Tahani Mazyad Almutairi

In this work, we report the synthesis, spectroscopic properties, electronic behavior, and DFT modeling of a hexa-coordinated chromium(iii) porphyrin complex, denoted as [Na(2,2,2crypt)][Cr^III(TPP)(NCO)₂]·0.406CHCl₃ (I).

This study reports the design, synthesis, and evaluation of four novel (E)-2-(2-(1-(5-chlorothiophen-2-yl)ethylidene)hydrazineyl)-4-(aryl)thiazole derivatives (4a–4d) as potential anti-biofilm agents against Candida albicans.

A novel series of 1,2,3-triazole/1,2,4-triazole hybrids 5a, 5b, and 6a–i was designed and synthesized as antiproliferative agents targeting aromatase enzymes. The antiproliferative activity of the new hybrids against four cancer cells was studied using Erlotinib as a control. Compounds 6a and 6b demonstrated the highest antiproliferative activity among these hybrids, with GI50 values of 40 nM and 35 nM, respectively. Compound 6b was the most potent derivative, with a GI50 of 35 nM, comparable to Erlotinib’s GI50 of 33 nM. Compound 6b inhibited all cancer cell lines with comparable efficacy to Erlotinib. Compounds 5a, 5b, and 6a–i were tested for inhibitory action against aromatase as a potential target for their antiproliferative activity. Results revealed that compounds 6a and 6b were the most potent aromatase inhibitors, with IC50 values of 0.12 ± 0.01 µM and 0.09 ± 0.01 µM, respectively, being more potent than the reference Ketoconazole (IC50 = 2.6 ± 0.20 µM) but less potent than Letrozole (IC50 = 0.002 ± 0.0002). These findings indicated that compounds 6a and 6b had significant aromatase inhibitory action and are potential antiproliferative candidates. The findings were further linked to molecular docking investigations, which gave models of strong interactions with the aromatase domain for inhibitors with high binding scores.

Ageing is associated with a decline in both Nrf2 activity and DNA repair efficiency, leading to the accumulation of DNA damage and an increased risk of cancer. Understanding the mechanisms behind the increased level of damaged DNA during ageing is crucial for developing interventions to mitigate age-related cancer risk and improve overall health in older individuals. (Poly)phenols are plant-derived bioactive compounds that undergo metabolism into simpler phenolic catabolites following ingestion. While these compounds have been associated with various health benefits, further analysis of their bioavailable catabolites is necessary. To this end, four phenolic catabolites derived from colonic microbiota were investigated for their ability to reduce DNA damage in response to oxidative challenge and modulate the Nrf2-Antixoidant Response Element pathway. Normal and adenocarcinoma colonocyte cell lines (CCD 841 CoN, & HT29 respectively) were exposed to sub cytotoxic concentrations (>10 µM,) of hydroxylated (4-hydroxybenzoic acid, 3-(3’-hydroxyphenyl) propionic acid) and non-hydroxylated (benzoic acid or 3-phenylpropionic acid) phenolic acids. Using the COMET assay, each catabolite demonstrated significant (p<0.001) geno-protective activity, albeit with varying potency. They also significantly modulated expression of key genes in the Nrf2-ARE pathway, including Nrf2, Heme oxygenase-1 (HO-1), and NAD(P)H dehydrogenase quinone 1 (NQO1). Hydroxylation of the phenolic acids appeared to have a limited effect with respect to bioactivity. Overall, the colon derived phenolic metabolites, when assessed at physiologically relevant concentrations, reduced DNA damage in both normal and adenocarcinoma colonic cells in response to oxidative challenge, mediated – at least in part via upregulation of the Nrf2-ARE pathway.

Healthcare textiles are gaining great attention in the textile industry. Electrospun nanofibers are considered the golden soldiers due to their strength, flexibility, and eco-friendly properties. The present study aimed to evaluate the potency of polyvinyl alcohol (PVA) nanofibers loaded with newly biosynthesized silver nanoparticles (Ag-NPs) as a wound healing dressing. Chocolate-band snail (Eobania vermiculata) mucus (which is part of the Mollusca defense system) was used as a novel reducing and stabilizing agent. Data indicated the effectiveness of Eobania vermiculata’s mucus in silver nanoparticle synthesis after a 24 h incubation time. The biosynthesized AgNPs-SM showed a 13.15 nm particle size, −22.5 mV ζ potential, and 0.37 PDI, which proved the stability of the synthesized nanoparticles. Eobania vermiculata mucus and AgNPs-SM showed potent antibacterial activity, especially against Pseudomonas aeruginosa. The electrospinning technique was applied in the fabrication of PVA/AgNPs-SM nanofibers, which were homogenous with a fine diameter of about 100–170 nm and showed a significantly high antimicrobial activity. In vitro and in vivo studies revealed that PVA/AgNPs-SM nanofibers were safe and efficiently enhanced the wound healing process (typical histological picture of the proliferative phase with compact and well aligned collagen fibers in the dermal tissue after 12 days) together with bacterial growth inhibition in the infected skin area.