Synthesis of Novel Chalcone-Based Phenothiazine Derivatives as Antioxidant and Anticancer Agents.

Based on reported results for the potential medicinal impact of phenothiazine core, as well as the chalcone skeleton that is widely present in many natural products, together with their reported bioactivities, the present work was aimed at combining both moieties in one molecular skeleton and to synthesize and characterize a novel series of chalone-based phenothiazine derivatives. For this purpose, 2-acetylphenothiazine was N-alkylated, followed by the Claisen-Schmidt reaction to produce the chalcones with good yield. Antioxidant activity, as evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging, was assessed to determine if their antioxidant potential was comparable with ascorbic acid, and attributable to the phenothiazine core. Screening anticancer activities of the synthesized chalone-based phenothiazine derivatives against human breast cancer cell line MCF-7 cells, and human hepatocellular carcinoma HepG-2 cells, compared with standard drugs cisplatin and doxorubicin, was evaluated. The results revealed that compounds 4a, 4b, 4d, 4h, 4j, 4k, 4m, 4o, and 4p were good against human hepatocellular carcinoma HepG-2 cells, and among these compounds 4b and 4k were the most effective compounds, with IC50 values of 7.14 µg/mL and 7.6 1 µg/mL, respectively. On the other hand, compounds 4a, 4b, 4k, and 4m were good against human breast cancer cell line MCF-7 cells and, among these compounds, 4k and 4b were the most effective compounds, with IC50 values of 12 µg/mL and 13. 8 µg/mL, respectively. The overall results suggest that these compounds could, potentially, be further modified for the formation of more potent antioxidant and anticancer agents.

Efficacy of chitosan nanoparticles and wax coatings on maintaining post-harvest quality of "Murcott" mandarins.

Because of its high degree of biodegradability, chitosan is widely used as a component in food packaging. However, its poor physical properties, such as permeability, limit its applicability. Consequently, applying nano chitosan is regarded as the most effective solution to this issue. In the current study, we studied the effect of using different materials in the coating process on the quality of "Murcott" mandarin during cold storage. We used different concentrations of nano chitosan (50 and 100 ppm) without wax and 100 ppm nano chitosan with wax. We investigated the impact of these compounds on the chemical composition and quality of fruits. The most successful treatment for preventing weight loss from discarded fresh fruit was a combination of wax and 100 ppm nano chitosan. This combination also prevented the deterioration of vitamin C, maintained the fruit pulp, and preserved the fruit's superior taste during cold storage and shelf life. It also maintains a better total soluble solids and total acidity level than other treatments. In addition, the activity of antioxidant enzymes and the total number of antioxidants indicates no degradation of plant tissues compared to those not coated with nano chitosan. It also reduces the microbial load on the coated fruits. Consequently, this coating combination could suggest prolonging post-harvest life and increasing the marketing period of mandarin fruits.

Synthesis and Biological Evaluation of Novel Imidazole Derivatives as Antimicrobial Agents.

Imidazole derivatives are considered potential chemical compounds that could be therapeutically effective against several harmful pathogenic microbes. The chemical structure of imidazole, with a five-membered heterocycle, three carbon atoms, and two double bonds, tends to show antibacterial activities. In the present study, novel imidazole derivatives were designed and synthesized to be evaluated as antimicrobial agents owing to the low number of attempts to discover new antimicrobial agents and the emerging cases of antimicrobial resistance. Two imidazole compounds were prepared and evaluated as promising candidates regarding in vitro cytotoxicity against human skin fibroblast cells and antimicrobial activity against several bacterial strains. The synthesized imidazole derivatives were chemically identified using nuclear magnetic resonance (NMR) and Fourier-transform infrared spectroscopy (FTIR). The results demonstrated a relatively high cell viability of one of the imidazole derivatives, i.e., HL2, upon 24 and 48 h cell exposure. Both derivatives were able to inhibit the growth of the tested bacterial strains. This study provides valuable insight into the potential application of imidazole derivatives for treating microbial infections; however, further in vitro and in vivo studies are required to confirm their safety and effectiveness.

Recent developments of gallic acid derivatives and their hybrids in medicinal chemistry: A review.

The leading cause of several degenerative diseases such as atherosclerosis, cancer, aging, cardiovascular, and inflammatory diseases is oxidative stress, a consequence of overproduction and accumulation of free radicals. Naturally occurring antioxidants polyphenols have unnumbered biological activities such as antibacterial, anticancer, antiviral, antifungal, anticholesterol, and antiulcer. A naturally occurring gallic acid (3,4,5-trihydroxybenzoic acid), is highly antioxidant and may play a protective role in healthy individuals by inhibiting apoptosis. Pharmacological agents containing gallic acid and of diverse therapeutic categories as antioxidants, anticancer, antimicrobial, chondro-protective effect, carbonic anhydrase inhibitors, antidiabetic activity, anti-ulcerogenic, cathepsin D inhibitor, etc. have made this nucleus as an indispensable anchor for designing and development of new pharmacological agents. This review is an update on the latest development of the chemistry and the medicinal impacts of pharmacophores containing gallic acids. In addition, fused gallic acid derivatives and hybrid molecules containing different bioactive moieties in the presence of gallic acid are also presented and discussed.