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Prions are infectious protein particles known to cause prion diseases. The biochemical entity of the pathogen is the misfolded prion protein (PrPSc) that forms insoluble amyloids to impair brain function. PrPSc interacts with the non-pathogenic, cellular prion protein (PrPC) and facilitates conversion into a nascent misfolded isoform. Several small molecules have been reported to inhibit the aggregation of PrPSc but no pharmacological intervention was well established thus far. We, here, report that acylthiosemicarbazides inhibit the prion aggregation. Compounds 7x and 7y showed almost perfect inhibition (EC50 = 5 µM) in prion aggregation formation assay. The activity was further confirmed by atomic force microscopy, semi-denaturing detergent agarose gel electrophoresis and real-time quaking induced conversion assay (EC50 = 0.9 and 2.8 µM, respectively). These compounds also disaggregated pre-existing aggregates in vitro and one of them decreased the level of PrPSc in cultured cells with permanent prion infection, suggesting their potential as a treatment platform. In conclusion, hydroxy-2-naphthoylthiosemicarbazides can be an excellent scaffold for the discovery of anti-prion therapeutics.

Inflammatory bowel disease (IBD) is a chronic immuno-inflammation in gastrointestinal tract. We have evaluated the activity of the compounds to inhibit the adhesion of monocytes to colon epithelial cells is triggered by a pro-inflammatory cytokine, tumour necrosis factor (TNF)-α. The in vitro activity of the compounds, 13b (an ureido-derivative), 14c, 14j, 14k, 14n (thioureido-), 18c and 18d (sulfonamido-), was in correlation with in vivo anti-colitis activity revealed as significant recovery in body- and colon-weights and colon myeloperoxidase level, a biochemical marker of inflammation reflecting neutrophil infiltration. In vivo, TNBS-induced changes in the expression of inflammatory cytokines (TNF-α, IL-6, IL-1β, IL-10, and TGF-β), NLRP3 inflammasome components (NLRP-3, Caspase-1, and IL-18), and epithelial junction molecules (E-cadherin, claudin2/3, and ZO-1) were blocked and recovered by oral administration of the compounds (1 mg/kg). Compound 14n which showed the best efficacy can be a promising lead for orally available therapeutics for pathology of IBD.

Herein, a QuEChERS (quick, easy, cheap, effective, rugged, and safe) procedure together with liquid chromatography and tandem mass spectrometry was applied to the multi-residue analysis of 203 pesticides in strawberries. To reduce the amount of co-eluents, we compared several dispersive solid-phase extraction cleanup procedures and found that cleanup using octadecylsilane provided the best recoveries. Spiked-sample recoveries of 70–120% with relative standard deviations of 0.99), and the limits of quantification (LOQs) were lower than the maximum residue limits recommended by the European Commission and Korea Food and Drug Administration. The developed method was applied to real samples, revealing that their pesticide contents exceeded the corresponding LOQs. The obtained results demonstrate that octadecylsilane-based dispersive solid-phase extraction is a rapid and high-throughput cleanup procedure for the multi-residue analysis of pesticides in strawberries.

The ability to readily determine the composition of brown rice vinegar is important for quality assurance purposes. To that end, solid–phase microextraction (SPME)–Arrow method was optimized for the determination of volatile organic compounds (VOCs) from brown rice vinegar. Compared to traditional SPME fibers, SPME–Arrow has a larger sorbent-phase volume and is more durable. The SPME–Arrow conditions, including coating material, extraction temperature, extraction time, and NaCl concentration, were examined, which led to optimum extraction conditions that include: carboxen/polydimethylsiloxane (CAR/PDMS) fiber, 50°C, 30 min of SPME–Arrow, and 0% NaCl (i.e., no added NaCl). The developed method was compared to an optimized method based on conventional SPME. Twelve major VOCs, including acetates, alcohols, aldehydes, acids, and furan derivatives, were extracted by SPME–Arrow, while only seven VOCs were extracted using the traditional SPME. Moreover, SPME–Arrow extracted more 1.3–2 times more VOCs than SPME. Hence, the CAR/PDMS SPME–Arrow fiber is suitable for acquiring VOC profiles from brown rice vinegar.

Sesame oil is a high-value edible vegetable oil, and concern about its authenticity has gained much attention for commercial and consumer health reasons. The present study compares the application of triacylglycerols (TAGs), fatty acids, and volatile organic compounds (VOCs) as markers for discriminating pure sesame oils from those adulterated with corn or soybean oils. The profiles of TAGs, fatty acids, and VOCs in oil samples were established by high-performance liquid chromatography-evaporative light scattering detector, gas chromatography (GC)-flame ionization detector, and GC-time-of-flight mass spectrometer, respectively. Data from six TAGs, seven fatty acids, and six VOCs were employed separately to classify oil samples via principal component analysis (PCA). The PCA results indicate that VOCs show much greater promise than TAGs and fatty acids for detecting corn or soybean oil adulteration (approximately 5% w/w content) of sesame oils.