scholarly journals Crystal Structure and Antitumor Activity of the Novel Zwitterionic Complex of tri-n-Butyltin(IV) with 2-Thiobarbituric Acid

2008 ◽  
Vol 2008 ◽  
pp. 1-5 ◽  
Author(s):  
Vasilios I. Balas ◽  
Sotiris K. Hadjikakou ◽  
Nick Hadjiliadis ◽  
Nikolaos Kourkoumelis ◽  
Mark E. Light ◽  
...  

A novel tri-n-butyl(IV) derivative of 2-thiobarbituric acid (HTBA) of formula[(n-Bu)3Sn(TBA)⋅H2O](1) has been synthesized and characterized by elemental analysis and119Sn-NMR and FT-IR spectroscopic techniques. The crystal structure of complex1has been determined by single crystal X-ray diffraction analysis at 120(2) K. The geometry around Sn(IV) is trigonal bipyramidal. Threen-butyl groups and one oxygen atom from a deprotonated 2-thiobarbituric ligand are bonded to the metal center. The geometry is completed with one oxygen from a water molecule. Compound1exhibits potent, in vitro, cytotoxicity against sarcoma cancer cells (mesenchymal tissue) from the Wistar rat, polycyclic aromatic hydrocarbons (PAH, benzo[a]pyrene) carcinogenesis. In addition, the inhibition caused by1, in the rate of lipoxygenase (LOX) catalyzed oxidation reaction of linoleic acid to hyperoxolinoleic acid, has been also kinetically and theoretically studied. The results are compared to that of cisplatin.

2019 ◽  
Vol 75 (3) ◽  
pp. 248-254 ◽  
Author(s):  
Zdeněk Trávníček ◽  
Pavel Štarha ◽  
Michal Čajan ◽  
Zdeněk Dvořák

A new electroneutral half-sandwich tantalum(V) dichlorido complex containing pentamethylcyclopentadienyl (Cp*) and the double-deprotonated version of the Schiff base 2-ethoxy-6-{(E)-[(2-hydroxyphenyl)imino]methyl}phenol (H2 L) as ligands, namely cis-dichlorido(2-ethoxy-6-{(E)-[(2-oxidophenyl)imino]methyl}phenolato-κ3 O,N,O′)(η5-pentamethylcyclopentadienyl)tantalum(V), [Ta(C10H15)(C15H13NO3)Cl2] or [Ta(η5-Cp*)(L)Cl2], has been prepared and thoroughly characterized by elemental analysis, IR and NMR spectroscopy, mass spectrometry, density functional theory (DFT) calculations and single-crystal X-ray diffraction. The molecular structure revealed that the TaV centre is coordinated by a η5-Cp* ligand, two monodentate chlorido ligands and one O,N,O′-tridentate L 2− ligand. The crystal structure is stabilized by C—H...C, C—H...Cl and C...C intermolecular interactions. Moreover, the complex shows notable in vitro cytotoxicity against the A2780 human ovarian carcinoma cell line, with IC50 = 14.4 µM, which is higher than that of the conventional platinum-based anticancer drug cisplatin (IC50 = 20.1 µM).


1986 ◽  
Vol 250 (2) ◽  
pp. F302-F307 ◽  
Author(s):  
J. M. Burnell ◽  
C. Liu ◽  
A. G. Miller ◽  
E. Teubner

To study the effects of bicarbonate and magnesium on bone, mild acidosis and/or hypermagnesemia were produced in growing rats by feeding ammonium chloride and/or magnesium sulfate. Bone composition, quantitative histomorphometry, and mineral x-ray diffraction (XRD) characteristics were measured after 6 wk of treatment. The results demonstrated that both acidosis (decreased HCO3) and hypermagnesemia inhibited periosteal bone formation, and, when combined, results were summative; and the previously observed in vitro role of HCO3- and Mg2+ as inhibitors of crystal growth were confirmed in vivo. XRD measurements demonstrated that decreased plasma HCO3 resulted in larger crystals and increased Mg resulted in smaller crystals. However, the combined XRD effects of acidosis and hypermagnesemia resembled acidosis alone. It is postulated that the final composition and crystal structure of bone are strongly influenced by HCO3- and Mg2+, and the effects are mediated by the combined influence on both osteoblastic bone formation and the growth of hydroxyapatite.


Author(s):  
K Sunand ◽  
K Vinay Kumar ◽  
K Ashwini ◽  
P Suresh Kumar ◽  
S Vishnu ◽  
...  

Aim: To synthesize and evaluate 4-aminoantipyrine related schiff’s bases as antibacterial agents. Objective: To synthesize, purify, characterize and evaluate 4-aminoantipyrine. Method: Schiff bases derived from 4-aminoantipyrine play a vital role in biological and pharmacological activities. Knowing the importance of 4-aminoatipyrine schiff bases and their analogues wide varieties of bioactivities like analgesic, antiviral, antipyretic, anti-rheumatic, antimicrobial and anti-inflammatory activities have been widely studied. 4-aminoantipyrine compounds C1 (anisaldehyde), C2 (p-hydroxybenzaldehyde) and C3(vanillin) were prepared by condensation between 4-amino antipyrine and substituted aromatic benzaldehydes. The products were purified by recrystallization by using ethanol, characterized by IR spectroscopy. The N-H stretching in 4-aminoantipyrine is shown at 3430 cm-1 and -3325 cm-1. The -HC=N- stretching is observed in the range of 1508-1504 cm-1 The –OCH3 stretching is found at 1888 cm-1. 4-amino antipyrine related schiff’s bases evaluated their activity as antimicrobials in-vitro by spread plate method against E.coli. Schiff bases have potent antibacterial activity with gram negative bacteria E.coli. Results: Synthesis and characterization of a schiff bases derived from substituted benzaldehydes and 4-aminoantipyrine was evaluated and characterized with the IR spectroscopic techniques and schiff bases have shown potent antibacterial activity against E.Coli.


2019 ◽  
Vol 41 (6) ◽  
pp. 1090-1090
Author(s):  
Mehmet Poyraz Mehmet Poyraz ◽  
Musa Sari Musa Sari ◽  
Halil Berber Halil Berber ◽  
Nursenem Karaca and Fatih Demirci Nursenem Karaca and Fatih Demirci

A new Schiff base, namely 2-methoxy-6-((2-(4 nitrophenyl) hydrazineylidene) methyl)phenol was synthesized and characterized by melting points, elemental analysis, thermogravimetric analysis and spectroscopic techniques (FT-IR, 1H-NMR and UV-VIS spectra). The chemical structure of compound was further confirmed by single crystal structural X-ray diffraction. The Schiff base is crystallized in the triclinic space group P-1. In the crystal, molecules are linked by O-H…O hydrogen bonds between the hydroxy “-O-” atom and the methoxy “-O-” atom. Furthermore, the synthesized Schiff base was tested for the in vitro anticandidal activities using CLSI broth microdilution method against human pathogenic Candida albicans, C. parapsilosis and C. krusei standard strains. In the anticandidal activity test results, the new Schiff base was found to be effective at 1 mg/mL - 0.25 mg/mL concentrations. (The last line omitted) (The sentence marked in red will be deleted)


Author(s):  
Rini Hamsidi ◽  
Wahyuni Wahyuni ◽  
Adryan Fristiohady ◽  
Muhammad Hajrul Malaka ◽  
Idin Sahidin ◽  
...  

Carthamus tinctorius Linn, also known as safflower, is a plant with the potential of being used in the production of antimalarial drugs. The purpose of this study was to isolate and identify the steroid compounds in the safflower and determine its antimalarial activity in vitro. The isolation process was conducted through extraction and chromatography methods. Then, the characterization of the isolated compounds was conducted through spectroscopic techniques which include Fourier Transform Infrared Spectroscopy (FT-IR), NMR 1-D (1H and 13C-NMR), and NMR 2-D (HMQC, HMBC, and H-H COZY) as well as comparing data with the existing literatures. In addition, the tests conducted were with variations of isolate concentrations (10, 1, 0.1, 0.01, and 0.001 μg/mL) against 3D7 strain of Plasmodium falciparum. Based on the FT-IR spectroscopic data, the steroid compounds isolated from safflowers might be stigmasterols. In addition, the isolates had -OH functional group in the region of 3431 cm-1, C-O in the region of 1053 cm-1, and Csp3-H in regions of 2960, 2934, and 2865 cm-1. The NMR 1-D data showed presence of 29 carbon atoms, while the protons were 48 in number. Furthermore, the IC50 value of the compound was 34.03 μg/mL with a percentage inhibition of 43.92% against the growth of P. falciparum. Therefore, it was classified as inactive agent in inhibiting the growth of malaria parasites, however, it could be used as a marker compound in C. tinctorius Linn extract.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 161 ◽  
Author(s):  
Eliana B. Souto ◽  
Selma B. Souto ◽  
Aleksandra Zielinska ◽  
Alessandra Durazzo ◽  
Massimo Lucarini ◽  
...  

We have developed a new cationic solid lipid nanoparticle (SLN) formulation, composed of Compritol ATO 888, poloxamer 188 and cetyltrimethylammonium bromide (CTAB), to load perillaldehyde 1,2-epoxide, and surface-tailored with a monoclonal antibody for site-specific targeting of human epithelial growth receptor 2 (HER2). Perillaldehyde 1,2-epoxide-loaded cationic SLN (cPa-SLN), with a mean particle size (z-Ave) of 275.31 ± 4.78 nm and polydispersity index (PI) of 0.303 ± 0.081, were produced by high shear homogenization. An encapsulation efficiency of cPa-SLN above 80% was achieved. The release of perillaldehyde 1,2-epoxide from cationic SLN followed the Korsemeyer–Peppas kinetic model, which is typically seen in nanoparticle formulations. The lipid peroxidation of cPa-SLN was assessed by the capacity to produce thiobarbituric acid-reactive substances, while the antioxidant activity was determined by the capacity to scavenge the stable radical DPPH. The surface functionalization of cPa-SLN with the antibody was done via streptavidin-biotin interaction, monitoring z-Ave, PI and ZP of the obtained assembly (cPa-SLN-SAb), as well as its stability in phosphate buffer. The effect of plain cationic SLN (c-SLN, monoterpene free), cPa-SLN and cPa-SLN-SAb onto the MCF-7 cell lines was evaluated in a concentration range from 0.01 to 0.1 mg/mL, confirming that streptavidin adsorption onto cPa-SLN-SAb improved the cell viability in comparison to the cationic cPa-SLN.


2017 ◽  
Vol 18 (4) ◽  
pp. 1406-1419
Author(s):  
F. Elmi ◽  
R. Chenarian Nakhaei ◽  
H. Alinezhad

Abstract This study is the first report of its type demonstrating the synthesis of mHAP on the basis of magnetic functionalization with nHAP, which were synthesized using Rutilus frisii kutum fish scale as a benign fishery waste by-product. The mHAP was characterized by X-ray diffraction (XRD), scanning electron microscopy (SEM), energy dispersive X-ray diffraction (EDX), and Fourier transform infrared (FT-IR) spectroscopic techniques. The XRD pattern confirmed the formation of a single-phase nHAP without any extra steady phases. It was also found that the pseudo-second-order kinetic model gave a satisfactory fit to the experimental data (R2 = 0.99). The maximum removal percentages of Cu and Zn ions in optimal conditions (adsorbent dosage at 0.1 g, 30 min contact time at 25 ± 1 °C and pH = 5 ± 0.1) by mHAP were 97.1% and 93.8%, respectively. Results also demonstrated that mHAP could be recycled for up to five cycles in the case of copper and zinc. The Langmuir isotherm was proved to have a better correlation compared with that of the Freundlich isotherm. The thermodynamic parameters indicated that it was a spontaneously endothermic reaction. In conclusion, mHAP could be regarded as a powerful candidate for efficient biosorbent, capable of adsorbing heavy metals from aqueous solutions.


2016 ◽  
Vol 71 (1) ◽  
pp. 51-55 ◽  
Author(s):  
Oscar E. Piro ◽  
Gustavo A. Echeverría ◽  
Beatriz S. Parajón-Costa ◽  
Enrique J. Baran

AbstractMagnesium acesulfamate, Mg(C4H4NO4S)2·6H2O, was prepared by the reaction of acesulfamic acid and magnesium carbonate in aqueous solution, and characterized by elemental analysis. Its crystal structure was determined by single crystal X-ray diffraction methods. The substance crystallizes in the triclinic space group P1̅ with one molecule per unit cell. The FTIR spectrum of the compound was also recorded and is briefly discussed. Some comparisons with other simple acesulfamate and saccharinate salts are also made.


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