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.
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.
Nitrogen-containing atoms in their core structures have been exclusive building blocks in drug discovery and development. One of the most significant and well-known heterocycles is the 1,3,4-thidiazole nucleus, which is found in a wide range of natural products and therapeutic agents. In the present work, certain tris-1,3,4-thiadiazole derivatives (6, 7) were synthesized through a multi-step synthesis approach. All synthesized compounds were characterized using different spectroscopic tools. Previously, thiadiazole compounds as anti-Toxoplasma gondii agents have been conducted and reported in vitro. However, this is the first study to test the anti-Toxoplasma gondii activity of manufactured molecular hybrids thiadiazole in an infected mouse model with the acute RH strain of T. gondii. All the observed results demonstrated compound (7)’s powerful activity, with a considerable reduction in the parasite count reaching 82.6% in brain tissues, followed by liver and spleen tissues (65.35 and 64.81%, respectively). Inflammatory and anti-inflammatory cytokines assessments proved that Compound 7 possesses potent antiparasitic effect. Furthermore, docking tests against TgCDPK1 and ROP18 kinase (two major enzymes involved in parasite invasion and egression) demonstrated compound 7’s higher potency compared to compound 6 and megazol. According to the mentioned results, tris-1,3,4-thiadiazole derivatives under test can be employed as potent antiparasitic agents against the acute RH strain of T. gondii.
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.
27 April 2022 in International Journal of Biological Macromolecules
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)][CrIII(TPP)(NCO)2]·0.406CHCl3 (I).