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Amyloid imaging using fluorine-19 magnetic resonance imaging ((19)F-MRI)

Tooyama I, Yanagisawa D, Taguchi H, Kato T, Hirao K, Shirai N, et al.

Ageing Res Rev, 2016 09;30:85-94.
PMID: 26772439 DOI: 10.1016/j.arr.2015.12.008

The formation of senile plaques followed by the deposition of amyloid-β is the earliest pathological change in Alzheimer's disease. Thus, the detection of senile plaques remains the most important early diagnostic indicator of Alzheimer's disease. Amyloid imaging is a noninvasive technique for visualizing senile plaques in the brains of Alzheimer's patients using positron emission tomography (PET) or magnetic resonance imaging (MRI). Because fluorine-19 ((19)F) displays an intense nuclear magnetic resonance signal and is almost non-existent in the body, targets are detected with a higher signal-to-noise ratio using appropriate fluorinated contrast agents. The recent introduction of high-field MRI allows us to detect amyloid depositions in the brain of living mouse using (19)F-MRI. So far, at least three probes have been reported to detect amyloid deposition in the brain of transgenic mouse models of Alzheimer's disease; (E,E)-1-fluoro-2,5-bis-(3-hydroxycarbonyl-4-hydroxy)styrylbenzene (FSB), 1,7-bis(4'-hydroxy-3'-trifluoromethoxyphenyl)-4-methoxycarbonylethyl-1,6-heptadiene3,5-dione (FMeC1, Shiga-Y5) and 6-(3',6',9',15',18',21'-heptaoxa-23',23',23'-trifluorotricosanyloxy)-2-(4'-dimethylaminostyryl)benzoxazole (XP7, Shiga-X22). This review presents the recent advances in amyloid imaging using (19)F-MRI, including our own studies.

Matched MeSH terms: Fluorine*
The quantification of PET-CT radiotracers to determine minimal scan time using quadratic formulation

Said MA, Musarudin M, Zulkaffli NF

Ann Nucl Med, 2020 Dec;34(12):884-891.
PMID: 33141408 DOI: 10.1007/s12149-020-01543-x

OBJECTIVE: 18F is the most extensively used radioisotope in current clinical practices of PET imaging. This selection is based on the several criteria of pure PET radioisotopes with an optimum half-life, and low positron energy that contributes to a smaller positron range. In addition to 18F, other radioisotopes such as 68Ga and 124I are currently gained much attention with the increase in interest in new PET tracers entering the clinical trials. This study aims to determine the minimal scan time per bed position (Tmin) for the 124I and 68Ga based on the quantitative differences in PET imaging of 68Ga and 124I relative to 18F.
METHODS: The European Association of Nuclear Medicine (EANM) procedure guidelines version 2.0 for FDG-PET tumor imaging has adhered for this purpose. A NEMA2012/IEC2008 phantom was filled with tumor to background ratio of 10:1 with the activity concentration of 30 kBq/ml ± 10 and 3 kBq/ml ± 10% for each radioisotope. The phantom was scanned using different acquisition times per bed position (1, 5, 7, 10 and 15 min) to determine the Tmin. The definition of Tmin was performed using an image coefficient of variations (COV) of 15%.
RESULTS: Tmin obtained for 18F, 68Ga and 124I were 3.08, 3.24 and 32.93 min, respectively. Quantitative analyses among 18F, 68Ga and 124I images were performed. Signal-to-noise ratio (SNR), contrast recovery coefficients (CRC), and visibility (VH) are the image quality parameters analysed in this study. Generally, 68Ga and 18F gave better image quality as compared to 124I for all the parameters studied.
CONCLUSION: We have defined Tmin for 18F, 68Ga and 124I SPECT CT imaging based on NEMA2012/IEC2008 phantom imaging. Despite the long scanning time suggested by Tmin, improvement in the image quality is acquired especially for 124I. In clinical practice, the long acquisition time, nevertheless, may cause patient discomfort and motion artifact.

Matched MeSH terms: Fluorine Radioisotopes/chemistry
Correlation between 18F-FDG dosage and SNR on various BMI patient groups tested in NEMA IEC PET phantom

Waeleh N, Saripan MI, Musarudin M, Mashohor S, Ahmad Saad FF

Appl Radiat Isot, 2021 Oct;176:109885.
PMID: 34385090 DOI: 10.1016/j.apradiso.2021.109885

The present study was conducted to determine quantitatively the correlation between injected radiotracer and signal-to-noise ratio (SNR) based on differences in physiques and stages of cancer. Eight different activities were evaluated with modelled National Electrical Manufacturers Association (NEMA) of the International Electrotechnical Commission (IEC) PET's phantom with nine different tumour-to-background ratio (TBR). The findings suggest that the optimal value of dosage is required for all categories of patients in the early stages of cancer diagnosis.

Matched MeSH terms: Fluorine Radioisotopes/administration & dosage*
Fulltext Ligninolytic fungus Polyporus sp. S133 mediated metabolic degradation of fluorene

Lazim ZM, Hadibarata T

Braz J Microbiol, 2016 Jul-Sep;47(3):610-6.
PMID: 27287336 DOI: 10.1016/j.bjm.2016.04.015

This study aimed to investigate the impact of nonionic surfactants on the efficacy of fluorine degradation by Polyporus sp. S133 in a liquid culture. Fluorene was observed to be degraded in its entirety by Polyporus sp. S133 subsequent to a 23-day incubation period. The fastest cell growth rate was observed in the initial 7 days in the culture that was supplemented with Tween 80. The degradation process was primarily modulated by the activity of two ligninolytic enzymes, laccase and MnP. The highest laccase activity was stimulated by the addition of Tween 80 (2443U/L) followed by mixed surfactant (1766U/L) and Brij 35 (1655U/L). UV-vis spectroscopy, TLC analysis and mass spectrum analysis of samples subsequent to the degradation process in the culture medium confirmed the biotransformation of fluorene. Two metabolites, 9-fluorenol (λmax 270, tR 8.0min and m/z 254) and protocatechuic acid (λmax 260, tR 11.3min and m/z 370), were identified in the treated medium.

Matched MeSH terms: Fluorine
Fluorinated photoreduced graphene oxide with semi-ionic C-F bonds: An effective carbon based photocatalyst for the removal of volatile organic compounds

Tai XH, Hung WS, Yang TCK, Lai CW, Lee KM, Chen CY, et al.

Chemosphere, 2024 Feb;349:140890.
PMID: 38072201 DOI: 10.1016/j.chemosphere.2023.140890

There is much interest in developing metal-free halogenated graphene such as fluorinated graphene for various catalytic applications. In this work, a fluorine-doped graphene oxide photocatalyst was investigated for photocatalytic oxidation (PCO) of a volatile organic compound (VOC), namely gaseous methanol. The fluorination process of graphene oxide (GO) was carried out via a novel and facile solution-based photoirradiation method. The fluorine atoms were doped on the surface of the GO in a semi-ionic C-F bond configuration. This presence of the semi-ionic C-F bonds induced a dramatic 7-fold increment of the hole charge carrier density of the photocatalyst. The fluorinated GO photocatalyst exhibited excellent photodegradation up to 93.5% or 0.493 h-1 according pseudo-first order kinetics for methanol. In addition, 91.7% of methanol was mineralized into harmless carbon dioxide (CO2) under UV-A irradiation. Furthermore, the photocatalyst demonstrated good stability in five cycles of methanol PCO. Besides methanol, other VOCs such as acetone and formaldehyde were also photodegraded. This work reveals the potential of fluorination in producing effective graphene-based photocatalyst for VOC removal.

Matched MeSH terms: Fluorine/chemistry
18F-PSMA-1007 PET/CT for Initial Staging of Renal Cell Carcinoma in an End-Stage Renal Disease Patient

Marafi F, Sasikumar A, Aldaas M, Esmail A

Clin Nucl Med, 2021 Jan;46(1):e65-e67.
PMID: 33181733 DOI: 10.1097/RLU.0000000000003354

A 46-year-old man with end-stage renal disease and renal cell carcinoma underwent F-FDG PET/CT for initial staging followed by F-PSMA-1007 PET/CT. Unlike F-FDG, which undergoes renal clearance, F-PSMA-1007 undergoes hepatobiliary clearance and thus generates superior quality images. F-PSMA-1007 PET/CT showed intense tracer-avid left renal mass lesion (FDG nonavid); lytic bone lesions (FDG avid) and single liver lesion (FDG nonavid). This case highlights the superiority of F-PSMA-1007 over F-FDG PET/CT in identifying primary lesion as well as metastatic sites in case of renal cell carcinoma even in the presence of end-stage renal disease.

Matched MeSH terms: Fluorine Radioisotopes
18F-labeled Bisphosphonate as an Alternative Candidate to the Gold Standard[18F]sodium fluoride ([18F]NaF) for PET Bone Imaging

Hassan H, Othman MF, Razak HRA

Curr Med Imaging, 2021;17(11):1271-1275.
PMID: 33593263 DOI: 10.2174/1573405617666210216091202

Bone metastases are a common source of malignancy in the skeleton and occur much more often than primary bone cancer. Several works were being performed to identify early markers for bone metastasis and novel drug targets to improve patients' quality of life. As some concerns exist with the [18F]sodiumfluoridein positron emission tomography (PET) bone imaging, there has been an increase in the number of targeted radiopharmaceutical markers for bone metastases imaging in its competitor, 68Ga. Since 18F properties are superior to those of 68Ga, there is a distinct motivation for developing 18F radiopharmaceuticals for bone metastases imaging.

Matched MeSH terms: Fluorine Radioisotopes
Optimising the Azeotropic Drying of 18F-Fluorine Wayto Improve the 18F-Fluorocholine Radiochemical Yield

Hassan H, Bakar SA, Halim KN, Idris J, Saad FF, Nordin AJ

Curr Radiopharm, 2016;9(2):121-7.
PMID: 26239237

BACKGROUND AND OBJECTIVE: 18F-Fluorocholine has been suggested as one of the reputable imaging tracers for diagnosis of prostate tumour in Positron Emission Tomography / Computed Tomography (PET/CT) modality. Nevertheless, it has never been synthesised in Malaysia. We acknowledged that the major problem with 18F-Fluorocholine is due to its relatively low radiochemical yield at the end of synthesis (EOS). Therefore, this article presents improved 18FFluorocholine radiochemical yields after carrying out optimisation on azeotropic drying of 18F-Fluorine.
METHODS: In the previous study, the azeotropic drying of non-carrier-added (n.c.a) 18F-Fluorine in the reactor was conducted at atmospheric pressure (0 atm) and shorter duration time. In this study, however, the azeotropic drying of non-carried-added (n.c.a) 18FFluorine was made at a high vacuum pressure (- 0.65 to - 0.85 bar) with an additional time of 30 seconds. At the end of the synthesis, the mean radiochemical yield was statistically compared between the two azeotropic drying conditions so as to observe whether the improvement made was significant to the radiochemical yield.
RESULTS: From the paired sample t-test analysis, the improvement done to the azeotropic drying of non-carrier-added (n.c.a) 18F-Fluorine was statistically significant (p < 0.05). With the improvement made, the 18F-Fluorcholine radiochemical yield was found to have increase by one fold.
CONCLUSION: Improved 18F-Fluorocholine radiochemical yields were obtained after the improvement had been done to the azeotropic drying of non-carrier-added (n.c.a) 18F-Fluorine. It was also observed that improvement made to the azeotropic drying of non-carrier-added (n.c.a) 18F-Fluorine did not affect the 18F-Fluorocholine quality control analysis.

Matched MeSH terms: Fluorine Radioisotopes/chemistry*
Analytical GC-FID Method for the Determination of Organic Solvents in Radiopharmaceuticals

Hassan H, Othman MF, Zakaria ZA, Saad FFA, Abdul Razak HR

Curr Radiopharm, 2021;14(2):131-144.
PMID: 33115398 DOI: 10.2174/1874471013999201027215704

BACKGROUND: Organic solvents play an indispensable role in most of the radiopharmaceutical production stages. It is almost impossible to remove them entirely in the final formulation of the product.
OBJECTIVE: In this presented work, an analytical method by gas chromatography coupled with flame ionization detection (GC-FID) has been developed to determine organic solvents in radiopharmaceutical samples. The effect of injection holding time, temperature variation in the injection port, and the column temperature on the analysis time and resolution (R ≥ 1.5) of ethanol and acetonitrile was studied extensively.
METHODS: The experimental conditions were optimized with the aid of further statistical analysis; thence, the proposed method was validated following the International Council for Harmonisation (ICH) Q2 (R1) guideline.
RESULTS: The proposed analytical method surpassed the acceptance criteria including the linearity > 0.990 (correlation coefficient of R2), precision < 2%, LOD, and LOQ, accuracy > 90% for all solvents. The separation between ethanol and acetonitrile was acceptable with a resolution R > 1.5. Further statistical analysis of Oneway ANOVA revealed that the increment in injection holding time and variation of temperature at the injection port did not significantly affect the analysis time. Nevertheless, the variation in injection port temperature substantially influenced the resolution of ethanol and acetonitrile peaks (p < 0.05).
CONCLUSION: The proposed analytical method has been successfully implemented to determine the organic solvent in the [18F]fluoro-ethyl-tyrosine ([18F]FET), [18F]fluoromisonidazole ([18F]FMISO), and [18F]fluorothymidine ([18F]FLT).

Matched MeSH terms: Fluorine Radioisotopes/analysis; Fluorine Radioisotopes/chemistry*
Fulltext Dataset of theoretical Molecular Electrostatic Potential (MEP), Highest Occupied Molecular Orbital-Lowest Unoccupied Molecular Orbital (HOMO-LUMO) band gap and experimental cole-cole plot of 4-(ortho-, meta- and para-fluorophenyl)thiosemicarbazide isomers

Silvarajoo S, Osman UM, Kamarudin KH, Razali MH, Yusoff HM, Bhat IUH, et al.

Data Brief, 2020 Oct;32:106299.
PMID: 32984485 DOI: 10.1016/j.dib.2020.106299

One-pot synthetic method was adopted to prepare three isomers 4-(ortho-fluorophenyl)thiosemi- carbazide), 4-(meta-fluorophenyl)thiosemicarbazide and 4-(para-fluorophenyl)thiosemicarbazide. The products were obtained in ethanolic solution from a reaction between ortho, meta and para derivatives of fluorophenyl isothiocyanate and hydrazine hydrate. This work presents the theoretical Molecular Electrostatic Potential (MEP) and Highest Occupied Molecular Orbital-Lowest Unoccupied Molecular Orbital (HOMO-LUMO) computational data through Gaussview 5.0.9 and Gaussian09 software. Experimental Cole-cole plot for conductivity determination was also illustrated. The present data is important to manipulate the properties of compounds according to the position of a fluorine atom.

Matched MeSH terms: Fluorine
Synthesis, characterization, and anti-cancer activity of new chalcone derivatives containing naphthalene and fluorine moieties

Lim YH, Oo CW, Koh RY, Voon GL, Yew MY, Yam MF, et al.

Drug Dev Res, 2020 Jul 28.
PMID: 32720715 DOI: 10.1002/ddr.21715

In recent years, chalcones and their derivatives have become the focus of global scientists due to increasing evidence reported towards their potency in antitumor and anti-cancer. Here, the chalcones designed and synthesized in our present study were derived from the derivatives of naphthaldehyde and acetophenone. Both these precursors have been reported in demonstrating a certain degree of anticancer property. Also, the substituents on these precursors such as hydroxyl, methoxy, prenyl, and chloro were shown able to enhance the anticancer efficiency. Hence, it is the interest of the current study to investigate the anticancer potential of the hybrid molecules (chalcones) consisting of these precursors with different alkoxy substituents and with or without the fluorine moiety. Two series of chalcone derivatives were designed, synthesized, and characterized using the elemental analysis, IR, 1 H and 13 C NMR spectroscopy, subsequently evaluated for their anti-cancer activity. Interestingly, the results showed that the fluorinated chalcones 11-15 exhibited stronger cytotoxic activity towards the breast cancer cell lines (4T1) compared to non-fluorinated chalcone derivatives. Remarkably, the selectivity index obtained for these fluorinated chalcones derivatives against the breast cancer 4T1 cell line was higher than those exhibited by cisplatin, which is one of the most frequently deployed chemotherapy agents in current medical practice. These findings could provide an insight towards the potential of fluorinated chalcones being developed as an anti-cancer agent with moderate activity towards breast cancer cell and low inhibition of fibroblast cell at a concentration of 100 μM.

Matched MeSH terms: Fluorine
Fulltext Synthesis of GO-ZnO via impregnation method for fluoride removal in wastewater

Mohamad Hanafi Mohamad Rosli, Nurulhuda Amri, Norhusna Mohamad Nor

ESTEEM Academic Journal, 2019;15(2):35-43.
MyJurnal

High concentration of fluoride in wastewater discharge from various industries is threatening the environment due to its hazardous effects and properties. This research work aims to develop an efficient adsorbent for fluoride removal in wastewater. Graphite oxide (GO) was impregnated
with ZnO nanoparticles as an adsorbent, and the effect of synthesis parameters of GO-ZnO adsorbent for fluoride removal were studied (sonication temperature, synthesis time, and ratio of GO to ZnO). The surface functional groups of these synthesized adsorbents were analyzed by
using FTIR. The synthesis parameters that contribute to the highest adsorption capacity and percentage removal are 5:1 ratio of GO-ZnO, 45 ºC of sonication temperature and 60 minutes of synthesis time, respectively. The highest value of adsorption capacity obtained from the fluoride
removal is 55.5 mg/g. The functional groups contained in the GO-ZnO adsorbent are hydroxyl group (O-H), C=O group, aromatics group, carboxyl group (C-O), epoxy group and alkoxy group. These functional groups showed significant impact towards fluoride adsorption due to the bonding of fluoride ion to the functional groups.

Matched MeSH terms: Fluorine; Fluorine Compounds
Improving the (18)F-fluoromethylcholine ((18)F-FCH) radiochemical yield via optimising the azeotropic drying of non-carrier-added (18)F-fluorine

Hassan H, Abu Bakar S, Halim KN, Idris J, Ahmad Saad FF, Nordin AJ

J Labelled Comp Radiopharm, 2015 Sep-Oct;58(11-12):458-9.
PMID: 26395258 DOI: 10.1002/jlcr.3347

(18)F-Fluoromethylcholine ((18)F-FCH) has been suggested as one of the reputable imaging tracers for diagnosis of prostate tumour in PET/CT examination. Nevertheless, it has never been synthesised in Malaysia. We acknowledged the major problem with (18)F-FCH is due to its relatively low radiochemical yield at the end of synthesis (EOS). Therefore, this technical note presents improved (18)F-FCH radiochemical yields after carrying out optimisation on azeotropic drying of non-carrier-added (18)F-Fluorine.

Matched MeSH terms: Fluorine
Fluorine-19 magnetic resonance imaging probe for the detection of tau pathology in female rTg4510 mice

Yanagisawa D, Ibrahim NF, Taguchi H, Morikawa S, Kato T, Hirao K, et al.

J Neurosci Res, 2018 05;96(5):841-851.
PMID: 29063641 DOI: 10.1002/jnr.24188

Aggregation of tau into neurofibrillary tangles (NFTs) is characteristic of tauopathies, including Alzheimer's disease. Recent advances in tau imaging have attracted much attention because of its potential contributions to early diagnosis and monitoring of disease progress. Fluorine-19 magnetic resonance imaging (19 F-MRI) may be extremely useful for tau imaging once a high-quality probe has been formulated. In this investigation, a novel fluorine-19-labeling compound has been developed as a probe for tau imaging using 19 F-MRI. This compound is a buta-1,3-diene derivative with a polyethylene glycol side chain bearing a CF3 group and is known as Shiga-X35. Female rTg4510 mice (a mouse model of tauopathy) and wild-type mice were intravenously injected with Shiga-X35, and magnetic resonance imaging of each mouse's head was conducted in a 7.0-T horizontal-bore magnetic resonance scanner. The 19 F-MRI in rTg4510 mice showed an intense signal in the forebrain region. Analysis of the signal intensity in the forebrain region revealed a significant accumulation of fluorine-19 magnetic resonance signal in the rTg4510 mice compared with the wild-type mice. Histological analysis showed fluorescent signals of Shiga-X35 binding to the NFTs in the brain sections of rTg4510 mice. Data collected as part of this investigation indicate that 19 F-MRI using Shiga-X35 could be a promising tool to evaluate tau pathology in the brain.

Matched MeSH terms: Fluorine*; Fluorine-19 Magnetic Resonance Imaging/methods*
Textitis as Seen on 18F-NaF Imaging Using an Ultra-High-Resolution Positron Emission Mammography Scanner

Usmani S, Rasheed R, Al Kandari F

J Nucl Med Technol, 2020 Jun;48(2):181-183.
PMID: 32111663 DOI: 10.2967/jnmt.119.235986

Textitis is a new term used to refer to the degenerative-strain osteoarthritis that comes from excessive use of a smart phone. 18F-NaF is increasingly used in diagnosing skeletal pain that is not identified on radiographs. We report a case of a 26-y-old woman with left breast cancer referred for 18F-NaF PET/CT, who was complaining of right thumb and wrist pain. Findings were negative for bone secondaries. Dedicated hands views were acquired on a positron emission mammography scanner and showed focal uptake at the first carpometacarpal and second metacarpophalangeal joints. On the basis of the strong history, the findings were likely due to active arthritic changes caused by repetitive strain injury from excessive text messaging.

Matched MeSH terms: Fluorine Radioisotopes*
Mottled enamel as evidenc of endemice fluorosis in the Sabak area of the Sg. Bernam, Kuala Selangor, Selangor

Tratman EK

Journal of the Malaya Branch of the British Medical Association, 1940;4:181-3.

Matched MeSH terms: Fluorine
Fulltext Controllable Electrochemical Synthesis of Reduced Graphene Oxide Thin-Film Constructed as Efficient Photoanode in Dye-Sensitized Solar Cells

Chong SW, Lai CW, Abd Hamid SB

Materials (Basel), 2016 Jan 25;9(2).
PMID: 28787869 DOI: 10.3390/ma9020069

A controllable electrochemical synthesis to convert reduced graphene oxide (rGO) from graphite flakes was introduced and investigated in detail. Electrochemical reduction was used to prepare rGO because of its cost effectiveness, environmental friendliness, and ability to produce rGO thin films in industrial scale. This study aimed to determine the optimum applied potential for the electrochemical reduction. An applied voltage of 15 V successfully formed a uniformly coated rGO thin film, which significantly promoted effective electron transfer within dye-sensitized solar cells (DSSCs). Thus, DSSC performance improved. However, rGO thin films formed in voltages below or exceeding 15 V resulted in poor DSSC performance. This behavior was due to poor electron transfer within the rGO thin films caused by poor uniformity. These results revealed that DSSC constructed using 15 V rGO thin film exhibited high efficiency (η = 1.5211%) attributed to its higher surface uniformity than other samples. The addition of natural lemon juice (pH ~ 2.3) to the electrolyte accelerated the deposition and strengthened the adhesion of rGO thin film onto fluorine-doped tin oxide (FTO) glasses.

Matched MeSH terms: Fluorine
Fulltext New Diethyl Ammonium Salt of Thiobarbituric Acid Derivative: Synthesis, Molecular Structure Investigations and Docking Studies

Barakat A, Al-Majid AM, Soliman SM, Lotfy G, Ghabbour HA, Fun HK, et al.

Molecules, 2015;20(11):20642-58.
PMID: 26610441 DOI: 10.3390/molecules201119710

The synthesis of the new diethyl ammonium salt of diethylammonium(E)-5-(1,5-bis(4-fluorophenyl)-3-oxopent-4-en-1-yl)-1,3-diethyl-4,6-dioxo-2-thioxohexaydropyrimidin-5-ide 3 via a regioselective Michael addition of N,N-diethylthiobarbituric acid 1 to dienone 2 is described. In 3, the carboanion of the thiobarbituric moiety is stabilized by the strong intramolecular electron delocalization with the adjacent carbonyl groups and so the reaction proceeds without any cyclization. The molecular structure investigations of 3 were determined by single-crystal X-ray diffraction as well as DFT computations. The theoretically calculated (DFT/B3LYP) geometry agrees well with the crystallographic data. The effect of fluorine replacement by chlorine atoms on the molecular structure aspects were investigated using DFT methods. Calculated electronic spectra showed a bathochromic shift of the π-π* transition when fluorine is replaced by chlorine. Charge decomposition analyses were performed to study possible interaction between the different fragments in the studied systems. Molecular docking simulations examining the inhibitory nature of the compound show an anti-diabetic activity with Pa (probability of activity) value of 0.229.

Matched MeSH terms: Fluorine
Fulltext Synthesis of [18F]F-γ-T-3, a Redox-Silent γ-Tocotrienol (γ-T-3) Vitamin E Analogue for Image-Based In Vivo Studies of Vitamin E Biodistribution and Dynamics

Roselt P, Cullinane C, Noonan W, Elsaidi H, Eu P, Wiebe LI

Molecules, 2020 Dec 03;25(23).
PMID: 33287202 DOI: 10.3390/molecules25235700

Vitamin E, a natural antioxidant, is of interest to scientists, health care pundits and faddists; its nutritional and biomedical attributes may be validated, anecdotal or fantasy. Vitamin E is a mixture of tocopherols (TPs) and tocotrienols (T-3s), each class having four substitutional isomers (α-, β-, γ-, δ-). Vitamin E analogues attain only low concentrations in most tissues, necessitating exacting invasive techniques for analytical research. Quantitative positron emission tomography (PET) with an F-18-labeled molecular probe would expedite access to Vitamin E's biodistributions and pharmacokinetics via non-invasive temporal imaging. (R)-6-(3-[18F]Fluoropropoxy)-2,7,8-trimethyl-2-(4,8,12-trimethyltrideca-3,7,11-trien-1-yl)-chromane ([18F]F-γ-T-3) was prepared for this purpose. [18F]F-γ-T-3 was synthesized from γ-T-3 in two steps: (i) 1,3-di-O-tosylpropane was introduced at C6-O to form TsO-γ-T-3, and (ii) reaction of this tosylate with [18F]fluoride in DMF/K222. Non-radioactive F-γ-T-3 was synthesized by reaction of γ-T-3 with 3-fluoropropyl methanesulfonate. [18F]F-γ-T-3 biodistribution in a murine tumor model was imaged using a small-animal PET scanner. F-γ-T-3 was prepared in 61% chemical yield. [18F]F-γ-T-3 was synthesized in acceptable radiochemical yield (RCY 12%) with high radiochemical purity (>99% RCP) in 45 min. Preliminary F-18 PET images in mice showed upper abdominal accumulation with evidence of renal clearance, only low concentrations in the thorax (lung/heart) and head, and rapid clearance from blood. [18F]F-γ-T-3 shows promise as an F-18 PET tracer for detailed in vivo studies of Vitamin E. The labeling procedure provides acceptable RCY, high RCP and pertinence to all eight Vitamin E analogues.

Matched MeSH terms: Fluorine Radioisotopes/pharmacokinetics; Fluorine Radioisotopes/chemistry*
Fulltext Fluorine-19 Magnetic Resonance Imaging for Detection of Amyloid β Oligomers Using a Keto Form of Curcumin Derivative in a Mouse Model of Alzheimer's Disease

Yanagisawa D, Ibrahim NF, Taguchi H, Morikawa S, Tomiyama T, Tooyama I

Molecules, 2021 Mar 04;26(5).
PMID: 33806326 DOI: 10.3390/molecules26051362

Recent evidence suggests that the formation of soluble amyloid β (Aβ) aggregates with high toxicity, such as oligomers and protofibrils, is a key event that causes Alzheimer's disease (AD). However, understanding the pathophysiological role of such soluble Aβ aggregates in the brain in vivo could be difficult due to the lack of a clinically available method to detect, visualize, and quantify soluble Aβ aggregates in the brain. We had synthesized a novel fluorinated curcumin derivative with a fixed keto form, named as Shiga-Y51, which exhibited high selectivity to Aβ oligomers in vitro. In this study, we investigated the in vivo detection of Aβ oligomers by fluorine-19 (19F) magnetic resonance imaging (MRI) using Shiga-Y51 in an APP/PS1 double transgenic mouse model of AD. Significantly high levels of 19F signals were detected in the upper forebrain region of APP/PS1 mice compared with wild-type mice. Moreover, the highest levels of Aβ oligomers were detected in the upper forebrain region of APP/PS1 mice in enzyme-linked immunosorbent assay. These findings suggested that 19F-MRI using Shiga-Y51 detected Aβ oligomers in the in vivo brain. Therefore, 19F-MRI using Shiga-Y51 with a 7 T MR scanner could be a powerful tool for imaging Aβ oligomers in the brain.

Matched MeSH terms: Fluorine-19 Magnetic Resonance Imaging/methods*

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