No abstract

No abstract

No abstract

The World Health Organization (WHO) reports that the emergence of multidrug-resistant and the slow advent of novel and more potent antitumor and antimicrobial chemotherapeutics continue to be of the highest concern for human health. Additionally, the stability, low solubility, and negative effects of existing drugs make them ineffective. Studies into alternative tactics to tackle such tenacious diseases was sparked by anticancer and antibacterial. Silver (Ag) and gold (Au) nanoparticles (NPs) were created from Trichoderma saturnisporum, the much more productive fungal strain. Functional fungal extracellular enzymes and proteins carried out the activities of synthesis and capping of the generated nano-metals. Characterization was done on the obtained Ag-NPs and Au-NPs through UV–vis, FTIR, XRD, TEM, and SEM. Additionally, versus methicillin-sensitive Staphylococcus aureus (MSSA) and methicillin-resistant Staphylococcus aureus (MRSA), Pseudomonas aeruginosa, and Klebsiella pneumoniae, the antibacterial activities of Ag-NPs and Au-NPs were assessed. In particular, the Ag-NPs were more effective against pathogenic bacteria than Au-NPs. Furthermore, antibiofilm study that shown Au-NPs had activity more than Ag-NPs. Interestingly, applying the DPPH procedure, these noble metallic NPs had antioxidant activity, in which the IC50 for Ag-NPs and Au-NPs was 73.5 μg/mL and 190.0 μg/mL, respectively. According to the cytotoxicity evaluation results, the alteration in the cells was shown as loss of their typical shape, partial or complete loss of monolayer, granulation, shrinking, or cell rounding with IC50 for normal Vero cell were 693.68 μg/mL and 661.24 μg/mL, for Ag-NPs and Au-NPs, respectively. While IC50 for cancer cell (Mcf7) was 370.56 μg/mL and 394.79 μg/mL for Ag-NPs and Au-NPs, respectively. Ag-NPs and Au-NPs produced via green synthesis have the potential to be employed in the medical industry as beneficial nanocompounds.

The crystal structure and unambiguous absolute configuration of meleagrin (1) isolated from fungus Emericella dentata Nq45 is reported herein to first time on the bases of single crystal X-ray diffraction. Together with 1, haenamindole (2), isorugulosuvine (3), secalonic acid D (4), ergosterol (5) and cerebroside A (6) were obtained and their structures were determined by ESI MS and NMR data analysis. Diverse biological activity of meleagrin (1) was investigated. Compound 1 pronounced potent cytotoxicity against the human cervix carcinoma cell line KB-3-1 and

A series of 3-[(1H-pyrazol-3-yl)imino]indolin-2-one derivatives were designed using the molecular hybridization method, characterized using different spectroscopic techniques, and evaluated for their in vitro antimicrobial activity. Most of the target compounds demonstrated good to moderate antimicrobial activity compared with ciprofloxacin and fluconazole. Four compounds (8b, 9a, 9c, and 10a) showed encouraging results, with minimal inhibitory concentration (MIC) values (53.45-258.32 µM) comparable to those of norfloxacin (100.31-200.63 µM) and ciprofloxacin (48.33-96.68 µM). Noticeably, the four derivatives revealed excellent bactericidal and fungicidal activities, except for the bacteriostatic potential of compounds 8b and 9a against Escherichia coli and Staphylococcus aureus, respectively. The time-killing kinetic study against S. aureus confirmed the efficacy of these derivatives. Furthermore, two of the four promising derivatives, 9a and 10a, could prevent the formation of biofilms of S. aureus without affecting the bacterial growth at low concentrations. A combination study with seven commercial antibiotics against the multidrug-resistant bacterium P. aeruginosa showed a notable reduction in the antibiotic MIC values, represented mainly through a synergistic or additive effect. The enzymatic assay implied that the most active derivatives had inhibition potency against DNA gyrase comparable to that of ciprofloxacin. Molecular docking and density functional theory calculations were performed to explore the binding mode and study the reactivity of the promising compounds.3-(pyrazol-3-yl)imino-2-oxoindoline derivatives, antibiofilm, antimicrobial activity, DFT calculations, DNA gyrase, drug combination, molecular docking, time-killing kinetics | INTRODUCTIONIn recent years, infectious diseases caused by bacterial pathogens have become a main public health problem due to the high occurrence of drug resistance. [1] Additionally, infections caused by multidrug-resistant bacteria are a major health concern worldwide. [2] Particularly important are infections caused by the Gram-positive bacteria Staphylococcus aureus and species of the genus Enterococcus due to the increasing incidence of infections caused by these microorganisms in hospitals and communities and their ability to

No abstract

No abstract