Activity

This is the first study comparing the efficacy of tigecycline and cefoperazone/sulbactam for CRAB infections. Cefoperazone/sulbactam appears to be more efficacious than tigecycline during treatment.A series of new compounds (5a-q), derived from 5-(1-(4-nitrophenylsulfonyl) piperidin-4-yl)-4-phenyl-4H-1,2,4-triazole-3-thiol (3) were proficiently synthesized to evaluate their biological activities. 1-(4-Nitrophenylsulfonyl) piperidine-4-carbohydrazide (2) was refluxed with phenylisothiocyanate to yield an adduct which was cyclized to compound 3 by reflux reaction with 10 % potassium hydroxide. The targeted compounds 5a-q, were synthesized by stirring alkyl/aralkyl halides (4a-q) and compound 3 in a polar aprotic solvent. 1H-NMR, 13C-NMR, EI-MS and IR spectral techniques were employed to confirm the structures of all the synthesized compounds. selleck compound The compounds were biologically evaluated for BSA binding studies followed by anti-bacterial, anti-inflammatory and acetylcholinesterase (AChE) activities. The active sites responsible for the best AChE inhibition were identified through molecular docking studies. Compound 5e bearing 4-chlorobenzyl moiety found most active antibacterial and anti-inflammatory agent among the synthesized compounds. The whole library of synthesized compounds except compounds 5d and 5f was found highly active for AChE inhibition and recommended for in vivo studies so that their therapeutic applications may come in utilization.Peroxynitrite is known as a strong deleterious species that may readily trigger several geriatric diseases via injuring cellular constituents. Proanthocyanidins, a biological flavonoids constituent of Pinus sylvestris L. bark, has been attributed a large variety of pharmacological functions to its antioxidant potential. The results revealed that peroxynitrite could cause the generation of hydroxyl radical, the breakage of φX-174 plasmid DNA brand as well as the nitration of L-tyrosine. However, pine (Pinus sylvestris L.) bark proanthocyanidins extracts at low concentration range markedly inhibited the peroxynitrite -induced the formation of open circular DNA form (IC50 = 5.03±0.39 mg/mL). The 3-Nitro-L-tyrosine generated by the reaction of peroxynitrite with L-tyrosine was reduced by PBP (IC50 = 1.01±0.01 mg/mL). Besides, electron spin resonance spectroscopy data indicates that the intensive signal of dimethyl pyridine N-oxide hydroxyl radical adduct from peroxynitrite was reversed by pine bark proanthocyanidins extracts (IC50 =1.02±0.04 mg/mL). Moreover, the obtained data shows that PBP provides more efficient protection against peroxynitrite than that of ascorbic acid. Together, the present study suggests that pine bark proanthocyanidins could exert potent preventive activity against peroxynitrite -elicited cytotoxicity on the biomacromolecules, a study-worthy finding with pharmacological importance.Humans are experiencing serious health issues like myocardial infarction and diabetes. Thrombosis is the reason of myocardial infarction that may cause death. Bioactive compounds or enzymes can be used to dissolve the clot. Whereas diabetes is a disorder of metabolism in which the level of glucose in blood becomes high. It can be controlled by inhibiting α-amylase enzyme. The current project was, therefore planned to investigate the thrombolytic, α-amylase inhibitory and cytotoxic (to access drug safety) potentials of the organic and aqueous bioactive fractions of Bacillus clausii KP10. The cytotoxicity was assessed with hemolytic assay, α-amylase inhibition assay was done by using DNS and in-vitro thrombolytic effect was checked with human blood. In our experiments, the maximum hemolytic activity was shown by ethyl acetate fraction (12.64%). Results were compared with standard Triton X-100 which showed 91.61% hemolytic activity whereas all other fractions showed least cytotoxic activity. The extracts were also evaluated as thrombolytic agents as correlated to streptokinase (73.83%). All the extracts showed clot lysis activity, among which water soluble fraction exhibited maximum (35.16%) clot lysis activity. In our experiment methanol soluble fraction of B. clausii KP10 showed maximum 26.49% α-amylase inhibitory activity. Results were analyzed statistically through analysis of variance (ANOVA).EGHB010 is a standardized herbal formula of the rhizome mixture of Paeonia lactiflora Pallas and Glycyrrhiza uralensis Fisch. Neovascularization in the retina is a common pathophysiology of diabetic retinal microvasculopathy and exudative macular degeneration. In this study, we evaluated the inhibitory effects of EGHB010 on abnormal retinal angiogenesis in a hyperoxia-induced neovascular retinopathy model. Vascular endothelial growth factor (VEGF)-mediated vascular tube formation was assayed in human umbilical vascular endothelial cells (HUVECs). Experimental angiogenesis in the retinas was induced by exposing C57BL/6 pups to hyperoxic environment (75% oxygen) on postnatal day 7 (P7) and then returning them to normal oxygen pressure on P12. EGHB010 (50 and 100 mg/kg/day) was administered intraperitoneally for 5 days (P12 – P16). Retinal flat mounts were prepared to measure the extent of retinal neovascularization on P17. The incubation of HUVECs with EGHB010 (1-25 μg/mL) resulted in the inhibition of VEGF-mediated tube formation in a dose-dependent manner. EGHB010 at doses of 50 and 100 mg/kg/day inhibited the formation of retinal neovascular tufts by 31.15±2.28% and 59.83±2.92%, respectively. Together, our results indicate that EGHB010 is a potent anti-angiogenic agent and may have potential for the control of abnormal retinal vessel growth in patients with ischemic retinopathy.High performance liquid chromatography with UV/vis detection was optimized and validated for simultaneous quantification of alprazolam with celecoxib and diclofenac sodium in pharmaceutical formulation and human serum. Chromatographic separation was achieved at detection wavelength of 230 nm on Shimadzu Shim-pack CLC-ODS (M) 25M column employing 8020 (v/v) methanol water (pH 3.5) as mobile phase with elution rate 1.0mL min-1. Analytes were quantified in the ranges 0.2-15, 0.3-20 and 0.6-40 µg mL-1 with detection limits 19.76, 17.29 and 11.83ng mL-1 respectively. Recoveries were in the range 98.15-101.15, 99.24-99.90 and 98.87-101.19% in pharmaceutical formulation and 98.05-101.01, 98.72-99.49 and 98.25-99.47% in human serum respectively and precision ranged from 0.19-1.84%. The analytes were successfully detected without any observable interference commonly present in pharmaceutical formulation and human serum demonstrating applicability of method.