Synthesis,spectral characterization,and evaluation of antimicrobial activity of O,O′-alkanediyl S-(N-phthalimidomethyl) dithiophosphates and zinc bis(O,O′-alkanediyl) dithiophosphates

The synthesis of novel dithiophosphate derivatives has been achieved. Two O,O′-alkanediyl S-(N-phthalimidomethyl) dithiophosphates and two Zinc bis(O,O′-alkanediyl) dithiophosphates are synthesized by an easy and facile chemical synthetic route. Zinc bis[O,O′-(2-methylpentane-2,4-diyl) dithiophosphate] L¹, Zinc bis[O,O′-(2-ethylhexane-1,3-diyl) dithiophosphate] L², O,O′-(2-methylpentane-2,4-diyl) S-(N-phthalimidomethyl) dithiophosphate L³ and O,O′-(2-ethylhexane-1,3-diyl) S-(N-phthalimidomethyl) dithiophosphate L⁴ are synthesized from the respective ammonium salts. Compounds L¹, L², L³, and L⁴ are characterized by (CHN) elemental analysis, ESI mass, FT-IR, ¹H, ¹³C, and ³¹P NMR techniques. The crystal structure of ammonium O,O′-(2-methylpentane-2,4-diyl) dithiophosphate is discussed. L¹, L², L³, and L⁴ were evaluated for antimicrobial activity. It was found that the phthalimide derivatives L³ and L⁴ showed much better antifungal potential against some species of fungus. The Zinc dithiophosphates L¹ and L² showed good antibacterial activity against Bacillus cereus and Escherichia coli.     

In Vivo Assessment of the Ameliorative Impact of Some Medicinal Plant Extracts on Lipopolysaccharide-Induced Multiple Sclerosis in Wistar Rats

Multiple sclerosis is a chronic autoimmune disorder that leads to the demyelination of nerve fibers, which is the major cause of non-traumatic disability all around the world. Herbal plants Nepeta hindustana L., Vitex negundo L., and Argemone albiflora L., in addition to anti-inflammatory and anti-oxidative effects, have shown great potential as neuroprotective agents. The study was aimed to develop a neuroprotective model to study the effectiveness of herbal plants (N. hindustana, V. negundo, and A. albiflora) against multiple sclerosis. The in vivo neuroprotective effects of ethanolic extracts isolated from N. hindustana, V. negundo, and A. albiflora were evaluated in lipopolysaccharides (LPS) induced multiple sclerosis Wistar rat model. The rat models were categorized into seven groups including group A as normal, B as LPS induced diseased group, while C, D, E, F, and G were designed as treatment groups. Histopathological evaluation and biochemical markers including stress and inflammatory (MMP-6, MDA, TNF-α, AOPPs, AGEs, NO, IL-17 and IL-2), antioxidant (SOD, GSH, CAT, GPx), DNA damage (Isop-2α, 8OHdG) as well as molecular biomarkers (RAGE, Caspase-8, p38) along with glutamate, homocysteine, acetylcholinesterase, and myelin binding protein (MBP) were investigated. The obtained data were analyzed using SPSS version 21 and GraphPad Prism 8.0. The different extract treated groups (C, D, E, F, G) displayed a substantial neuroprotective effect regarding remyelination of axonal terminals and oligodendrocytes migration, reduced lymphocytic infiltrations, and reduced necrosis of Purkinje cells. The levels of stress, inflammatory, and DNA damage markers were observed high in the diseased group B, which were reduced after treatments with plant extracts. The antioxidant activity was significantly reduced in diseased induced group B, however, their levels were raised after treatment with plant extract. Group F (a mélange of all the extracts) showed the most significant change among all other treatment groups (C, D, E, G). The communal dose of selected plant extracts regulates neurodegeneration at the cellular level resulting in restoration and remyelination of axonal neurons. Moreover, 400 mg/kg dose of three plants in conjugation (Group F) were found to be more effective in restoring the normal activities of all measured parameters than independent doses (Group C, D, E) and is comparable with standard drug nimodipine (Group G) clinically used for the treatment of multiple sclerosis. The present study, for the first time, reported the clinical evidence of N. hindustana, V. negundo, and A. albiflora against multiple sclerosis and concludes that all three plants showed remyelination as well neuroprotective effects which may be used as a potential natural neurotherapeutic agent against multiple sclerosis.     

Production, Purification, and Characterization of Exoglucanase by Aspergillus fumigatus

Fungi are considered good producers of industrially valuable enzymes with higher enzymatic activities. Among these cellulases are group of extracellular enzymes commonly employed in many industries for the hydrolysis of cellulolytic material. Aspergillus fumigatus produced exoglucanase having high enzymatic activity (83 U/gds) during the solid-state fermentation of wheat straw under optimum physical and nutritional conditions. Maximum production was obtained after 72 h of fermentation, at 55 °C temperature, pH 5.5, 80 % moisture level, and 2 mL fungal inoculum. Production was further increased by the addition of fructose (0.3 %) as additional carbon source, peptone (0.4 %) as nitrogen source, Tween-80 (0.3 %) as surfactant, and ammonium sulfate (0.2 %) in media. Exoglucanase was 2.30-folds purified by adding 40 % ammonium sulfate with volumetric activity 95.4 U/gds and specific activity 14.74 U/mg. Further, it was 5.18-folds purified by gel filtration chromatography with volumetric activity 115.2 U/gds and specific activity 33.10 U/mg. Purified exoglucanase has maximum activity at 55 °C and pH 4.8 using 1 % Avicel aqueous solution as substrate. The K _m and V _max were 4.34 mM and 7.29 μM/min, respectively. Calcium, magnesium, and zinc ions have positive effect on exoglucanase activity.     

A simple and rapid pre-confirmation method to distinguish endogenous human haemoglobin from synthetic haemoglobin-based oxygen carriers in doping control

A specific, sensitive and rapid analytical procedure based on capillary electrophoresis with UV/Vis detection at 405 and 415?nm was developed and validated to detect human haemoglobin and haemoglobin-based oxygen carriers (Hemopure?, Oxyglobin? and Polyheme?) in blood samples collected for doping control. The electrophoretic separation, based on capillary dynamic coating, was achieved in less than 10 min. The effects of capillary temperature, injection conditions and initial ramping were investigated. The optimum separation voltage was 25 kV with a capillary temperature of 20 °C, initial ramping of 1?kV/s and an injection pressure of 0.5?psi for 10?s. The removal of haptoglobin using anti-human haptoglobin antibody prior to the analysis was mandatory to increase the specificity of the analysis. Sufficient resolution between endogenous haemoglobin variants and the three haemoglobin-based oxygen carriers here investigated was obtained, thus allowing discrimination between a normal haemolysed sample and a sample in which Oxyglobin?, Hemopure? or Polyheme? is present. Good repeatability of migration times (CV% less than 1), peak resolution and adequate sensitivity (limit of detection: 2.5?mg/mL) was obtained.     

Synthesis and characterisation of aromatic ethynyl-bridged ferrocenes

A series of aromatic ethynyl-bridged ferrocenes with the general formula Fc-CC-R-CC-Fc (Fc=ferrocenyl, R=C₆H₂(-p-CH₃)₂ (1), C₆H₄-p-C₆H₄ (2), C₅H₃N (3), 9,10-C₁₄H₈ (4), C₄H₂S (5), (C₄H₂S)₂ (6) and (C₄H₂S)₃ (7)) has been synthesised by the reaction of ethynyl ferrocene with the appropriate dibromo-arenes. The new complexes have been characterised by spectroscopic techniques. The structures of 3 and 7 were determined via X-ray crystallography, and both show the trans-trans configuration of the two ethynyl ferrocene groups with respect to the central R group. The electronic properties of the compounds have been studied via optical spectroscopy and cyclic voltammetry.