scholarly journals Hetero-Binuclear Complexes of Lanthanum (III) Using Bridging N,N′-Bis(2-Pyridylmethyl)Oxamide and Terminal 1,10-Phenanthroline: Synthesis, Characterization and Biological Evaluation

Author(s):  
P. R. Chetana ◽  
Vibha Vinayakumar Bhat ◽  
Mohan A. Dhale

In the present study, hetero-binuclear La(III) complexes were newly synthesized using well known bridging ligand N,N′-bis(2-pyridylmethyl)oxamide (2PMO, 1) and “complexes as ligands” [Cu(2PMO)] (2) and [Ni(2PMO)] (3). The newly synthesized mononuclear (4) as well as hetero-binuclear complexes (5 and 6) were characterized by analytical and spectroscopic techniques. The newly synthesized complexes were tested for their binding ability towards CT-DNA and chemical nuclease property towards SC pUC 19 DNA. The complexes were tested for antibacterial activities against Gram negative bacteria (E. coli and K. pneumonia) and Gram positive bacteria (B. subtilis and S. aureus), antioxidant activities by DPPH radical scavenging and ferrous-ion chelation methods and cytotoxicity against MCF-7 cell lines by MTT assay. The structure-activity relationship revealed that the newly synthesized hetero-binuclear complexes show potent DNA binding and chemical nuclease activities, antibacterial, antioxidant and cytotoxic activities.

2014 ◽  
Vol 9 (6) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Rui Jiang ◽  
Liwei Sun ◽  
Yanbing Wang ◽  
Jianzeng Liu ◽  
Xiaodan Liu ◽  
...  

Panax ginseng C.A.Meyer is one of the most valuable traditional Chinese medicines. In this study, the essential oil of ginseng leaves (EOGL), collected using hydrodistillation and analyzed by GC/MS, contained a complex mixture of aliphatic (69.0%), terpenoid (21.5%) and aromatic compounds (2.4%). Among 54 components identified, the major ones were palmitic acid (36.1%), β-farnesene (15.4%), linoleic acid (9.8%) and phytol (5.6%). In the cytotoxicity study, EOGL exhibited obvious cytotoxic activities against different cancer cell lines, including Hela, A549, ZR-75-1, HT-29, SGC7901 and B16 cells. Furthermore, Annexin V-FITC/PI staining assay indicated that EOGL can induce late apoptosis of ZR-75-1 cells, and the percentage of apoptotic cells increased in a concentration-dependent manner (0.9% to 5.6% and 67.4%). In addition to this, we also found that EOGL exhibited weak DPPH radical scavenging (12.0 ± 0.4 mg/mL) and ABTS radical scavenging activities (1.6 ± 0.1 mg/mL), and showed antibacterial activity against the Gram-positive bacteria, Staphylococcus aureus and Bacillus subtilis, and the Gram-negative bacterium, Escherichia coli. The data suggest that EOGL, which possesses important biological activities, especially significant anticancer activity, could be a potential medicinal resource.


2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Mallappa Kumara Swamy ◽  
Uma Rani Sinniah ◽  
Mohd. Sayeed Akhtar

We investigated the effect of different solvents (ethyl acetate, methanol, acetone, and chloroform) on the extraction of phytoconstituents fromLantana camaraleaves and their antioxidant and antibacterial activities. Further, GC-MS analysis was carried out to identify the bioactive chemical constituents occurring in the active extract. The results revealed the presence of various phytocompounds in the extracts. The methanol solvent recovered higher extractable compounds (14.4% of yield) and contained the highest phenolic (92.8 mg GAE/g) and flavonoid (26.5 mg RE/g) content. DPPH radical scavenging assay showed the IC50value of 165, 200, 245, and 440 μg/mL for methanol, ethyl acetate, acetone, and chloroform extracts, respectively. The hydroxyl scavenging activity test showed the IC50value of 110, 240, 300, and 510 μg/mL for methanol, ethyl acetate, acetone, and chloroform extracts, respectively. Gram negative bacterial pathogens (E. coliandK. pneumoniae) were more susceptible to all extracts compared to Gram positive bacteria (M. luteus,B. subtilis, andS. aureus). Methanol extract had the highest inhibition activity against all the tested microbes. Moreover, methanolic extract ofL. camaracontained 32 bioactive components as revealed by GC-MS study. The identified major compounds included hexadecanoic acid (5.197%), phytol (4.528%), caryophyllene oxide (4.605%), and 9,12,15-octadecatrienoic acid, methyl ester, (Z,Z,Z)- (3.751%).


2021 ◽  
Vol 11 (4) ◽  
pp. 12178-12185

In this study, some thiazole-based pyrrolidine derivatives were synthesized, characterized by FT-IR and 1H NMR spectroscopic techniques, and evaluated as potential antibacterial agents. Their antibacterial activities were evaluated by broth microdilution method and expressed as minimum inhibitory concentration; against Escherichia coli, Salmonella typhimurium, Bacillus cereus, and Staphylococcus aureus. Cytotoxicity studies of synthesized compounds were also conducted to minimize the toxic effects on healthy mammalian cells. From synthesized compounds, 4-F-phenyl derivative compound (11) has been found to inhibit Gram-positive bacteria with minimum toxicity selectively.


2017 ◽  
Vol 6 (3) ◽  
pp. 77-87 ◽  
Author(s):  
Latifa El Ouasif ◽  
Abdelhakim Bouyahya ◽  
Rachid Zniber ◽  
Mostafa El Ghoul ◽  
Redouane Achour ◽  
...  

In the present study, a series of novel 2-mercapto-benzimidazolium were synthesized from 2-mercapto-benzimidazole with hydrocarbon chains. All compounds obtained are reported for the first time, and the structures of these compounds were confirmed by means of 1H-NMR, 13C-NMR and mass spectrometry. The newly synthesized compounds were subjected to in vitro biological evaluation. The antibacterial activity was evaluated will diffusion assay and density optic method. The antioxidant activity was carried out using DPPH free radical scavenging assay. The result indicated that some compounds show convincing antibacterial activities against two microorganisms: Escherichia coli and Staphylococcus aureus. While, these molecules have not shown interesting antioxidant effects.


2021 ◽  
Vol 76 (5) ◽  
pp. 303-312
Author(s):  
Muhammad Ashram ◽  
Ahmed Al-Mustafa ◽  
Wael A. Al-Zereini ◽  
Firas F. Awwadi ◽  
Islam Ashram

Abstract Pyrazino[1,2-a]indoles fused with various heterocycles, such as oxazolidine, oxazinane, imidazolidine, hexahydropyrimidine and benzimidazole, were synthesized transition metal-free by domino reactions which involved the condensation of 1-(2-bromoethyl)-3-chloro-1H-indole-2-carbaldehydes 28–31 with various nucleophilic amines, resulting in the formation of two new interesting fused heterocycles. The anticholinesterase, antioxidant and antibacterial activities of the compounds were evaluated. Acetylcholinesterase (AChE) inhibitory activities were tested by Ellman’s assay, antioxidant activities were detected using the 2,2-azinobis[3-ethylbenzthiazoline]-6-sulfonic acid (ABTS•+) free-radical scavenging method and antibacterial activities were determined by agar diffusion tests. The oxazolo-pyrazino[1,2-a]indoles (8, 10), the oxazino-pyrazino[1,2-a]indoles (16, 18, 19), the pyrimido-pyrazino[1,2-a]indole (22), and the benzoimidazo-pyrazino[1,2-a]indole (27) possessed the highest inhibitory activity against AChE with IC50 values in the range 20–40 μg mL−1. The oxazolo-pyrazino[1,2-a]indoles (8, 9), the imidazo-pyrazino[1,2-a]indoles (12, 13), and the benzoimidazo-pyrazino[1,2-a]indole (24) revealed the highest antioxidant values with IC50 values less than 300 μg mL−1. However, the oxazolo-pyrazino[1,2-a]indole (11) and imidazo-pyrazino[1,2-a]indoles (12, 13) exhibited weak to moderate bioactivities against all tested Gram-positive bacteria, namely Staphylococcus aureus, Bacillus subtilis and Bacillus cereus.


2021 ◽  
Author(s):  
E.K. Soltani ◽  
K. Zaim ◽  
K. Mokhnache ◽  
N. Haichour ◽  
S. Mezaache-Aichour ◽  
...  

The propolis, an extremely complex resinous material, exhibits valuable pharmacological and biological properties, mainly attributed to the presence of polyphenols. The composition of propolis depends on time, vegetation, and the area of collection. Total flavonoid and polyphenol contents of aqueous extracts of propolis samples from different areas of Algeria, determined by using aluminum chloride and Folin–Ciocalteu colorimetric methods, were in the range of 3.047 ± 0.004–5.273 ± 0.013 mg/g and 96.833 ± 0.027–458.833 ± 0.0005 mg/g crude extract of propolis, respectively. This study examined the antioxidant and antimicrobial activities of propolis. Aqueous extracts of propolis were obtained in order to evaluate their antioxidant activities by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging, β-carotene and electrochemical assays. All tested propolis samples had relatively strong antioxidant activities, which were also correlated with the total polyphenol and flavonoid content present. The percentage of inhibition of lipid peroxidation of linoleic acid emulsion during 24 h varied between 86.04 ± 0.42 and 90.60 ± 3.77% among the tested samples. The highest DPPH radical scavenging activity was observed by ABAL (Ain Abassa Aqueous Extract) with IC50 = 8.49 ± 5.07 10−5 μg/ml, and the lowest was observed by SAL (Setif Aqueous Extract) with IC50 of 21.16 ± 0.0001 μg/ml. The most important antibacterial activity was obtained with Ain Abassa extract; the zones of inhibition obtained for this excerpt vary from 15.22 to 15.5 mm. Followed by the Setif extract with areas of 12.33 to 12.75 mm, the Tizi-Ouzou extract with areas of 10.11 to 11.11 mm. This study will bring an innovation for further studies with regard to the antioxidant and antibacterial properties of the aqueous extracts of propolis. This study corroborates that Algerian propolis is a rich source of natural antioxidants, properties which could be used in the prevention of different diseases, both in humans and in animals.


2021 ◽  
Vol 17 ◽  
Author(s):  
Hummera Rafique ◽  
Aamer Saeed ◽  
Muhammad Naseem ◽  
Tauqeer Riaz ◽  
Fouzia Perveen ◽  
...  

Background: Heterocyclic compounds display versatile biological applications, so the aim of this paper was to prepare biologically important heterocycles with enhanced bacterial resistance and to evaluate for their various structural features that are responsible for their biological properties. Objective: The objective was to synthesize bacterial resistance compounds with enhanced antibacterial properties. Method: Ester moiety containing thiazole ring was converted into its hydrazide derivatives. These heterocyclic derivatives were cyclized into another ring oxadiazole; hence a hybrid ring system of two biologically active rings was prepared. Result: All the synthesized compounds were characterized by spectroscopic techniques and were screened for their antibacterial potential; they possess significant antibacterial activities. Conclusion: New hybrid heterocyclic ring systems were synthesized by cyclization of hydrazide derivatives by adopting two step strategy in good yields. All the synthesized compounds were evaluated for their antioxidant activities; they showed moderate to significant activities. QSAR and Molecular docking studies were performed to determine the mode of interaction. Experimental and computational data is in accordance with the determined antibacterial activities.


2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Kenza Ammor ◽  
Dalila Bousta ◽  
Sanae Jennan ◽  
Bahia Bennani ◽  
Abdellah Chaqroune ◽  
...  

The aim of this study is to investigate in vitro antioxidant and antibacterial activities of the aqueous and hydroethanolic extracts for aerial parts of Herniaria hirsuta. Extracts were screened for their possible antioxidant activities by three tests: DPPH free radical-scavenging, reducing power, and molybdenum systems. The screening of antibacterial activity of extracts was individually evaluated against sixteen bacteria species using a disc diffusion method. Flavonoids, total phenols, and tannins content were performed for both extracts. It shows higher content in the hydroethanolic extract. The hydroethanolic extract showed a significant antioxidant activity for the three methods studies to the aqueous extract, but nonsignificant results compared to the reference (BHT). However, both extracts have negative effect on the strains studies for the antibacterial activity.


Antibiotics ◽  
2021 ◽  
Vol 10 (11) ◽  
pp. 1365
Author(s):  
Nurul Ainaa Farhanah Mat Ramlan ◽  
Aina Syahirah Md Zin ◽  
Nur Fatihah Safari ◽  
Kim Wei Chan ◽  
Norhasnida Zawawi

In the honey industry, heat treatments are usually applied to maintain honey’s quality and shelf life. Heat treatment is used to avoid crystallisation and allow the easy use of honey, but treatment with heat might affect the antioxidant and antibacterial activities, which are the immediate health effects of honey. This study will determine the effect of heat treatment on Malaysian and Australian stingless bee honey (SBH) produced by the common bee species in both countries. Eighteen honey samples were subjected to heat at 45 °C, 55 °C and 65 °C for one hour and subsequently analysed for their total phenolic content (TPC), total flavonoid content (TFC), DPPH radical scavenging activity, ferric reducing antioxidant power (FRAP) and minimum inhibitory concentration (MIC). The results show that all samples had high TPC, TFC and antioxidant activities before the treatment. The heat treatments did not affect (p < 0.05) the TPC, TFC and antioxidant activities in most samples, but did inhibit the antibacterial activities consistently in most of the samples, regardless of the bee species and country of origin. This study also confirms a strong correlation between TPC and TFC with FRAP activities for the non-heated and heated honey samples (p < 0.05). Other heat-sensitive bioactive compounds in SBH should be measured to control the antibacterial properties present.


2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
M. K. Prashanth ◽  
M. Madaiah ◽  
H. D. Revanasiddappa ◽  
K. N. Amruthesh

Condensation of amine 1 with aldehyde 2 gives Schiff base, N-(4-((benzofuran-2-ylmethylene) amino)phenyl)acetamide 3. Schiff base on N-acylation with different substituted acid chlorides in the presence of triethylamine gives the corresponding benzamides, N-acetyl-N-(4-((benzofuran-2-ylmethylene)amino)phenyl)substitutedbenzamide (NABP) 5a–j. The structures of newly synthesized compounds were characterized by elemental analysis, 1H NMR, 13C NMR FT-IR, and mass spectral studies. Compounds 3 and 5a–j have been screened for their antimicrobial activity using the disc diffusion and minimum inhibitory concentration (MIC) method against the selected bacterial and fungal strain. Compounds 5a, 5e, 5g, and 5h were found to be more active against all tested strains. The antioxidant properties were evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide radical scavenging methods. Compounds 5i and 5j showed predominant antioxidant activities among the synthesized analogues. The interaction between NABP and bovine serum albumin (BSA) was investigated using fluorescence and ultraviolet spectroscopic techniques at 298 K under imitated physiological conditions. The results revealed that NABP caused the fluorescence quenching of BSA through a static quenching procedure. The binding constants and the number of binding sites were calculated. The binding distance between the donor (BSA) and acceptor (NABP) was determined based on Forster’s theory.


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