scholarly journals ANTIBACTERIAL PHOTODYNAMIC THERAPEUTIC STUDIES OF METALLATED PORPHYRIN AGAINST CHRONIC WOUND COLONISING BACTERIAL ISOLATES

2021 ◽  
Vol 46 (2) ◽  
Author(s):  
O. B Daramola ◽  
A. A Olajide ◽  
N Torimiro ◽  
R. C George

Wound infections have become life threatening as a result of treatment failures caused by multi-drug resistant pathogens. The search for newer compounds potent against antibiotic resistant bacteria associated with wounds is crucial. Hence this study investigated the application of antibacterial photodynamic therapy using meso tetra-(4-phenyl) porphyrin (TPP), metallated with zinc, tin and silver (ZnTPP, SnTPP and AgTPP), meso tetra-(4-sulphonatephenyl) porphyrin (TPPS) and the corresponding metallo meso tetra-(4-sulphonatephenyl) porphyrin (MTPPS) as photosensitizers. The in-vitro toxicity and photo-toxicity properties on four chronic wound colonizing multi-drug resistant bacterial strains: Staphylococcus aureus, Klebsiella sp., Proteus sp., and Escherichia coli were assessed using agar well diffusion method. Photo-toxicity of the compounds was investigated using 100 Watt tungsten lamp. Inhibitory activity of porphyrins tested against these bacterial strains showed Staphylococcus aureus to have both lowest (11±0.0 mm) and highest (33±1.1 mm) susceptibility to SnTPPS and ZnTPPS respectively. The sequence of data also showed appreciable improvement in the antimicrobial activities of five metalloporphyrins (SnTPP, AgTPP, ZnTPPS, SnTPPS and AgTPPS) exposed to light rays than when tested against bacterial strains in dark condition. ZnTPPS exhibited the best activity with improved photo-toxic activities against all bacterial strains (Staphylococcus aureus 33±1.1 mm, Klebsiella sp. 32±0.7 mm, Proteus sp. 28±0.7 mm and Escherichia coli 30±1.4 mm) examined in this study.

2012 ◽  
Vol 9 (4) ◽  
pp. 2354-2370 ◽  
Author(s):  
N. L. Obasi ◽  
Okoye C. O. Benedict ◽  
P. O. Ukoha ◽  
A. O. Anaga

N-(benzothiazol-2-yl)benzenesulphonamide (BS2ABT) was synthesized by the condensation (by refluxing) of 2-aminobenzothiazole and benzenesulphonylchloride in acetone at 140ºC. The resulting crude precipitates were recrystallized from dimethylformamide (DMF). Five metal complexes of copper(I), nickel(II), manganese(II), cobalt(II) and zinc(II) of the ligands were synthesized. The compounds were characterized using magnetic susceptibility measurements, UV/VIS spectrophotometry, infra red, proton and13C nmr spectroscopies. The antimicrobial tests of the ligands and its metal complexes were carried out on both multi-resistant bacterial strains isolated under clinical conditions and cultured species using agar-well diffusion method. The multi-resistant bacterial strains used wereEscherichia coli, Proteusspecies,Pseudomonas aeroginosa and Staphylococcus aureuswhich were isolated from dogs. The culture species werePseudomonas aeruginosa(ATCC 27853),Escherichia Coli(ATCC 25922)Staphylococcus aureus(ATCC 25923), and the fungi,Candida krusei(ATCC 6258) andCandida albicans(ATCC 90028). The tests were bothin vitroandin vivo. Thus the Inhibition Zone Diameter (IZD), the Minimum Inhibitory Concentration (MIC), and the Lethal and Effective Concentrations (LC50and EC50) were determined. The antimicrobial activities of the compounds were compared with those of Ciprofloxacin and trimethoprim-sulphamethoxazole as antibacterial agents and Fluconazole as an antifungal drug. All the compounds showed varying activities against the cultured typed bacteria and fungi used. However, they were less active than the standard drugs used except Fluconazole which did not show any activity againstCandida krusei(ATCC 6258) but most of the compounds synthesized were very active against it. The Lethal Concentration (LC50) ranged from 26.25±4.9-1833.88±186.92 ppm. These are within the permissible concentrations.


2020 ◽  
Vol 7 (1) ◽  
pp. 26-32
Author(s):  
Bendella Amina nor elhouda ◽  
Ghazi Kheira ◽  
Meliani Samia

AbstractThe aim of this study is to test two different methods for evaluating the in vitro antibacterial effect of Thymus fontanesii Boiss. et Reut. essential oil against standard and clinical bacterial strains responsible for bovine mastitis: the disc diffusion method or the aromatogram which allows the demonstration of the antibacterial power of essential oils on the bacterial strains tested, Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923 and two strains isolated from bovine mastitis milk S. aureus and E. coli. The inhibition activity of the essential oil of T. fontanesii on bacterial strains by the two methods shows that the antimicrobial power of this oil is very important and is characterized by bactericidal and bacteriostatic action against gram negative and gram positive bacteria. The antimicrobial evaluation by the aromatogram showed good antibacterial activity against all the strains tested, the zones of inhibition of the bacteria were between 23,33±1,527mm and 37,5±3,535 mm. The search for minimum inhibitory concentrations MIC and bactericides CMB made it possible to quantitatively assess the antimicrobial power of this essential oil. In this work, the MIC was 0,625 µl/ml for all strains tested, and the lowest CMB was that of T. fontanesii against E. coli ATCC 25922 was 0,625 µl/ml.


2012 ◽  
Vol 13 (1) ◽  
pp. 63
Author(s):  
Taswin Yacob ◽  
Rita Endriani

The benefit and efficacy of ketepeng cina (Senna alata) in the treatment of infection has shown that have antibacterialactivity, inhibiting and killing bacteria that cause infection. The objective of this study was evaluate the antibacterialactivity of ketepeng cina against Staphylococcus aureus dan Escherichia coli in vitro. This study was a laboratoryexperimental research which use completely randomized design with diffusion method. Ethanol extract of Sennaalata leaves devided into 4 doses, i.c. 100, 50, 25 and 12.5. Amoxiclave were used as positive control and aquadestnegative control. The data were analyzed by Analysis of Varian continued with Duncan’s Multiple Range Test. Theresult of this study showed that antimicrobial activity of ethanol extract Senna alata leaves inhibited the growth ofStaphylococcus aureus, but not Escherichia coli. The optimum effect was showed given by the concentration 100at 17.7 mm.


2019 ◽  
Author(s):  
Peter Spanogiannopoulos ◽  
Patrick H. Bradley ◽  
Jonathan Melamed ◽  
Ysabella Noelle Amora Malig ◽  
Kathy N. Lam ◽  
...  

Microbiome surveys indicate that pharmaceuticals are the top predictor of inter-individual variations in gut microbial community structure1, consistent with in vitro evidence that non-antibiotic (i.e. host-targeted) drugs inhibit gut bacterial growth2and are subject to extensive metabolism by the gut microbiome3,4. In oncology, bacterial metabolism has been implicated in both drug efficacy5,6and toxicity7,8; however, the degree to which bacterial sensitivity and metabolism can be driven by conserved pathways also found in mammalian cells remains poorly understood. Here, we show that anticancer fluoropyrimidine drugs broadly inhibit the growth of diverse gut bacterial strains. Media supplementation, transcriptional profiling (RNA-seq), and bacterial genetics implicated pyrimidine metabolism as a key target in bacteria, as in mammalian cells. Drug resistant bacteria metabolized 5FU to its inactive metabolite dihydrofluorouracil (DHFU) mimicking the major host pathway for drug clearance. Functional orthologs of the bacterial operon responsible (preTA) are widespread across human gut bacteria from the Firmicutes and Proteobacteria phyla. The observed conservation of both the targets and pathways for metabolism of therapeutics across domains highlights the need to distinguish the relative contributions of human and microbial cells to drug disposition9, efficacy, and side effect profiles.


2019 ◽  
Vol 2 (1) ◽  
pp. 19
Author(s):  
Murni Halim

A study was carried out to screen for phytochemical constituents and assess the antioxidant and antimicrobial activities of Senna alata and Senna tora leaf extracts. The leaves were first dried at room temperature and 50°C in an oven prior to solvent extraction using ethanol and methanol. The in-vitro qualitative assays showed that both S. alata and S. tora leaf extracts contained bioactive and secondary metabolites components such as tannins, steroids, saponin, terpenoids, glycosides, flavonoids and phenols. The antioxidant activity and capacity test were carried out by conducting free radical of 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity and Ferric reduction antioxidant plasma (FRAP) assays. Both assays showed S. tora leaf extract has higher antioxidant capacity than S. alata leaf extract. The efficacy of these leaf extracts were tested against skin pathogens through agar well diffusion method. S. alata extract showed an inhibition zone (1.15 – 1.59 mm) against Pseudomonas aeruginosa while S. tora extracts exhibited a strong antimicrobial activity against S. epidermidis (inhibition zone of 12 – 16.94 mm) followed by P. aeruginosa (inhibition zone of 1 – 1.59 mm). Nonetheless, no inhibition zone was observed for S. aureus by both leaf extracts. The phytochemicals and antioxidant constituents as well as inhibitory potential on skin pathogens possessed by S. alata and S. tora leave highlighted their potential utilization in the development of natural drugs or cosmetics to treat skin related diseases or infections.


2020 ◽  
Vol 8 (4) ◽  
pp. 110-115
Author(s):  
Afsaneh Molamirzaei ◽  
Maryam Allahdadian ◽  
Monir Doudi

Background: Using smoke from burning donkey dung has been popular in the treatment of many diseases in Iran. Objective: This study aimed to investigating the antimicrobial properties of donkey dung smoke on multi-drug resistant (MDR) bacteria isolated from urinary infection. Materials and Methods: First, 300 and 200 urine samples were collected from pregnant and non-pregnant women in Isfahan, Iran. Then in each group, 100 bacterial isolates including Escherichia coli, Klebsiella pneumonia, Proteus vulgaris, Staphylococcus epidermidis, Staphylococcus aureus, Pseudomonas aeruginosa, and Staphylococcus saprophyticus were isolated. Antibiotic resistant protocol was determined by antibiogram test. Donkey dung was sterilized, disintegrated, and heated. The smokes were concentrated in n-hexane solvent (65%) and were collected after evaporation of the solvent. Finally, the antibacterial activities of the concentrations of 0.25, 0.5 and 1 mg/mL of the smokes were detected using disk diffusion and macrodilution methods. Results: The most abundant MDR isolates causing urinary infections in pregnant and non-pregnant women was Escherichia coli. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of donkey dung smoke on MDR isolates from pregnant women were 0.25 mg/mL and 0.5 mg/mL, respectively. In the case of MDR isolates in non-pregnant women, the MIC of the smoke on Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus was 0.25 mg/mL, and the MBC on these isolates was 0.5 mg/mL. Conclusion: The smokes from donkey dung investigated in the present study have suitable potentials for controlling the infections after In vivo analysis.


2021 ◽  
Vol 11 (4) ◽  
pp. 12434-12446

In our present work, we reported an effective synthesis, molecular docking, and antimicrobial properties of novel 5-(4-substituted-benzyl)-2-(furan/thiophen-2-ylmethylene hydrazono) thiazolidin-4-ones (6a-g) and (7a-i). The structures of the synthesized compounds (6a-g) and (7a-i) were elucidated by 1H-NMR spectroscopy. The molecular docking studies were performed for all the synthesized compounds against GlcN-6P using AutoDock-tools-1.5.6 and recorded the extent of H-bonding and binding affinities. The preselected compounds via molecular docking were further tested for in vitro antimicrobial activity against five bacterial strains (Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus) and two fungal strains (Candida albicans and Cryptococcus neoformans). The antimicrobial findings exhibited that the compounds possessed significant antimicrobial potential.


2016 ◽  
Author(s):  
Mayram Tuysuz ◽  
Sibel Dosler ◽  
Ayse Seher Birteksoz Tan ◽  
Gulten Otuk

Background: Because of increasing antibiotic resistance, herbal teas are the most popular natural alternatives, which are gaining even more importance. We examined the antimicrobial activities of 31 herbal teas both alone and in combination with antibiotics or antifungals against the standard and clinical isolates of Pseudomonas aeruginosa, Acinetobacter baumannii, Escherichia coli, Klebsiella pneumoniae, Enterococcus faecalis, methicillin susceptible/resistant Staphylococcus aureus and Candida albicans. Methods: The antimicrobial activities of the teas were determined by using the disk diffusion and microbroth dilution methods, and the combination studies were examined by using the microbroth checkerboard and time killing curve methods. Results: Rosehip, rosehip bag, pomegranate blossom, thyme, wormwood, mint, echinacea bag, cinnamon, black, and green teas were active against most of the studied microorganisms. In the combination studies, we characterized all the expected effects (synergistic, additive, and antagonistic) between the teas and the antimicrobials. While synergy was observed more frequently between ampicillin, ampicillin-sulbactam, or nystatine, and the various tea combinations, most of the effects between the ciprofloxacin, erythromycin, cefuroxime, or amikacin and various tea combinations, particularly rosehip, rosehip bag, and pomegranate blossom teas, were antagonistic. The results of the time kill curve analyses showed that none of the herbal teas were bactericidal in their usage concentrations; however, in combination they were. Discussion: Some herbal teas, particularly rosehip and pomegranate blossom should be avoided because of antagonistic interactions during the course of antibiotic treatment or should be consumed alone.


2019 ◽  
Vol 16 (6) ◽  
pp. 931-938
Author(s):  
Hany M. Mohamed ◽  
Ashraf H.F. Abd El-Wahab

Background: Synthetic azo compounds and their derivatives have been studied extensively due to their biological and pharmacological activities. Pyranopyridines, pyranopyrimidines and tetrazoles derivatives have emerged as a promising and attractive scaffold in the development of potent biological and pharmacological agents. Objectives: To design a series of new benzochromeno(pyridine/pyrimidine/tetrazole) derivatives and evaluate their antimicrobial activity against some bacterial strains (Gram-positive and Gram-negative) and some fungal strains. Materials and Methods: The (E)-7-(4-chlorophenyl)-5-(phenyldiazenyl)-10-thioxo-7,9,10,11-tetrahydro-8Hnaptho[ 1,2-b]pyrano[2,3-d]pyrimidin-8-one (4) was synthesized by the reaction of 4H-naphtho[1,2-b]pyran-3- carbonitrile (3) with carbon disulfide in alcoholic potassium hydroxide solution. Reaction of 3 with sodium azide in DMF and in presence of ammonium chloride afforded 6-(phenyldiazenyl)-3-(1H-tetrazol-5-yl)-4Hbenzo[ h]chromen-2-amine (7) while with malononitrile, thiourea or urea gave chromeno[2,3-b]pyridine-9- carbonitrile (8), chromeno[2,3-d]pyrimidine-10-thione (9) and chromeno[2,3-d]pyrimidin-10-one (10), respectively. The assignment structures were established on the basis of spectral data. Results: In this study, the antimicrobial activity of the synthesized compounds 3-12 was examined for their in vitro antimicrobial activity by using agar diffusion method such as Mueller-Hinton agar medium for bacteria and Sabouraud’s agar medium for fungi. Ampicillin and mycostatine were included in the experiments as reference drugs. Conclusion: A series of new benzochromeno(pyridine/pyrimidine/tetrazole) derivatives were synthesized in this work. All compounds were evaluated in antimicrobial activities.


Chemotherapy ◽  
2021 ◽  
Author(s):  
Lluvia Itzel López-López ◽  
Ernesto Rivera-Ávalos ◽  
Cecilia Villarreal-Reyes ◽  
Fidel Martínez-Gutiérrez ◽  
Denisse de Loera

Background: The synthesis and biological evaluation of 1,4-naphthoquinone derivatives are of great interest since these compounds exhibit strong antibacterial, antifungal, antimalarial, and anticancer activities. The electronic properties of naphthoquinones are usually modulated by attaching functional groups containing nitrogen, oxygen and sulfur atoms, which tune their biological potency and selectivity. Methods: A series of 13 amino acid 1,4-naphthoquinone derivatives were synthesized under assisted microwave and ultrasound conditions. The antibacterial activity compounds was tested against American type Culture Collection (ATCC): Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Enterococcus faecalis, as well two multidrug resistant pathogens: Escherichia coli and Staphylococcus aureus from clinical isolated. Minimal inhibitory concentration (MIC) was determined using the broth microdilution method. Results: MIC of derivatives 4–11, 14 and 16 showed antimicrobial activity against gram-positive and gram-negative bacteria. Antimicrobial activities of the compounds 4–8 and 14 were ≤MIC 24.7 μg∙mL-1 against all the reference strain, even more the compound 6 showed the most potent activity with a MIC of 3.9 μg∙mL-1 on S. aureus. On the clinical isolated the compounds 7, 8 and 14 showed a MIC of 49.7 and 24.7 μg∙mL-1 against S. aureus y E. coli respectively. About ADME properties and Osiris analysis, the compounds 4-16 presented high gastrointestinal absorption and good characteristics for oral bioavailability and the compound 14 was the less toxic. Conclusion: amino acid 1,4-naphthoquinone derivatives showed good in vitro antibacterial activity against clinical strains, and modifications on C-3 with cloride atom enhanced the efficiency against same pathogens.


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