scholarly journals Synthesis, Characterization and Biological Activity of Two New Copper (II) Complexes with N-sulfonamide Ligand

2019 ◽  
Vol 70 (11) ◽  
pp. 4060-4067
Author(s):  
Adriana Corina Hangan ◽  
Laura Gratiela Vicas ◽  
Roxana Liana Stan ◽  
Emoke Pall ◽  
Luminita Simona Oprean ◽  
...  

Despite the fact that a large number of chemotherapeutic anticancer agents have been discovered, cancer still remains a great cause of deaths worldwide. The purpose of our researches is to discover a new antitumor drug. In this aim, two new Cu(II) complexes, [Cu(L)2(py)2(H2O)2](C1) and [Cu(L)2(phen)](C2) with a new ligand, N-(5-trifluoromethyl-[1,3,4]-thiadiazole-2-yl)-benzensulfonamide(HL) were synthesized. The complexes were characterized by elemental analysis, spectral and magnetic determinations. The nuclease activity studies of the complexes confirm their capacity to cleavage the DNA molecule. Both complexes have in vitro antioxidant activity (DPPH, FRAP methods), in vitro (using xanthine /xanthine oxidase system) and in vivo (using S.cerevisiae)SOD mimetic activity.The results of MTT assay on two carcinoma cell lines (HeLa and WM35) indicate that both complexes have antitumor activity, but (C2) has a superior activity compared with (C1) and with Cisplatin. On normal fibroblast (HDFa), (C1) showed toxicity comparable with Cisplatin, but (C2) showed a lower one. Bacterial assays were also performed (by the disk diffusion method) and both complexes have antibacterial activity against S. aureus, E. coli, P. aeroginosa and B. cereus. All the biological studies are in concordance and show that both complexes have biologic activity but (C2)is much more active.

2019 ◽  
Vol 70 (11) ◽  
pp. 4060-4067

Despite the fact that a large number of chemotherapeutic anticancer agents have been discovered, cancer still remains a great cause of deaths worldwide. The purpose of our researches is to discover a new antitumor drug. In this aim, two new Cu(II) complexes, (C1) and (C2) with a new ligand, N-(5-trifluoromethyl-<1,3,4>-thiadiazole-2-yl)-benzensulfonamide(HL) were synthesized. The complexes were characterized by elemental analysis, spectral and magnetic determinations. The nuclease activity studies of the complexes confirm their capacity to cleavage the DNA molecule. Both complexes have in vitro antioxidant activity (DPPH, FRAP methods), in vitro (using xanthine /xanthine oxidase system) and in vivo (using S.cerevisiae)SOD mimetic activity.The results of MTT assay on two carcinoma cell lines (HeLa and WM35) indicate that both complexes have antitumor activity, but (C2) has a superior activity compared with (C1) and with Cisplatin. On normal fibroblast (HDFa), (C1) showed toxicity comparable with Cisplatin, but (C2) showed a lower one. Bacterial assays were also performed (by the disk diffusion method) and both complexes have antibacterial activity against S. aureus, E. coli, P. aeroginosa and B. cereus. All the biological studies are in concordance and show that both complexes have biologic activity but (C2)is much more active. Keywords: oxidative DNA cleavage, antioxidant capacity, SOD-mimetic activity, cytotoxicity, antibacterial properties


Molecules ◽  
2020 ◽  
Vol 25 (19) ◽  
pp. 4519
Author(s):  
Marzena Kucia ◽  
Ewa Wietrak ◽  
Mateusz Szymczak ◽  
Paweł Kowalczyk

In this present study, the bacteriostatic effect of Salistat SGL03 and the Lactobacillus salivarius strain contained in it was investigated in adults in in vivo and in vitro tests on selected red complex bacteria living in the subgingival plaque, inducing a disease called periodontitis, i.e., chronic periodontitis. Untreated periodontitis can lead to the destruction of the gums, root cementum, periodontium, and alveolar bone. Anaerobic bacteria, called periopathogens or periodontopathogens, play a key role in the etiopathogenesis of periodontitis. The most important periopathogens of the oral microbiota are: Porphyromonas gingivalis, Tannerella forsythia, Treponema denticola and others. Our hypothesis was verified by taking swabs of scrapings from the surface of the teeth of female hygienists (volunteers) on full and selective growth media for L. salivarius. The sizes of the zones of growth inhibition of periopathogens on the media were measured before (in vitro) and after consumption (in vivo) of Salistat SGL03, based on the disk diffusion method, which is one of the methods of testing antibiotic resistance and drug susceptibility of pathogenic microorganisms. Additionally, each of the periopathogens analyzed by the reduction inoculation method, was treated with L. salivarius contained in the SGL03 preparation and incubated together in Petri dishes. The bacteriostatic activity of SGL03 preparation in selected periopathogens was also analyzed using the minimum inhibition concentration (MIC) and minimum bactericidal concentration (MBC) tests. The obtained results suggest the possibility of using the Salistat SGL03 dietary supplement in the prophylaxis and support of the treatment of periodontitis—already treated as a civilization disease.


Dose-Response ◽  
2020 ◽  
Vol 18 (3) ◽  
pp. 155932582095679
Author(s):  
Muhammad Amjad Chishti ◽  
Ejaz Mohi-Ud-Din ◽  
Shahbaz Ahmad Zakki ◽  
Muhammad Rahil Aslam ◽  
Sheraz Siddiqui ◽  
...  

The present study was conducted to evaluate the antibacterial activity, in vitro and in vivo cytotoxicity, cell viability and safety of Eastern Medicine coded medicinal formulation Eczegone comprising extracts of Azadirachta indica (Azin) , Fumaria indica (Fuin) , Sphaeranthus indicus (Spin) and Lawsonia inermis (Lain). This work also evaluated antibacterial activity of Eczegone formulation having above mentioned plants ethanolic extracts against different bacteria’s by disk diffusion method. In vitro toxicity of Eczegone formulation was investigated by using human skin keratinocytes HaCaT cell line, crystal violet stained cells, and methyl tetrazolium cytotoxicity (MTT) assay. In vivo acute oral and dermal cytotoxicity was determined by using Swiss albino mice and albino rabbits, respectively. The Eczegone formulation showed antibacterial activity against 3 gram negative bacteria including Escherichia coli, Klebsiella pneumonia, Proteus vulgaris and a gram positive Staphylococcus aureus. We didn’t observe any toxic effect of Eczegone formulation on the skin keratinocytes. Furthermore, the Ezcegone formulation was non-irritant according to draize score (OECD TG404, 2002). After rigorous safety evaluation by in vitro and in vivo acute oral and dermal toxicity analysis, we concluded that Eczegone formualtion possessses antibacterial effects and is safe, non-toxic, non-irritant, and the drug would be subjected for further biochemical and clinical studies.


Author(s):  
Ruvanthika Pn ◽  
Manikandan S

Objective: The objective of the study was to evaluate whether ethanolic extracts of Nelumbo nucifera (EENN) seedpod and quercetin (active component of NN) possess antibacterial proprieties against Gram (-) bacteria such as Escherichia coli and Pseudomonas aeruginosa and Gram (+) bacteria such as Staphylococcus aureus. Methods: Antibacterial activities of EENN seedpod and quercetin were investigated using disc diffusion method, minimum inhibitory concentration against E. coli and P. aeruginosa and Gram (+) bacteria such as S. aureus. Results: The antibacterial activity of both EENN seedpod and quercetin was found to be increased in dose-dependent manner. The maximum zone of inhibition was exhibited by both EENN seedpod and quercetin against E. coli (14 mm and 15 mm) and P. aeruginosa (13 mm and 15 mm). Gram-negative bacteria were more susceptible to the EENN seedpod extract and quercetin than Gram-positive bacteria.Conclusion: The results of the present study suggested that the effect of EENN seedpod and quercetin against the tested bacteria in vitro may contribute to the in vivo activities of the EENN seedpod and quercetin.


2015 ◽  
Vol 43 (2) ◽  
pp. 327-334 ◽  
Author(s):  
Mihaela NICULAE ◽  
Laura STAN ◽  
Emoke PALL ◽  
Anamaria Ioana PAȘTIU ◽  
Iulia Maria BALACI ◽  
...  

The study was aimed to characterize the chemical composition and the antimicrobial activity of Romanian propolis ethanolic extracts (EEP) against antibiotic-sensitive and antibiotic-resistant E. coli strains isolated from bovine mastitis. The preliminary antimicrobial screening was performed by a disk diffusion method, followed by determination of minimum inhibitory concentrations (MIC) and minimum bactericidal concentrations (MBC) based on broth microdilution assay; further, the synergistic action of propolis with antimicrobial drugs was assessed by a disk diffusion method on agar containing subinhibitory concentrations of propolis. For the chemical characterisation of EEP, the flavonoids (flavones/flavonols, flavanones/dihydroflavonols) and total phenolics were evaluated by spectrophotometric methods. The phenolic compounds of these extracts were also determined using HPLC. The results indicated for Romanian propolis ethanolic extracts the typical poplar composition profile with flavonoids and phenolic acids as main biological active compounds, with chromatographic analysis data confirmed also spectrophotometrically. In addition, positively correlated with the chemical composition, a strong antimicrobial efficacy was exhibited towards E. coli strains, along with interesting synergistic interaction with antibiotics that can be further investigated to obtain propolis-based formulation with antibacterial properties. Subsequent in vitro and in vivo studies evaluating the safety and efficacy are intended to consider propolis in veterinary therapeutic protocols.


2019 ◽  
Author(s):  
Shijun Feng ◽  
Huarui Li ◽  
Dongfang Ai ◽  
Hua Yan ◽  
Guangjing Zhang ◽  
...  

Abstract Objectives Systemic diseases or oral situation changes can result in oral infections like candidiasis. Mouthwash is the most prevalent method to prevent or cure these infections. To formulate a more effective mouthwash, we combined Clotrimazole with a low dose of Chlorhexidine to investigate the in vitro effect against Candida spp.Methods and Materials Combinations of Chlorhexidine (0.03-16ug/ml) and Clotrimazole (0.03-16ug/ml) were tested against Candida spp. by microdilution chequerboard technique and disk diffusion method.Results From the chequerboard combination assay, the MICs of Chlorhexidine and Clotrimazole against Candida spp. decreased from >16µg/ml to 2–1µg/ml and from 2-0.25µg/ml to 0.5–0.125µg/ml, respectively, demonstrating favorable synergistic effects against 21 (84%) strains of Candida spp. The disk diffusion method showed an increase in halo size for the combination group when compared to the Clotrimazole alone group.Conclusions Studies have shown that combinations of antiseptic and antifungal agents are effective in nature. In our study, we found that low concentrations of Chlorhexidine can enhance the antifungal effect of Clotrimazole against Candida spp.. We predict that the mechanism of this synergism could be due to the increased penetration of Clotrimazole brought about by the binding of Chlorhexidine to the cell membrane. Further studies to determine the mechanism and in vivo effects could increase its probable usage in clinical studies.


2021 ◽  
Author(s):  
Bondy Lourenço ◽  
Asimbawe Kiza ◽  
Abrão Amândio João ◽  
Clemência Félix Odala Niconte ◽  
Pompílio Armando Vintuar ◽  
...  

Abstract Background: Currently, several studies are being conducted to test antibacterial activity of various medicinal plants, in attempt to develop new antibiotics or to potentiate the action of antibiotics of known clinical use. In this research, phytochemical analysis and in vitro antibacterial activity of leaf extracts of Lantana camara L were performed.Methods The extracts were obtained through maceration with 90% ethanol. In phytochemical analysis, alkaloids, flavonoids, tannins and saponins were identified using specific reagents for each class.The antibacterial activity was analyzed using the disk diffusion method according to Kirby-Bauer, against Escherichia coli and Staphylococus aureus.Key findings The diameters of the inhibition halos varied between 0.7 and 12 mm, with an average of 8.26 mm for strains of S. aureus and there was no inhibition for E. coli. The results showed a significant difference between the inhibition halos and the tested concentrations for S. aureus. In conclusion L. camara leaf extracts are rich in bioactive compounds and have a good antibacterial potential against S. aureus and not for E. coli. And there was no relationship between the concentration of the extract and the diameter of the halo of inhibition of the evaluated microorganism.


Molecules ◽  
2021 ◽  
Vol 26 (20) ◽  
pp. 6140
Author(s):  
Amal A. Alyamani ◽  
Salim Albukhaty ◽  
Salman Aloufi ◽  
Faizah A. AlMalki ◽  
Hassan Al-Karagoly ◽  
...  

Green nanoparticle synthesis is an environmentally friendly approach that uses natural solvents. It is preferred over chemical and physical techniques due to the time and energy savings. This study aimed to synthesize zinc oxide nanoparticles (ZnO NPs) through a green method that used Phlomis leaf extract as an effective reducing agent. The synthesis and characterization of ZnO NPs were confirmed by UV-Vis spectrophotometry, Fourier Transform Infrared Spectroscopy (FTIR), X-Ray Diffraction (XRD), Dynamic light scattering (DLS), Zeta potential, and Field Emission Scanning Electron Microscope (FESEM) techniques. In vitro cytotoxicity was determined in L929 normal fibroblast cells using MTT assay. The antibacterial activity of ZnO nanoparticles was investigated using a disk-diffusion method against S. aureus and E. coli, as well as minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) content concentrations. XRD results confirmed the nanoparticles’ crystalline structure. Nanoparticle sizes were found to be around 79 nm by FESEM, whereas the hydrodynamic radius of nanoparticles was estimated to be around 165 3 nm by DLS. FTIR spectra revealed the formation of ZnO bonding and surfactant molecule adsorption on the surface of ZnO NPs. It is interesting to observe that aqueous extracts of phlomis leave plant are efficient reducing agents for green synthesis of ZnO NPs in vitro, with no cytotoxic effect on L929 normal cells and a significant impact on the bacteria tested.


Author(s):  
V. V. Pantyo ◽  
M. M. Fizer ◽  
O. I. Fizer ◽  
G. M. Koval ◽  
E.M. Danko

Annotation. The development and rapid pace of the spread of resistance to antimicrobial agents predetermines the search for new methods of counteracting pathogenic and conditionally pathogenic microorganisms. In this context, studies of the antimicrobial activity of newly synthesized chemicals, which in the future can be considered as candidates for antiseptic and disinfectants, are relevant. The aim of the work was to determine the antimicrobial activity of new ionic associates based on the surface-active cetylpyridinium cation with respect to certain opportunistic microorganisms. The antimicrobial activity of four ionic associates based on the cetylpyridinium cation with respect to clinical isolates of E. coli, P. vulgaris, K. pneumonia, P. aeruginosa, S. aureus, as well as the collection test strains of S. aureus ATCC 25923, E. coli ATCC 29522 and P. aeruginosa ATCC 27853 was studied. Screening studies were performed by the disk diffusion method. With substances that showed an antimicrobial effect, quantitative studies were carried out by the method of serial macro-dilutions in a liquid nutrient media. Screening studies revealed the antibacterial activity of the substances against E. coli ATCC 25923, E. coli (clinical isolate), P. vulgaris and K. pneumonia. With these microorganisms quantitative studies were carried out with the determination of the minimum inhibitory and minimum bactericidal concentrations. The most pronounced antimicrobial activity for the investigated microflora was shown by tetraphenylborate and cetylpyridinium perchlorate. The MIC and MBC values of these substances ranged between 1.625–3.125 mmol / L and 3.125–12.5 mmol / L, respectively. The studied associates showed high antimicrobial activity against representatives of the Enterobacteriaceae family in in vitro studies. Promising is the further study of the effect of the counter-anion associates of cationic surfactants on the biofilm formation of conditionally pathogenic microorganisms.


Author(s):  
Amresh Kumar Yadav ◽  
Sanjeev Kumar Ambasta ◽  
Surendra Kumar Prasad ◽  
M. P. Trivedi

Objective: To evaluate the antibacterial property of crude, aqueous and organic solvent extract from leaf, stem and root parts of two different var. of Catharanthus roseus (i.e. “rosea” and “alba”) under in vitro conditions on various human pathogenic bacteria.Methods: Antibacterial activity of crude (fresh), aqueous, ethanolic, methanolic and equimolar (1:1) mixture of ethanolic dried leaf extract of variety “rosea” and “alba” was evaluated against various pathogenic bacteria viz. Bacillus subtilis, Escherichia coli and Staphylococcus aureus by disk diffusion method under in vitro conditions.Results: Gram-positive bacteria were found to be more susceptible than Gram-negative. Dried extracts of root, stem and leaf of C. roseus var. “rosea” and “alba” plants showed maximum antibacterial potency against all the test microorganisms. The equimolar mixture of ethanolic dried leaf extracts of species “rosea” and “alba” exhibited the maximum zone of inhibition against B. subtilis, E. coli and S. aureus as compare to extract prepared from individual parts. The findings of the ethanolic mixture of dried leaves of the two varieties on the tested bactera confirm that the effect is potentiating which may be synergistic or additive.Conclusion: From the findings, it could be inferred that C. roseus var. “rosea” and “alba” could be efficiently used in the development of new life-saving drugs against bacterial pathogens. 


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