerland) at 570 nm. Absorbance was normalized by a second reading at 690 nM to avoid interference by the turbidity of biological samples.
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Publication 2023
Biological Assay Biopharmaceuticals Bromides Cell Proliferation Cells Cell Survival Fenretinide Formazans naxitamab Oxidoreductase Sodium Chloride Spermidine Sulfate, Sodium Dodecyl Tetrazolium Salts
Fenretinide nanomicelles were prepared according to a method previously reported [20 (link),21 (link)]. Briefly, soy phosphatidylcholine (4 mmoles), glyceryl tributyrate (2 mmoles), 2-hydroxypropyl beta cyclodextrin (0.4 mmoles), and KOH 10 N (400 µL, 4 mmoles) were mixed to homogeneity to obtain a semisolid phase. A solution of fenretinide (1.2 mmoles) in ethanol (300 µL) and KOH 10 N (120 µL) was added to the semisolid phase and the resultant mixture was homogeneously dispersed in PBS pH 7.4 to 50 mg/mL. The coarse nanomicelle suspension obtained was filtered through 0.2 µm filters, dialyzed for 72 h (dialysis membrane Mw cutoff 10 KD) against PBS pH 7.4, and then, the dialyzed phase was finally lyophilized. The dry product was reconstituted with water to 50 mg/mL NF and stored at −22 °C until use. Spermidine nanomicelles were prepared as previously reported [22 (link)] by mixing soy phosphatidylcholine (4 mmoles), glyceryl tributyrate (2 mmoles), 2-hydroxypropyl beta cyclodextrin (0.4 mmoles), KOH 10 N (400 µL, 4 mmoles), and spermidine (2 mmoles) to homogeneity to obtain a semisolid phase that was dispersed in PBS pH 7.4 to 50 mg/mL. The coarse nanomicelle suspension obtained was filtered through 0.2 µm filters, dialyzed for 72 h (dialysis membrane Mw cutoff 10 KD) against PBS pH 7.4, and then, the dialyzed phase was lyophilized. The dry product was reconstituted with water to 50 mg/mL NS and stored at −22 °C until use. Empty nanomicelles (No) were prepared by the same procedure but without addition of drugs.
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Publication 2023
2-Hydroxypropyl-beta-cyclodextrin Dialysis Ethanol Fenretinide Pharmaceutical Preparations Phosphatidylcholines Spermidine Tissue, Membrane tributyrin
The loading of fenretinide and spermidine in the nanomicelles was evaluated as previously described [22 (link)]. Briefly, the reconstituted nanomicelle dispersions (50 mg/mL) were diluted (1:3, v/v) with an ethanol:water (1:1, v/v) mixture and analyzed for drug content in comparison with the empty nanomicelles. The content of fenretinide was obtained by UV spectroscopy (Shimadzu UV-1601) at 360 nm. Spermidine content was evaluated by fluorimetry after production of hydrogen peroxide from spermidine and reaction of hydrogen peroxide with a fluorometric probe (Ex/Em = 535/587 nm) generating a signal proportional to the polyamine concentration. The reactions were carried out by a polyamine assay kit (Merck Milan, Italy) according to the manufacturer’s instructions. Mean size, polydispersity index and zeta potential were measured at 37 °C on nanomicelle suspensions in PBS at 0.05 mg/mL (Malvern Nano-ZS Spectrometer, Malvern, UK). A minimum of 12 measurements were made per sample. The results were the combination of 3 runs of 10 min each for a total accumulation correlation function time of 30 min. The nanomicelle stability to drug leakage was measured by the release of spermidine and fenretinide from NS and NF, respectively, by dialysis at 37 °C, as previously described [20 (link),21 (link),22 (link)]. Briefly, the reconstituted nanomicelles suspensions (50 mg/mL) were diluted with PBS 7.4 containing 10% Human Serum (HS) to a final concentration of 0.05 mg/mL. A total of 1 mL of the diluted suspension was introduced into a release chamber separated by a dialysis membrane (Mw cutoff 5KD, Fisher Scientific) from a receiving compartment filled with 10 mL PBS pH 7.4 containing 10% HS. Leakage from the nanomicelles was determined by evaluating the concentrations of fenretinide or spermidine in the receiving phase at increasing time intervals. The concentration of fenretinide was evaluated spectrophotometrically by its maximum absorption wavelength (360 nm) and the concentration of spermidine was determined by the previously described polyamine assay kit. Sink conditions were maintained throughout the experiment.
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Publication 2023
Biological Assay Dialysis Ethanol Fenretinide Fluorometry Homo sapiens Peroxide, Hydrogen Pharmaceutical Preparations Polyamines Serum Spectrum Analysis Spermidine Tissue, Membrane

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Ethanol absolute anhydrous is a pure, anhydrous form of ethyl alcohol. It is a clear, colorless liquid with a characteristic odor. The product is suitable for various laboratory and analytical applications where a high-purity alcohol is required.
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Fenretinide is a synthetic retinoid compound used in laboratory research. It is a vitamin A derivative that has been studied for its potential biological activities. The core function of Fenretinide is to serve as a tool for scientific investigation, without extrapolation on its intended use.
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Glyceryl tributyrate is a chemical compound used as a standard and reference material in analytical chemistry. It is a colorless, viscous liquid with a characteristic odor. Glyceryl tributyrate is commonly used as a calibration standard for various analytical techniques, including gas chromatography and mass spectrometry.
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Soy L-α-phosphatidylcholine is a major component of soy lecithin. It is a naturally occurring phospholipid that can be used as a laboratory reagent. The primary function of this product is to provide a source of phosphatidylcholine, which is a key structural lipid found in cell membranes.
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4-HPR is a laboratory reagent used in biochemical and cell biology research. It functions as a synthetic retinoid compound. The core purpose of 4-HPR is to serve as a research tool without interpretation of its intended use.
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β-actin is a cytoskeletal protein that is ubiquitously expressed in eukaryotic cells. It is an important component of the microfilament system and is involved in various cellular processes such as cell motility, structure, and integrity.
Fenretinide is a synthetic retinoid compound. It functions as an inhibitor of fatty acid synthase, which is involved in the biosynthesis of long-chain fatty acids. Fenretinide has been investigated for its potential applications in various research areas.
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Thapsigargin is a naturally occurring compound isolated from the plant Thapsia garganica. It functions as a selective inhibitor of the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) pump, which is responsible for the active uptake of calcium ions into the endoplasmic reticulum. Thapsigargin is a valuable tool for researchers studying calcium signaling and homeostasis in biological systems.

More about "Fenretinide"

Fenretinide, also known as 4-HPR, is a synthetic retinoid compound that has been extensively studied for its potential applications in cancer prevention and treatment.
This lipophilic vitamin A analogue has demonstrated remarkable antiproliferative and pro-apoptotic effects across a variety of cancer cell lines, making it a promising candidate for oncological research and therapeutics.
One of the key mechanisms by which fenretinide exerts its anti-cancer effects is through its ability to induce cell cycle arrest and programmed cell death (apoptosis).
Additionally, fenretinide has been shown to inhibit angiogenesis, the process of new blood vessel formation, as well as metastasis, the spread of cancer cells to distant sites in the body.
These multifaceted mechanisms of action have generated significant interest in exploring fenretinide's potential to enhance the efficacy of other antineoplastic (anti-cancer) agents.
Ongoing research on fenretinide is also examining its pharmacokinetics, toxicology, and optimal dosing regimens to maximize its therapeutic potential while minimizing adverse effects.
Complementary studies have explored the compound's ability to modulate the immune system, further expanding its potential clinical applications.
Fenretinide, a structural analogue of ethanol absolute anhydrous, glyceryl tributyrate, and soy L-α-phosphatidylcholine, has been extensively studied in cell culture and animal models using techniques such as Image-Pro software and β-actin immunoblotting.
These investigations have shed light on fenretinide's mechanism of action and its potential synergies with other compounds, such as thapsigargin, in the context of cancer therapeutics.
By leveraging the insights gained from the comprehensive MeSH term description and the metadescription provided, researchers can optimize their fenretinide-related studies, enhancing reproducibility, accuracy, and the likelihood of uncovering novel therapeutic avenues.
The PubCompare.ai platform, for example, can be a valuable tool in this endeavor, enabling AI-driven comparisons of protocols from literature, preprints, and patents to identify the most effective approaches.