Efficient click chemistry towards fatty acids containing 1,2,3-triazole: Design and synthesis as potential antifungal drugs for Candida albicans.

Candida is an important opportunistic human fungal pathogen. The cis-2-dodecenoic acid (BDSF) showing in vitro activity of against C. albicans growth, germ-tube germination and biofilm formation has been a potential inhibitor for Candida and other fungi. In this study, facile synthetic strategies toward a novel family of BDSF analogue, 1-alkyl-1H-1,2,3-triazole-4-carboxylic acids (ATCs) was developed. The straightforward synthetic method including converting the commercial available alkyl bromide to alkyl azide, consequently with a typical click chemistry method, copper(II) sulfate and sodium ascorbate as catalyst in water to furnish ATCs with mild to good yields. According to antifungal assay, 1-decyl-4,5-dihydro-1H-1,2,3-triazole-4-carboxylic acid (5d) showed antifungal capability slightly better than BDSF. The 1,2,3-triazole unit played a crucial role for the bioactivity of ATCs was also confirmed when compared with two alkyl-aromatic carboxylic acids. Given its simplicity, high antifungal activity, and wide availability of compounds with halide atoms on the end part of the alkyl chains, the method can be extended to develop more excellent ATC drugs for accomplishing the challenges in future antifungal applications.

Thermally Activated Delayed Fluorescence Organic Dots (TADF Odots) for Time-Resolved and Confocal Fluorescence Imaging in Living Cells and In Vivo.

The fluorophores with long-lived fluorescent emission are highly desirable for time-resolved fluorescence imaging (TRFI) in monitoring target fluorescence. By embedding the aggregates of a thermally activated delayed fluorescence (TADF) dye, 2,3,5,6-tetracarbazole-4-cyano-pyridine (CPy), in distearoyl-sn-glycero-3-phosphoethanolamine-poly(ethylene glycol) (DSPE-PEG2000) matrix, CPy-based organic dots (CPy-Odots) with a long fluorescence lifetime of 9.3 µs (in water at ambient condition) and high brightness (with an absolute fluorescence quantum efficiency of 38.3%) are fabricated. CPy-Odots are employed in time-resolved and confocal fluorescence imaging in living Hela cells and in vivo. The green emission from the CPy-Odots is readily differentiated from the cellular autofluorescence background because of their stronger emission intensities and longer lifetimes. Unlike other widely studied DSPE-PEG2000 encapsulated Odots which are always distributed in cytoplasm, CPy-Odots are located mainly in plasma membrane. In addition, the application of CPy-Odots as a bright microangiography agent for TRFI in zebrafish is also demonstrated. Much broader application of CPy-Odots is also prospected after further surface functionalization. Given its simplicity, high fluorescence intensity, and wide availability of TADF materials, the method can be extended to develop more excellent TADF Odots for accomplishing the challenges in future bioimaging applications.

Distribution, sources, and potential risk of polycyclic aromatic hydrocarbons in soils from an industrial district in Shanxi, China.

Concentration, composition profile, orientation distribution, sources, and potential risks of 16 polycyclic aromatic hydrocarbons (PAHs) were analyzed in 76 surface (0-25 cm) soil samples collected from the Changzhi industrial district in July 2014 using a gas chromatography mass spectrometer (GC-MS QP2010 Ultra) system. The composition patterns of the PAHs were dominated by the presence of four-ring PAHs (average 42.9%), followed by three-ring (average 25.9%), five-ring PAHs (average 25.6%), two-ring PAHs (average 5.03%), and lastly, six-ring PAHs (average 0.641%). Source apportionment of the soil PAHs was also performed by the diagnostic ratios, principal component analysis (PCA), and coefficient of divergence (CD) analysis indicated signatures of PAHs sources (including incineration, coal/wood combustion, and vehicular exhaust emission). The total concentration of 16 PAHs (∑16PAHs) found in the roadsides soils (RS) ranged from 2197 to 25,041 µg kg-1, with an arithmetic mean value of 12,245 µg kg-1; followed by the village soils (VS), which ranged from 2059 to 21,240 µg kg-1, with a mean of 8976 µg kg-1; and lastly, the agricultural soils (AS), which ranged from 794 to 16,858 µg kg-1, with a mean of 3456 µg kg-1. According to the numerical effect-based soils quality guidelines of Maliszewska-Kordybach, the levels of PAHs in the sampled industrial areas range from high to heavy contamination. The values of total benzo[a]pyrene toxicity equivalent values (∑Bapeq16PAHs) in the sample areas ranged from 0.087 to 3611 µg kg-1 with an average of 969 µg kg-1. According to the soil quality guidelines of Canada, values found in the highest range (100 µg kg-1), which are equal to those of ∑Bapeq16PAHs found in the industrial area samples, will exert adverse biological effects. The results of this research could potentially be useful for local governments to control toxicity exposure, promote actions to alleviate PAHs contamination, and to manage human health at both work and industrial areas.