scholarly journals Bioactivities of holmium(III) and gadolinium(III) complexes of thymoquinone

2021 ◽  
Vol 35 (1) ◽  
pp. 87-96
Author(s):  
N. S. Awwad ◽  
H. A. Ibrahium ◽  
A. A. Shati ◽  
M. A. Alshehri ◽  
K. M. Al-Syaad ◽  
...  

Chemotherapeutic agents which are the main stay in cancer treatment are toxic with numerous contrary side effects. A number of chemical, physical, and computational techniques were applied to synthesize and elucidate the structural and functional characterization of the new designed bioligands and their metal complexes. Besides, several biological techniques for developing therapeutics and diagnostics agents of these new designed materials were used. The trivalent holmium(III) and gadolinium(III) metal complexes of thymoquinone (TQ) were synthesized. Toxicities and other bioactivites were undertaken with existing drug combinations and more effective tumor models will be established. The molecular structures of TQ-metal complexes were elucidated based on particular spectral approaches. The NF-kB (nuclear factor kappa-light-chain enhancer of activated B Cells) luciferase, elastase release, superoxide anion (O2•−) generation, and DPPH (1,1-diphenyl-2-picryl hydrazyl) free-radical scavenging activities of TQ and its synthesized complexes were elucidated and discussed. The core research is to use coordination and organometallic chemistry to design new bioligands and binary, ternary, mixed ligand, multi metal multi ligand complexes pursing a bio target continuously with structure-activity relationships (SARS).                     KEY WORDS: Thymoquinone, Holmium, Gadolinium, Bioactivities   Bull. Chem. Soc. Ethiop. 2021, 35(1), 87-96. DOI: https://dx.doi.org/10.4314/bcse.v35i1.7

Author(s):  
Erik Ekengard ◽  
Ida Bergare ◽  
Josefine Hansson ◽  
Isa Doverbratt ◽  
Magda Monari ◽  
...  

The synthesis and characterization of N-(2-((7-chloroquinolin-4-yl)amino)ethyl)pyrazine-2-carboxamide (<strong>L</strong>), an aminoquinoline – pyrazinamide hybrid, and the complexes (N-(2-((7-chloroquinolin-4-yl)amino)ethyl)pyrazine-2-carboxamide)(cyclopentadienyl) chlorido-rhodium or iridium hexafluorophosphate ([M(<strong>L</strong>)(Cp*)Cl] PF<sub>6</sub>; M = Rh, Ir) and the corresponding chlorido salts ([M(<strong>L</strong>)(Cp*) Cl]Cl; M = Rh, Ir) are described. The ligand and the hexafluorophosphate salts of the metal complexes have been evaluated for anti-plasmodial and anti-mycobacterial activity. The rhodium and the iridium complexes were significantly more active against <em>M. tuberculosis</em> than the free ligand. The crystallographically determined molecular structures of complexes (N-(2-((7-chloroquinolin-4-yl)amino)ethyl)pyrazine-2-carboxamide)(cyclopentadienyl)chlororhodium hexafluoro-phosphate and (N-(2-((7-chloroquinolin-4-yl)amino)ethyl)pyrazine-2-carboxamide)(cyclopentadienyl)chloro-iridium chloride are presented.


2012 ◽  
Vol 2012 ◽  
pp. 1-6 ◽  
Author(s):  
Ahmed A. Al-Amiery ◽  
Abdul Amir H. Kadhum ◽  
Abu Bakar Mohamad

Metal complexes of (Z)-2-(pyrrolidin-2-ylidene)hydrazinecarbothioamide (L) with Cu(II), Co(II), and Ni(II) chlorides were tested against selected types of fungi and were found to have significant antifungal activities. The free-radical-scavenging ability of the metal complexes was determined by their interaction with the stable free radical 2,2′′-diphenyl-1-picrylhydrazyl, and all the compounds showed encouraging antioxidant activities. DFT calculations of the Cu complex were performed using molecular structures with optimized geometries. Molecular orbital calculations provide a detailed description of the orbitals, including spatial characteristics, nodal patterns, and the contributions of individual atoms.


2021 ◽  
Author(s):  
Muhammad Saleem ◽  
Samiullah Malik ◽  
Hafiza Mahreen Mehwish ◽  
Muhammad Waqas Ali ◽  
Nazim Hussain ◽  
...  

Abstract Presently, exopolysaccharide (EPS), due to its exceptional biological features is used as an efficient biopolymer. Therefore, the present study aimed is the EPS production by Lactobacillus Plantarum S123, its biopotential investigation and technological functional characterization. The results of microscopic examination suggested that the S123 EPS has a major portion of amorphous spongy like structure with partial crystalline nature. The FTIR and NMR results suggested that the S123 EPS consists on carbonyl and hydroxyl group respectively. Furthermore, the results of biopotential investigation suggested that the S123 EPS exhibited excellent antimicrobial activity against Gram’s positive (7.2mm) and Gram’s negative bacteria (11.5mm), DPPH radical scavenging activity (> 65%), water holding capacity (326.6 ± 0.5%), oil holding capacity (995.3 ± 0.2%), flocculation (89.5 ± 0.6%), and emulsifying (80.1 ± 1.1%) activities. Overall, the present results suggested that due to highly porous structure, efficient biotechnological potential the S123 EPS from Lactobacillus plantarum S123 can be used in the functional food product.


2021 ◽  
Vol 11 (2) ◽  
pp. 861
Author(s):  
Seungkyun Nam ◽  
Chan-Yang Lee ◽  
Soon-Mi Shim ◽  
Dong-Un Lee ◽  
Suyong Lee

Marigold powder was utilized as a food ingredient to produce lutein-fortified fresh noodles for eye health, and its functionalities were characterized in terms of thermo-rheological, structural, and antioxidant properties. The pasting parameters and starch-gelatinization enthalpy values of wheat flour had a tendency to decrease with increasing levels of marigold powder. The use of marigold powder led to decreases in the storage and loss moduli of wheat flour pastes by weakening their cellular microstructure, which was confirmed by the scanning electron microscopic images. When marigold powder was incorporated into the formulation of fresh noodles, the cooking loss and water absorption of the noodles were not negatively affected at a level of 2% (w/w). Also, the noodles with 2% marigold powder were not significantly different from the control for the maximum resistance to extension. The levels of lutein in the noodles prepared with marigold powder (61.2 to 204.9 mg/100 g) were reduced by almost 50% after cooking. However, they seemed to satisfy the recommended daily dose of lutein for visual functions. Moreover, the use of marigold powder provided antioxidant properties for noodles by enhancing the 2,2′-diphenyl-1-picrylhydrazyl (DPPH) and 2,2-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical-scavenging activities.


2014 ◽  
Vol 70 (11) ◽  
pp. 3066-3079 ◽  
Author(s):  
Angélique Cocaign ◽  
Xavier Kubiak ◽  
Ximing Xu ◽  
Guillaume Garnier ◽  
Inès Li de la Sierra-Gallay ◽  
...  

Mycobacterium abscessusis the most pathogenic rapid-growing mycobacterium and is one of the most resistant organisms to chemotherapeutic agents. However, structural and functional studies ofM. abscessusproteins that could modify/inactivate antibiotics remain nonexistent. Here, the structural and functional characterization of an arylamineN-acetyltransferase (NAT) fromM. abscessus[(MYCAB)NAT1] are reported. This novel prokaryotic NAT displays significantN-acetyltransferase activity towards aromatic substrates, including antibiotics such as isoniazid andp-aminosalicylate. The enzyme is endogenously expressed and functional in both the rough and smoothM. abscessusmorphotypes. The crystal structure of (MYCAB)NAT1 at 1.8 Å resolution reveals that it is more closely related toNocardia farcinicaNAT than to mycobacterial isoforms. In particular, structural and physicochemical differences from other mycobacterial NATs were found in the active site. Peculiarities of (MYCAB)NAT1 were further supported by kinetic and docking studies showing that the enzyme was poorly inhibited by the piperidinol inhibitor of mycobacterial NATs. This study describes the first structure of an antibiotic-modifying enzyme fromM. abscessusand provides bases to better understand the substrate/inhibitor-binding specificities among mycobacterial NATs and to identify/optimize specific inhibitors. These data should also contribute to the understanding of the mechanisms that are responsible for the pathogenicity and extensive chemotherapeutic resistance ofM. abscessus.


2013 ◽  
Vol 78 (8) ◽  
pp. C1152-C1158 ◽  
Author(s):  
Edgar I. Jiménez-Ruiz ◽  
Ana M. Calderón de la Barca ◽  
Rogerio R. Sotelo-Mundo ◽  
Guillermo E. Arteaga-Mackinney ◽  
Martin Valenzuela-Melendez ◽  
...  

2020 ◽  
Vol 477 (7) ◽  
pp. 1261-1286 ◽  
Author(s):  
Marie Anne Richard ◽  
Hannah Pallubinsky ◽  
Denis P. Blondin

Brown adipose tissue (BAT) has long been described according to its histological features as a multilocular, lipid-containing tissue, light brown in color, that is also responsive to the cold and found especially in hibernating mammals and human infants. Its presence in both hibernators and human infants, combined with its function as a heat-generating organ, raised many questions about its role in humans. Early characterizations of the tissue in humans focused on its progressive atrophy with age and its apparent importance for cold-exposed workers. However, the use of positron emission tomography (PET) with the glucose tracer [18F]fluorodeoxyglucose ([18F]FDG) made it possible to begin characterizing the possible function of BAT in adult humans, and whether it could play a role in the prevention or treatment of obesity and type 2 diabetes (T2D). This review focuses on the in vivo functional characterization of human BAT, the methodological approaches applied to examine these features and addresses critical gaps that remain in moving the field forward. Specifically, we describe the anatomical and biomolecular features of human BAT, the modalities and applications of non-invasive tools such as PET and magnetic resonance imaging coupled with spectroscopy (MRI/MRS) to study BAT morphology and function in vivo, and finally describe the functional characteristics of human BAT that have only been possible through the development and application of such tools.


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