Thienopyrimidine-based agents bearing diphenylurea: Design, synthesis, and evaluation of antiproliferative and antiangiogenic activity.

An important role has been considered for the vascular endothelial growth factor receptor 2 (VEGFR-2) in the angiogenesis process, so that its inhibition is an important scientific way for cancer treatment. In this work, new thienopyrimidine derivatives were synthesized and evaluated. Compared with sorafenib, the majority of the target compounds had antiproliferative activity against the PC3, HepG2, MCF7, SW480, and HUVEC cell lines, especially 9h with IC50 values of 4.5-15.1 µM, confirming the noticeable cytotoxic effects on the listed cell lines (PC3, HepG2, SW480, and HUVEC). Analyses by flow cytometry on SW480 and HUVEC cells revealed that 9n, 9k, 9h, and 9q led to apoptotic cell death. The result of the chick chorioallantoic membrane assay showed that 9h effectively reduced the number of corresponding blood vessels. Finally, the inhibitory effect on VEGFR-2 phosphorylation was considered as the outcome of Western blot analysis of compound 9h.

Smart monitoring of gas/temperature changes within food packaging based on natural colorants.

The development of smart packaging and innovation in common food packaging technology will greatly help to meet market needs, including consumer preference for "safe" foods, high-quality products and mitigate the negative environmental impacts of food packaging. In addition, consumers' tendency to use natural ingredients such as pigments and biopolymers has provided the basis for their application in the food industry, including smart food packaging. Hence, smart packaging in addition to protecting food products against environmental damage can also reveal a sign (colorimetric, chemical, electric, etc.) in real time in response to any changes in the packaging conditions and food quality. This comprehensive review emphasizes on the gas/temperature-sensitive smart films based on natural colorants and their key applications in the food packaging systems. Technological considerations associated with the natural colorant-responsive films, smart packaging, biopolymers, and importance of natural colorants versus synthetic dyes are investigated. In practice, the most common designed colorimetric indicators for monitoring gas and temperature changes and application of relevant smart films in real food models have also been discussed. Gas and time-temperature indicators provide a rapid, reliable, and online assessment and a visual indication of the food product quality level, usually through a color change, which is directly related to gas and temperature conditions during distribution and storage of relevant food products. However, future studies need to consider main points such as cost, consumers' acceptance, and confidence, regulatory aspects (i.e., labeling) and multifunctionality of smart packaging to be commercially sustainable.

Derivatization of γ-Amino Butyric Acid Analogues for Their Determination in the Biological Samples and Pharmaceutical Preparations: A Comprehensive Review.

γ-Aminobutyric acid (GABA) plays an important role in regulating neuronal excitability. Four structurally related drugs to GABA including pregabalin (PGB), gabapentin (GBP), vigabatrin (VGB), and baclofen are used for the treatment of central nervous system disorders. These drugs are small aliphatic molecules having neither fluorescent nor strong absorbance in the ultraviolet/visible region; therefore, direct determination of these analytes by optical methods is difficult. Additionally, their high boiling point makes gas chromatography impossible. Accordingly, the amine or acid moiety in these drugs is derivatized in order to improve their selectivity and sensitivity during determination in the biological samples. This review focuses on derivatization based methods and their different reactions for determination of PGB, GBP, VGB, and baclofen in the biological samples and pharmaceutical preparations reported between 1980 and 2020. High-performance liquid chromatography methods coupled with different detectors are a commonly used methods for determination of GABA analogs after derivatization. These methods cover 38.89% of all developed methods for determination of GABA analogs.

Titanium dioxide nanoparticles as multifunctional surface-active materials for smart/active nanocomposite packaging films.

Environmental issues such as plastic packaging and high demand for fresh and safe food has increased the interest for developing smart/active food packaging films with colloidal nanoparticles (NPs). Titanium dioxide nanoparticles (TNPs) are cost effective and stable metal oxide NPs which could be used as a functional nano-filler for biodegradable food packaging due to their excellent biocompatibility, photo catalyzing, and antimicrobial properties. This article has comprehensively reviewed the functional properties and advantages of TNPs-containing smart/active films. The advantage of adding TNPs for ameliorating food packaging materials such as their physical, mechanical, moisture/light barrier, optical, thermal resistance, microstructure and chemical properties as well as, antibacterial, and photocatalytic properties are discussed. Also, the practical and migration properties of administrating TNPs in food packaging material are investigated. The ethylene decomposition activity of TNPs containing active films, could be used for increasing the shelf life of fruits/vegetables after harvesting. TNPs are safe with negligible migration rates which could be used for fabrication of multifunctional smart/active packaging films due to their antimicrobial properties and ethylene gas scavenging activities.