Lactosyl ceramide analogues carrying novel bifunctional BODIPY-based fluorescent tags were designed and synthesised for live cell imaging. Addition of azide functionality on the fluorophore facilitated isobaric tagging for quantitative multiplexed analysis of biomolecules based on tandem mass spectrometry.

Thymic stromal lymphopoietin (TSLP) plays an important role in the differentiation and proliferation of Th2 cells, resulting in eosinophilic inflammation and numerous allergic diseases. Baicalein ( 1 ), a major component of Scutellaria baicalensis , was found to be the first small molecule to block TSLP signaling pathways. It inhibited effectively eosinophil infiltration in house dust mite-induced and ovalbumin-challenged mouse models. Structure-activity relationship studies identified compound 11a , a biphenyl flavanone analog, as a novel human TSLP inhibitor for the discovery and development of new anti-allergic drugs.

Four novel chiral anionic surfactants having carbohydrate hydrophilic heads, sodium n-dodecyl 1-thio-beta-D-glucopyranoside 6-hydrogen sulfate (6-betaGlcD), sodium n-dodecyl 1-thio-beta-L-glucopyranoside 6-hydrogen sulfate (6-betaGlcL), sodium n-dodecyl 1-thio-beta-L-fucopyranoside 3-hydrogen sulfate (3-betaFucL), and sodium n-dodecyl 1-thio-alpha-L-rhamnopyranoside 3-hydrogen sulfate (3-alphaRhaL), were synthesized by selective sulfation of the corresponding thioglycosides. Their CMC determined by fluorescence using pyrene as a probe in water was 1.3-2.7 mM. These surfactants found to be useful as chiral selectors for enantiomeric separation by MEKC. The enantiomeric separation was optimized with respect to pH, buffer concentration, and surfactant concentration. Under the optimized conditions (50 mM phosphate buffer at pH 6.5, 30 mM surfactant, 20 kV), the enantiomeric separations of five dansylated amino acids (Dns-AAs) were achieved within approximately 20 min with the migration order of Val

There are few hybrid positron emission tomography (PET)/fluorescence imaging agents available for brain imaging. For this purpose, BODIPY dye is very attractive because one of its fluorine atoms can be readily exchanged with 18F, and it can be modified to produce red-shifted fluorescence. In this study, therefore, we synthesized and investigated a 18F-labeled red-shifted BODIPY dye as a prosthetic group for brain hybrid PET/optical imaging agents and determined the optimal dose of this radioligand for hybrid imaging. The red-shifted BODIPY dye (1) was synthesized, and one of its fluorine atoms was exchanged with 18F using SnCl4 in high yield. Partition coefficients of 18F-labeled BODIPY dye ([18F]1) and 1 were measured using its radioactivity and fluorescence, respectively, which were shown to be suitable for brain penetration. Optimal dose for hybrid imaging was determined by analysis of PET/CT and optical images of Balb/C nude mice injected with [18F]1 and 1, respectively. Hybrid PET/optical images of mice injected with optimal dose of [18F]1 showed strong radioactivity and fluorescence signal in the brain at 2 min after injection, with rapid clearance by 30 min. Tissue distribution data confirmed the in vivo and ex vivo PET/optical imaging data, indicating desirable brain pharmacokinetics of the radioligand. Taken together, the results of this study suggest that [18F]1 can be widely used as a prosthetic group for brain hybrid PET/optical imaging agents.

Two novel asymmetric BODIPY fluoroionophores with dipicolylamine (BDP-DPA, dipicolylamine: bis(pyridylmethyl)) and terpyridine (BDP-TPY) are described. These fluoroionophores display opposite wavelength responses on complexation with heavy metal ions. Furthermore, the fluorescence spectra vary depending on the ionic species. In particular, BDP-DPA shows a high affinity toward Cr 3+ and upon complexation, the fluorescence spectrum blue-shifts from 591 to 566 nm. In contrast, BDP-TPY preferentially binds to Zn 2+ and the fluorescence spectra red-shifts from 539 to 567 nm. BDP-TPY is the first example of asymmetric BODIPY with a pyridyl receptor at the 3 position showing redshifted fluorescence by complexation with metal ions. The concentration of each metal ion was successfully determined by ratiometric measurement. The wavelength-responses characteristics of these fluoroionophores could be very useful in the development of novel ratiometric fluoroionophores for metal ions.The conservation and protection of the natural environment from trace contaminants are becoming increasingly important, and in particular, heavy metals pose severe risks to human health and to the environment because of their toxicity.1 For instance, chromium (Cr) is a common heavy metal contaminant used throughout the world, and its compounds can have genotoxic effects on humans and increase the risk of lung cancer.2 It originates primarily from industrial uses, such as electroplating, metal finishing, and leather tanning.3 Zinc (Zn) is also one of the major heavy metal pollutants because of its widespread industrial applications in chemical and alloyed products, fabricated metal products, and paper products. 4 Zn compounds have hazardous effects not only on humans but also on fish and plants. 5 Currently, the most common analytical methods for heavy metals are atomic absorption spectrometry (AAS) and inductively coupled plasma (ICP) spectroscopy. 6,7 Although precise, these analytical instruments are expensive and often require complex sample preparation. In addition, they are not applicable to continuous on-site monitoring and measure only the total concentration of heavy metals. Therefore, an inexpensive and simple method is needed for determining levels of heavy metal ions, which is appropriate for monitoring industrial and environmental samples.Fluorescence spectroscopy is a desirable method for quantifying heavy metal ions because of its high sensitivity, operational simplicity, and versatile instrumentation.8 The design and development of novel fluoroionophores remain an active area of research, and various fluoroionophores for heavy metal ions have been reported. 911 In terms of sensitivity, fluoroionophores that exhibit ratiometric spectral changes induced by complexation with heavy metal ions are more favorable than those exhibiting only fluorescence enhancement ("turn-on") or fluorescence quenching ("turn-off"). Ratiometric fluoroionophores provide more detailed information about the analyte in a sample, as well as allowing reliable...