scholarly journals Structure and Properties of the di- ((2S) -2-amino-3- (1H-indol-3-yl)propionate)-dihydro-tetraiodide

2021 ◽  
Vol 74 (2) ◽  
pp. 86-102
Author(s):  
A.N. Sabitov ◽  
◽  
S. Turganbay ◽  
A. Dzhumagazieva ◽  
◽  
...  

New organic iodine complex in the amino acid - alkali metal salt - iodine - water systemwas synthesized. The physico-chemical properties of complexdi- ((2S) -2-amino-3- (1H-indol-3-yl) propionate)-dihydro-tetraiodide were studied. Microscopic analysis shows that particles of complex have elongated needle-like linear stick-like shapes with average size 2.50-4.00 µm. The cytotoxicity test on MDCK cell culture, antimicrobial activity on S. aureus ATCC 6538-Р (museum susceptible strain); S. aureus ATCC-BAA-39 (museum multiresistant strain); E. coli ATCC 8739 (museum susceptible strain); E. coli ATCC-BAA-196 (museum multiresistant strain); P. aeruginosa ATCC 9027 (museum susceptible strain); P. aeruginosa TA2were observed. Complex has low cytotoxicity, direct antiviral effect, and antimicrobial activity against antibiotic-resistant strains of microorganisms. Di- ((2S) -2-amino-3- (1H-indol-3-yl) propionate)-dihydro-tetraiodide does not cause any mutagenic effect on mammalian cells of the L5178Y line, both in the presence and in the absence of metabolic activation.

2000 ◽  
Vol 350 (2) ◽  
pp. 429-441 ◽  
Author(s):  
Stuart M. PITSON ◽  
Richard J. D'ANDREA ◽  
Lucianne VANDELEUR ◽  
Paul A. B. MORETTI ◽  
Pu XIA ◽  
...  

Sphingosine 1-phosphate (S1P) is a novel lipid messenger that has important roles in a wide variety of mammalian cellular processes including growth, differentiation and death. Basal levels of S1P in mammalian cells are generally low, but can increase rapidly and transiently when cells are exposed to mitogenic agents and other stimuli. This increase is largely due to increased activity of sphingosine kinase (SK), the enzyme that catalyses its formation. In the current study we have purified, cloned and characterized the first human SK to obtain a better understanding of its biochemical activity and possible activation mechanisms. The enzyme was purified to homogeneity from human placenta using ammonium sulphate precipitation, anion-exchange chromatography, calmodulin-affinity chromatography and gel-filtration chromatography. This resulted in a purification of over 106-fold from the original placenta extract. The enzyme was cloned and expressed in active form in both HEK-293T cells and Escherichia coli, and the recombinant E. coli-derived SK purified to homogeneity. To establish whether post-translational modifications lead to activation of human SK activity we characterized both the purified placental enzyme and the purified recombinant SK produced in E. coli, where such modifications would not occur. The premise for this study was that post-translational modifications are likely to cause conformational changes in the structure of SK, which may result in detectable changes in the physico-chemical or catalytic properties of the enzyme. Thus the enzymes were characterized with respect to substrate specificity and kinetics, inhibition kinetics and various other physico-chemical properties. In all cases, both the native and recombinant SKs displayed remarkably similar properties, indicating that post-translational modifications are not required for basal activity of human SK.


2017 ◽  
Vol 3 (1) ◽  
Author(s):  
RC Jagessar ◽  
S Hope ◽  
S Issacs ◽  
Y Crepaul

The aqueous and ethanolic extract of Passiflora edulis and Vicia faba L. (Fabaceae) exhibited antimicrobial activity against the pathogenic microorganisms: E. coli, S. aureus, K. pneumoniae and C. albicans. This was evaluated using the Disc Diffusion Assay under asceptic conditions. Antimicrobial activity wasn’t induced by the solvent, ethanol nor water. The highest AZOI was 153.9 mm2 and the lowest 12.56 mm2. Negligible Zone of Inhibition, ZOI were observed in several instances. The aqueous extract of the fruit also induced negligible Zone of Inhibition, ZOI. In comparison to the reference, Ampicillin and Nystatin, these values are less. As the concentration of the metal salt, Zn(OAc)2.2H2O and ethanolic extract increases, there seem to be a variation in antimicrobial activity. Zn(OAc)2.2H2O appears to intensify the antimicrobial activity of the plant ethanolic and aqueous extract. Zn (OAc)2.2H2O in the absence of any extracts exhibited antimicrobial activity. The AZOI range from 47.2 mm2 to 117.8 mm2. Antimicrobial selectivity was also observed in several instances.


Author(s):  
Ratnamala P. Sonawane

The synthesis of 2-[1-(2,4- dihydroxyphenyl)ethylene]hydrazinecarboxamide and its Zn(II) metal complex was achieved. 2, 4 dihydroxy acetophenone is synthesized by resorcinol with glacial acetic acid. This further treated with semicarbazide hydrochloride to form its semicarbazone. Zn(II) metal complex was prepared by dissolving equimolar quantities of metal salt and Schiff base ligand in ethanol. All the target compounds were characterized by M.P, TLC and UV-visible and IR spectral data. Antimicrobial activities of these synthesized compounds were studied in sterile saline by Agar well diffusion method against M. luteus, B. subtilis, S. aureus, E. coli, P. aeruginosa bacteria. All the synthesized compounds have shown good to moderate antimicrobial activity.


2014 ◽  
Vol 3 (6) ◽  
pp. 92 ◽  
Author(s):  
Anna M. Witkowska ◽  
Dara K. Hickey ◽  
Martin G. Wilkinson

<p>The objective of this study was to determine and quantify the influence of various food components (carbohydrates, fat, protein or NaCl contents) or chemical properties (pH, water activity levels) on the antimicrobial efficacy of oregano and clove essential oils (EOs). Growth of <em>Listeria innocua</em> or <em>Escherichia coli</em> treated with oregano or clove EOs was monitored following separate addition of various food components. Antimicrobial activity of EOs was enhanced in presence of NaCl (? 0.5 g/100 ml), or in media with low pH values (? 5.0), especially when adjusted with organic acids. Enhanced antimicrobial activity was observed following reduction in water activity, which appeared related to the nature of solute used. Antibacterial activity of EOs was reduced in presence of vegetable oil (? 1 ml/100 ml), protein (? 1 g/100 ml) or starch (? 10 g/100 ml).<strong> </strong>Based on data obtained, the composition of vegetable soup was altered to optimise the efficacy of EOs, by lowering the pH to 5.0 using citric acid. A combination of oregano EO and acidification appeared to control growth of <em>L. innocua</em> and <em>E. coli</em> during storage at 4 or 10<sup> </sup>ºC. Thus, reformulation treatments including EO addition should be considered to improve the shelf-life of chilled ready meals.</p>


Author(s):  
J. P. Petrali ◽  
E. J. Donati ◽  
L. A. Sternberger

Specific contrast is conferred to subcellular antigen by applying purified antibodies, exhaustively labeled with uranium under immunospecific protection, to ultrathin sections. Use of Seligman’s principle of bridging osmium to metal via thiocarbohydrazide (TCH) intensifies specific contrast. Ultrathin sections of osmium-fixed materials were stained on the grid by application of 1) thiosemicarbazide (TSC), 2) unlabeled specific antiserum, 3) uranium-labeled anti-antibody and 4) TCH followed by reosmication. Antigens to be localized consisted of vaccinia antigen in infected HeLa cells, lysozyme in monocytes of patients with monocytic or monomyelocytic leukemia, and fibrinogen in the platelets of these leukemic patients. Control sections were stained with non-specific antiserum (E. coli).In the vaccinia-HeLa system, antigen was localized from 1 to 3 hours following infection, and was confined to degrading virus, the inner walls of numerous organelles, and other structures in cytoplasmic foci. Surrounding architecture and cellular mitochondria were unstained. 8 to 14 hours after infection, antigen was localized on the outer walls of the viral progeny, on cytoplasmic membranes, and free in the cytoplasm. Staining of endoplasmic reticulum was intense and focal early, and weak and diffuse late in infection.


Planta Medica ◽  
2013 ◽  
Vol 79 (13) ◽  
Author(s):  
M Niculae ◽  
CD Sandru ◽  
E Pall ◽  
S Popescu ◽  
L Stan ◽  
...  

Author(s):  
Singh Gurvinder ◽  
Singh Prabhsimran ◽  
Dhawan R. K.

In order to develop new antimicrobial agents, a series of 3-formyl indole based Schiff bases were synthesized by reacting 3-formyl indole(indole-3-carboxaldehyde) with substituted aniline taking ethanol as solvent. The reaction was carried in the presence of small amount of p-toluene sulphonic acid as catalyst.All the synthesized compounds were characterized by IR, 1H-NMR spectral analysis. All the synthesized compounds were evaluated for antimicrobial activity against two gram positive bacterial strains (B. subtilisand S. aureus) and two gram negative bacterial strains (P. aeruginosaand E. coli) and one fungal strain (C. albicans). All the synthesized compounds were found to have moderate to good antimicrobial activity. The  standard drug amoxicillin, fluconazole were used for antimicrobial activity. Among the synthesized compounds, the maximum antimicrobial activity was shown by compounds GS04, GS07, GS08 and GS10.


2019 ◽  
Vol 10 ◽  
pp. 1864-1872
Author(s):  
Prof. Teodora P. Popova

The effect of ionized aqueous solutions (anolytes and catholyte) in the processing of fruits (cherries, morellos, and strawberries) for decontamination has been tested. Freshly prepared analytes and catholyte without the addition of salts were used, as well as stored for 7 months anolytes, prepared with 0.5% NaCl and a combination of 0.5% NaCl and 0.5% Na2CO3. The anolyte prepared with a combination of 0.5% NaCl and 0.5% Na2CO3, as well as the anolyte obtained with 0.5% NaCl, exhibit high antimicrobial activity against the surface microflora of strawberries, cherries, and sour cherries. They inactivate E. coli for 15 minutes. The other species of the fam. Enterobacteriaceae were also affected to the maximum extent, as is the total number of microorganisms, especially in cherries and sour cherries. Even stored for 7 months, they largely retain their antimicrobial properties. Anolyte and catholyte, obtained without the addition of salts, showed a lower effect on the total number of microorganisms, but had a significant effect on Gram-negative bacteria, and especially with regard to the sanitary indicative E. coli.


2018 ◽  
Author(s):  
Todd D. Gruber ◽  
Chithra Krishnamurthy ◽  
Jonathan B. Grimm ◽  
Michael R. Tadross ◽  
Laura M. Wysocki ◽  
...  

<p>The utility of<b> </b>small molecules to probe or perturb biological systems is limited by the lack of cell-specificity. ‘Masking’ the activity of small molecules using a general chemical modification and ‘unmasking’ it only within target cells could overcome this limitation. To this end, we have developed a selective enzyme–substrate pair consisting of engineered variants of <i>E. coli</i> nitroreductase (NTR) and a 2‑nitro-<i>N</i>-methylimidazolyl (NM) masking group. To discover and optimize this NTR–NM system, we synthesized a series of fluorogenic substrates containing different nitroaromatic masking groups, confirmed their stability in cells, and identified the best substrate for NTR. We then engineered the enzyme for improved activity in mammalian cells, ultimately yielding an enzyme variant (enhanced NTR, or eNTR) that possesses up to 100-fold increased activity over wild-type NTR. These improved NTR enzymes combined with the optimal NM masking group enable rapid, selective unmasking of dyes, indicators, and drugs to genetically defined populations of cells.</p>


Author(s):  
Umadevi M ◽  
Rani T ◽  
Balakrishnan T ◽  
Ramanibai R

Nanotechnology has great promise for improving the therapeutic potential of medicinal molecules and related agents. In this study, silver nanoparticles of different sizes were synthesized in an ultrasonic field using the chemical reduction method with sodium borohydride as a reducing agent. The size effect of silver nanoparticles on antimicrobial activity were tested against the microorganisms Staphylococcus aureus (MTCC No. 96), Bacillus subtilis (MTCC No. 441), Streptococcus mutans (MTCC No. 497), Escherichia coli (MTCC No. 739) and Pseudomonas aeruginosa (MTCC No. 1934). The results shows that B. subtilis, and E. coli were more sensitive to silver nanoparticles and its size, indicating the superior antimicrobial efficacy of silver nanoparticles. 


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