scholarly journals Antimicrobial Activity of Cationic Poly(3-hexylthiophene) Nanoparticles Coupled with Dual Fluorescent and Electrochemical Sensing: Theragnostic Prospect

Sensors ◽  
2021 ◽  
Vol 21 (5) ◽  
pp. 1715
Author(s):  
Nada Elgiddawy ◽  
Shiwei Ren ◽  
Wadih Ghattas ◽  
Waleed M. A. El Rouby ◽  
Ahmed O. El-Gendy ◽  
...  

Designing therapeutic and sensor materials to diagnose and eliminate bacterial infections remains a significant challenge for active theragnostic nanoprobes. In the present work, fluorescent/electroactive poly(3-hexylthiophene) P3HT nanoparticles (NPs) stabilized with quaternary ammonium salts using cetyltrimethylammonium bromide (CTAB), (CTAB-P3HT NPs) were prepared using a simple mini-emulsion method. The morphology, spectroscopic properties and electronic properties of CTAB-P3HT NPs were characterized by DLS, zeta potential, SEM, TEM, UV-vis spectrophotometry, fluorescence spectroscopy and electrochemical impedance spectroscopy (EIS). In an aqueous solution, CTAB-P3HT NPs were revealed to be uniformly sized, highly fluorescent and present a highly positively charged NP surface with good electroactivity. Dual detection was demonstrated as the binding of the bacteria to NPs could be observed by fluorescence quenching as well as by the changes in EIS. Binding of E. coli to CTAB-P3HT NPs was demonstrated and LODs of 5 CFU/mL and 250 CFU/mL were obtained by relying on the fluorescence spectroscopy and EIS, respectively. The antimicrobial activity of CTAB-P3HT NPs on bacteria and fungi was also studied under dark and nutritive conditions. An MIC and an MBC of 2.5 µg/mL were obtained with E. coli and with S. aureus, and of 0.312 µg/mL with C. albicans. Additionally a good biocompatibility toward normal human cells (WI38) was observed, which opens the way to their possible use as a therapeutic agent.

2021 ◽  
Author(s):  
Smita J. Pawar ◽  
Amol Kale ◽  
Priya Zori ◽  
Rahul Dorugade

Abstract Abstract The new series of 2-(substituted amino)-N-(6- substituted-1,3-benzothiazol-2yl) acetamide BTC(a-t) has been synthesized by appropriate synthetic route from substituted 2-amino benzothiazole. The synthesized compounds were screened experimentally for its antimicrobial property against gram positive, gram negative bacteria and fungi. Zone of inhibition and minimum inhibitory concentration of compounds was determined against selected bacterial and fungal strains. Compound BTC-j N-(6-methoxy-1,3-benzothiazol-2-yl)-2-(pyridine-3-yl amino) acetamide and compound BTC-r N-(6-nitro-1,3-benzothiazol-2-yl)-2-(pyridine-3-yl amino) acetamide found to have good antimicrobial potential. The compound BTC-j has shown good antibacterial activity against S. aureus at MIC of 12.5 µg/ml, B. subtilis at MIC of 6.25µg/ml, E. coli at MIC of 3.125µg/ml and P. aeruginosa at MIC of 6.25µg/ml. No statistical difference in antimicrobial activity of standard and test compounds was found indicating test compounds have comparable activity. Further docking study was carried out to check the probable interactions with the selected protein using V-life MDS 3.5 software. (DNA gyrase, PDB: 3G75). The dock score of compounds and antimicrobial activity found to be consistent.


2017 ◽  
Vol 12 (1) ◽  
pp. 77 ◽  
Author(s):  
Ganesh Tapadiya ◽  
Mayura A. Kale ◽  
Shweta Saboo

<p class="Abstract">The methanolic extract of <em>Alysicarpus </em>vaginalis was selected for fractionation due to its known reported biological activity. The four fractions were separated and subjected for<em> in vitro</em> antimitotic and anti-proliferative assays along with anti-cancer activity on two human cancers cell lines (SK-MEL-2 and Hep-G2). The antimicrobial potential of fractions had been evaluated against bacteria and fungi. From all fractions, acetone and n-butanol fractions were effective against the cell lines. They show strong inhibitory action with mitotic index 6.2 and 8.4 mg/mL and IC<sub>50 </sub>values of anti-proliferative assay in between 19.7 to 14.2 mg/mL respectively, which was found to be comparable to the standard methothrexate 5.9 mg/mL and 13.2 mg/mL respectively. In antimicrobial activity, the zone of inhibition had been observed in the range of 12-27 mm and MIC value was found in the range of 0.2-0.1 mg/mL. The acetone fraction was found to be most active against fungi, and<em> E. coli</em> whereas chloroform and n-butanol fractions were more effective against <em>S. aureus</em> and <em>B. </em>subtilis. The phytochemical characterization by HPLC analysis indicated the presence of important polyphenolic and steroidal compounds.</p>


Author(s):  
SHIBU GEORGE ◽  
MEVLIN JOY

Objective: The objective of this study was to evaluate the antimicrobial activity of methanolic extract of Ludwigia parviflora L. using standard bacterial strains and compare its activity with that of standard antibiotics. Methods: The antibacterial activity and antibiotic susceptibility tests were done by disk diffusion method using MTCC bacterial strains. Results: The study revealed that the methanolic extract of the whole plant of L. parviflora L. was effective to inhibit the growth of Staphylococcus aureus, Pseudomonas aeruginosa, Klebsiella pneumoniae, and Escherichia coli. Among the tested strains, S. aureus, P. aeruginosa, K. pneumoniae, and E. coli were more susceptible to the methanolic extract of L. parviflora than the commonly using antibiotic tetracycline 30 mcg. The activity of methanolic extract was also higher than the activity of gentamicin 10 mcg against the P. aeruginosa. Conclusion: The study concluded that the crude methanolic extract of the whole plant of L. parviflora L. is a good source for antibacterial agent against S. aureus, P. aeruginosa, K. pneumoniae, and E. coli. Hence, this plant can be used as a natural alternative to the common antibiotics such as gentamicin and tetracycline against common bacterial infections after validating its pharmacological and toxicological activities.


2020 ◽  
Vol 09 ◽  
Author(s):  
Yamuna Saravanan ◽  
Bala Subramaniam Devaraj ◽  
Nithesh Kumar Velusamy ◽  
Pooja Shree Soundirarajan ◽  
Kumaravel Kandaswamy

Background:: Phytochemicals such as tannins, alkaloids, flavonoids, and peptides been found to have antimicrobial activity against a variety of bacterial strains. Objective:: However, optimal extraction procedures for these phytochemicals and their efficacy evaluation against certain pathogenic bacterial strains remain unclear. Method:: Therefore, in this study phytochemicals from Leucas aspera (L. aspera) and Dahlia pinnata (D. pinnata) were extracted by hot and cold extraction methods using water and methanol as solvents. In addition, antimicrobial activity of L. aspera and D. pinnata extracts against bacterial strains such as the gram-negative Escherichia coli (E. coli) and the gram-positive Enterococcus faecalis (E. faecalis) were performed by Minimal Inhibitory Concentration (MIC) and CFU quantification assays. Results:: The majority of the phytochemicals such as protein, carbohydrate, tannins, flavonoids, phenols, and saponins were present in our extracts but steroids were absent in the extract. Protein, tannins, flavonoids, phenols, and saponins were present in both L. aspera and D. pinnata. The yield of proteins was high (1.990 ± 0.091 mg/ml) in methanol extracts of L. aspera and low (0.199 mg/ml) in aqueous extracts. However, the yield of tannins was high (1.713 ± 0.079 mg/ml) in methanol extracts of D. pinnata and low (0.528 ± 0.136 mg/ml) aqueous extracts. The MIC of D. pinnata extracts were found to be 200 mg/ml for both E. coli and E. faecalis. However the L. aspera extracts had a MIC of 100 mg/ml and 200 mg/ml on E. coli and E. faecalis, respectively. Conclusion:: This article demonstrated the potential use of phytochemicals as novel antimicrobial compounds against bacterial infections.


2017 ◽  
Vol 61 (8) ◽  
Author(s):  
Beatrix Wulkersdorfer ◽  
David Jaros ◽  
Sabine Eberl ◽  
Stefan Poschner ◽  
Walter Jäger ◽  
...  

ABSTRACT It has been known from previous studies that body fluids, such as cerebrospinal fluid, lung surfactant, and urine, have a strong impact on the bacterial killing of many anti-infective agents. However, the influence of human bile on the antimicrobial activity of antibiotics is widely unknown. Human bile was obtained and pooled from 11 patients undergoing cholecystectomy. After sterilization of the bile fluid by gamma irradiation, its effect on bacterial killing was investigated for linezolid (LZD) and tigecycline (TGC) against Enterococcus faecalis ATCC 29212. Further, ciprofloxacin (CIP), meropenem (MEM), and TGC were tested against Escherichia coli ATCC 25922. Time-kill curves were performed in pooled human bile and Mueller-Hinton broth (MHB) over 24 h. Bacterial counts (in CFU per milliliter after 24 h) of bile growth controls were approximately equal to MHB growth controls for E. coli and approximately 2-fold greater for E. faecalis, indicating a promotion of bacterial growth by bile for the latter strain. Bile reduced the antimicrobial activity of CIP, MEM, and TGC against E. coli as well as the activity of LZD and TGC against E. faecalis. This effect was strongest for TGC against the two strains. Degradation of TGC in bile was identified as the most likely explanation. These findings may have important implications for the treatment of bacterial infections of the gallbladder and biliary tract and should be explored in more detail.


2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Lin Zhang ◽  
Jienan Chen ◽  
Wenji Yu ◽  
Qingfeng Zhao ◽  
Jin Liu

Nanocomposites of Ag with organic montmorillonite (Ag-OMMT), Ag with montmorillonite (Ag-MMT), and organic montmorillonite (OMMT) were successfully prepared via a one-step solution-intercalated method. Sodium MMT, silver nitrate, and dimethyl octadecyl hydroxy ethyl ammonium nitrate were used as precursors. X-ray diffraction, Fourier transform infrared spectroscopy, transmission electron microscopy, and energy dispersive spectroscopy analyses confirmed that the MMT layers were intercalated, and Ag+ was partly reduced to silver nanoparticles with diameters within 10–20 nm in Ag-OMMT. The decomposition temperature of the organic cations in OMMT and Ag-OMMT increased to 220°C, as revealed by differential scanning calorimetry-thermogravimetric analysis. The antimicrobial activity of the nanocomposites was tested by measuring the minimum inhibitory concentration (MIC) and killing rate. The MICs of Ag-OMMT against Staphylococcus aureus, Escherichia coli, and Candida albicans were 0.313, 2.5, and 0.625 mg/mL, respectively. Because of the presence of quaternary ammonium nitrate, Ag-OMMT has a better MIC against Gram-positive bacteria compared to Gram-negative bacteria and fungi. OMMT did not show antimicrobial activity against Escherichia coli and Candida albicans. In 2 h, 0.0125 mg/mL Ag-OMMT could kill 100% of S. aureus, E. coli, and C. albicans in solution, and Ag-MMT could kill 99.995% of S. aureus, 90.15% of E. coli, and 93.68% of C. albicans. These antimicrobial functional nanocomposites have the potential for application in the area of surface decoration films.


2008 ◽  
Vol 52 (12) ◽  
pp. 4351-4355 ◽  
Author(s):  
Oscar Cirioni ◽  
Roberto Ghiselli ◽  
Carmela Silvestri ◽  
Wojciech Kamysz ◽  
Fiorenza Orlando ◽  
...  

ABSTRACT We investigated the efficacy of tachyplesin III and clarithromycin in two experimental rat models of severe gram-negative bacterial infections. Adult male Wistar rats were given either (i) an intraperitoneal injection of 1 mg/kg Escherichia coli 0111:B4 lipopolysaccharide or (ii) 2 × 1010 CFU of E. coli ATCC 25922. For each model, the animals received isotonic sodium chloride solution, 1 mg/kg tachyplesin III, 50 mg/kg clarithromycin, or 1 mg/kg tachyplesin III combined with 50 mg/kg clarithromycin intraperitoneally. Lethality, bacterial growth in the blood and peritoneum, and the concentrations of endotoxin and tumor necrosis factor alpha (TNF-α) in plasma were evaluated. All the compounds reduced the lethality of the infections compared to that for the controls. Tachyplesin III exerted a strong antimicrobial activity and achieved a significant reduction of endotoxin and TNF-α concentrations in plasma compared to those of the control and clarithromycin-treated groups. Clarithromycin exhibited no antimicrobial activity but had a good impact on endotoxin and TNF-α plasma concentrations. A combination of tachyplesin III and clarithromycin resulted in significant reductions in bacterial counts and proved to be the most-effective treatment in reducing all variables measured.


2018 ◽  
Vol 15 (1) ◽  
pp. 21-30
Author(s):  
Deboleena Dhara ◽  
Dhanya Sunil ◽  
Pooja R. Kamath ◽  
K. Ananda ◽  
S. Shrilakshmi ◽  
...  

Introduction: The escalating threat due to dwindling effect of antibiotics and challenge of tackling rising drug-resistant infections has gathered high focus in current medicinal research. Methods: In an attempt to find new molecules that can defeat microbial resistance, two new series of 2-[2-substituted ethenyl]-5-(substituted methoxy)-1,3,4-oxadiazole derivatives were synthesized. Various aromatic hydrazides were allowed to undergo cyclization to substituted oxadiazole-2- amines in the presence of cyanogen bromide and further condensed with different heterocyclic aldehydes to give new oxadiazole derivatives. The synthesized molecules were fully characterized by various spectral techniques and tested for antimicrobial activity. Results: Almost all the newly synthesized compounds especially (5g-5l) displayed remarkable growth inhibition against three bacterial strains: M. smegmatis, S. aureus, E. coli and fungi C. albicans. The antimicrobial activity was further confirmed by MIC assay against the same microorganisms. Oxadiazole 5g displayed promising activity with a MIC value of 0.025 mM for two bacteria and fungi, whereas MIC of this compound for E. coli was 0.1 mM. Other active compounds (5h-5l) also exhibited good MIC ranging between 0.313 to 5.0 mM against the selected microorganisms. Docking simulations were generated to explore the potential binding approaches of ligand 5g at the D-alanine:d-alanine ligase (Ddl) protein of E. coli and S. aureus. Conclusion: Molecule 5g was active even at a lower concentration and could probably act as a prospective lead molecule for targeting the drug resistant microorganisms.


Author(s):  
Abu- Safieh Rana ◽  
Muhi- Eldeen Zuhair ◽  
Alsarahni Aseel ◽  
Al-Kaissi Elham

A new series of 7-methoxy-2-[4-(t-amino-1-yl)oxy]-naphthalene derivatives; 7-methoxy-2-{[4-(2-methylpiperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ2), 7-methoxy-2-{[4-(2,6-dimethylpiperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ3), 7-methoxy-2{[4-(piperidine)but-2-yn-1-yl]oxy}-naphthalene (RZ4), 7-methoxy-2-{[4-(pyrrolidine)but-2-yn-1-yl]oxy}-naphthalene (RZ5), 7-methoxy-2-{[4-(N-methylpiperazine)but-2-yn-1-yl]oxy}-naphthalene (RZ6), 7-methoxy -2-{[4-(hexamethyleneimine)but-2-yn-1-yl]oxy}-naphthalene (RZ7) were synthesized and screened in vitro as potential antimicrobial agents. Antimicrobial activity were evaluated by measuring the minimum inhibitory and bactericidal/fungicidal concentration (MIC, MBC and MFC). RZ2, RZ5, RZ6 and RZ7 showed the highest antimicrobial activity against S. aureus with MIC value 62.5 µg/ml, compounds RZ2, RZ4, RZ5, and RZ7 have the highest antimicrobial activity against B. subtilis with MIC vale 62.5 µg/ml, RZ3, RZ6 have the same antimicrobial activity with MIC value 125µg/ml, compounds. RZ4, RZ5, RZ6 and RZ7 have the highest antimicrobial activity against E. coli with MIC value 125 µg/ml, all compounds have the same MIC value against P. aeruginosa (125 µg/ml). RZ2, RZ4, RZ5, RZ6, RZ7 showed the highest antifungal activity with MIC of 62.5 µg/ml. In conclusion, the synthesized compounds showed good antimicrobial activity and promising potency against gram positive bacteria, gram negative bacteria and fungi.


2018 ◽  
Vol 42 (2) ◽  
pp. 155-170
Author(s):  
Sunil Makwane ◽  
SD Srivastava ◽  
Rajiv Dua ◽  
SK Srivastava

A new series of 5-benzylidene-3-(5-ethyl-[1,3,4]thiadiazol-2-yl)-2-phenyl-thiazolidin-4-ones (3a-3m) were synthesized. The reaction of thioglycolic acid with benzylidene-(5-ethyl-[1,3,4] thiadiazol-2-yl)-amine 1a in the presence of anhydrous ZnCl2 afforded the new heterocyclic compounds 5-benzylidene-3-(5-ethyl-[1,3,4] thiadiazole-yl)-2-phenyl-thiazolidin-4-one, 2a. The latter product on treatment with several selected substituted aromatic aldehydes in the presence of sodium ethoxide underwent the Knoevenagel reaction to yield 5-benzylidene-3-(5-ethyl-[1,3,4] thiadiazol-2-yl)-2-phenyl-thiazolidin-4-ones, 3a-3m. The structures of the compounds were confirmed by IR, 1H-NMR, 13C-NMR and mass spectroscopy and by chemical analysis. All the above compounds were screened for their antimicrobial activity against some selected bacteria and fungi such as E. coli, B. Subtilis, and S. Typhi bacteria and A.niger, A. Flavus and F. oxisporium Fungi. Journal of Bangladesh Academy of Sciences, Vol. 42, No. 2, 155-170, 2018


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