A new series of 1,3,4-oxadiazoles derivatives was synthesized, characterized, and evaluated for their in vitro and in vivo anti-thrombotic activity. Compounds (3a–3i) exhibited significant clot lysis with respect to reference drug streptokinase (30,000 IU), and enhanced clotting time (CT) values (130–342 s) than heparin (110 s). High affinity towards 1NFY with greater docking score was observed for the compounds (3a, 3i, 3e, 3d, and 3h) than the control ligand RPR200095. In addition, impressive inhibitory potential against factor Xa (F-Xa) was observed with higher docking scores (5612–6270) with Atomic Contact Energy (ACE) values (−189.68 to −352.28 kcal/mol) than the control ligand RPR200095 (Docking score 5192; ACE −197.81 kcal/mol). In vitro, in vivo, and in silico results proposed that these newly synthesized compounds might be used as anticoagulant agents.
The escalating threat of drug-resistant microbes underscores the urgent need for novel antimicrobial agents. In response, considerable research effort has been directed towards developing innovative frameworks and strategies to address this challenge. Chalcones, known for their broad-spectrum biological activities, have emerged as promising candidates for combating drug resistance. In this study, a series of 2′-Hydroxychalcones (5a, 5b, 5c, and 5d) with varying electron withdrawing and donating groups were synthesized via Claisen Schmidt condensation. FT-IR, 1H NMR, and 13C NMR analyses were employed to confirm the structure of the synthesized compounds. Subsequent evaluation of the synthesized compounds revealed their potential as antibacterial and antibiofilm agents. Notably, compounds 5a and 5d exhibited potent antibacterial activity against multidrug-resistant (MDR) bacteria E. coli, P. aeruginosa, K. pneumoniae, and S. aureus, surpassing the reference drug Ciprofloxacin (30 μg/mL) and other synthesized compounds. Compound 5d showed a notable 19.5 mm zone of inhibition against K. pneumoniae. Furthermore, 5a (at a concentration of 30 μg) and 5d (at a concentration of 50 μg) exhibited statistically significant (P > 0.05) biofilm inhibition efficacy compared to Ciprofloxacin (30 μg/mL). The synthesized chalcones 5a-5d were also docked via PachDock molecular docking software for Glucosamine-6-phosphate (GlcN-6-P) synthase inhibition and showed that ligand 5a exhibited outstanding results with score 4238 and ACE value −160.89 kcal/mol, consistent with the observed antibacterial activity. These findings underscore the potential of chalcones, particularly 5a and 5d, as promising candidates for the development of new antimicrobial agents targeting drug-resistant microbes and biofilm formation.
12 February 2024 in Polish Journal of Environmental Studies
Titanium dioxide nanoparticles (TiO2(Aq) and TiO2(Et)) were synthesized by treating titanium tetraisopropoxide (TTIP) with the aqueous/ethanolic extracts of Morus nigra leaves. The synthetic method is an environmentally friendly, inexpensive and beneficial as the plant leaves act as stabilizing and reducing agents. The obtained NPs were characterized by FTIR spectroscopy, X-ray diffraction (XRD) analysis, scanning electron microscopy (SEM) and Raman spectroscopy. The crystallite sizes of TiO2(Aq) and TiO2(Et) NPs were found to be 0.17 and 0.076 nm, respectively. FTIR spectroscopy have shown the coating of plant material upon the surface of nanoparticles. SEM analysis has shown the round shape and irregular surface morphologies of nanoparticles. The bio-synthesized TiO2 NPs displayed negligible toxic hemolytic effects and had a little inhibition of Staphylococcus aureus and Proteus Mirabilis bacteria as compared to ciprofloxacin.
24 February 2023 in Polish Journal of Environmental Studies
Most of synthetic dyes are toxic for the environment. On the other hand, natural dyes are ecofriendly and can replace synthetic toxic dyes. In the present studies, a natural dye was extracted from rinsed and grinded olive peel in 1:10 ratio (m/V) with water. Then, fabrics (wool and silk) were dyed with the peel extract by using different types of dulling and shining mordants (FeSO4, CuSO4, CoSO4, SnCl2, K2SO4, Al2(SO4)3, ZnSO4 and NiSO4). The mordants have shown best results for wool at the acidic pH (4-5) and for silk at the basic pH (8-9). After dyeing wool (at 70-80ºC) and silk (at 100ºC) with olive peel extract, by simultaneous mordanting method, an interesting variety of beige, buff and khaki shades were obtained. Color fastness was noted by matching the dyed fabric color with grey scale. The colors of dyed fabric were again noted after its washing, pressing by iron, rubbing and light exposure. The fastness results were found quite satisfactory. The investigated procedure of natural dye extraction is eco-friendly, safe for the environment and a safe technique as it does not involve any organic solvent. The natural dyes can be satisfactory potential substitutes of the synthetic environmentally hazardous dyes.