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1.
Rational Design,Synthesis, and Evaluation of Tetrahydroxamic Acid Chelators for Stable Complexation of Zirconium(IV) 下载免费PDF全文
Dr. François Guérard Dr. Yong‐Sok Lee Dr. Martin W. Brechbiel 《Chemistry (Weinheim an der Bergstrasse, Germany)》2014,20(19):5584-5591
Metals of interest for biomedical applications often need to be complexed and associated in a stable manner with a targeting agent before use. Whereas the fundamentals of most transition‐metal complexation processes have been thoroughly studied, the complexation of ZrIV has been somewhat neglected. This metal has received growing attention in recent years, especially in nuclear medicine, with the use of 89Zr, which a β+‐emitter with near ideal characteristics for cancer imaging. However, the best chelating agent known for this radionuclide is the trishydroxamate desferrioxamine B (DFB), the ZrIV complex of which exhibits suboptimal stability, resulting in the progressive release of 89Zr in vivo. Based on a recent report demonstrating the higher thermodynamic stability of the tetrahydroxamate complexes of ZrIV compared with the trishydroxamate complexes analogues to DFB, we designed a series of tetrahydroxamic acids of varying geometries for improved complexation of this metal. Three macrocycles differing in their cavity size (28 to 36‐membered rings) were synthesized by using a ring‐closing metathesis strategy, as well as their acyclic analogues. A solution study with 89Zr showed the complexation to be more effective with increasing cavity size. Evaluation of the kinetic inertness of these new complexes in ethylenediaminetetraacetic acid (EDTA) solution showed significantly improved stabilities of the larger chelates compared with 89Zr‐DFB, whereas the smaller complexes suffered from insufficient stabilities. These results were rationalized by a quantum chemical study. The lower stability of the smaller chelates was attributed to ring strain, whereas the better stability of the larger cyclic complexes was explained by the macrocyclic effect and by the structural rigidity. Overall, these new chelating agents open new perspectives for the safe and efficient use of 89Zr in nuclear imaging, with the best chelators providing dramatically improved stabilities compared with the reference DFB. 相似文献
2.
Many mushroom species are consumed as food, while significant numbers are also utilised medicinally. Mushrooms are rich in nutrients and bioactive compounds. A growing body of in vitro, in vivo, and human research has revealed their therapeutic potentials, which include such properties as anti-pathogenic, antioxidant, anti-inflammatory, immunomodulatory, gut microbiota enhancement, and angiotensin-converting enzyme 2 specificity. The uses of medicinal mushrooms (MMs) as extracts in nutraceuticals and other functional food and health products are burgeoning. COVID-19 presents an opportunity to consider how, and if, specific MM compounds might be utilised therapeutically to mitigate associated risk factors, reduce disease severity, and support recovery. As vaccines become a mainstay, MMs may have the potential as an adjunct therapy to enhance immunity. In the context of COVID-19, this review explores current research about MMs to identify the key properties claimed to confer health benefits. Considered also are barriers or limitations that may impact general recommendations on MMs as therapy. It is contended that the extraction method used to isolate bioactive compounds must be a primary consideration for efficacious targeting of physiological endpoints. Mushrooms commonly available for culinary use and obtainable as a dietary supplement for medicinal purposes are included in this review. Specific properties related to these mushrooms have been considered due to their potential protective and mediating effects on human exposure to the SARS CoV-2 virus and the ensuing COVID-19 disease processes. 相似文献
3.
The effect of irradiation on concentrations and relaxation behaviour of brain metabolites was studied by means of high-resolution 1H NMR in vitro. The studies were performed on rat brains irradiated with the doses of 20 Gy applied in fractions of 2 Gy. Standard procedures were used to obtain HClO4 extracts of rat brains. The 1H NMR studies of the extracts solutions in D2O were performed using a Varian Inova-300 NMR spectrometer. The integral intensities of the metabolite signals were found to change during the irradiation cycle and after it. These changes are accompanied by the variations in the T1 relaxation times. N-acetylaspartate, glycerophosphocholine, phosphocholine, choline, creatine and phosphocreatine, myoinositol and taurine were analysed as potential markers of irradiation injury. 相似文献
4.
PrF3 as well as PrF3-LiF and PrF3-MgF2 mixtures were investigated by means of high-energetic excitation with synchrotron radiation. In the PrF3 emission spectrum bands due to the intra-configurational 4f24f2 transitions originating from the 1S0 level of the Pr3+ ion have been identified. The emission from the 3P0 multiplet is very weak due to non-radiative decay by cross-relaxation processes. Therefore, PrF3 is not an efficient direct cascade emitter. In the PrF3 excitation spectra in the ultraviolet/vacuum-ultraviolet spectral range, the 3H41S0 transition at 46858 cm-1 as well as broad bands due to the inter-configurational 4f24f5d transitions are observed. By comparison with data of Pr3+ doped YF3, the branching ratios of the emission transitions for PrF3 from the 1S0 were determined; these are 0.008, 0.075, 0.262, 0.023 and 0.629 for transitions 1S03H4, 3F4, 1G4, 1D2 and 1I6, respectively. For the polycrystalline PrF3-LiF and PrF3-MgF2 samples investigated by us, the measured emission and excitation spectra are nearly identical
to those of PrF3. For polycrystalline PrF3-KMgF3 the observed spectra are superpositions of the PrF3 and Pr3+:KMgF3 spectra. PACS 42.70.-a; 78.55.-m; 78.55.Hx 相似文献
5.
6.
Moxifloxacin is a representative of the fourth generation of fluoroquinolones. It possesses bacteriostatic activity against Gram-positive and Gram-negative bacteria. A simple and fast high performance liquid chromatography-ultraviolet detection (HPLC-UV) method was developed for moxifloxacin analysis. The separation was performed on C18 column. The mobile phase was a mixture of acetonitrile and 0.4% triethylamine solution. The regression curve was linear over the range 0.2–10.0?µg/mL. The validation parameters obey the European Medicine Agency limits. The in vivo study confirmed the practical application of the method. 相似文献
7.
Malek SN Lee GS Hong SL Yaacob H Wahab NA Faizal Weber JF Shah SA 《Molecules (Basel, Switzerland)》2011,16(6):4539-4548
Investigations on the cytotoxic effects of the crude methanol and fractionated extracts (hexane, ethyl acetate) C. mangga against six human cancer cell lines, namely the hormone-dependent breast cell line (MCF-7), nasopharyngeal epidermoid cell line (KB), lung cell line (A549), cervical cell line (Ca Ski), colon cell lines (HCT 116 and HT-29), and one non-cancer human fibroblast cell line (MRC-5) were conducted using an in-vitro neutral red cytotoxicity assay. The crude methanol and fractionated extracts (hexane and ethyl acetate) displayed good cytotoxic effects against MCF-7, KB, A549, Ca Ski and HT-29 cell lines, but exerted no damage on the MRC-5 line. Chemical investigation from the hexane and ethyl acetate fractions resulted in the isolation of seven pure compounds, namely (E)-labda-8(17),12-dien-15,16-dial (1), (E)-15,16-bisnor-labda-8(17),11-dien-13-on (2), zerumin A (3), β-sitosterol, curcumin, demethoxycurcumin and bis-demethoxycurcumin. Compounds 1 and 3 exhibited high cytotoxic effects against all six selected cancer cell lines, while compounds 2 showed no anti-proliferative activity on the tested cell lines. Compound 1 also demonstrated strong cytotoxicity against the normal cell line MRC-5. This paper reports for the first time the cytotoxic activities of C. mangga extracts on KB, A549, Ca Ski, HT-29 and MRC-5, and the occurrence of compound 2 and 3 in C. mangga. 相似文献
8.
Michelle Min Fang Yee Kok-Yong Chin Soelaiman Ima-Nirwana Sok Kuan Wong 《Molecules (Basel, Switzerland)》2021,26(6)
Vitamin A is a fat-soluble micronutrient essential for growth, immunity, and good vision. The preformed retinol is commonly found in food of animal origin whereas provitamin A is derived from food of plant origin. This review summarises the current evidence from animal, human and cell-culture studies on the effects of vitamin A towards bone health. Animal studies showed that the negative effects of retinol on the skeleton were observed at higher concentrations, especially on the cortical bone. In humans, the direct relationship between vitamin A and poor bone health was more pronounced in individuals with obesity or vitamin D deficiency. Mechanistically, vitamin A differentially influenced the stages of osteogenesis by enhancing early osteoblastic differentiation and inhibiting bone mineralisation via retinoic acid receptor (RAR) signalling and modulation of osteocyte/osteoblast-related bone peptides. However, adequate vitamin A intake through food or supplements was shown to maintain healthy bones. Meanwhile, provitamin A (carotene and β-cryptoxanthin) may also protect bone. In vitro evidence showed that carotene and β-cryptoxanthin may serve as precursors for retinoids, specifically all-trans-retinoic acid, which serve as ligand for RARs to promote osteogenesis and suppressed nuclear factor-kappa B activation to inhibit the differentiation and maturation of osteoclasts. In conclusion, we suggest that both vitamin A and provitamin A may be potential bone-protecting agents, and more studies are warranted to support this hypothesis. 相似文献
9.
Giuseppe Chirico Prof. Maddalena Collini Prof. Laura D'Alfonso Prof. Franck Denat Prof. Yuri A. Diaz‐Fernandez Dr. Luca Pasotti Dr. Yoann Rousselin Dr. Nicolas Sok Dr. Piersandro Pallavicini Prof. 《Chemphyschem》2008,9(12):1729-1737
Potentiometric titrations, fluorescence versus pH titrations, dynamic light scattering and fluorescence polarization anisotropy studies demonstrate that inside the nanodimensioned Triton X‐100 micelles, 1‐pyrenecarboxylic acid, PCOO?, forms an apical complex with the Zn2+ cation encircled by a lipophilic cyclen ligand and hugely increasing its fluorescence. The ability of the Zn2+‐cyclen‐PCOO? complex plus its micellar container to act as a fluorescent sensor to evaluate the lipophilicity of molecular species is demonstrated on the fatty acid series CH3(CH2)xCOOH (x=0–16). At pH 7.4 a decrease in fluorescence is observed on the addition of fatty acids that is directly related to their chain length, that is, to their tendency to enter the micellar containers, where they dislocate PCOO? from the Zn2+ centre. The independent determination of fatty acid pKa values in the presence of Triton X‐100 micelles confirms that our fluorescent micellar device is capable of sensing their lipophilicity. 相似文献
10.
I. Sokólska 《Applied physics. B, Lasers and optics》2000,71(2):157-162
LaGaO3 crystals doped with Er3+ ions were grown by the Czochralski method and their optical properties were examined. The Er3+ energy levels have been determined from the low-temperature absorption and emission spectra. The results of Judd–Ofelt analysis
are presented and compared with experimental data. The emission cross sections are determined for the 4
I
13/2→4
I
15/2 (1.55 μm) and 4
I
11/2→4
I
13/2 (2.85 μm) transitions of erbium.
Received: 6 December 1999 / Revised version: 10 February 2000 / Published online: 27 April 2000 相似文献